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
CHEMBL526091 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
44571257 191094 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 518 9 3 4 4.3 CC(C)c1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL518772 191094 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 518 9 3 4 4.3 CC(C)c1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
11192346 2024 57 None 1 3 Human 7.7 pIC50 = 7.7 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 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 1 3 Human 7.7 pIC50 = 7.7 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 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 1 3 Human 7.7 pIC50 = 7.7 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 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
56661444 65775 0 None - 1 Human 7.7 pIC50 = 7.7 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 614 6 3 8 5.1 CC(C)(C)NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834717 65775 0 None - 1 Human 7.7 pIC50 = 7.7 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 614 6 3 8 5.1 CC(C)(C)NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44425637 85987 0 None 3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230405 85987 0 None 3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44425637 85987 0 None 3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230405 85987 0 None 3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44425629 86026 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230616 86026 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44442593 147200 0 None - 1 Human 6.7 pIC50 = 6.7 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 CCNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL392814 147200 0 None - 1 Human 6.7 pIC50 = 6.7 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 CCNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
57344218 68948 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 484 7 3 3 4.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922806 68948 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 484 7 3 3 4.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2)CC1 10.1016/j.bmcl.2011.09.113
44563038 186039 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 554 7 1 5 5.0 CCOC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ncccc23)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL487074 186039 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 554 7 1 5 5.0 CCOC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ncccc23)CC1 10.1016/j.bmcl.2008.10.061
21098512 85089 0 None - 1 Human 4.7 pIC50 = 4.7 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 351 5 2 5 3.5 O=[N+]([O-])c1cccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL224594 85089 0 None - 1 Human 4.7 pIC50 = 4.7 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 351 5 2 5 3.5 O=[N+]([O-])c1cccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
21098530 143559 0 None - 1 Human 4.7 pIC50 = 4.7 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 351 5 2 5 3.5 O=[N+]([O-])c1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL389915 143559 0 None - 1 Human 4.7 pIC50 = 4.7 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 351 5 2 5 3.5 O=[N+]([O-])c1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
44447426 94609 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 8 1 2 7.0 C=CCC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL252208 94609 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 8 1 2 7.0 C=CCC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
145961667 161354 0 None - 1 Human 4.7 pIC50 = 4.7 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 461 6 1 5 4.2 CN1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4126007 161354 0 None - 1 Human 4.7 pIC50 = 4.7 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 461 6 1 5 4.2 CN1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
44447426 94609 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 8 1 2 7.0 C=CCC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL252208 94609 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 8 1 2 7.0 C=CCC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
145963369 161386 0 None - 1 Human 6.7 pIC50 = 6.7 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 522 7 1 4 6.8 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC(c2ccccc2)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4126360 161386 0 None - 1 Human 6.7 pIC50 = 6.7 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 522 7 1 4 6.8 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC(c2ccccc2)CC1 10.1016/j.bmc.2018.05.027
11548199 89922 0 None 707 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 expressed in THP1 cells assessed as MCP1-induced calcium fluxAntagonist activity at CCR2 expressed in THP1 cells assessed as MCP1-induced calcium flux
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237967 89922 0 None 707 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 expressed in THP1 cells assessed as MCP1-induced calcium fluxAntagonist activity at CCR2 expressed in THP1 cells assessed as MCP1-induced calcium flux
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
22143255 187858 0 None - 1 Human 8.7 pIC50 = 8.7 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 523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL496343 187858 0 None - 1 Human 8.7 pIC50 = 8.7 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 523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
22143155 188062 0 None - 1 Human 8.7 pIC50 = 8.7 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 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL497788 188062 0 None - 1 Human 8.7 pIC50 = 8.7 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 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
44593555 188784 0 None 2 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL505722 188784 0 None 2 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44570714 189794 0 None 9 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 565 9 5 6 3.6 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL516224 189794 0 None 9 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 565 9 5 6 3.6 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
9850318 95245 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxisAntagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxis
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL256154 95245 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxisAntagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxis
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
10392978 167459 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxisAntagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxis
ChEMBL 558 6 2 5 5.3 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL429849 167459 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxisAntagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxis
ChEMBL 558 6 2 5 5.3 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
54754968 65742 0 None - 1 Human 8.7 pIC50 = 8.7 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 502 7 3 6 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834634 65742 0 None - 1 Human 8.7 pIC50 = 8.7 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 502 7 3 6 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44425647 86101 0 None 5 2 Human 8.7 pIC50 = 8.7 Functional
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231039 86101 0 None 5 2 Human 8.7 pIC50 = 8.7 Functional
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44423283 85307 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced calcium flux in human monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced calcium flux in human monocytes
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
CHEMBL226065 85307 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced calcium flux in human monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced calcium flux in human monocytes
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
44583283 188286 0 None - 1 Human 8.6 pIC50 = 8.6 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 714 11 3 8 6.0 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL500175 188286 0 None - 1 Human 8.6 pIC50 = 8.6 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 714 11 3 8 6.0 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2009.05.041
127026243 138269 0 None - 1 Human 8.6 pIC50 = 8.6 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 456 3 2 6 2.5 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(C)(C)C)c(Cl)s3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770591 138269 0 None - 1 Human 8.6 pIC50 = 8.6 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 456 3 2 6 2.5 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(C)(C)C)c(Cl)s3)CC2)C1 10.1039/C5MD00362H
53321616 58460 0 None 5 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 495 6 1 4 5.0 CC[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683063 58460 0 None 5 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 495 6 1 4 5.0 CC[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
11433008 77637 0 None - 1 Human 8.6 pIC50 = 8.6 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 564 8 2 5 4.9 Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088378 77637 0 None - 1 Human 8.6 pIC50 = 8.6 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 564 8 2 5 4.9 Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
10289827 187976 0 None - 1 Human 8.6 pIC50 = 8.6 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 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 8.6 pIC50 = 8.6 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 571 9 2 6 3.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
25110716 155206 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced monocyte chemotaxisAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced monocyte chemotaxis
ChEMBL 515 4 0 3 7.0 C[C@H]1CN([C@@H]2CC[C@@]3(CCO[C@H]3OCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.016
CHEMBL402532 155206 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced monocyte chemotaxisAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced monocyte chemotaxis
ChEMBL 515 4 0 3 7.0 C[C@H]1CN([C@@H]2CC[C@@]3(CCO[C@H]3OCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.016
53318853 58456 0 None 27 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683059 58456 0 None 27 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2011.01.015
11597 674 5 None 11 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulationAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulation
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00373
23725180 674 5 None 11 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulationAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulation
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00373
CHEMBL4781426 674 5 None 11 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulationAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulation
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00373
11387511 74541 0 None - 1 Human 8.6 pIC50 = 8.6 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 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ccncc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029419 74541 0 None - 1 Human 8.6 pIC50 = 8.6 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 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ccncc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
44453441 97689 0 None - 1 Human 8.6 pIC50 = 8.6 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 498 6 3 4 3.2 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL271289 97689 0 None - 1 Human 8.6 pIC50 = 8.6 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 498 6 3 4 3.2 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
46885213 8460 0 None 52 3 Human 8.6 pIC50 = 8.6 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)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093802 8460 0 None 52 3 Human 8.6 pIC50 = 8.6 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)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
57391767 71019 0 None - 1 Human 8.6 pIC50 = 8.6 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 534 8 3 6 3.3 CCOc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
CHEMBL1951779 71019 0 None - 1 Human 8.6 pIC50 = 8.6 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 534 8 3 6 3.3 CCOc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
127029034 138215 0 None - 1 Human 8.6 pIC50 = 8.6 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 440 3 2 6 1.9 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(C)(C)C)c(F)s3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770008 138215 0 None - 1 Human 8.6 pIC50 = 8.6 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 440 3 2 6 1.9 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(C)(C)C)c(F)s3)CC2)C1 10.1039/C5MD00362H
11192346 2024 57 None -1 3 Rat 8.6 pIC50 = 8.6 Functional
Antagonist activity at rat CCR2Antagonist activity at rat CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 2024 57 None -1 3 Rat 8.6 pIC50 = 8.6 Functional
Antagonist activity at rat CCR2Antagonist activity at rat CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 2024 57 None -1 3 Rat 8.6 pIC50 = 8.6 Functional
Antagonist activity at rat CCR2Antagonist activity at rat CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
10300284 73732 0 None - 1 Human 7.7 pIC50 = 7.7 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 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018396 73732 0 None - 1 Human 7.7 pIC50 = 7.7 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 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
57396998 71014 0 None - 1 Human 7.7 pIC50 = 7.7 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)(c3cncnc3)CC2)C1 10.1021/ml200030q
CHEMBL1951773 71014 0 None - 1 Human 7.7 pIC50 = 7.7 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)(c3cncnc3)CC2)C1 10.1021/ml200030q
54755919 65759 0 None - 1 Human 7.7 pIC50 = 7.7 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 6 2 7 4.5 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834651 65759 0 None - 1 Human 7.7 pIC50 = 7.7 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 6 2 7 4.5 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
54755801 65760 0 None - 1 Human 7.7 pIC50 = 7.7 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 559 8 3 8 3.7 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834652 65760 0 None - 1 Human 7.7 pIC50 = 7.7 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 559 8 3 8 3.7 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
56659295 65810 0 None - 1 Human 7.7 pIC50 = 7.7 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 503 7 2 7 4.2 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4noc5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834852 65810 0 None - 1 Human 7.7 pIC50 = 7.7 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 503 7 2 7 4.2 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4noc5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44425629 86026 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230616 86026 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
9956238 60198 1 None 3 4 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1688889 60198 1 None 3 4 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1739922 60198 1 None 3 4 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
57656833 75229 0 None -42 4 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at rat CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036782 75229 0 None -42 4 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at rat CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44421923 85082 0 None - 1 Human 5.7 pIC50 = 5.7 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 Nc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL224535 85082 0 None - 1 Human 5.7 pIC50 = 5.7 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 Nc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
9857714 85131 2 None - 1 Human 5.7 pIC50 = 5.7 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 306 4 2 3 3.6 c1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL224885 85131 2 None - 1 Human 5.7 pIC50 = 5.7 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 306 4 2 3 3.6 c1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
44421855 85114 0 None - 1 Human 4.7 pIC50 = 4.7 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 2 4 3.0 c1cncc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL224746 85114 0 None - 1 Human 4.7 pIC50 = 4.7 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 2 4 3.0 c1cncc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
11723420 136551 5 None - 1 Human 4.7 pIC50 = 4.7 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(CN2CCC(Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
CHEMBL373759 136551 5 None - 1 Human 4.7 pIC50 = 4.7 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(CN2CCC(Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
57656887 75212 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 376 4 1 3 3.4 O=C(Nc1cccc(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036763 75212 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 376 4 1 3 3.4 O=C(Nc1cccc(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
44447427 154847 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 538 7 1 2 7.1 CC(C)C(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL400516 154847 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 538 7 1 2 7.1 CC(C)C(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
44447427 154847 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 538 7 1 2 7.1 CC(C)C(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL400516 154847 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 538 7 1 2 7.1 CC(C)C(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
11570431 91982 0 None -2 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 564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241502 91982 0 None -2 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 564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
22143346 172651 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 634 11 4 6 4.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL449672 172651 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 634 11 4 6 4.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)C1 10.1016/j.bmcl.2008.07.123
10175423 188446 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 reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 614 10 4 6 4.4 CCNC(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502515 188446 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 reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 614 10 4 6 4.4 CCNC(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
10312346 188462 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 reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 614 9 3 6 4.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502795 188462 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 reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 614 9 3 6 4.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N(C)C)cc1 10.1016/j.bmcl.2009.05.041
10152864 187874 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 543 8 3 6 3.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL496432 187874 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 543 8 3 6 3.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
49763931 65426 0 None - 1 Human 7.7 pIC50 = 7.7 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 499 6 3 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc4[nH]cnc4c3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829617 65426 0 None - 1 Human 7.7 pIC50 = 7.7 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 499 6 3 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc4[nH]cnc4c3)CC2)C1 10.1016/j.bmcl.2011.06.080
44453330 95502 0 None - 1 Human 7.7 pIC50 = 7.7 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 483 6 2 3 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257316 95502 0 None - 1 Human 7.7 pIC50 = 7.7 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 483 6 2 3 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
44453300 97436 0 None - 1 Human 7.7 pIC50 = 7.7 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 7 2 4 3.5 CSc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL270005 97436 0 None - 1 Human 7.7 pIC50 = 7.7 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 7 2 4 3.5 CSc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
44416274 158554 0 None - 1 Human 6.7 pIC50 = 6.7 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 6.7 pIC50 = 6.7 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
24801523 97855 0 None - 1 Human 6.7 pIC50 = 6.7 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 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 6.7 pIC50 = 6.7 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 493 7 3 4 4.0 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
10458152 77801 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL209267 77801 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
10458152 77801 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL209267 77801 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
49764446 65440 0 None - 1 Human 7.7 pIC50 = 7.7 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 518 7 3 5 3.1 CN(C)c1cccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2011.06.080
CHEMBL1829631 65440 0 None - 1 Human 7.7 pIC50 = 7.7 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 518 7 3 5 3.1 CN(C)c1cccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2011.06.080
44453474 97871 0 None - 1 Human 7.7 pIC50 = 7.7 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 512 6 3 4 2.6 Nc1ccc(I)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272284 97871 0 None - 1 Human 7.7 pIC50 = 7.7 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 512 6 3 4 2.6 Nc1ccc(I)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
56659196 65803 0 None - 1 Human 7.7 pIC50 = 7.7 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 522 8 3 8 3.4 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834796 65803 0 None - 1 Human 7.7 pIC50 = 7.7 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 522 8 3 8 3.4 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
22143258 183879 0 None - 1 Human 7.7 pIC50 = 7.7 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 522 9 3 5 3.9 CSc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481010 183879 0 None - 1 Human 7.7 pIC50 = 7.7 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 522 9 3 5 3.9 CSc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
57656942 75039 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 376 4 1 3 3.4 O=C(Nc1ccc(Cl)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2035000 75039 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 376 4 1 3 3.4 O=C(Nc1ccc(Cl)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
57403699 68937 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cnccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922795 68937 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cnccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44453004 95264 0 None - 1 Human 4.7 pIC50 = 4.7 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 6 2 3 3.9 CC(NC(=O)c1cccc(C(F)(F)F)c1)C(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL256256 95264 0 None - 1 Human 4.7 pIC50 = 4.7 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 6 2 3 3.9 CC(NC(=O)c1cccc(C(F)(F)F)c1)C(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
10471319 84803 5 None - 1 Human 4.7 pIC50 = 4.7 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 321 4 1 3 4.1 Fc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
CHEMBL223336 84803 5 None - 1 Human 4.7 pIC50 = 4.7 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 321 4 1 3 4.1 Fc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
44439169 90774 0 None - 1 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 622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239170 90774 0 None - 1 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 622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44447446 154879 0 None - 1 Human 6.6 pIC50 = 6.6 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
CHEMBL400724 154879 0 None - 1 Human 6.6 pIC50 = 6.6 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
44447424 94608 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 CC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL252206 94608 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 CC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
44447446 154879 0 None - 1 Human 6.6 pIC50 = 6.6 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
CHEMBL400724 154879 0 None - 1 Human 6.6 pIC50 = 6.6 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
11306757 73737 0 None - 1 Human 7.6 pIC50 = 7.6 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 508 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018401 73737 0 None - 1 Human 7.6 pIC50 = 7.6 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 508 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
11489078 73805 0 None - 1 Human 7.6 pIC50 = 7.6 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 509 12 4 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(OC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018530 73805 0 None - 1 Human 7.6 pIC50 = 7.6 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 509 12 4 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(OC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
44570781 192565 0 None - 1 Human 7.6 pIC50 = 7.6 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 515 8 4 4 3.7 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc3[nH]ccc3c2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL521275 192565 0 None - 1 Human 7.6 pIC50 = 7.6 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 515 8 4 4 3.7 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc3[nH]ccc3c2)C1 10.1016/j.bmcl.2008.12.062
46830335 8215 8 None - 1 Human 7.6 pIC50 = 7.6 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 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 7.6 pIC50 = 7.6 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 565 8 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
46842383 8345 0 None - 1 Human 7.6 pIC50 = 7.6 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 530 8 2 4 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092929 8345 0 None - 1 Human 7.6 pIC50 = 7.6 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 530 8 2 4 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
70689915 74553 0 None - 1 Human 7.6 pIC50 = 7.6 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 611 6 3 9 3.3 O=C(N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1)C1(O)CCN(c2cc(C(F)(F)F)ccn2)CC1 10.1021/ml200199c
CHEMBL2029572 74553 0 None - 1 Human 7.6 pIC50 = 7.6 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 611 6 3 9 3.3 O=C(N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1)C1(O)CCN(c2cc(C(F)(F)F)ccn2)CC1 10.1021/ml200199c
44453472 155538 1 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404259 155538 1 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
54586021 62543 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 494 4 0 5 4.1 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N2CCC3COCCC32)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782375 62543 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 494 4 0 5 4.1 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N2CCC3COCCC32)C1 10.1016/j.bmcl.2011.01.034
57396723 68946 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 457 6 2 3 3.5 NC(=O)C(NC1CCc2ccccc21)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922804 68946 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 457 6 2 3 3.5 NC(=O)C(NC1CCc2ccccc21)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
10360623 85206 5 None - 1 Human 4.6 pIC50 = 4.6 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 351 4 1 3 5.0 Clc1ccc(CN2CCCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
CHEMBL225492 85206 5 None - 1 Human 4.6 pIC50 = 4.6 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 351 4 1 3 5.0 Clc1ccc(CN2CCCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
44447424 94608 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 CC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL252206 94608 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 CC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
44583280 172449 0 None - 1 Human 7.6 pIC50 = 7.6 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 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 7.6 pIC50 = 7.6 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 640 9 3 6 4.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
10281316 73722 0 None -2 3 Human 7.6 pIC50 = 7.6 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 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1016/j.bmcl.2012.03.007
CHEMBL2018386 73722 0 None -2 3 Human 7.6 pIC50 = 7.6 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 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1016/j.bmcl.2012.03.007
44453327 95095 25 None - 1 Human 7.6 pIC50 = 7.6 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 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL255408 95095 25 None - 1 Human 7.6 pIC50 = 7.6 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 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
10162782 73706 0 None - 1 Human 6.6 pIC50 = 6.6 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 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018370 73706 0 None - 1 Human 6.6 pIC50 = 6.6 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 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
44442590 93772 0 None 169 2 Human 6.6 pIC50 = 6.6 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 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247455 93772 0 None 169 2 Human 6.6 pIC50 = 6.6 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 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
49763804 65425 0 None - 1 Human 6.6 pIC50 = 6.6 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 528 7 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(N4CCCC4)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829616 65425 0 None - 1 Human 6.6 pIC50 = 6.6 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 528 7 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(N4CCCC4)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
11510932 75202 0 None - 1 Human 6.6 pIC50 = 6.6 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 460 5 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(Cc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036753 75202 0 None - 1 Human 6.6 pIC50 = 6.6 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 460 5 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(Cc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
145962732 161357 0 None - 1 Human 5.6 pIC50 = 5.6 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 554 8 0 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Oc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4126032 161357 0 None - 1 Human 5.6 pIC50 = 5.6 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 554 8 0 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Oc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
44580591 187859 0 None - 1 Human 7.6 pIC50 = 7.6 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 9 4 6 3.1 CCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL496344 187859 0 None - 1 Human 7.6 pIC50 = 7.6 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 9 4 6 3.1 CCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
49763682 65421 0 None - 1 Human 7.6 pIC50 = 7.6 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 489 7 2 4 4.0 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
CHEMBL1829612 65421 0 None - 1 Human 7.6 pIC50 = 7.6 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 489 7 2 4 4.0 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
44447432 154848 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CCC(CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL400517 154848 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CCC(CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44447432 154848 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CCC(CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL400517 154848 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CCC(CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
50991056 62566 0 None - 1 Human 7.6 pIC50 = 7.6 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(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782572 62566 0 None - 1 Human 7.6 pIC50 = 7.6 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(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
57394966 68927 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 495 6 2 2 6.2 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CNC2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922785 68927 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 495 6 2 2 6.2 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CNC2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2011.09.113
145953092 161338 0 None - 1 Human 5.6 pIC50 = 5.6 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 539 8 1 6 3.9 CN(C1CCN(CCCN2CCc3cnc(Nc4ccc(Cl)c(Cl)c4)cc3C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4125768 161338 0 None - 1 Human 5.6 pIC50 = 5.6 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 539 8 1 6 3.9 CN(C1CCN(CCCN2CCc3cnc(Nc4ccc(Cl)c(Cl)c4)cc3C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
22143309 187941 0 None - 1 Human 7.6 pIC50 = 7.6 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 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL496959 187941 0 None - 1 Human 7.6 pIC50 = 7.6 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 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
10111333 175467 0 None 19 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4577133 175467 0 None 19 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10142792 93741 0 None 26 2 Human 6.6 pIC50 = 6.6 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 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247245 93741 0 None 26 2 Human 6.6 pIC50 = 6.6 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 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
57656869 75221 0 None - 1 Human 6.6 pIC50 = 6.6 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 412 4 1 4 3.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@H]2CN(C3CC3)CCO2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036774 75221 0 None - 1 Human 6.6 pIC50 = 6.6 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 412 4 1 4 3.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@H]2CN(C3CC3)CCO2)CC1 10.1016/j.bmcl.2012.04.118
52943756 19290 0 None -23 2 Mouse 6.6 pIC50 = 6.6 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 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 Mouse 6.6 pIC50 = 6.6 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 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
49764196 65442 0 None - 1 Human 7.6 pIC50 = 7.6 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 519 6 3 6 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829633 65442 0 None - 1 Human 7.6 pIC50 = 7.6 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 519 6 3 6 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
44570717 183832 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 544 8 3 4 4.2 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL480620 183832 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 544 8 3 4 4.2 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.12.062
56676474 65812 0 None - 1 Human 7.6 pIC50 = 7.6 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 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834854 65812 0 None - 1 Human 7.6 pIC50 = 7.6 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 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
183790 3742 11 None -1 5 Human 7.6 pIC50 = 7.6 Functional
Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/s0960-894x(00)00347-4
783 3742 11 None -1 5 Human 7.6 pIC50 = 7.6 Functional
Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/s0960-894x(00)00347-4
CHEMBL1178786 3742 11 None -1 5 Human 7.6 pIC50 = 7.6 Functional
Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/s0960-894x(00)00347-4
44425309 142357 0 None - 1 Human 7.6 pIC50 = 7.6 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@@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388867 142357 0 None - 1 Human 7.6 pIC50 = 7.6 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@@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
183790 3742 11 None -1 5 Human 7.6 pIC50 = 7.6 Functional
Inhibition of chemotactic protein to CCR2bInhibition of chemotactic protein to CCR2b
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm010468s
783 3742 11 None -1 5 Human 7.6 pIC50 = 7.6 Functional
Inhibition of chemotactic protein to CCR2bInhibition of chemotactic protein to CCR2b
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm010468s
CHEMBL1178786 3742 11 None -1 5 Human 7.6 pIC50 = 7.6 Functional
Inhibition of chemotactic protein to CCR2bInhibition of chemotactic protein to CCR2b
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm010468s
183790 3742 11 None -1 5 Human 7.6 pIC50 = 7.6 Functional
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3742 11 None -1 5 Human 7.6 pIC50 = 7.6 Functional
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3742 11 None -1 5 Human 7.6 pIC50 = 7.6 Functional
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
22143334 187808 0 None - 1 Human 7.6 pIC50 = 7.6 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 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL495924 187808 0 None - 1 Human 7.6 pIC50 = 7.6 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 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
57344297 68953 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2F)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922815 68953 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2F)CC1 10.1016/j.bmcl.2011.09.113
11711078 75220 0 None - 1 Human 6.6 pIC50 = 6.6 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 400 4 1 4 2.9 CCN1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036773 75220 0 None - 1 Human 6.6 pIC50 = 6.6 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 400 4 1 4 2.9 CCN1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
46240584 83580 0 None - 1 Human 7.6 pIC50 = 7.6 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 532 6 3 6 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nc4ccccc4s3)CC2)C1 10.1021/ml300260s
CHEMBL2204262 83580 0 None - 1 Human 7.6 pIC50 = 7.6 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 532 6 3 6 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nc4ccccc4s3)CC2)C1 10.1021/ml300260s
46944854 65429 0 None - 1 Human 7.6 pIC50 = 7.6 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 COc1cnccc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
CHEMBL1829620 65429 0 None - 1 Human 7.6 pIC50 = 7.6 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 COc1cnccc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
54756156 65785 0 None - 1 Human 7.6 pIC50 = 7.6 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 507 9 2 7 3.6 C=CCn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(=O)OCC)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834779 65785 0 None - 1 Human 7.6 pIC50 = 7.6 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 507 9 2 7 3.6 C=CCn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(=O)OCC)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44447431 94671 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL252611 94671 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44425642 142346 0 None 12 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL388675 142346 0 None 12 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44447431 94671 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL252611 94671 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44425642 142346 0 None 12 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL388675 142346 0 None 12 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
11678573 90639 0 None - 1 Human 6.6 pIC50 = 6.6 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 566 13 1 5 7.4 CCN(CC)CCCC(C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238936 90639 0 None - 1 Human 6.6 pIC50 = 6.6 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 566 13 1 5 7.4 CCN(CC)CCCC(C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
57656713 75205 0 None - 1 Human 6.6 pIC50 = 6.6 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 488 7 1 3 5.5 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036756 75205 0 None - 1 Human 6.6 pIC50 = 6.6 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 488 7 1 3 5.5 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
44447433 94694 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
CHEMBL252813 94694 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
44447433 94694 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
CHEMBL252813 94694 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
22143293 188027 0 None - 1 Human 6.5 pIC50 = 6.5 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 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497577 188027 0 None - 1 Human 6.5 pIC50 = 6.5 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 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
44447434 94695 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
CHEMBL252814 94695 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
44453535 155174 1 None - 1 Human 6.5 pIC50 = 6.5 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 473 6 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2Cl)C1 10.1016/j.bmcl.2008.02.015
CHEMBL402322 155174 1 None - 1 Human 6.5 pIC50 = 6.5 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 473 6 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2Cl)C1 10.1016/j.bmcl.2008.02.015
44447434 94695 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
CHEMBL252814 94695 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
155521447 170584 0 None 3 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4450561 170584 0 None 3 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
11227168 74550 0 None - 1 Human 7.5 pIC50 = 7.5 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 596 6 2 9 3.6 O=C(C1CCN(c2nccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029569 74550 0 None - 1 Human 7.5 pIC50 = 7.5 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 596 6 2 9 3.6 O=C(C1CCN(c2nccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
46884818 7871 0 None - 1 Human 7.5 pIC50 = 7.5 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)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089881 7871 0 None - 1 Human 7.5 pIC50 = 7.5 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)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
145963669 161559 0 None - 1 Human 5.5 pIC50 = 5.5 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 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3cc(Cl)cc(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128832 161559 0 None - 1 Human 5.5 pIC50 = 5.5 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 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3cc(Cl)cc(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
44416157 80595 0 None - 1 Human 8.5 pIC50 = 8.5 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 8 1 2 7.5 C[C@H]1CN(CC[C@H](CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL215020 80595 0 None - 1 Human 8.5 pIC50 = 8.5 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 8 1 2 7.5 C[C@H]1CN(CC[C@H](CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
22143309 187941 0 None - 1 Human 8.5 pIC50 = 8.5 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 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL496959 187941 0 None - 1 Human 8.5 pIC50 = 8.5 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 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
22143112 188445 0 None - 1 Human 8.5 pIC50 = 8.5 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 594 11 5 6 3.7 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC)C1 10.1016/j.bmcl.2008.07.123
CHEMBL502513 188445 0 None - 1 Human 8.5 pIC50 = 8.5 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 594 11 5 6 3.7 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC)C1 10.1016/j.bmcl.2008.07.123
57395219 71011 0 None - 1 Human 8.5 pIC50 = 8.5 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 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncc3)CC2)C1 10.1021/ml200030q
CHEMBL1951770 71011 0 None - 1 Human 8.5 pIC50 = 8.5 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 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncc3)CC2)C1 10.1021/ml200030q
11756884 19089 0 None 25 2 Human 8.5 pIC50 = 8.5 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 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289083 19089 0 None 25 2 Human 8.5 pIC50 = 8.5 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 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
54754969 65740 0 None - 1 Human 8.5 pIC50 = 8.5 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 515 6 3 6 4.2 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834632 65740 0 None - 1 Human 8.5 pIC50 = 8.5 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 515 6 3 6 4.2 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
44425645 86082 0 None 7 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL230933 86082 0 None 7 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44453442 97690 0 None - 1 Human 8.5 pIC50 = 8.5 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 434 6 3 4 2.7 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271290 97690 0 None - 1 Human 8.5 pIC50 = 8.5 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 434 6 3 4 2.7 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
44425645 86082 0 None 7 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL230933 86082 0 None 7 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
57395217 71009 0 None - 1 Human 8.5 pIC50 = 8.5 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 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccccn3)CC2)C1 10.1021/ml200030q
CHEMBL1951768 71009 0 None - 1 Human 8.5 pIC50 = 8.5 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 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccccn3)CC2)C1 10.1021/ml200030q
50992246 58471 2 None -1 5 Human 8.5 pIC50 = 8.5 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(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683074 58471 2 None -1 5 Human 8.5 pIC50 = 8.5 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(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
50992246 58471 2 None -1 5 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683074 58471 2 None -1 5 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
44593561 12663 0 None - 1 Human 8.5 pIC50 = 8.5 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 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL1187238 12663 0 None - 1 Human 8.5 pIC50 = 8.5 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 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494580 12663 0 None - 1 Human 8.5 pIC50 = 8.5 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 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
11192346 2024 57 None 1 3 Human 8.5 pIC50 = 8.5 Functional
Inhibition of CCR2-mediated calcium mobilizationInhibition of CCR2-mediated calcium mobilization
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 2024 57 None 1 3 Human 8.5 pIC50 = 8.5 Functional
Inhibition of CCR2-mediated calcium mobilizationInhibition of CCR2-mediated calcium mobilization
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 2024 57 None 1 3 Human 8.5 pIC50 = 8.5 Functional
Inhibition of CCR2-mediated calcium mobilizationInhibition of CCR2-mediated calcium mobilization
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
67011331 74545 0 None - 1 Human 8.5 pIC50 = 8.5 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 557 7 3 7 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncco4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029424 74545 0 None - 1 Human 8.5 pIC50 = 8.5 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 557 7 3 7 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncco4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
44425653 86229 0 None 4 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL231246 86229 0 None 4 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44425290 153531 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL397997 153531 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
11627639 94933 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CCR2 receptor expressed in THP1 cells assessed as MCP-1-induced calcium flux by chemotaxis assayAntagonist activity at CCR2 receptor expressed in THP1 cells assessed as MCP-1-induced calcium flux by chemotaxis assay
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL254355 94933 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CCR2 receptor expressed in THP1 cells assessed as MCP-1-induced calcium flux by chemotaxis assayAntagonist activity at CCR2 receptor expressed in THP1 cells assessed as MCP-1-induced calcium flux by chemotaxis assay
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
44425653 86229 0 None 4 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL231246 86229 0 None 4 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44425290 153531 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL397997 153531 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44453472 155538 1 None - 1 Human 8.4 pIC50 = 8.4 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 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404259 155538 1 None - 1 Human 8.4 pIC50 = 8.4 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 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
24801689 97794 0 None - 1 Human 8.4 pIC50 = 8.4 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 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 8.4 pIC50 = 8.4 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 651 9 5 6 3.5 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)cc1 10.1021/jm701488f
46830336 7850 0 None - 1 Human 8.4 pIC50 = 8.4 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 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 8.4 pIC50 = 8.4 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 567 8 2 5 2.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
11421712 74543 0 None - 1 Human 8.4 pIC50 = 8.4 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 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cnccn4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029421 74543 0 None - 1 Human 8.4 pIC50 = 8.4 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 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cnccn4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
10008367 2022 50 None 2 3 Human 8.4 pIC50 = 8.4 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 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
777 2022 50 None 2 3 Human 8.4 pIC50 = 8.4 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 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL1289316 2022 50 None 2 3 Human 8.4 pIC50 = 8.4 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 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL2426341 2022 50 None 2 3 Human 8.4 pIC50 = 8.4 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 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
44425647 86101 0 None 5 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL231039 86101 0 None 5 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
57395218 71010 0 None - 1 Human 8.4 pIC50 = 8.4 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 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnc3)CC2)C1 10.1021/ml200030q
CHEMBL1951769 71010 0 None - 1 Human 8.4 pIC50 = 8.4 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 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnc3)CC2)C1 10.1021/ml200030q
11192346 2024 57 None 1 3 Human 8.4 pIC50 = 8.4 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 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 1 3 Human 8.4 pIC50 = 8.4 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 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 1 3 Human 8.4 pIC50 = 8.4 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 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
50992246 58471 2 None -1 5 Human 8.4 pIC50 = 8.4 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(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683074 58471 2 None -1 5 Human 8.4 pIC50 = 8.4 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(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
508869 95440 1 None - 1 Human 8.4 pIC50 = 8.4 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 446 7 3 4 3.1 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257066 95440 1 None - 1 Human 8.4 pIC50 = 8.4 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 446 7 3 4 3.1 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
44425647 86101 0 None 5 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL231039 86101 0 None 5 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44425643 86042 0 None 14 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230722 86042 0 None 14 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
46241717 83567 0 None - 1 Human 7.5 pIC50 = 7.5 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 520 8 3 6 2.9 CCOc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204249 83567 0 None - 1 Human 7.5 pIC50 = 7.5 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 520 8 3 6 2.9 CCOc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
46208367 83581 13 None - 1 Human 7.5 pIC50 = 7.5 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)(c3cncs3)CC2)C1 10.1021/ml300260s
CHEMBL2204263 83581 13 None - 1 Human 7.5 pIC50 = 7.5 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)(c3cncs3)CC2)C1 10.1021/ml300260s
24801522 161137 0 None - 1 Human 7.5 pIC50 = 7.5 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 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 7.5 pIC50 = 7.5 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 573 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(I)cc1 10.1021/jm701488f
56657929 65792 0 None - 1 Human 7.5 pIC50 = 7.5 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 485 6 2 5 4.5 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccccc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834785 65792 0 None - 1 Human 7.5 pIC50 = 7.5 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 485 6 2 5 4.5 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccccc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
46842383 8345 0 None - 1 Human 7.5 pIC50 = 7.5 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 530 8 2 4 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092929 8345 0 None - 1 Human 7.5 pIC50 = 7.5 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 530 8 2 4 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
44425308 153706 0 None - 1 Human 7.5 pIC50 = 7.5 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
CHEMBL398150 153706 0 None - 1 Human 7.5 pIC50 = 7.5 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
10111333 175467 0 None 19 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4577133 175467 0 None 19 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
44425308 153706 0 None - 1 Human 7.5 pIC50 = 7.5 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
CHEMBL398150 153706 0 None - 1 Human 7.5 pIC50 = 7.5 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
54585107 62561 0 None - 1 Human 7.5 pIC50 = 7.5 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(c3ccnc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782567 62561 0 None - 1 Human 7.5 pIC50 = 7.5 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(c3ccnc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44353447 3775 0 None - 1 Human 6.5 pIC50 = 6.5 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 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
785 3775 0 None - 1 Human 6.5 pIC50 = 6.5 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 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
CHEMBL337246 3775 0 None - 1 Human 6.5 pIC50 = 6.5 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 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
137654404 158569 0 None - 1 Human 5.5 pIC50 = 5.5 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(=O)N(CC(C)C)CC(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)=C3)cc1 10.1016/j.ejmech.2017.04.046
CHEMBL4091736 158569 0 None - 1 Human 5.5 pIC50 = 5.5 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(=O)N(CC(C)C)CC(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)=C3)cc1 10.1016/j.ejmech.2017.04.046
44421922 144550 0 None - 1 Human 5.5 pIC50 = 5.5 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 321 4 3 4 3.2 Nc1cccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL390736 144550 0 None - 1 Human 5.5 pIC50 = 5.5 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 321 4 3 4 3.2 Nc1cccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
9836178 85077 2 None - 1 Human 4.5 pIC50 = 4.5 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 306 4 2 3 3.6 c1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)CC2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL224500 85077 2 None - 1 Human 4.5 pIC50 = 4.5 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 306 4 2 3 3.6 c1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)CC2)cc1 10.1016/j.bmc.2006.09.052
10245340 168937 5 None - 1 Human 4.5 pIC50 = 4.5 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
CHEMBL438783 168937 5 None - 1 Human 4.5 pIC50 = 4.5 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
67011331 74545 0 None - 1 Human 7.5 pIC50 = 7.5 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 557 7 3 7 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncco4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029424 74545 0 None - 1 Human 7.5 pIC50 = 7.5 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 557 7 3 7 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncco4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
57656657 75209 0 None - 1 Human 7.5 pIC50 = 7.5 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 444 4 1 3 4.4 O=C(Nc1ccc(C(F)(F)F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036760 75209 0 None - 1 Human 7.5 pIC50 = 7.5 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 444 4 1 3 4.4 O=C(Nc1ccc(C(F)(F)F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
56671792 65794 0 None - 1 Human 7.5 pIC50 = 7.5 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 472 6 3 5 3.9 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834787 65794 0 None - 1 Human 7.5 pIC50 = 7.5 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 472 6 3 5 3.9 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.08.074
162666730 182274 1 None 562 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182274 1 None 562 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
122181149 121837 0 None - 1 Human 6.5 pIC50 = 6.5 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 494 7 1 4 4.8 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589844 121837 0 None - 1 Human 6.5 pIC50 = 6.5 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 494 7 1 4 4.8 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.02.019
11534473 90699 0 None 117 2 Human 7.5 pIC50 = 7.5 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 14 1 5 8.0 CCN(CC)CCCC(NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)C(C)C 10.1016/j.bmcl.2006.10.060
CHEMBL239144 90699 0 None 117 2 Human 7.5 pIC50 = 7.5 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 14 1 5 8.0 CCN(CC)CCCC(NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)C(C)C 10.1016/j.bmcl.2006.10.060
10117480 73716 0 None - 1 Human 7.5 pIC50 = 7.5 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 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018380 73716 0 None - 1 Human 7.5 pIC50 = 7.5 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 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
70688149 75224 0 None - 1 Human 7.5 pIC50 = 7.5 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 413 4 2 4 2.8 CC(C)N1CCN[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036777 75224 0 None - 1 Human 7.5 pIC50 = 7.5 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 413 4 2 4 2.8 CC(C)N1CCN[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44296219 101314 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2
ChEMBL 435 4 1 5 5.2 Cc1ccc2c(c1)C1(CCN(CCc3nc(-c4ccc(F)cc4)oc3C)CC1)OC(=O)N2 10.1016/s0960-894x(00)00347-4
CHEMBL296609 101314 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2
ChEMBL 435 4 1 5 5.2 Cc1ccc2c(c1)C1(CCN(CCc3nc(-c4ccc(F)cc4)oc3C)CC1)OC(=O)N2 10.1016/s0960-894x(00)00347-4
44442598 154387 0 None - 1 Human 6.5 pIC50 = 6.5 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 465 9 5 5 1.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2N)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL398747 154387 0 None - 1 Human 6.5 pIC50 = 6.5 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 465 9 5 5 1.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2N)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
71452241 83568 0 None - 1 Human 7.5 pIC50 = 7.5 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 574 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OCC(F)(F)F)nc3)CC2)C1 10.1021/ml300260s
CHEMBL2204250 83568 0 None - 1 Human 7.5 pIC50 = 7.5 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 574 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OCC(F)(F)F)nc3)CC2)C1 10.1021/ml300260s
10120067 73729 0 None - 1 Human 7.5 pIC50 = 7.5 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 550 12 5 5 4.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018393 73729 0 None - 1 Human 7.5 pIC50 = 7.5 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 550 12 5 5 4.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)(C)C 10.1016/j.bmcl.2012.03.007
70689914 74552 0 None - 1 Human 7.5 pIC50 = 7.5 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 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 7.5 pIC50 = 7.5 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 552 6 2 9 3.0 N#Cc1ccnc(N2CCC(C(=O)N3CC[C@H](N[C@H]4CC[C@@](O)(c5ccc(-c6ncccn6)cn5)CC4)C3)CC2)c1 10.1021/ml200199c
70689915 74553 0 None - 1 Human 7.5 pIC50 = 7.5 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 611 6 3 9 3.3 O=C(N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1)C1(O)CCN(c2cc(C(F)(F)F)ccn2)CC1 10.1021/ml200199c
CHEMBL2029572 74553 0 None - 1 Human 7.5 pIC50 = 7.5 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 611 6 3 9 3.3 O=C(N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1)C1(O)CCN(c2cc(C(F)(F)F)ccn2)CC1 10.1021/ml200199c
162666730 182274 1 None 562 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182274 1 None 562 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
56659197 65804 0 None - 1 Human 7.5 pIC50 = 7.5 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 506 6 2 7 4.3 Cc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
CHEMBL1834797 65804 0 None - 1 Human 7.5 pIC50 = 7.5 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 506 6 2 7 4.3 Cc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
22725647 173699 0 None 52 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4535696 173699 0 None 52 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
155521447 170584 0 None 3 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4450561 170584 0 None 3 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
145954949 161644 0 None - 1 Human 6.5 pIC50 = 6.5 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 539 8 2 6 3.9 CS(=O)(=O)NC1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4130191 161644 0 None - 1 Human 6.5 pIC50 = 6.5 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 539 8 2 6 3.9 CS(=O)(=O)NC1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
10129343 173265 0 None - 1 Human 7.5 pIC50 = 7.5 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 642 11 3 6 5.2 CCN(CC)C(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL452509 173265 0 None - 1 Human 7.5 pIC50 = 7.5 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 642 11 3 6 5.2 CCN(CC)C(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
56668309 65776 0 None - 1 Human 7.5 pIC50 = 7.5 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 558 6 3 8 3.6 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834718 65776 0 None - 1 Human 7.5 pIC50 = 7.5 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 558 6 3 8 3.6 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
54756038 65778 0 None - 1 Human 7.5 pIC50 = 7.5 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 468 7 2 7 3.2 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3noc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834720 65778 0 None - 1 Human 7.5 pIC50 = 7.5 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 468 7 2 7 3.2 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3noc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
49763571 65418 0 None - 1 Human 7.5 pIC50 = 7.5 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 459 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829609 65418 0 None - 1 Human 7.5 pIC50 = 7.5 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 459 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
46945254 65435 0 None - 1 Human 7.5 pIC50 = 7.5 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 475 6 3 5 2.9 Nc1cccnc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
CHEMBL1829626 65435 0 None - 1 Human 7.5 pIC50 = 7.5 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 475 6 3 5 2.9 Nc1cccnc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
57344305 68939 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922797 68939 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44453373 97811 0 None - 1 Human 7.5 pIC50 = 7.5 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 435 7 2 4 2.8 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271935 97811 0 None - 1 Human 7.5 pIC50 = 7.5 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 435 7 2 4 2.8 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
54755079 65741 0 None - 1 Human 7.5 pIC50 = 7.5 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 528 8 4 5 3.5 NC(=O)Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cc1 10.1016/j.bmcl.2011.08.074
CHEMBL1834633 65741 0 None - 1 Human 7.5 pIC50 = 7.5 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 528 8 4 5 3.5 NC(=O)Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cc1 10.1016/j.bmcl.2011.08.074
3547 141373 71 None -8 8 Human 4.5 pIC50 = 4.5 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 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1016/j.bmc.2006.09.052
CHEMBL38380 141373 71 None -8 8 Human 4.5 pIC50 = 4.5 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 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1016/j.bmc.2006.09.052
CHEMBL541388 141373 71 None -8 8 Human 4.5 pIC50 = 4.5 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 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1016/j.bmc.2006.09.052
3547 141373 71 None -8 8 Human 4.5 pIC50 = 4.5 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1016/j.bmc.2006.10.028
CHEMBL38380 141373 71 None -8 8 Human 4.5 pIC50 = 4.5 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1016/j.bmc.2006.10.028
CHEMBL541388 141373 71 None -8 8 Human 4.5 pIC50 = 4.5 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1016/j.bmc.2006.10.028
122181236 121851 0 None 13 2 Human 6.5 pIC50 = 6.5 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 588 8 1 4 6.3 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589950 121851 0 None 13 2 Human 6.5 pIC50 = 6.5 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 588 8 1 4 6.3 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
11319072 74542 0 None - 1 Human 7.4 pIC50 = 7.4 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 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cncnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029420 74542 0 None - 1 Human 7.4 pIC50 = 7.4 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 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cncnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
57344296 68951 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922813 68951 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2011.09.113
23630215 62544 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782376 62544 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
44453134 98064 0 None - 1 Human 6.4 pIC50 = 6.4 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 455 7 2 4 3.4 O=C(CNC(=O)c1cccc(OC(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL273195 98064 0 None - 1 Human 6.4 pIC50 = 6.4 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 455 7 2 4 3.4 O=C(CNC(=O)c1cccc(OC(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
67220645 75230 0 None - 1 Human 6.4 pIC50 = 6.4 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 399 2 2 4 1.6 CN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036783 75230 0 None - 1 Human 6.4 pIC50 = 6.4 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 399 2 2 4 1.6 CN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44453298 155239 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 421 6 3 4 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL402723 155239 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 421 6 3 4 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
44442599 93649 0 None 31 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL246804 93649 0 None 31 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
11353843 74547 0 None - 1 Human 7.4 pIC50 = 7.4 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 594 6 2 7 4.8 O=C(C1CCN(c2cccc(C(F)(F)F)c2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029566 74547 0 None - 1 Human 7.4 pIC50 = 7.4 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 594 6 2 7 4.8 O=C(C1CCN(c2cccc(C(F)(F)F)c2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
56683121 65811 0 None - 1 Human 7.4 pIC50 = 7.4 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 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834853 65811 0 None - 1 Human 7.4 pIC50 = 7.4 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 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
10196988 169465 0 None - 1 Human 7.4 pIC50 = 7.4 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 628 10 4 6 4.8 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL442929 169465 0 None - 1 Human 7.4 pIC50 = 7.4 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 628 10 4 6 4.8 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
57401954 68959 0 None - 1 Human 7.4 pIC50 = 7.4 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/c2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922822 68959 0 None - 1 Human 7.4 pIC50 = 7.4 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/c2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
57656854 75228 0 None - 1 Human 7.4 pIC50 = 7.4 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 425 3 2 4 2.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C(=O)[C@H]2CN(C3CC3)CCN2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036781 75228 0 None - 1 Human 7.4 pIC50 = 7.4 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 425 3 2 4 2.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C(=O)[C@H]2CN(C3CC3)CCN2)CC1 10.1016/j.bmcl.2012.04.118
22143255 187858 0 None - 1 Human 7.4 pIC50 = 7.4 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 523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL496343 187858 0 None - 1 Human 7.4 pIC50 = 7.4 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 523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
10323427 79760 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2008.01.023
CHEMBL211775 79760 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2008.01.023
145953765 161525 0 None - 1 Human 5.4 pIC50 = 5.4 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 7 4.2 CN(C1CCN(CCCn2ccc3c(Nc4ccc(Cl)c(Cl)c4)nccc3c2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128372 161525 0 None - 1 Human 5.4 pIC50 = 5.4 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 7 4.2 CN(C1CCN(CCCn2ccc3c(Nc4ccc(Cl)c(Cl)c4)nccc3c2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
44442587 93809 0 None - 1 Human 7.4 pIC50 = 7.4 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 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCc2ccccc2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247608 93809 0 None - 1 Human 7.4 pIC50 = 7.4 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 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCc2ccccc2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
10323427 79760 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2008.01.023
CHEMBL211775 79760 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2008.01.023
10129343 173265 0 None - 1 Human 7.4 pIC50 = 7.4 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 642 11 3 6 5.2 CCN(CC)C(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL452509 173265 0 None - 1 Human 7.4 pIC50 = 7.4 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 642 11 3 6 5.2 CCN(CC)C(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
145962575 161468 0 None - 1 Human 6.4 pIC50 = 6.4 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 567 9 1 6 4.7 CCS(=O)(=O)N(C)C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4127580 161468 0 None - 1 Human 6.4 pIC50 = 6.4 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 567 9 1 6 4.7 CCS(=O)(=O)N(C)C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
10268598 58875 0 None - 1 Human 5.4 pIC50 = 5.4 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 334 2 3 5 2.7 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1ccc(O)c(Cl)c1 10.1021/jm1012903
CHEMBL1688877 58875 0 None - 1 Human 5.4 pIC50 = 5.4 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 334 2 3 5 2.7 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1ccc(O)c(Cl)c1 10.1021/jm1012903
10436083 79877 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL212306 79877 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
44415880 169339 0 None - 1 Human 8.4 pIC50 = 8.4 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 550 7 1 2 7.1 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL441856 169339 0 None - 1 Human 8.4 pIC50 = 8.4 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 550 7 1 2 7.1 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
46241010 83584 0 None - 1 Human 8.4 pIC50 = 8.4 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 540 8 3 7 3.3 CC(C)Oc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204266 83584 0 None - 1 Human 8.4 pIC50 = 8.4 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 540 8 3 7 3.3 CC(C)Oc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
56643545 68960 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 by chemotaxis functional assayAntagonist activity at CCR2 by chemotaxis functional assay
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922823 68960 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 by chemotaxis functional assayAntagonist activity at CCR2 by chemotaxis functional assay
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
10281316 73722 0 None 2 3 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 in mouse monocytes assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in mouse monocytes assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1016/j.bmcl.2012.03.007
CHEMBL2018386 73722 0 None 2 3 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 in mouse monocytes assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in mouse monocytes assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1016/j.bmcl.2012.03.007
25154827 174584 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 494 6 2 4 4.3 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL455683 174584 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 494 6 2 4 4.3 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
56657930 65793 0 None - 1 Human 8.4 pIC50 = 8.4 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 528 7 2 6 4.6 CN(C)c1cccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)c1 10.1016/j.bmcl.2011.08.074
CHEMBL1834786 65793 0 None - 1 Human 8.4 pIC50 = 8.4 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 528 7 2 6 4.6 CN(C)c1cccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)c1 10.1016/j.bmcl.2011.08.074
44425643 86042 0 None 14 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230722 86042 0 None 14 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
10120907 73724 0 None - 1 Human 8.4 pIC50 = 8.4 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 577 12 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018388 73724 0 None - 1 Human 8.4 pIC50 = 8.4 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 577 12 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCC1 10.1016/j.bmcl.2012.03.007
11227168 74550 0 None - 1 Human 8.4 pIC50 = 8.4 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 596 6 2 9 3.6 O=C(C1CCN(c2nccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029569 74550 0 None - 1 Human 8.4 pIC50 = 8.4 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 596 6 2 9 3.6 O=C(C1CCN(c2nccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
11527661 2021 30 None - 1 Human 8.3 pIC50 = 8.3 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 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
9045 2021 30 None - 1 Human 8.3 pIC50 = 8.3 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 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
CHEMBL1963131 2021 30 None - 1 Human 8.3 pIC50 = 8.3 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 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
11527661 2021 30 None - 1 Human 8.3 pIC50 = 8.3 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 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9045 2021 30 None - 1 Human 8.3 pIC50 = 8.3 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 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL1963131 2021 30 None - 1 Human 8.3 pIC50 = 8.3 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 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
22143346 172651 0 None - 1 Human 8.3 pIC50 = 8.3 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 634 11 4 6 4.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL449672 172651 0 None - 1 Human 8.3 pIC50 = 8.3 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 634 11 4 6 4.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)C1 10.1016/j.bmcl.2008.07.123
11753466 77640 0 None - 1 Human 8.3 pIC50 = 8.3 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 575 8 2 6 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C#N)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088380 77640 0 None - 1 Human 8.3 pIC50 = 8.3 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 575 8 2 6 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C#N)cc2)C1 10.1016/j.bmcl.2012.08.002
51039119 176217 33 None -1 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulationAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulation
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
CHEMBL4594419 176217 33 None -1 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulationAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulation
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
24801526 97616 0 None - 1 Human 8.3 pIC50 = 8.3 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 541 7 5 6 1.5 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(S(N)(=O)=O)cc1 10.1021/jm701488f
CHEMBL270959 97616 0 None - 1 Human 8.3 pIC50 = 8.3 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 541 7 5 6 1.5 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(S(N)(=O)=O)cc1 10.1021/jm701488f
11330837 74551 0 None - 1 Human 7.4 pIC50 = 7.4 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 596 6 2 9 3.6 O=C(C1CCN(c2cc(C(F)(F)F)ncn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029570 74551 0 None - 1 Human 7.4 pIC50 = 7.4 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 596 6 2 9 3.6 O=C(C1CCN(c2cc(C(F)(F)F)ncn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
56671925 65749 0 None - 1 Human 7.4 pIC50 = 7.4 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 481 7 2 7 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834640 65749 0 None - 1 Human 7.4 pIC50 = 7.4 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 481 7 2 7 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
22725647 173699 0 None 52 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4535696 173699 0 None 52 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
54582215 62560 0 None - 1 Human 7.4 pIC50 = 7.4 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(c3cncc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782566 62560 0 None - 1 Human 7.4 pIC50 = 7.4 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(c3cncc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
10436083 79877 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL212306 79877 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
9858433 85078 0 None - 1 Human 5.4 pIC50 = 5.4 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 324 4 2 3 3.8 Fc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL224509 85078 0 None - 1 Human 5.4 pIC50 = 5.4 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 324 4 2 3 3.8 Fc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
127025091 138210 0 None - 1 Human 7.4 pIC50 = 7.4 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 424 3 2 7 1.2 COc1sc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)(C)C)CCN3)CC2)nc1C 10.1039/C5MD00362H
CHEMBL3769934 138210 0 None - 1 Human 7.4 pIC50 = 7.4 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 424 3 2 7 1.2 COc1sc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)(C)C)CCN3)CC2)nc1C 10.1039/C5MD00362H
22143305 183612 0 None - 1 Human 7.4 pIC50 = 7.4 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 506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480228 183612 0 None - 1 Human 7.4 pIC50 = 7.4 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 506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44425306 142369 0 None - 1 Human 7.4 pIC50 = 7.4 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
CHEMBL388949 142369 0 None - 1 Human 7.4 pIC50 = 7.4 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
44453592 160055 24 None - 1 Human 6.4 pIC50 = 6.4 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 405 6 2 3 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL410829 160055 24 None - 1 Human 6.4 pIC50 = 6.4 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 405 6 2 3 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2)C1 10.1016/j.bmcl.2008.02.015
44453565 169007 0 None - 1 Human 6.4 pIC50 = 6.4 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 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2Cl)C1 10.1016/j.bmcl.2008.02.015
CHEMBL439252 169007 0 None - 1 Human 6.4 pIC50 = 6.4 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 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2Cl)C1 10.1016/j.bmcl.2008.02.015
49764447 65422 0 None - 1 Human 7.4 pIC50 = 7.4 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 475 6 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829613 65422 0 None - 1 Human 7.4 pIC50 = 7.4 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 475 6 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
24801525 97609 0 None - 1 Human 7.4 pIC50 = 7.4 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 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 7.4 pIC50 = 7.4 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 526 7 4 5 1.9 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
11598084 75204 0 None - 1 Human 7.4 pIC50 = 7.4 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 474 6 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036755 75204 0 None - 1 Human 7.4 pIC50 = 7.4 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 474 6 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
57656641 75222 0 None - 1 Human 7.4 pIC50 = 7.4 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 414 4 1 4 3.3 CC(C)N1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036775 75222 0 None - 1 Human 7.4 pIC50 = 7.4 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 414 4 1 4 3.3 CC(C)N1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44425306 142369 0 None - 1 Human 7.4 pIC50 = 7.4 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
CHEMBL388949 142369 0 None - 1 Human 7.4 pIC50 = 7.4 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
57656749 75210 0 None - 1 Human 6.4 pIC50 = 6.4 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 444 4 1 3 4.4 O=C(Nc1ccc(Cl)c(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036761 75210 0 None - 1 Human 6.4 pIC50 = 6.4 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 444 4 1 3 4.4 O=C(Nc1ccc(Cl)c(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
44413147 139713 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccsc1 10.1016/j.bmcl.2008.01.023
CHEMBL379818 139713 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccsc1 10.1016/j.bmcl.2008.01.023
44413147 139713 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccsc1 10.1016/j.bmcl.2008.01.023
CHEMBL379818 139713 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccsc1 10.1016/j.bmcl.2008.01.023
46241718 83571 0 None - 1 Human 7.4 pIC50 = 7.4 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 546 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OC4CCC4)nc3)CC2)C1 10.1021/ml300260s
CHEMBL2204253 83571 0 None - 1 Human 7.4 pIC50 = 7.4 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 546 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OC4CCC4)nc3)CC2)C1 10.1021/ml300260s
44453471 97870 0 None - 1 Human 7.4 pIC50 = 7.4 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 470 7 3 5 2.9 Nc1ccc(OC(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272283 97870 0 None - 1 Human 7.4 pIC50 = 7.4 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 470 7 3 5 2.9 Nc1ccc(OC(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
44453562 155654 0 None - 1 Human 7.4 pIC50 = 7.4 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 431 7 3 6 2.0 Nc1ccc([N+](=O)[O-])cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404837 155654 0 None - 1 Human 7.4 pIC50 = 7.4 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 431 7 3 6 2.0 Nc1ccc([N+](=O)[O-])cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
10312346 188462 0 None - 1 Human 7.4 pIC50 = 7.4 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 9 3 6 4.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502795 188462 0 None - 1 Human 7.4 pIC50 = 7.4 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 9 3 6 4.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N(C)C)cc1 10.1016/j.bmcl.2009.05.041
54581190 62562 0 None - 1 Human 7.4 pIC50 = 7.4 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(c3cncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782568 62562 0 None - 1 Human 7.4 pIC50 = 7.4 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(c3cncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
70696470 75218 0 None - 1 Human 5.4 pIC50 = 5.4 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 367 4 1 4 2.6 N#Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1 10.1016/j.bmcl.2012.04.118
CHEMBL2036769 75218 0 None - 1 Human 5.4 pIC50 = 5.4 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 367 4 1 4 2.6 N#Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1 10.1016/j.bmcl.2012.04.118
46241608 83569 0 None - 1 Human 7.4 pIC50 = 7.4 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 534 8 3 6 3.2 CC(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204251 83569 0 None - 1 Human 7.4 pIC50 = 7.4 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 534 8 3 6 3.2 CC(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
11756884 19089 0 None -25 2 Mouse 6.4 pIC50 = 6.4 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 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289083 19089 0 None -25 2 Mouse 6.4 pIC50 = 6.4 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 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
508729 95535 1 None - 1 Human 6.4 pIC50 = 6.4 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 416 7 2 5 2.4 O=C(CNC(=O)c1cccc([N+](=O)[O-])c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257510 95535 1 None - 1 Human 6.4 pIC50 = 6.4 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 416 7 2 5 2.4 O=C(CNC(=O)c1cccc([N+](=O)[O-])c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
145963612 161439 0 None - 1 Human 5.4 pIC50 = 5.4 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 448 6 1 5 4.2 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCOCC1 10.1016/j.bmc.2018.05.027
CHEMBL4127249 161439 0 None - 1 Human 5.4 pIC50 = 5.4 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 448 6 1 5 4.2 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCOCC1 10.1016/j.bmc.2018.05.027
54582216 62565 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 500 6 1 8 2.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782571 62565 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 500 6 1 8 2.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
54583186 62572 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 496 6 1 5 4.3 CCC1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782578 62572 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 496 6 1 5 4.3 CCC1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
122181151 121839 0 None 7 2 Human 6.3 pIC50 = 6.3 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 622 7 1 3 7.6 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589846 121839 0 None 7 2 Human 6.3 pIC50 = 6.3 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 622 7 1 3 7.6 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
54754722 65752 0 None - 1 Human 7.3 pIC50 = 7.3 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 439 6 3 6 2.4 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](CO)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834643 65752 0 None - 1 Human 7.3 pIC50 = 7.3 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 439 6 3 6 2.4 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](CO)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44453171 95737 0 None - 1 Human 6.3 pIC50 = 6.3 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 2 3 3.2 O=C(CNC(=O)c1cccc(Br)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL258364 95737 0 None - 1 Human 6.3 pIC50 = 6.3 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 2 3 3.2 O=C(CNC(=O)c1cccc(Br)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
57344221 68957 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 568 8 3 4 5.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922819 68957 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 568 8 3 4 5.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.09.113
145955877 161404 0 None - 1 Human 5.3 pIC50 = 5.3 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 503 8 1 6 3.1 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3cccc(F)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4126634 161404 0 None - 1 Human 5.3 pIC50 = 5.3 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 503 8 1 6 3.1 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3cccc(F)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
22143334 187808 0 None - 1 Human 8.3 pIC50 = 8.3 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 509 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL495924 187808 0 None - 1 Human 8.3 pIC50 = 8.3 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 509 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
10209478 73721 0 None - 1 Human 8.3 pIC50 = 8.3 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 551 12 6 5 3.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC 10.1016/j.bmcl.2012.03.007
CHEMBL2018385 73721 0 None - 1 Human 8.3 pIC50 = 8.3 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 551 12 6 5 3.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC 10.1016/j.bmcl.2012.03.007
11591776 145486 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL391459 145486 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2011.09.113
10239991 188447 0 None - 1 Human 8.3 pIC50 = 8.3 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 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 8.3 pIC50 = 8.3 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 585 10 3 6 4.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44593555 188784 0 None 2 2 Human 8.3 pIC50 = 8.3 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 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL505722 188784 0 None 2 2 Human 8.3 pIC50 = 8.3 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 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44453408 95438 0 None - 1 Human 8.3 pIC50 = 8.3 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 436 6 4 5 2.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257064 95438 0 None - 1 Human 8.3 pIC50 = 8.3 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 436 6 4 5 2.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
44573608 187551 0 None - 1 Human 8.3 pIC50 = 8.3 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 522 8 2 3 6.3 CCCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494540 187551 0 None - 1 Human 8.3 pIC50 = 8.3 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 522 8 2 3 6.3 CCCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
10167417 73725 0 None - 1 Human 8.3 pIC50 = 8.3 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 591 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018389 73725 0 None - 1 Human 8.3 pIC50 = 8.3 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 591 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCCC1 10.1016/j.bmcl.2012.03.007
44453440 97688 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271288 97688 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
44425293 153464 0 None - 1 Human 8.3 pIC50 = 8.3 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@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397948 153464 0 None - 1 Human 8.3 pIC50 = 8.3 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@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
22143155 188062 0 None - 1 Human 8.3 pIC50 = 8.3 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 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL497788 188062 0 None - 1 Human 8.3 pIC50 = 8.3 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 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
11330529 74540 0 None - 1 Human 8.3 pIC50 = 8.3 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 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cccnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029418 74540 0 None - 1 Human 8.3 pIC50 = 8.3 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 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cccnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
22143146 183906 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481202 183906 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44453298 155239 0 None - 1 Human 8.3 pIC50 = 8.3 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 421 6 3 4 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL402723 155239 0 None - 1 Human 8.3 pIC50 = 8.3 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 421 6 3 4 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
57396999 71018 0 None - 1 Human 8.3 pIC50 = 8.3 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 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
CHEMBL1951777 71018 0 None - 1 Human 8.3 pIC50 = 8.3 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 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
11192943 77624 0 None - 1 Human 8.2 pIC50 = 8.2 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 628 8 2 5 5.4 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088212 77624 0 None - 1 Human 8.2 pIC50 = 8.2 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 628 8 2 5 5.4 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.08.002
53322809 58457 0 None 13 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@@H]2CCOC[C@@H]2C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683060 58457 0 None 13 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@@H]2CCOC[C@@H]2C)C1 10.1016/j.bmcl.2011.01.015
57391765 71015 0 None - 1 Human 8.2 pIC50 = 8.2 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)(c3cccnn3)CC2)C1 10.1021/ml200030q
CHEMBL1951774 71015 0 None - 1 Human 8.2 pIC50 = 8.2 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)(c3cccnn3)CC2)C1 10.1021/ml200030q
69035439 77648 0 None - 1 Human 8.2 pIC50 = 8.2 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 576 7 1 5 5.2 CC(C)N(C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088388 77648 0 None - 1 Human 8.2 pIC50 = 8.2 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 576 7 1 5 5.2 CC(C)N(C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
57656833 75229 0 None 4 4 Human 8.2 pIC50 = 8.2 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 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 4 4 Human 8.2 pIC50 = 8.2 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 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
10323427 79760 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against CCR2 assessed as inhibition of MCP1-induced calcium flux in human monocytesAntagonist activity against CCR2 assessed as inhibition of MCP1-induced calcium flux in human monocytes
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2006.04.045
CHEMBL211775 79760 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against CCR2 assessed as inhibition of MCP1-induced calcium flux in human monocytesAntagonist activity against CCR2 assessed as inhibition of MCP1-induced calcium flux in human monocytes
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2006.04.045
57400160 68925 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 3 5.6 O=C(O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922783 68925 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 3 5.6 O=C(O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
54584109 62547 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 509 5 1 6 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782379 62547 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 509 5 1 6 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
44421868 85158 0 None - 1 Human 5.3 pIC50 = 5.3 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 296 4 2 4 3.2 c1coc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL225167 85158 0 None - 1 Human 5.3 pIC50 = 5.3 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 296 4 2 4 3.2 c1coc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
21098480 144143 0 None - 1 Human 5.3 pIC50 = 5.3 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 Clc1cccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL390389 144143 0 None - 1 Human 5.3 pIC50 = 5.3 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 Clc1cccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
145962604 161527 0 None - 1 Human 5.3 pIC50 = 5.3 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 541 8 1 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(C(C)(C)C)cc3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128399 161527 0 None - 1 Human 5.3 pIC50 = 5.3 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 541 8 1 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(C(C)(C)C)cc3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
11180383 77623 0 None - 1 Human 7.3 pIC50 = 7.3 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 550 8 2 5 4.6 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088211 77623 0 None - 1 Human 7.3 pIC50 = 7.3 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 550 8 2 5 4.6 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
22143200 187765 0 None - 1 Human 6.3 pIC50 = 6.3 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 480 8 4 5 2.8 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL495718 187765 0 None - 1 Human 6.3 pIC50 = 6.3 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 480 8 4 5 2.8 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.07.123
44442586 93811 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247621 93811 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
10164316 154792 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 506 9 4 4 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL400196 154792 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 506 9 4 4 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
56667036 65427 0 None - 1 Human 7.3 pIC50 = 7.3 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 460 6 2 4 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829618 65427 0 None - 1 Human 7.3 pIC50 = 7.3 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 460 6 2 4 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.06.080
56677288 65443 0 None - 1 Human 7.3 pIC50 = 7.3 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 517 6 3 5 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCC4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829634 65443 0 None - 1 Human 7.3 pIC50 = 7.3 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 517 6 3 5 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCC4)CC2)C1 10.1016/j.bmcl.2011.06.080
11409228 74534 0 None - 1 Human 7.3 pIC50 = 7.3 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 490 6 3 5 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccccn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029412 74534 0 None - 1 Human 7.3 pIC50 = 7.3 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 490 6 3 5 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccccn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
46842084 7915 0 None - 1 Human 6.3 pIC50 = 6.3 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 544 8 2 4 3.9 Cc1ccccc1C(=O)N1CCC(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
CHEMBL1090206 7915 0 None - 1 Human 6.3 pIC50 = 6.3 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 544 8 2 4 3.9 Cc1ccccc1C(=O)N1CCC(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
57396722 68944 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 536 4 3 3 5.0 O=C1NC2(CCC(c3c[nH]c4ccccc34)CC2)NC1C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922801 68944 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 536 4 3 3 5.0 O=C1NC2(CCC(c3c[nH]c4ccccc34)CC2)NC1C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
11721085 166859 0 None - 1 Human 7.3 pIC50 = 7.3 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 565 13 2 5 7.4 CCN(CC)CCCC(C)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL428559 166859 0 None - 1 Human 7.3 pIC50 = 7.3 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 565 13 2 5 7.4 CCN(CC)CCCC(C)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44353447 3775 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3775 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3775 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
46927116 65437 0 None - 1 Human 7.3 pIC50 = 7.3 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 475 6 3 4 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829628 65437 0 None - 1 Human 7.3 pIC50 = 7.3 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 475 6 3 4 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
57656871 75227 0 None - 1 Human 7.3 pIC50 = 7.3 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 413 3 2 4 2.0 CCN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036780 75227 0 None - 1 Human 7.3 pIC50 = 7.3 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 413 3 2 4 2.0 CCN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
145962608 161533 0 None - 1 Human 6.3 pIC50 = 6.3 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 486 8 1 7 2.4 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccccn3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128514 161533 0 None - 1 Human 6.3 pIC50 = 6.3 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 486 8 1 7 2.4 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccccn3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
46241509 83562 0 None - 1 Human 7.3 pIC50 = 7.3 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 506 7 3 6 2.5 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204244 83562 0 None - 1 Human 7.3 pIC50 = 7.3 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 506 7 3 6 2.5 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
44423283 85307 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human CCR2 receptor in human monocytes assessed as inhibition of chemotaxisAntagonist activity against human CCR2 receptor in human monocytes assessed as inhibition of chemotaxis
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
CHEMBL226065 85307 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human CCR2 receptor in human monocytes assessed as inhibition of chemotaxisAntagonist activity against human CCR2 receptor in human monocytes assessed as inhibition of chemotaxis
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
44442587 93809 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCc2ccccc2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247608 93809 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCc2ccccc2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
46944855 65434 0 None - 1 Human 7.2 pIC50 = 7.2 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](c3ccncc3O)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829625 65434 0 None - 1 Human 7.2 pIC50 = 7.2 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](c3ccncc3O)CC2)C1 10.1016/j.bmcl.2011.06.080
44416273 138941 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 496 6 1 2 6.2 O=C(CCCN1CCC2(C=Cc3ccccc32)CC1)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL378449 138941 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 496 6 1 2 6.2 O=C(CCCN1CCC2(C=Cc3ccccc32)CC1)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
44416273 138941 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 496 6 1 2 6.2 O=C(CCCN1CCC2(C=Cc3ccccc32)CC1)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL378449 138941 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 496 6 1 2 6.2 O=C(CCCN1CCC2(C=Cc3ccccc32)CC1)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
57656938 75215 0 None - 1 Human 6.2 pIC50 = 6.2 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 410 4 1 3 3.7 O=C(Nc1cccc(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036766 75215 0 None - 1 Human 6.2 pIC50 = 6.2 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 410 4 1 3 3.7 O=C(Nc1cccc(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
44442590 93772 0 None 169 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247455 93772 0 None 169 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442593 147200 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 549 11 5 5 3.7 CCNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL392814 147200 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 549 11 5 5 3.7 CCNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
11647276 75207 0 None - 1 Human 7.2 pIC50 = 7.2 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 412 4 1 3 4.3 CC(C)N1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036758 75207 0 None - 1 Human 7.2 pIC50 = 7.2 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 412 4 1 3 4.3 CC(C)N1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
70681778 75217 0 None - 1 Human 5.2 pIC50 = 5.2 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 367 4 1 4 2.6 N#Cc1cccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)c1 10.1016/j.bmcl.2012.04.118
CHEMBL2036768 75217 0 None - 1 Human 5.2 pIC50 = 5.2 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 367 4 1 4 2.6 N#Cc1cccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)c1 10.1016/j.bmcl.2012.04.118
11690139 75225 0 None - 1 Human 6.2 pIC50 = 6.2 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 412 3 1 3 3.4 CCN1CCC[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036778 75225 0 None - 1 Human 6.2 pIC50 = 6.2 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 412 3 1 3 3.4 CCN1CCC[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
57656719 75216 0 None - 1 Human 6.2 pIC50 = 6.2 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 410 4 1 3 3.7 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036767 75216 0 None - 1 Human 6.2 pIC50 = 6.2 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 410 4 1 3 3.7 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
56643545 68960 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 by calcium mobilization assayAntagonist activity at CCR2 by calcium mobilization assay
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922823 68960 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 by calcium mobilization assayAntagonist activity at CCR2 by calcium mobilization assay
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44580591 187859 0 None - 1 Human 8.2 pIC50 = 8.2 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 9 4 6 3.1 CCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL496344 187859 0 None - 1 Human 8.2 pIC50 = 8.2 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 9 4 6 3.1 CCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
44571218 183878 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481009 183878 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
22143258 183879 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 522 9 3 5 3.9 CSc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481010 183879 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 522 9 3 5 3.9 CSc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
11584094 188932 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 494 6 2 4 4.3 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL508015 188932 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 494 6 2 4 4.3 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
11613399 188945 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 526 6 2 4 5.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL508073 188945 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 526 6 2 4 5.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
11527661 2021 30 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human CCR2-mediated intracellular calcium mobilization by cell based assayInhibition of human CCR2-mediated intracellular calcium mobilization by cell based assay
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
9045 2021 30 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human CCR2-mediated intracellular calcium mobilization by cell based assayInhibition of human CCR2-mediated intracellular calcium mobilization by cell based assay
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
CHEMBL1963131 2021 30 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human CCR2-mediated intracellular calcium mobilization by cell based assayInhibition of human CCR2-mediated intracellular calcium mobilization by cell based assay
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
11353843 74547 0 None - 1 Human 8.2 pIC50 = 8.2 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 594 6 2 7 4.8 O=C(C1CCN(c2cccc(C(F)(F)F)c2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029566 74547 0 None - 1 Human 8.2 pIC50 = 8.2 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 594 6 2 7 4.8 O=C(C1CCN(c2cccc(C(F)(F)F)c2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
44453329 155351 0 None - 1 Human 8.2 pIC50 = 8.2 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 431 7 2 3 3.5 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL403281 155351 0 None - 1 Human 8.2 pIC50 = 8.2 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 431 7 2 3 3.5 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
53325639 58470 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683073 58470 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
54583111 62545 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 512 6 0 6 3.7 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782377 62545 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 512 6 0 6 3.7 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44583281 188235 0 None - 1 Human 8.2 pIC50 = 8.2 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 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 8.2 pIC50 = 8.2 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 626 9 3 6 4.5 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)cc1 10.1016/j.bmcl.2009.05.041
11421712 74543 0 None - 1 Human 8.2 pIC50 = 8.2 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 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cnccn4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029421 74543 0 None - 1 Human 8.2 pIC50 = 8.2 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 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cnccn4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
50925394 19328 0 None 2 2 Human 8.2 pIC50 = 8.2 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 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 Human 8.2 pIC50 = 8.2 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 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
53324304 58464 0 None 3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 497 6 1 5 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683067 58464 0 None 3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 497 6 1 5 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
46240484 83579 0 None - 1 Human 7.2 pIC50 = 7.2 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 496 6 3 6 2.8 Cc1cnc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204261 83579 0 None - 1 Human 7.2 pIC50 = 7.2 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 496 6 3 6 2.8 Cc1cnc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
57394969 68940 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 499 7 2 3 4.5 NC(=O)C(NC1CCC(c2ccccc2)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922798 68940 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 499 7 2 3 4.5 NC(=O)C(NC1CCC(c2ccccc2)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44421888 85193 0 None - 1 Human 5.2 pIC50 = 5.2 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(CN2CCC(Oc3ccc4[nH]ncc4c3)CC2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL225434 85193 0 None - 1 Human 5.2 pIC50 = 5.2 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(CN2CCC(Oc3ccc4[nH]ncc4c3)CC2)cc1 10.1016/j.bmc.2006.09.052
44421862 136380 0 None - 1 Human 5.2 pIC50 = 5.2 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 c1csc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL373512 136380 0 None - 1 Human 5.2 pIC50 = 5.2 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 c1csc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
145961982 161532 0 None 10 2 Human 7.2 pIC50 = 7.2 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 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128498 161532 0 None 10 2 Human 7.2 pIC50 = 7.2 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 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
122181237 121852 0 None - 1 Human 5.2 pIC50 = 5.2 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 574 7 2 4 6.0 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1cc(O)ccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
CHEMBL3589951 121852 0 None - 1 Human 5.2 pIC50 = 5.2 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 574 7 2 4 6.0 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1cc(O)ccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
46842232 7882 0 None - 1 Human 6.2 pIC50 = 6.2 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 544 8 2 4 3.9 Cc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL1089965 7882 0 None - 1 Human 6.2 pIC50 = 6.2 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 544 8 2 4 3.9 Cc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
11567495 75199 0 None - 1 Human 6.2 pIC50 = 6.2 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 CCN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036750 75199 0 None - 1 Human 6.2 pIC50 = 6.2 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 CCN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
24801526 97616 0 None - 1 Human 7.2 pIC50 = 7.2 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 541 7 5 6 1.5 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(S(N)(=O)=O)cc1 10.1021/jm701488f
CHEMBL270959 97616 0 None - 1 Human 7.2 pIC50 = 7.2 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 541 7 5 6 1.5 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(S(N)(=O)=O)cc1 10.1021/jm701488f
145953762 161434 0 None - 1 Human 6.2 pIC50 = 6.2 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 539 8 1 6 3.9 CN(C1CCN(CCCN2CCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4127135 161434 0 None - 1 Human 6.2 pIC50 = 6.2 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 539 8 1 6 3.9 CN(C1CCN(CCCN2CCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
10240278 172897 0 None - 1 Human 7.2 pIC50 = 7.2 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 654 10 4 6 5.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL451597 172897 0 None - 1 Human 7.2 pIC50 = 7.2 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 654 10 4 6 5.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
57344298 68952 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cccc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922814 68952 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cccc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44453409 95439 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257065 95439 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
57656715 75206 0 None - 1 Human 7.2 pIC50 = 7.2 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 410 4 1 3 4.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036757 75206 0 None - 1 Human 7.2 pIC50 = 7.2 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 410 4 1 3 4.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
57344315 68941 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 530 8 2 5 3.9 COc1ccc(C2CCC(NC(C(N)=O)C3CCN(C(=O)/C=C/c4cc(F)c(F)c(F)c4)CC3)CC2)cn1 10.1016/j.bmcl.2011.09.113
CHEMBL1922799 68941 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 530 8 2 5 3.9 COc1ccc(C2CCC(NC(C(N)=O)C3CCN(C(=O)/C=C/c4cc(F)c(F)c(F)c4)CC3)CC2)cn1 10.1016/j.bmcl.2011.09.113
44447436 154692 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 9 1 2 6.8 C=CCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL399717 154692 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 9 1 2 6.8 C=CCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
44447436 154692 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 9 1 2 6.8 C=CCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL399717 154692 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 9 1 2 6.8 C=CCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
46240785 83582 0 None - 1 Human 7.2 pIC50 = 7.2 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 510 7 3 6 3.1 CCc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204264 83582 0 None - 1 Human 7.2 pIC50 = 7.2 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 510 7 3 6 3.1 CCc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
23630215 62544 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782376 62544 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
54754724 65754 0 None - 1 Human 7.2 pIC50 = 7.2 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 479 9 2 6 3.6 C=CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834645 65754 0 None - 1 Human 7.2 pIC50 = 7.2 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 479 9 2 6 3.6 C=CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
54580190 62571 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 512 7 1 6 3.7 CCO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782577 62571 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 512 7 1 6 3.7 CCO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
46842235 7836 0 None - 1 Human 6.2 pIC50 = 6.2 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 598 8 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089629 7836 0 None - 1 Human 6.2 pIC50 = 6.2 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 598 8 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
49764322 65441 0 None - 1 Human 7.2 pIC50 = 7.2 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 505 7 3 5 3.1 COc1ccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
CHEMBL1829632 65441 0 None - 1 Human 7.2 pIC50 = 7.2 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 505 7 3 5 3.1 COc1ccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
11365166 74544 1 None - 1 Human 7.2 pIC50 = 7.2 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 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 7.2 pIC50 = 7.2 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 573 7 3 7 4.0 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4nccs4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
135981707 65790 0 None - 1 Human 7.2 pIC50 = 7.2 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 556 8 2 6 4.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNC3=NC(Cc4ccccc4)c4ccc(C(F)(F)F)cc43)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834783 65790 0 None - 1 Human 7.2 pIC50 = 7.2 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 556 8 2 6 4.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNC3=NC(Cc4ccccc4)c4ccc(C(F)(F)F)cc43)C2)CC1 10.1016/j.bmcl.2011.08.074
44425654 86230 0 None 2 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL231247 86230 0 None 2 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44425654 86230 0 None 2 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL231247 86230 0 None 2 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
57344316 68934 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 554 7 4 4 5.0 O=C(NO)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922792 68934 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 554 7 4 4 5.0 O=C(NO)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
46240687 83585 0 None - 1 Human 7.2 pIC50 = 7.2 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 528 7 3 7 3.2 CSc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204267 83585 0 None - 1 Human 7.2 pIC50 = 7.2 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 528 7 3 7 3.2 CSc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
44439166 90546 0 None - 1 Human 7.2 pIC50 = 7.2 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 595 12 5 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238731 90546 0 None - 1 Human 7.2 pIC50 = 7.2 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 595 12 5 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
122181144 121832 0 None 35 2 Human 6.2 pIC50 = 6.2 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 514 6 1 3 5.7 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2015.02.019
CHEMBL3589839 121832 0 None 35 2 Human 6.2 pIC50 = 6.2 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 514 6 1 3 5.7 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2015.02.019
10182382 93962 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 450 9 4 4 1.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248418 93962 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 450 9 4 4 1.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
22143293 188027 0 None - 1 Human 8.2 pIC50 = 8.2 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 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497577 188027 0 None - 1 Human 8.2 pIC50 = 8.2 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 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
44583282 172695 0 None - 1 Human 8.2 pIC50 = 8.2 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 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 8.2 pIC50 = 8.2 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 656 9 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCOCC2)cc1 10.1016/j.bmcl.2009.05.041
22143241 183250 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 510 8 3 4 3.8 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL479642 183250 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 510 8 3 4 3.8 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.12.062
56643545 68960 0 None - 1 Human 8.2 pIC50 = 8.2 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 8.2 pIC50 = 8.2 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
11591595 186157 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 512 6 2 4 4.5 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL487238 186157 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 512 6 2 4 4.5 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
54755560 65779 0 None - 1 Human 8.2 pIC50 = 8.2 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 495 8 2 7 3.4 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(CC)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834721 65779 0 None - 1 Human 8.2 pIC50 = 8.2 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 495 8 2 7 3.4 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(CC)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56661451 65798 0 None - 1 Human 8.2 pIC50 = 8.2 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 500 6 2 6 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834791 65798 0 None - 1 Human 8.2 pIC50 = 8.2 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 500 6 2 6 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
56683044 65802 0 None - 1 Human 8.2 pIC50 = 8.2 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 521 6 3 8 3.4 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834795 65802 0 None - 1 Human 8.2 pIC50 = 8.2 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 521 6 3 8 3.4 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
56662695 65805 0 None - 1 Human 8.2 pIC50 = 8.2 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 520 7 2 7 4.6 CCc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
CHEMBL1834798 65805 0 None - 1 Human 8.2 pIC50 = 8.2 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 520 7 2 7 4.6 CCc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
10232019 73730 0 None - 1 Human 8.1 pIC50 = 8.1 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 584 14 5 5 5.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NCc1ccccc1 10.1016/j.bmcl.2012.03.007
CHEMBL2018394 73730 0 None - 1 Human 8.1 pIC50 = 8.1 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 584 14 5 5 5.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NCc1ccccc1 10.1016/j.bmcl.2012.03.007
57398750 71016 0 None - 1 Human 8.1 pIC50 = 8.1 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)(c3ccnnc3)CC2)C1 10.1021/ml200030q
CHEMBL1951775 71016 0 None - 1 Human 8.1 pIC50 = 8.1 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)(c3ccnnc3)CC2)C1 10.1021/ml200030q
127025092 138223 0 None - 1 Human 8.1 pIC50 = 8.1 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 414 2 2 6 1.5 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ncc(Cl)s3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770125 138223 0 None - 1 Human 8.1 pIC50 = 8.1 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 414 2 2 6 1.5 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ncc(Cl)s3)CC2)C1 10.1039/C5MD00362H
10152864 187874 0 None - 1 Human 8.1 pIC50 = 8.1 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 543 8 3 6 3.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL496432 187874 0 None - 1 Human 8.1 pIC50 = 8.1 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 543 8 3 6 3.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
57391768 71013 0 None - 1 Human 8.1 pIC50 = 8.1 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)(c3ccncn3)CC2)C1 10.1021/ml200030q
CHEMBL1951772 71013 0 None - 1 Human 8.1 pIC50 = 8.1 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)(c3ccncn3)CC2)C1 10.1021/ml200030q
25022597 95339 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1 10.1016/j.bmcl.2008.02.015
CHEMBL256629 95339 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1 10.1016/j.bmcl.2008.02.015
44425633 86041 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL230721 86041 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44425633 86041 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL230721 86041 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
50991056 62566 0 None - 1 Human 8.1 pIC50 = 8.1 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 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782572 62566 0 None - 1 Human 8.1 pIC50 = 8.1 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 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
10008367 2022 50 None -2 3 Mouse 8.1 pIC50 = 8.1 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 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
777 2022 50 None -2 3 Mouse 8.1 pIC50 = 8.1 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 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL1289316 2022 50 None -2 3 Mouse 8.1 pIC50 = 8.1 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 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL2426341 2022 50 None -2 3 Mouse 8.1 pIC50 = 8.1 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 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
44425635 153532 0 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL398000 153532 0 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
46240585 83583 0 None - 1 Human 7.2 pIC50 = 7.2 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 524 7 3 6 3.6 CC(C)c1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204265 83583 0 None - 1 Human 7.2 pIC50 = 7.2 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 524 7 3 6 3.6 CC(C)c1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
44353447 3775 0 None - 1 Human 7.2 pIC50 = 7.2 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 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
785 3775 0 None - 1 Human 7.2 pIC50 = 7.2 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 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
CHEMBL337246 3775 0 None - 1 Human 7.2 pIC50 = 7.2 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 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
10272003 58879 1 None 2 3 Human 6.2 pIC50 = 6.2 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 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 Human 6.2 pIC50 = 6.2 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 395 2 2 5 3.4 Cc1nn(C)c2ncc(C(=O)NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc12 10.1021/jm1012903
10272003 58879 1 None 2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 395 2 2 5 3.4 Cc1nn(C)c2ncc(C(=O)NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc12 10.1021/jm1012903
CHEMBL1688888 58879 1 None 2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 395 2 2 5 3.4 Cc1nn(C)c2ncc(C(=O)NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc12 10.1021/jm1012903
21098469 142352 0 None - 1 Human 5.2 pIC50 = 5.2 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 Clc1ccccc1CN1CCC(Nc2ccc3[nH]ncc3c2)C1 10.1016/j.bmc.2006.09.052
CHEMBL388742 142352 0 None - 1 Human 5.2 pIC50 = 5.2 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 Clc1ccccc1CN1CCC(Nc2ccc3[nH]ncc3c2)C1 10.1016/j.bmc.2006.09.052
54585108 62563 0 None - 1 Human 7.2 pIC50 = 7.2 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(c3ccnc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782569 62563 0 None - 1 Human 7.2 pIC50 = 7.2 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(c3ccnc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
54583187 62574 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 484 5 2 6 2.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2O)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782580 62574 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 484 5 2 6 2.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2O)C1 10.1016/j.bmcl.2011.01.034
46885214 7698 0 None - 1 Human 6.2 pIC50 = 6.2 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(CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1)N1CCN(C(=O)c2ccccc2)CC1 10.1016/j.bmcl.2010.02.072
CHEMBL1088810 7698 0 None - 1 Human 6.2 pIC50 = 6.2 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(CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1)N1CCN(C(=O)c2ccccc2)CC1 10.1016/j.bmcl.2010.02.072
145960485 161551 0 None - 1 Human 6.1 pIC50 = 6.1 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 546 6 1 4 7.0 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC2(C=Cc3ccccc32)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4128742 161551 0 None - 1 Human 6.1 pIC50 = 6.1 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 546 6 1 4 7.0 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC2(C=Cc3ccccc32)CC1 10.1016/j.bmc.2018.05.027
44442586 93811 0 None - 1 Human 6.1 pIC50 = 6.1 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 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247621 93811 0 None - 1 Human 6.1 pIC50 = 6.1 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 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
54583112 62546 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 513 6 0 7 3.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782378 62546 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 513 6 0 7 3.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
46241826 83561 0 None - 1 Human 7.1 pIC50 = 7.1 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 490 6 3 5 2.8 Cc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204243 83561 0 None - 1 Human 7.1 pIC50 = 7.1 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 490 6 3 5 2.8 Cc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
145954490 161635 0 None - 1 Human 7.1 pIC50 = 7.1 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 519 8 1 6 3.6 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)cc3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4130047 161635 0 None - 1 Human 7.1 pIC50 = 7.1 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 519 8 1 6 3.6 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)cc3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
70693849 73731 0 None - 1 Human 7.1 pIC50 = 7.1 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 491 11 5 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNc1n[nH]c2ccc(C(F)(F)F)cc12 10.1016/j.bmcl.2012.03.007
CHEMBL2018395 73731 0 None - 1 Human 7.1 pIC50 = 7.1 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 491 11 5 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNc1n[nH]c2ccc(C(F)(F)F)cc12 10.1016/j.bmcl.2012.03.007
44453507 168978 0 None - 1 Human 7.1 pIC50 = 7.1 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 531 7 2 3 5.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2-c2ccc3ccccc3c2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL439062 168978 0 None - 1 Human 7.1 pIC50 = 7.1 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 531 7 2 3 5.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2-c2ccc3ccccc3c2)C1 10.1016/j.bmcl.2008.02.015
54583185 62564 0 None - 1 Human 7.1 pIC50 = 7.1 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(c3cc(C(F)(F)F)ncn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782570 62564 0 None - 1 Human 7.1 pIC50 = 7.1 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(c3cc(C(F)(F)F)ncn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
57393249 68961 0 None - 1 Human 6.1 pIC50 = 6.1 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
CHEMBL1922824 68961 0 None - 1 Human 6.1 pIC50 = 6.1 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
22143196 183987 0 None -3 2 Human 7.1 pIC50 = 7.1 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 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 7.1 pIC50 = 7.1 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 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 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481790 183987 0 None -3 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
57656825 75208 0 None - 1 Human 7.1 pIC50 = 7.1 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 394 4 1 3 3.5 O=C(Nc1ccc(F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036759 75208 0 None - 1 Human 7.1 pIC50 = 7.1 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 394 4 1 3 3.5 O=C(Nc1ccc(F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
46842086 7979 0 None - 1 Human 6.1 pIC50 = 6.1 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 544 8 2 4 3.9 Cc1cccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
CHEMBL1090548 7979 0 None - 1 Human 6.1 pIC50 = 6.1 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 544 8 2 4 3.9 Cc1cccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
122181145 121833 0 None 1 2 Human 5.1 pIC50 = 5.1 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 528 6 1 3 6.1 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589840 121833 0 None 1 2 Human 5.1 pIC50 = 5.1 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 528 6 1 3 6.1 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)O1 10.1016/j.bmc.2015.02.019
44413411 77738 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.4 CC1CCN(CCN[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1 10.1016/j.bmcl.2008.01.023
CHEMBL209002 77738 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.4 CC1CCN(CCN[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1 10.1016/j.bmcl.2008.01.023
44413411 77738 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.4 CC1CCN(CCN[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1 10.1016/j.bmcl.2008.01.023
CHEMBL209002 77738 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.4 CC1CCN(CCN[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1 10.1016/j.bmcl.2008.01.023
44453534 97881 0 None - 1 Human 7.1 pIC50 = 7.1 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 451 7 3 5 2.5 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)ccc1O 10.1016/j.bmcl.2008.02.015
CHEMBL272331 97881 0 None - 1 Human 7.1 pIC50 = 7.1 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 451 7 3 5 2.5 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)ccc1O 10.1016/j.bmcl.2008.02.015
44413144 139219 0 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
CHEMBL378784 139219 0 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
44413144 139219 0 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
CHEMBL378784 139219 0 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
145960924 161545 0 None - 1 Human 5.1 pIC50 = 5.1 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 581 10 1 6 4.2 CN(C1CCN(CCCN2CCCc3c(ccnc3NCCc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128658 161545 0 None - 1 Human 5.1 pIC50 = 5.1 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 581 10 1 6 4.2 CN(C1CCN(CCCN2CCCc3c(ccnc3NCCc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
162658125 181096 0 None 100 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181096 0 None 100 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
57335017 70338 0 None 1380 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.1% BSAAntagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.1% BSA
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944776 70338 0 None 1380 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.1% BSAAntagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.1% BSA
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
10142792 93741 0 None 26 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247245 93741 0 None 26 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
22143112 188445 0 None - 1 Human 8.1 pIC50 = 8.1 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 594 11 5 6 3.7 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC)C1 10.1016/j.bmcl.2008.07.123
CHEMBL502513 188445 0 None - 1 Human 8.1 pIC50 = 8.1 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 594 11 5 6 3.7 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC)C1 10.1016/j.bmcl.2008.07.123
22143305 183612 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480228 183612 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44570781 192565 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 515 8 4 4 3.7 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc3[nH]ccc3c2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL521275 192565 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 515 8 4 4 3.7 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc3[nH]ccc3c2)C1 10.1016/j.bmcl.2008.12.062
56664979 65743 0 None - 1 Human 8.1 pIC50 = 8.1 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 529 6 2 7 4.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834635 65743 0 None - 1 Human 8.1 pIC50 = 8.1 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 529 6 2 7 4.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44425635 153532 0 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL398000 153532 0 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
11421840 77638 0 None - 1 Human 8.1 pIC50 = 8.1 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 578 9 2 5 5.2 CCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088379 77638 0 None - 1 Human 8.1 pIC50 = 8.1 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 578 9 2 5 5.2 CCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
11273379 74548 0 None - 1 Human 8.1 pIC50 = 8.1 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(c2cccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029567 74548 0 None - 1 Human 8.1 pIC50 = 8.1 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(c2cccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
44453365 97527 0 None - 1 Human 8.1 pIC50 = 8.1 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 465 7 4 6 2.0 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
CHEMBL270435 97527 0 None - 1 Human 8.1 pIC50 = 8.1 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 465 7 4 6 2.0 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
53322810 58472 0 None 2 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683075 58472 0 None 2 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
44425630 86027 0 None 14 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230617 86027 0 None 14 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
9956238 60198 1 None 3 4 Human 7.1 pIC50 = 7.1 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 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 3 4 Human 7.1 pIC50 = 7.1 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 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 3 4 Human 7.1 pIC50 = 7.1 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 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
9956238 60198 1 None 3 4 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1688889 60198 1 None 3 4 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1739922 60198 1 None 3 4 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
21098478 142640 0 None - 1 Human 5.1 pIC50 = 5.1 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 Clc1cccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL389168 142640 0 None - 1 Human 5.1 pIC50 = 5.1 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 Clc1cccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
21098468 144673 0 None - 1 Human 5.1 pIC50 = 5.1 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 Clc1ccccc1CN1CCCC(Nc2ccc3[nH]ncc3c2)C1 10.1016/j.bmc.2006.09.052
CHEMBL390837 144673 0 None - 1 Human 5.1 pIC50 = 5.1 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 Clc1ccccc1CN1CCCC(Nc2ccc3[nH]ncc3c2)C1 10.1016/j.bmc.2006.09.052
68616341 73733 0 None - 1 Human 7.1 pIC50 = 7.1 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 479 11 4 4 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018397 73733 0 None - 1 Human 7.1 pIC50 = 7.1 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 479 11 4 4 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
57400161 68926 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 553 7 2 3 5.9 CN(C1CCC(c2c[nH]c3ccccc23)CC1)C(C(=O)O)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922784 68926 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 553 7 2 3 5.9 CN(C1CCC(c2c[nH]c3ccccc23)CC1)C(C(=O)O)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44442598 154387 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 465 9 5 5 1.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2N)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL398747 154387 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 465 9 5 5 1.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2N)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
11843812 79904 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL212423 79904 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
11606702 145754 0 None - 1 Human 7.1 pIC50 = 7.1 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 580 14 1 5 7.8 CCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL391662 145754 0 None - 1 Human 7.1 pIC50 = 7.1 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 580 14 1 5 7.8 CCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
57344307 68938 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922796 68938 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44413399 79529 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 CC1CCCCN1CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL211404 79529 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 CC1CCCCN1CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2008.01.023
11843812 79904 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL212423 79904 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
44413399 79529 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 CC1CCCCN1CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL211404 79529 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 CC1CCCCN1CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2008.01.023
10187492 147790 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 549 11 5 5 3.7 CCNc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H](CNCc1ccc(C)cc1C)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL393267 147790 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 549 11 5 5 3.7 CCNc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H](CNCc1ccc(C)cc1C)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
54754723 65753 0 None - 1 Human 7.1 pIC50 = 7.1 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 8 2 6 3.4 CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834644 65753 0 None - 1 Human 7.1 pIC50 = 7.1 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 8 2 6 3.4 CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
57394967 68928 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 509 6 2 2 6.5 CC(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922786 68928 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 509 6 2 2 6.5 CC(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44413137 78892 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1cccs1 10.1016/j.bmcl.2008.01.023
CHEMBL211292 78892 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1cccs1 10.1016/j.bmcl.2008.01.023
162658125 181096 0 None 100 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181096 0 None 100 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
44425308 153706 0 None - 1 Human 7.1 pIC50 = 7.1 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
CHEMBL398150 153706 0 None - 1 Human 7.1 pIC50 = 7.1 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
44413137 78892 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1cccs1 10.1016/j.bmcl.2008.01.023
CHEMBL211292 78892 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1cccs1 10.1016/j.bmcl.2008.01.023
155514261 169836 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4439854 169836 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
155514261 169836 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4439854 169836 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
11273379 74548 0 None - 1 Human 7.1 pIC50 = 7.1 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(c2cccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029567 74548 0 None - 1 Human 7.1 pIC50 = 7.1 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(c2cccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
122181150 121838 0 None 125 2 Human 7.1 pIC50 = 7.1 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 608 7 1 3 7.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
CHEMBL3589845 121838 0 None 125 2 Human 7.1 pIC50 = 7.1 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 608 7 1 3 7.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
781 3396 80 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3396 80 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3396 80 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
10165625 73728 0 None - 1 Human 8.1 pIC50 = 8.1 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 536 13 5 5 4.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018392 73728 0 None - 1 Human 8.1 pIC50 = 8.1 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 536 13 5 5 4.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)C 10.1016/j.bmcl.2012.03.007
46884898 7717 0 None - 1 Human 8.1 pIC50 = 8.1 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 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 8.1 pIC50 = 8.1 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 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
46885027 8421 0 None - 1 Human 8.1 pIC50 = 8.1 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 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 8.1 pIC50 = 8.1 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 531 8 2 5 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
53325460 58494 0 None 2 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 538 6 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(F)(F)F)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683190 58494 0 None 2 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 538 6 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(F)(F)F)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
56671923 65739 0 None - 1 Human 8.1 pIC50 = 8.1 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 471 6 3 4 4.5 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834631 65739 0 None - 1 Human 8.1 pIC50 = 8.1 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 471 6 3 4 4.5 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
44425630 86027 0 None 14 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230617 86027 0 None 14 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
127025089 138305 0 None - 1 Human 8.0 pIC50 = 8.0 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 398 2 2 6 1.0 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ncc(F)s3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770951 138305 0 None - 1 Human 8.0 pIC50 = 8.0 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 398 2 2 6 1.0 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ncc(F)s3)CC2)C1 10.1039/C5MD00362H
44453325 155541 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 466 7 4 6 2.1 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1O 10.1016/j.bmcl.2008.02.015
CHEMBL404269 155541 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 466 7 4 6 2.1 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1O 10.1016/j.bmcl.2008.02.015
57395216 71012 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)(c3ncccn3)CC2)C1 10.1021/ml200030q
CHEMBL1951771 71012 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)(c3ncccn3)CC2)C1 10.1021/ml200030q
44453372 155744 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 433 7 2 3 3.4 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL405633 155744 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 433 7 2 3 3.4 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
10281715 73723 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 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018387 73723 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 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
54582217 62570 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 512 7 1 6 3.7 CCO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782576 62570 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 512 7 1 6 3.7 CCO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
57344314 68930 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 553 7 2 4 5.7 COC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922788 68930 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 553 7 2 4 5.7 COC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
57394968 68929 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 525 7 3 3 5.5 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)NC2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922787 68929 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 525 7 3 3 5.5 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)NC2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2011.09.113
57391487 68935 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 540 7 3 4 4.6 NC(=O)C(NC1CCC(C2CNc3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922793 68935 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 540 7 3 4 4.6 NC(=O)C(NC1CCC(C2CNc3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
70692344 75198 0 None - 1 Human 6.0 pIC50 = 6.0 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 370 3 2 3 3.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(CC2CCCNC2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036749 75198 0 None - 1 Human 6.0 pIC50 = 6.0 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 370 3 2 3 3.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(CC2CCCNC2)CC1 10.1016/j.bmcl.2012.04.118
57398493 68950 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 473 6 4 3 4.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccccc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922811 68950 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 473 6 4 3 4.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccccc2)CC1 10.1016/j.bmcl.2011.09.113
44563071 186695 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 525 6 2 4 4.0 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ncccc23)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL488433 186695 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 525 6 2 4 4.0 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ncccc23)CC1 10.1016/j.bmcl.2008.10.061
11632418 75197 1 None - 1 Human 6.0 pIC50 = 6.0 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 384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036748 75197 1 None - 1 Human 6.0 pIC50 = 6.0 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 384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44415898 81121 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
CHEMBL215654 81121 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
44415898 81121 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
CHEMBL215654 81121 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
57344317 68932 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 552 7 3 3 5.3 CNC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922790 68932 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 552 7 3 3 5.3 CNC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
57344318 68933 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 566 7 2 3 5.6 CN(C)C(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922791 68933 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 566 7 2 3 5.6 CN(C)C(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44453327 95095 25 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 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL255408 95095 25 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 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2010.02.072
57393497 69132 0 None - 0 Human 6.0 pKd = 6 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 645 10 2 6 6.8 COc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924022 69132 0 None - 0 Human 6.0 pKd = 6 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 645 10 2 6 6.8 COc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
15985912 83975 0 None - 0 Human 5.0 pKd = 5 Functional
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-stimulated monocyte shape changeAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-stimulated monocyte shape change
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207081 83975 0 None - 0 Human 5.0 pKd = 5 Functional
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-stimulated monocyte shape changeAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-stimulated monocyte shape change
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
57400128 69125 0 None - 0 Human 5.9 pKd = 5.9 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 629 9 2 5 7.1 Cc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924015 69125 0 None - 0 Human 5.9 pKd = 5.9 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 629 9 2 5 7.1 Cc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
57400125 69114 0 None - 0 Human 5.8 pKd = 5.8 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924004 69114 0 None - 0 Human 5.8 pKd = 5.8 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
44180522 69134 0 None - 0 Human 6.6 pKd = 6.6 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 631 10 2 6 6.4 COc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924024 69134 0 None - 0 Human 6.6 pKd = 6.6 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 631 10 2 6 6.4 COc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
57393496 69131 0 None - 0 Human 5.6 pKd = 5.6 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 629 9 2 5 7.1 Cc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924021 69131 0 None - 0 Human 5.6 pKd = 5.6 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 629 9 2 5 7.1 Cc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
57656833 75229 0 None 4 4 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human CCR2 in human peripheral whole blood assessed as inhibition of MCP1-induced L-selectin sheddingAntagonist activity at human CCR2 in human peripheral whole blood assessed as inhibition of MCP1-induced L-selectin shedding
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036782 75229 0 None 4 4 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human CCR2 in human peripheral whole blood assessed as inhibition of MCP1-induced L-selectin sheddingAntagonist activity at human CCR2 in human peripheral whole blood assessed as inhibition of MCP1-induced L-selectin shedding
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
57393219 69122 0 None - 0 Human 5.5 pKd = 5.5 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 581 9 2 5 6.5 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924012 69122 0 None - 0 Human 5.5 pKd = 5.5 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 581 9 2 5 6.5 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
57400127 69124 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 616 9 2 6 6.2 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924014 69124 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 616 9 2 6 6.2 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
57393220 69126 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 645 10 2 6 6.8 COc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924016 69126 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 645 10 2 6 6.8 COc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
57397001 69128 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 615 9 2 5 6.7 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924018 69128 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 615 9 2 5 6.7 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
57400420 69129 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 631 10 2 6 6.4 COc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924019 69129 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 631 10 2 6 6.4 COc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
57393495 69130 0 None - 0 Human 5.4 pKd = 5.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 637 9 2 5 6.7 O=C(NCCN1CCC(F)(F)C1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924020 69130 0 None - 0 Human 5.4 pKd = 5.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 637 9 2 5 6.7 O=C(NCCN1CCC(F)(F)C1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
57400129 69127 0 None - 0 Human 6.3 pKd = 6.3 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 601 9 2 5 6.4 O=C(NCCN1CCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924017 69127 0 None - 0 Human 6.3 pKd = 6.3 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 601 9 2 5 6.4 O=C(NCCN1CCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
57395221 69133 0 None - 0 Human 6.3 pKd = 6.3 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 615 9 2 5 6.7 Cc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924023 69133 0 None - 0 Human 6.3 pKd = 6.3 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 615 9 2 5 6.7 Cc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
57398458 69123 0 None - 0 Human 6.2 pKd = 6.2 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 615 9 2 5 6.8 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924013 69123 0 None - 0 Human 6.2 pKd = 6.2 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 615 9 2 5 6.8 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
16124598 10729 0 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 472 6 2 5 5.3 O=C(O)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171008 10729 0 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 472 6 2 5 5.3 O=C(O)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798435 10703 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 472 6 2 5 5.3 O=C(O)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170828 10703 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 472 6 2 5 5.3 O=C(O)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2010.04.142
49798434 10702 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 490 6 2 5 5.5 O=C(O)c1c(F)cccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170827 10702 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 490 6 2 5 5.5 O=C(O)c1c(F)cccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798461 10693 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170725 10693 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
17756652 10730 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 473 6 2 6 4.7 O=C(O)c1cncc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171011 10730 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 473 6 2 6 4.7 O=C(O)c1cncc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2010.04.142
49798461 10693 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1170725 10693 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
57398458 69123 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 615 9 2 5 6.8 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924013 69123 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 615 9 2 5 6.8 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
57393220 69126 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 645 10 2 6 6.8 COc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924016 69126 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 645 10 2 6 6.8 COc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
15985914 83974 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serum
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207080 83974 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serum
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
15985914 83974 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serum
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207080 83974 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serum
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
15985912 83975 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serum
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207081 83975 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serum
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
57394938 69118 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924008 69118 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
57394938 69118 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924008 69118 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
49798291 10557 0 None - 0 Mouse 6.0 pKi = 6 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 428 6 2 5 4.5 N#Cc1ccc(Oc2ccccc2C(=O)O)c(NS(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1169652 10557 0 None - 0 Mouse 6.0 pKi = 6 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 428 6 2 5 4.5 N#Cc1ccc(Oc2ccccc2C(=O)O)c(NS(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2010.04.142
49798289 10650 0 None - 0 Mouse 6.0 pKi = 6 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1170391 10650 0 None - 0 Mouse 6.0 pKi = 6 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798289 10650 0 None - 0 Human 5.0 pKi = 5 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1170391 10650 0 None - 0 Human 5.0 pKi = 5 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798462 10596 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 463 5 1 5 5.7 O=S(=O)(Nc1cc(Cl)cnc1Oc1cncc(Cl)c1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1169994 10596 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 463 5 1 5 5.7 O=S(=O)(Nc1cc(Cl)cnc1Oc1cncc(Cl)c1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
44296310 188269 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 458 10 2 3 5.4 CN(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL49994 188269 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 458 10 2 3 5.4 CN(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
44296310 188269 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 458 10 2 3 5.4 CN(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL49994 188269 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 458 10 2 3 5.4 CN(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
44296310 188269 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 458 10 2 3 5.4 CN(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL49994 188269 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 458 10 2 3 5.4 CN(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
49798289 10650 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1170391 10650 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
9870980 154647 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL399472 154647 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
49798265 10728 0 None - 0 Human 4.9 pKi = 4.9 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171006 10728 0 None - 0 Human 4.9 pKi = 4.9 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798461 10693 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1170725 10693 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
57393218 69117 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924007 69117 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
9870980 154647 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL399472 154647 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
44296287 101687 0 None - 0 Human 4.9 pKi = 4.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 472 10 3 3 5.3 CC(=O)Nc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL299379 101687 0 None - 0 Human 4.9 pKi = 4.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 472 10 3 3 5.3 CC(=O)Nc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
57400125 69114 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924004 69114 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
57400126 69115 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924005 69115 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
44296265 194595 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 491 10 2 2 7.0 O=C(/C=C/c1ccc(-c2ccccc2)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL53131 194595 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 491 10 2 2 7.0 O=C(/C=C/c1ccc(-c2ccccc2)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296265 194595 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 491 10 2 2 7.0 O=C(/C=C/c1ccc(-c2ccccc2)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53131 194595 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 491 10 2 2 7.0 O=C(/C=C/c1ccc(-c2ccccc2)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296265 194595 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 491 10 2 2 7.0 O=C(/C=C/c1ccc(-c2ccccc2)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53131 194595 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 491 10 2 2 7.0 O=C(/C=C/c1ccc(-c2ccccc2)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
49798463 10597 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 454 5 1 6 4.9 N#Cc1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cn1 10.1016/j.bmcl.2010.04.142
CHEMBL1169995 10597 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 454 5 1 6 4.9 N#Cc1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cn1 10.1016/j.bmcl.2010.04.142
49798289 10650 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1170391 10650 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798347 10575 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.04.142
CHEMBL1169824 10575 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.04.142
49798323 10788 0 None - 0 Mouse 6.8 pKi = 6.8 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171760 10788 0 None - 0 Mouse 6.8 pKi = 6.8 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
19430534 10772 0 None - 0 Mouse 5.8 pKi = 5.8 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 471 6 2 4 5.7 O=C(O)c1ccccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171586 10772 0 None - 0 Mouse 5.8 pKi = 5.8 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 471 6 2 4 5.7 O=C(O)c1ccccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
57396690 69120 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924010 69120 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
57400128 69125 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 629 9 2 5 7.1 Cc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924015 69125 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 629 9 2 5 7.1 Cc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
44296501 101786 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 472 8 3 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(00)00347-4
CHEMBL300025 101786 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 472 8 3 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(00)00347-4
44296501 101786 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 472 8 3 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
CHEMBL300025 101786 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 472 8 3 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
44296501 101786 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 472 8 3 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
CHEMBL300025 101786 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 472 8 3 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
44296264 194594 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 471 9 2 2 6.6 CC(C)(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL53130 194594 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 471 9 2 2 6.6 CC(C)(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
44446951 94604 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 12 2 2 6.7 CCCCc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL252186 94604 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 12 2 2 6.7 CCCCc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
44446951 94604 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 12 2 2 6.7 CCCCc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL252186 94604 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 12 2 2 6.7 CCCCc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
49798438 10692 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 429 5 1 5 5.0 O=S(=O)(Nc1cc(Cl)cnc1Oc1cccnc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170722 10692 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 429 5 1 5 5.0 O=S(=O)(Nc1cc(Cl)cnc1Oc1cccnc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798323 10788 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171760 10788 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798464 10629 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 430 5 1 6 4.4 O=S(=O)(Nc1cc(Cl)cnc1Oc1cccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170187 10629 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 430 5 1 6 4.4 O=S(=O)(Nc1cc(Cl)cnc1Oc1cccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798264 10787 0 None - 0 Mouse 5.7 pKi = 5.7 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171758 10787 0 None - 0 Mouse 5.7 pKi = 5.7 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
57400129 69127 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 601 9 2 5 6.4 O=C(NCCN1CCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924017 69127 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 601 9 2 5 6.4 O=C(NCCN1CCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
57400125 69114 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924004 69114 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
57391450 69119 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924009 69119 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
44296268 101843 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 513 9 3 3 6.7 Cc1[nH]c2ccc(O)cc2c1C1CCN(CCCCCNC(=O)/C=C/c2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL300455 101843 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 513 9 3 3 6.7 Cc1[nH]c2ccc(O)cc2c1C1CCN(CCCCCNC(=O)/C=C/c2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(00)00347-4
57393496 69131 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 629 9 2 5 7.1 Cc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924021 69131 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 629 9 2 5 7.1 Cc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
57393497 69132 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 645 10 2 6 6.8 COc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924022 69132 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 645 10 2 6 6.8 COc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
49798437 10559 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 515 8 3 6 4.4 O=C(NCCO)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1169660 10559 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 515 8 3 6 4.4 O=C(NCCO)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
44296155 101502 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 455 7 2 2 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL297950 101502 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 455 7 2 2 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296155 101502 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 455 7 2 2 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL297950 101502 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 455 7 2 2 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
57391449 69116 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924006 69116 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
49798264 10787 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171758 10787 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798292 10558 0 None - 0 Mouse 6.6 pKi = 6.6 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 421 6 2 4 4.8 O=C(O)c1ccccc1Oc1ccc(F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1169653 10558 0 None - 0 Mouse 6.6 pKi = 6.6 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 421 6 2 4 4.8 O=C(O)c1ccccc1Oc1ccc(F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798265 10728 0 None - 0 Mouse 6.6 pKi = 6.6 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171006 10728 0 None - 0 Mouse 6.6 pKi = 6.6 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
57391450 69119 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924009 69119 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
44296155 101502 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 455 7 2 2 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL297950 101502 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 455 7 2 2 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
57394939 69121 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924011 69121 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
44296269 194735 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 440 9 2 3 5.2 N#Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL53557 194735 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 440 9 2 3 5.2 N#Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
44296269 194735 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 440 9 2 3 5.2 N#Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL53557 194735 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 440 9 2 3 5.2 N#Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
44296287 101687 0 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 472 10 3 3 5.3 CC(=O)Nc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL299379 101687 0 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 472 10 3 3 5.3 CC(=O)Nc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
57400127 69124 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 616 9 2 6 6.2 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924014 69124 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 616 9 2 6 6.2 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
49798436 10704 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 472 6 2 5 5.3 O=C(O)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1170829 10704 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 472 6 2 5 5.3 O=C(O)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2010.04.142
49798349 10791 0 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171786 10791 0 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798399 10700 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 438 6 2 5 4.7 O=C(O)c1ccccc1Oc1ncccc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170801 10700 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 438 6 2 5 4.7 O=C(O)c1ccccc1Oc1ncccc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798265 10728 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171006 10728 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
25110660 94796 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL253424 94796 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
25110660 94796 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL253424 94796 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
44296630 101365 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 493 9 2 2 6.1 O=C(/C=C/c1ccc(Br)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL297033 101365 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 493 9 2 2 6.1 O=C(/C=C/c1ccc(Br)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296630 101365 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 493 9 2 2 6.1 O=C(/C=C/c1ccc(Br)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL297033 101365 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 493 9 2 2 6.1 O=C(/C=C/c1ccc(Br)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296630 101365 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 493 9 2 2 6.1 O=C(/C=C/c1ccc(Br)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL297033 101365 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 493 9 2 2 6.1 O=C(/C=C/c1ccc(Br)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296366 189426 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3cc(O)ccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL51332 189426 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3cc(O)ccc23)CC1 10.1016/s0960-894x(00)00347-4
44296384 194933 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3cccc(O)c23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL54192 194933 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3cccc(O)c23)CC1 10.1016/s0960-894x(00)00347-4
49798292 10558 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 421 6 2 4 4.8 O=C(O)c1ccccc1Oc1ccc(F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1169653 10558 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 421 6 2 4 4.8 O=C(O)c1ccccc1Oc1ccc(F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798264 10787 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serum
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171758 10787 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serum
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798264 10787 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serum
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171758 10787 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serum
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798397 10698 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 439 6 2 6 4.1 O=C(O)c1ccccc1Oc1ncncc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170799 10698 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 439 6 2 6 4.1 O=C(O)c1ccccc1Oc1ncncc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798351 10793 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 341 5 2 4 3.2 CS(=O)(=O)Nc1cc(Cl)ccc1Oc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.142
CHEMBL1171788 10793 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 341 5 2 4 3.2 CS(=O)(=O)Nc1cc(Cl)ccc1Oc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.142
49798325 10806 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1c(Cl)cccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171938 10806 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1c(Cl)cccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
57400420 69129 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 631 10 2 6 6.4 COc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924019 69129 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 631 10 2 6 6.4 COc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
57391449 69116 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924006 69116 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
44296087 101655 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 483 9 2 2 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL299153 101655 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 483 9 2 2 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296087 101655 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL299153 101655 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296344 162554 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 513 9 2 4 6.4 Cn1cc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)c2cc(O)ccc21 10.1016/s0960-894x(00)00347-4
CHEMBL416833 162554 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 513 9 2 4 6.4 Cn1cc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)c2cc(O)ccc21 10.1016/s0960-894x(00)00347-4
44296087 101655 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL299153 101655 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296469 194758 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 471 9 2 2 6.2 O=C(Cc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL53779 194758 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 471 9 2 2 6.2 O=C(Cc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296409 194826 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccccc1Cl)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL53930 194826 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccccc1Cl)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296469 194758 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 9 2 2 6.2 O=C(Cc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53779 194758 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 9 2 2 6.2 O=C(Cc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296409 194826 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccccc1Cl)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53930 194826 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccccc1Cl)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296469 194758 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 9 2 2 6.2 O=C(Cc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53779 194758 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 9 2 2 6.2 O=C(Cc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296409 194826 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccccc1Cl)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53930 194826 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccccc1Cl)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296629 101679 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 541 9 2 2 6.0 O=C(/C=C/c1ccc(I)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL299322 101679 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 541 9 2 2 6.0 O=C(/C=C/c1ccc(I)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296629 101679 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 541 9 2 2 6.0 O=C(/C=C/c1ccc(I)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL299322 101679 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 541 9 2 2 6.0 O=C(/C=C/c1ccc(I)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296629 101679 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 541 9 2 2 6.0 O=C(/C=C/c1ccc(I)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL299322 101679 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 541 9 2 2 6.0 O=C(/C=C/c1ccc(I)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
49798350 10792 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 443 6 2 5 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)s1 10.1016/j.bmcl.2010.04.142
CHEMBL1171787 10792 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 443 6 2 5 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)s1 10.1016/j.bmcl.2010.04.142
10436045 3516 4 None - 1 Human 7.3 pKi = 7.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(00)00347-4
782 3516 4 None - 1 Human 7.3 pKi = 7.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(00)00347-4
CHEMBL432713 3516 4 None - 1 Human 7.3 pKi = 7.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(00)00347-4
10436045 3516 4 None - 1 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2007.12.072
782 3516 4 None - 1 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2007.12.072
CHEMBL432713 3516 4 None - 1 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2007.12.072
49798398 10699 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 438 6 2 5 4.7 O=C(O)c1ccccc1Oc1cnccc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170800 10699 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 438 6 2 5 4.7 O=C(O)c1ccccc1Oc1cnccc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798489 10733 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 434 5 1 6 4.6 Cc1ncccc1Oc1ncc(C#N)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171035 10733 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 434 5 1 6 4.6 Cc1ncccc1Oc1ncc(C#N)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
10436045 3516 4 None - 1 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2007.12.072
782 3516 4 None - 1 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2007.12.072
CHEMBL432713 3516 4 None - 1 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2007.12.072
49798325 10806 0 None - 0 Mouse 6.3 pKi = 6.3 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1c(Cl)cccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171938 10806 0 None - 0 Mouse 6.3 pKi = 6.3 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1c(Cl)cccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
25110679 168152 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 457 8 2 2 6.3 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(00)00347-4
CHEMBL433081 168152 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 457 8 2 2 6.3 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(00)00347-4
25110679 168152 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 457 8 2 2 6.3 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
CHEMBL433081 168152 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 457 8 2 2 6.3 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
25110679 168152 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 457 8 2 2 6.3 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
CHEMBL433081 168152 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 457 8 2 2 6.3 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
44296428 101761 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL299855 101761 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296428 101761 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL299855 101761 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296428 101761 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL299855 101761 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
25110564 194773 0 None - 0 Human 5.3 pKi = 5.3 Functional
Compound was evaluated for the antagonist activity against human C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against human C-C chemokine receptor type 2
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL53819 194773 0 None - 0 Human 5.3 pKi = 5.3 Functional
Compound was evaluated for the antagonist activity against human C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against human C-C chemokine receptor type 2
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(00)00347-4
25110564 194773 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL53819 194773 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(00)00347-4
25110564 194773 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL53819 194773 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2007.12.072
25110564 194773 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL53819 194773 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2007.12.072
44296398 188290 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 429 9 2 2 5.7 Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL50025 188290 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 429 9 2 2 5.7 Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
44296398 188290 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL50025 188290 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
44296410 194719 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1cccc(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL53476 194719 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1cccc(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296410 194719 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1cccc(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53476 194719 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1cccc(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296398 188290 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL50025 188290 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
44296410 194719 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1cccc(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53476 194719 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1cccc(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
10940216 191208 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 513 10 2 3 6.7 COc1ccc2[nH]cc(C3CCN(CCCCCNC(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1016/s0960-894x(00)00347-4
CHEMBL51895 191208 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 513 10 2 3 6.7 COc1ccc2[nH]cc(C3CCN(CCCCCNC(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1016/s0960-894x(00)00347-4
44296077 101884 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 485 10 2 2 6.6 O=C(CCc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL300744 101884 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 485 10 2 2 6.6 O=C(CCc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296077 101884 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 485 10 2 2 6.6 O=C(CCc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL300744 101884 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 485 10 2 2 6.6 O=C(CCc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44180522 69134 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 631 10 2 6 6.4 COc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924024 69134 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 631 10 2 6 6.4 COc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
57393219 69122 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 581 9 2 5 6.5 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924012 69122 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 581 9 2 5 6.5 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
57393495 69130 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 637 9 2 5 6.7 O=C(NCCN1CCC(F)(F)C1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924020 69130 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 637 9 2 5 6.7 O=C(NCCN1CCC(F)(F)C1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
57400126 69115 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924005 69115 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
49798265 10728 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171006 10728 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798291 10557 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 428 6 2 5 4.5 N#Cc1ccc(Oc2ccccc2C(=O)O)c(NS(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1169652 10557 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 428 6 2 5 4.5 N#Cc1ccc(Oc2ccccc2C(=O)O)c(NS(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2010.04.142
49798326 10746 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 417 6 2 4 4.9 Cc1ccc(NS(=O)(=O)c2ccc(Cl)cc2)c(Oc2ccccc2C(=O)O)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171207 10746 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 417 6 2 4 4.9 Cc1ccc(NS(=O)(=O)c2ccc(Cl)cc2)c(Oc2ccccc2C(=O)O)c1 10.1016/j.bmcl.2010.04.142
49798326 10746 0 None - 0 Mouse 6.2 pKi = 6.2 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 417 6 2 4 4.9 Cc1ccc(NS(=O)(=O)c2ccc(Cl)cc2)c(Oc2ccccc2C(=O)O)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171207 10746 0 None - 0 Mouse 6.2 pKi = 6.2 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 417 6 2 4 4.9 Cc1ccc(NS(=O)(=O)c2ccc(Cl)cc2)c(Oc2ccccc2C(=O)O)c1 10.1016/j.bmcl.2010.04.142
44296309 188628 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 431 9 3 3 5.1 O=C(/C=C/c1ccc(O)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL50301 188628 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 431 9 3 3 5.1 O=C(/C=C/c1ccc(O)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296309 188628 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 431 9 3 3 5.1 O=C(/C=C/c1ccc(O)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL50301 188628 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 431 9 3 3 5.1 O=C(/C=C/c1ccc(O)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296309 188628 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 431 9 3 3 5.1 O=C(/C=C/c1ccc(O)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL50301 188628 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 431 9 3 3 5.1 O=C(/C=C/c1ccc(O)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
9870980 204285 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL71297 204285 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
57394939 69121 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924011 69121 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
9870980 204285 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL71297 204285 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
44296154 189154 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 469 8 2 2 6.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL51094 189154 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 469 8 2 2 6.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296154 189154 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 469 8 2 2 6.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL51094 189154 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 469 8 2 2 6.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296154 189154 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 469 8 2 2 6.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL51094 189154 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 469 8 2 2 6.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
49798348 10775 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171614 10775 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.142
25110678 194547 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 467 8 2 2 5.7 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL52956 194547 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 467 8 2 2 5.7 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1016/s0960-894x(00)00347-4
25110678 194547 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 467 8 2 2 5.7 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL52956 194547 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 467 8 2 2 5.7 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1016/j.bmcl.2007.12.072
25110678 194547 0 None - 0 Human 5.1 pKi = 5.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 467 8 2 2 5.7 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL52956 194547 0 None - 0 Human 5.1 pKi = 5.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 467 8 2 2 5.7 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1016/j.bmcl.2007.12.072
44296137 101576 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 576 11 3 4 6.0 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(CCCCCNC(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1016/s0960-894x(00)00347-4
CHEMBL298562 101576 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 576 11 3 4 6.0 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(CCCCCNC(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1016/s0960-894x(00)00347-4
25110660 154872 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL400698 154872 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
57393218 69117 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924007 69117 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
15985912 83975 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serum
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207081 83975 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serum
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71214709 83978 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serum
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207084 83978 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serum
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71214709 83978 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serum
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207084 83978 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serum
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
25110660 154872 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL400698 154872 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
44296628 188715 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 483 9 2 2 6.4 O=C(/C=C/c1cccc(C(F)(F)F)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL50460 188715 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 483 9 2 2 6.4 O=C(/C=C/c1cccc(C(F)(F)F)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296266 194853 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 429 9 2 2 5.7 Cc1cccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)c1 10.1016/s0960-894x(00)00347-4
CHEMBL53991 194853 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 429 9 2 2 5.7 Cc1cccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)c1 10.1016/s0960-894x(00)00347-4
44296628 188715 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.4 O=C(/C=C/c1cccc(C(F)(F)F)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL50460 188715 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.4 O=C(/C=C/c1cccc(C(F)(F)F)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296266 194853 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1cccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)c1 10.1016/j.bmcl.2007.12.072
CHEMBL53991 194853 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1cccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)c1 10.1016/j.bmcl.2007.12.072
57396690 69120 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924010 69120 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
49798396 10758 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 439 6 2 6 4.1 O=C(O)c1ccccc1Oc1nccnc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171398 10758 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 439 6 2 6 4.1 O=C(O)c1ccccc1Oc1nccnc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
19430534 10772 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 471 6 2 4 5.7 O=C(O)c1ccccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171586 10772 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 471 6 2 4 5.7 O=C(O)c1ccccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
44296628 188715 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.4 O=C(/C=C/c1cccc(C(F)(F)F)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL50460 188715 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.4 O=C(/C=C/c1cccc(C(F)(F)F)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296266 194853 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1cccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)c1 10.1016/j.bmcl.2007.12.072
CHEMBL53991 194853 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1cccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)c1 10.1016/j.bmcl.2007.12.072
57397001 69128 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 615 9 2 5 6.7 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924018 69128 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 615 9 2 5 6.7 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
57395221 69133 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 615 9 2 5 6.7 Cc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924023 69133 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 615 9 2 5 6.7 Cc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
44296429 194706 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 415 9 2 2 5.3 O=C(/C=C/c1ccccc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL53402 194706 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 415 9 2 2 5.3 O=C(/C=C/c1ccccc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296429 194706 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 415 9 2 2 5.3 O=C(/C=C/c1ccccc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53402 194706 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 415 9 2 2 5.3 O=C(/C=C/c1ccccc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296429 194706 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 415 9 2 2 5.3 O=C(/C=C/c1ccccc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53402 194706 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 415 9 2 2 5.3 O=C(/C=C/c1ccccc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
8921 3138 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Calculated from ng/ml based on a mol weight of ~150kDa.Calculated from ng/ml based on a mol weight of ~150kDa.
Guide to Pharmacology None None None None None
11185 1991 42 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.
Guide to Pharmacology 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 None
25134303 1991 42 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.
Guide to Pharmacology 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 None
CHEMBL2178573 1991 42 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.
Guide to Pharmacology 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 None
DB16066 1991 42 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.
Guide to Pharmacology 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 None
769 827 0 None -28 3 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
769 827 0 None -28 3 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15207250
11192346 2024 57 None 1 3 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 24900280
9032 2024 57 None 1 3 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 24900280
CHEMBL2029422 2024 57 None 1 3 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 24900280
11527661 2021 30 None - 1 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 24900329
9045 2021 30 None - 1 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 24900329
CHEMBL1963131 2021 30 None - 1 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 24900329
776 853 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15207250
759 866 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
759 866 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9276730
759 866 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9346309
11597 674 5 None 11 2 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 34141082
23725180 674 5 None 11 2 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 34141082
CHEMBL4781426 674 5 None 11 2 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 34141082
46213922 546 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 3 2 4 1.8 O=C(N1CCN(CC1)C(=O)[C@@H]1NCCN(C1)C(C)C)Nc1ccc(c(c1)F)Cl None
57656761 546 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 3 2 4 1.8 O=C(N1CCN(CC1)C(=O)[C@@H]1NCCN(C1)C(C)C)Nc1ccc(c(c1)F)Cl None
7825 546 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 3 2 4 1.8 O=C(N1CCN(CC1)C(=O)[C@@H]1NCCN(C1)C(C)C)Nc1ccc(c(c1)F)Cl None
772 869 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
770 828 0 None -7 2 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
770 828 0 None -7 2 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9276730
68764898 672 2 None 3 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 25893046
9430 672 2 None 3 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 25893046
CHEMBL3577945 672 2 None 3 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 25893046
771 838 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10770925
771 838 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
771 838 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15207250
771 838 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9276730
771 838 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9346309
775 849 0 None -316 2 Human 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15207250
10000456 3389 33 None 1 2 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 390 3 1 3 4.8 O=C1Nc2ccccc2C2(O1)CCN(CC2)CCc1ccc(cc1)C(F)(F)F 10770925
779 3389 33 None 1 2 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 390 3 1 3 4.8 O=C1Nc2ccccc2C2(O1)CCN(CC2)CCc1ccc(cc1)C(F)(F)F 10770925
CHEMBL1593104 3389 33 None 1 2 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 390 3 1 3 4.8 O=C1Nc2ccccc2C2(O1)CCN(CC2)CCc1ccc(cc1)C(F)(F)F 10770925
774 3977 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
10008367 2022 50 None -2 3 Mouse 8.0 pIC50 None 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 16210643
777 2022 50 None -2 3 Mouse 8.0 pIC50 None 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 16210643
CHEMBL1289316 2022 50 None -2 3 Mouse 8.0 pIC50 None 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 16210643
CHEMBL2426341 2022 50 None -2 3 Mouse 8.0 pIC50 None 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 16210643
773 1937 0 None 12 2 Human 8.3 pIC50 None 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9789057
5071702 3392 0 None - 1 Human 8.5 pIC50 None 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 235 3 1 2 2.9 Clc1cccc(c1)Cn1cccc1C(=O)O 10770925
780 3392 0 None - 1 Human 8.5 pIC50 None 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 235 3 1 2 2.9 Clc1cccc(c1)Cn1cccc1C(=O)O 10770925
778 2468 0 None - 1 Human 8.8 pIC50 None 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600978
486830 4002 0 None 6 5 Human 9.1 pIC50 None 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9287217
768 4002 0 None 6 5 Human 9.1 pIC50 None 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9287217


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
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Value		 Assay
Type		 Assay
Description		 Source

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weight		 Rot
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 DOI
183790 3742 11 None -6 2 Human 10.5 pIC50 = 10.5 Binding
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
783 3742 11 None -6 2 Human 10.5 pIC50 = 10.5 Binding
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
CHEMBL1178786 3742 11 None -6 2 Human 10.5 pIC50 = 10.5 Binding
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
4410 3137 106 None - 1 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
65015 3137 106 None - 1 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
844 3137 106 None - 1 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
CHEMBL18442 3137 106 None - 1 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
DB06809 3137 106 None - 1 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
183790 3742 11 None -6 2 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
783 3742 11 None -6 2 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
CHEMBL1178786 3742 11 None -6 2 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
4410 3137 106 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
65015 3137 106 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
844 3137 106 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
CHEMBL18442 3137 106 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
DB06809 3137 106 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
68767577 109816 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 545 8 1 5 3.7 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233186 109816 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 545 8 1 5 3.7 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)C)C1 10.1016/j.bmcl.2014.02.013
68988296 109818 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 559 7 1 5 4.1 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233188 109818 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 559 7 1 5 4.1 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
11627840 95699 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 525 6 2 3 6.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL258205 95699 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 525 6 2 3 6.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
68764898 672 2 None - 3 Human 9.6 pIC50 = 9.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
9430 672 2 None - 3 Human 9.6 pIC50 = 9.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
CHEMBL3577945 672 2 None - 3 Human 9.6 pIC50 = 9.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
183790 3742 11 None -6 2 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MCP1 from CCR2 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
783 3742 11 None -6 2 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MCP1 from CCR2 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
CHEMBL1178786 3742 11 None -6 2 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MCP1 from CCR2 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
90656027 111126 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 557 4 1 5 4.6 CNC(=O)c1cccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4COc5ccc(C(F)(F)F)cc5C4)C3)CC2)c1 10.1016/j.bmcl.2014.03.036
CHEMBL3263286 111126 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 557 4 1 5 4.6 CNC(=O)c1cccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4COc5ccc(C(F)(F)F)cc5C4)C3)CC2)c1 10.1016/j.bmcl.2014.03.036
91884571 181460 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 471 5 3 5 2.5 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(C)(C)C)n2)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4764460 181460 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 471 5 3 5 2.5 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(C)(C)C)n2)C1=O 10.1021/acsmedchemlett.1c00082
46886055 8044 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 593 9 1 5 4.8 CCN(C(C)C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1090893 8044 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 593 9 1 5 4.8 CCN(C(C)C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
68767577 109816 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 545 8 1 5 3.7 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233186 109816 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 545 8 1 5 3.7 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)C)C1 10.1016/j.bmcl.2014.02.013
10289827 187976 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 571 9 2 6 3.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL497202 187976 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 571 9 2 6 3.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
46886536 8306 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 593 8 1 5 4.7 Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1092678 8306 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 593 8 1 5 4.7 Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)cc1 10.1016/j.bmcl.2010.03.035
154572822 171101 1 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 542 7 2 7 2.8 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](NS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
CHEMBL4457723 171101 1 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 542 7 2 7 2.8 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](NS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
16064151 121239 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 491 6 1 5 5.2 CC(C)[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
CHEMBL3577948 121239 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 491 6 1 5 5.2 CC(C)[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
44425292 85968 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230281 85968 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
68764925 121237 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 477 6 1 5 4.9 CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
CHEMBL3577946 121237 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 477 6 1 5 4.9 CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
46865775 8114 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2014.02.013
CHEMBL1091605 8114 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2014.02.013
68769744 109817 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 533 8 1 5 4.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)c3)C2=O)[C@H](CS(=O)(=O)C(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233187 109817 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 533 8 1 5 4.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)c3)C2=O)[C@H](CS(=O)(=O)C(C)C)C1 10.1016/j.bmcl.2014.02.013
11192346 2024 57 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of CCR2-mediated Erk phosphorylationInhibition of CCR2-mediated Erk phosphorylation
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 2024 57 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of CCR2-mediated Erk phosphorylationInhibition of CCR2-mediated Erk phosphorylation
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 2024 57 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of CCR2-mediated Erk phosphorylationInhibition of CCR2-mediated Erk phosphorylation
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
68764925 121237 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 477 6 1 5 4.9 CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
CHEMBL3577946 121237 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 477 6 1 5 4.9 CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
68767049 121234 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 553 9 3 4 4.9 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NCC)C1=O 10.1021/ml500505q
CHEMBL3577942 121234 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 553 9 3 4 4.9 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NCC)C1=O 10.1021/ml500505q
162668957 182760 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 495 5 3 7 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(C)(C)C)nc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4790208 182760 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 495 5 3 7 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(C)(C)C)nc23)C1=O 10.1021/acsmedchemlett.1c00082
68769143 109814 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 531 8 1 5 3.3 CCS(=O)(=O)C[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(F)(F)F)c2)C1=O 10.1016/j.bmcl.2014.02.013
CHEMBL3233184 109814 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 531 8 1 5 3.3 CCS(=O)(=O)C[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(F)(F)F)c2)C1=O 10.1016/j.bmcl.2014.02.013
11643006 95274 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 618 8 3 5 5.3 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL256301 95274 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 618 8 3 5 5.3 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
11540494 95470 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 493 6 2 3 4.9 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL257191 95470 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 493 6 2 3 4.9 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11598 673 9 None - 1 Human 9.2 pIC50 = 9.2 Binding
Inhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assayInhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
23725177 673 9 None - 1 Human 9.2 pIC50 = 9.2 Binding
Inhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assayInhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
CHEMBL4442783 673 9 None - 1 Human 9.2 pIC50 = 9.2 Binding
Inhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assayInhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
11598 673 9 None - 1 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00082
23725177 673 9 None - 1 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00082
CHEMBL4442783 673 9 None - 1 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00082
68767802 109811 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 506 7 1 6 2.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233181 109811 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 506 7 1 6 2.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
68764898 672 2 None - 3 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
9430 672 2 None - 3 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
CHEMBL3577945 672 2 None - 3 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
68764898 672 2 None - 3 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
9430 672 2 None - 3 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
CHEMBL3577945 672 2 None - 3 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
11597 674 5 None - 0 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00082
23725180 674 5 None - 0 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00082
CHEMBL4781426 674 5 None - 0 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00082
46865774 8113 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1091604 8113 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
46886539 8349 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 597 8 1 5 4.5 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cc(F)cc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1092941 8349 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 597 8 1 5 4.5 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cc(F)cc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
46865774 8113 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
CHEMBL1091604 8113 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
44425294 143365 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 651 8 3 5 6.8 CNC(=O)Nc1nc([C@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL389771 143365 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 651 8 3 5 6.8 CNC(=O)Nc1nc([C@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
46865774 8113 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1021/ml500505q
CHEMBL1091604 8113 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1021/ml500505q
66767933 121225 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 531 12 6 5 3.2 CCC[C@H](O)[C@H](CNCC(C)(C)C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
CHEMBL3577933 121225 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 531 12 6 5 3.2 CCC[C@H](O)[C@H](CNCC(C)(C)C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
11192943 77624 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 628 8 2 5 5.4 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088212 77624 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 628 8 2 5 5.4 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.08.002
68772423 171964 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 541 7 1 7 3.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](CS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
CHEMBL4470701 171964 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 541 7 1 7 3.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](CS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
50925394 19328 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290636 19328 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
22143334 187808 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 509 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL495924 187808 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 509 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
68988296 109818 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 559 7 1 5 4.1 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233188 109818 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 559 7 1 5 4.1 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
11721374 94993 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 604 8 3 5 4.4 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL254772 94993 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 604 8 3 5 4.4 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
44448839 155454 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 526 6 3 4 4.7 Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL403889 155454 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 526 6 3 4 4.7 Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
44448879 155668 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 527 6 3 4 4.8 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL404904 155668 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 527 6 3 4 4.8 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
46865775 8114 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1091605 8114 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
46865775 8114 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2014.02.013
CHEMBL1091605 8114 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2014.02.013
57402219 71008 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
CHEMBL1951766 71008 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
68767049 121234 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 553 9 3 4 4.9 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NCC)C1=O 10.1021/ml500505q
CHEMBL3577942 121234 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 553 9 3 4 4.9 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NCC)C1=O 10.1021/ml500505q
68867935 109815 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 539 9 1 5 4.0 CCS(=O)(=O)C[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(-c3ccccc3)c2)C1=O 10.1016/j.bmcl.2014.02.013
CHEMBL3233185 109815 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 539 9 1 5 4.0 CCS(=O)(=O)C[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(-c3ccccc3)c2)C1=O 10.1016/j.bmcl.2014.02.013
11598 673 9 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
23725177 673 9 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
CHEMBL4442783 673 9 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
11598 673 9 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00082
23725177 673 9 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00082
CHEMBL4442783 673 9 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00082
66768099 121224 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 517 13 6 5 2.9 CCC[C@H](O)[C@H](CNCC(C)C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
CHEMBL3577932 121224 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 517 13 6 5 2.9 CCC[C@H](O)[C@H](CNCC(C)C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
69035439 77648 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 576 7 1 5 5.2 CC(C)N(C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088388 77648 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 576 7 1 5 5.2 CC(C)N(C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
68767124 109810 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 505 7 1 5 3.2 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233180 109810 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 505 7 1 5 3.2 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
68769143 109814 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 531 8 1 5 3.3 CCS(=O)(=O)C[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(F)(F)F)c2)C1=O 10.1016/j.bmcl.2014.02.013
CHEMBL3233184 109814 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 531 8 1 5 3.3 CCS(=O)(=O)C[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(F)(F)F)c2)C1=O 10.1016/j.bmcl.2014.02.013
89845025 109819 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 575 8 1 6 4.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(OC(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233189 109819 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 575 8 1 6 4.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(OC(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
44593562 187495 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 187495 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
46865774 8113 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1021/ml500505q
CHEMBL1091604 8113 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1021/ml500505q
68768923 109820 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 577 7 1 5 4.3 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cc(F)cc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233190 109820 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 577 7 1 5 4.3 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cc(F)cc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
10240064 188428 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 599 10 2 6 4.6 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502247 188428 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 599 10 2 6 4.6 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
10129192 188459 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 599 11 2 6 4.6 CCN(CC)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
CHEMBL502793 188459 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 599 11 2 6 4.6 CCN(CC)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
91884571 181460 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 471 5 3 5 2.5 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(C)(C)C)n2)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4764460 181460 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 471 5 3 5 2.5 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(C)(C)C)n2)C1=O 10.1021/acsmedchemlett.1c00082
10144709 166884 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 574 6 2 3 6.7 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL428602 166884 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 574 6 2 3 6.7 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2007.12.029
44425245 85776 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 608 7 2 5 6.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(N)n2)CCC12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL229316 85776 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 608 7 2 5 6.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(N)n2)CCC12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
44425281 153246 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 4 5 6.2 N=C(N)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397749 153246 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 4 5 6.2 N=C(N)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
11606411 85308 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
CHEMBL226066 85308 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
11598 673 9 None - 1 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1016/j.ejmech.2020.112736
23725177 673 9 None - 1 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1016/j.ejmech.2020.112736
CHEMBL4442783 673 9 None - 1 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1016/j.ejmech.2020.112736
57335017 70338 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944776 70338 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
10175425 193533 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 614 10 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL526752 193533 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 614 10 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2009.05.041
155531379 171605 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 532 7 1 5 2.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](N(C)S(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
CHEMBL4465351 171605 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 532 7 1 5 2.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](N(C)S(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
44454820 97890 8 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.016
CHEMBL272369 97890 8 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.016
44425293 153464 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397948 153464 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44423283 85307 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
CHEMBL226065 85307 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
44593563 193110 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
CHEMBL522688 193110 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
44593562 187495 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 187495 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
71768865 111122 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 499 3 0 4 4.8 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCO[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 10.1016/j.bmcl.2014.03.036
CHEMBL3263282 111122 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 499 3 0 4 4.8 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCO[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 10.1016/j.bmcl.2014.03.036
162666730 182274 1 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182274 1 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
162656188 180915 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 429 5 3 5 1.4 CN[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
CHEMBL4757857 180915 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 429 5 3 5 1.4 CN[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
24794583 181093 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 464 5 3 6 2.3 CN[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
CHEMBL4760098 181093 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 464 5 3 6 2.3 CN[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
44425254 142260 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388487 142260 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
16066354 121235 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 567 9 3 4 5.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C1=O 10.1021/ml500505q
CHEMBL3577943 121235 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 567 9 3 4 5.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C1=O 10.1021/ml500505q
122178128 121232 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 503 9 2 3 5.1 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CCc2ccccc2)C1 10.1021/ml500505q
CHEMBL3577940 121232 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 503 9 2 3 5.1 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CCc2ccccc2)C1 10.1021/ml500505q
42606792 109808 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 517 7 1 5 3.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233178 109808 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 517 7 1 5 3.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
42606792 109808 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 517 7 1 5 3.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
CHEMBL3233178 109808 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 517 7 1 5 3.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
44425250 86052 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 630 9 2 5 6.9 CC(=O)Nc1nc(C(CCN2CCC(c3ccc(F)cc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230790 86052 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 630 9 2 5 6.9 CC(=O)Nc1nc(C(CCN2CCC(c3ccc(F)cc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
16216716 153529 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397996 153529 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
22143255 187858 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL496343 187858 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
11753466 77640 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 575 8 2 6 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C#N)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088380 77640 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 575 8 2 6 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C#N)cc2)C1 10.1016/j.bmcl.2012.08.002
69035677 77649 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 590 8 1 5 5.6 CCN(C(C)C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088389 77649 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 590 8 1 5 5.6 CCN(C(C)C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
155529593 171455 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 518 7 2 5 2.2 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](NS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
CHEMBL4463290 171455 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 518 7 2 5 2.2 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](NS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
44425652 168768 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL437359 168768 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
50925394 19328 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290636 19328 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
52941377 19329 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290637 19329 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
68004034 86582 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315922 86582 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1 10.1016/j.bmcl.2012.12.017
76315270 84900 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 576 9 2 7 4.4 CCO[C@@H]1CN([C@H]2CC[C@@](O)(c3ccc4c(c3)OCO4)CC2)C[C@@H]1NC(=O)CCC(=O)c1cccc(C(F)(F)F)c1 10.1007/s00044-010-9497-9
CHEMBL2236474 84900 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 576 9 2 7 4.4 CCO[C@@H]1CN([C@H]2CC[C@@](O)(c3ccc4c(c3)OCO4)CC2)C[C@@H]1NC(=O)CCC(=O)c1cccc(C(F)(F)F)c1 10.1007/s00044-010-9497-9
162666730 182274 1 None - 1 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182274 1 None - 1 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
53389845 172961 0 None - 1 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4517518 172961 0 None - 1 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
11663882 95111 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 541 7 2 4 5.1 COc1cccc2c(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c[nH]c12 10.1016/j.bmcl.2008.05.010
CHEMBL255500 95111 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 541 7 2 4 5.1 COc1cccc2c(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c[nH]c12 10.1016/j.bmcl.2008.05.010
11713221 95601 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL257768 95601 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11606147 155343 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 525 6 2 3 5.7 O=C(/C=C/c1cccc(C(F)(F)F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL403250 155343 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 525 6 2 3 5.7 O=C(/C=C/c1cccc(C(F)(F)F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
44448807 155398 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 558 6 4 4 5.7 O=C(O)c1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)Nc5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL403581 155398 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 558 6 4 4 5.7 O=C(O)c1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)Nc5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
57656715 75206 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 410 4 1 3 4.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036757 75206 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 410 4 1 3 4.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
70693849 73731 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 491 11 5 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNc1n[nH]c2ccc(C(F)(F)F)cc12 10.1016/j.bmcl.2012.03.007
CHEMBL2018395 73731 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 491 11 5 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNc1n[nH]c2ccc(C(F)(F)F)cc12 10.1016/j.bmcl.2012.03.007
49763682 65421 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 489 7 2 4 4.0 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
CHEMBL1829612 65421 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 489 7 2 4 4.0 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
44441352 93383 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 509 7 1 2 6.8 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL245686 93383 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 509 7 1 2 6.8 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
44441347 93792 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 455 7 1 2 6.1 Cc1ccc(-c2ccc(/C=C/C(=O)Nc3ccc(C[N+](C)(C)C4CCOCC4)cc3)cc2)cc1 10.1016/j.bmcl.2007.01.115
CHEMBL247537 93792 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 455 7 1 2 6.1 Cc1ccc(-c2ccc(/C=C/C(=O)Nc3ccc(C[N+](C)(C)C4CCOCC4)cc3)cc2)cc1 10.1016/j.bmcl.2007.01.115
44425631 142075 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 564 5 1 2 7.6 CCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL388007 142075 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 564 5 1 2 7.6 CCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44413089 77907 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 459 8 1 3 5.1 CN(C)CC/C=N/[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL209411 77907 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 459 8 1 3 5.1 CN(C)CC/C=N/[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
11319072 74542 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cncnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029420 74542 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cncnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
11330837 74551 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2cc(C(F)(F)F)ncn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029570 74551 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2cc(C(F)(F)F)ncn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
11756884 19089 0 None - 0 Mouse 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289083 19089 0 None - 0 Mouse 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
11562947 89826 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 544 6 3 4 5.6 O=C(O)C(C1CCN(C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237754 89826 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 544 6 3 4 5.6 O=C(O)C(C1CCN(C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
12093170 872 31 None - 1 Human 8.0 pIC50 = 8 Binding
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.6b01309
9431 872 31 None - 1 Human 8.0 pIC50 = 8 Binding
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.6b01309
CHEMBL4519152 872 31 None - 1 Human 8.0 pIC50 = 8 Binding
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.6b01309
CHEMBL5268600 193572 0 None - 1 Human 8.0 pIC50 = 8 Binding
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C2CCC(O)(c3ccc4c(c3)OCO4)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/acs.jmedchem.6b01309
57395216 71012 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ncccn3)CC2)C1 10.1021/ml200030q
CHEMBL1951771 71012 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ncccn3)CC2)C1 10.1021/ml200030q
53322809 58457 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@@H]2CCOC[C@@H]2C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683060 58457 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@@H]2CCOC[C@@H]2C)C1 10.1016/j.bmcl.2011.01.015
53321483 58475 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 498 7 1 6 3.5 CCC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683078 58475 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 498 7 1 6 3.5 CCC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
57391766 71017 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cnccn3)CC2)C1 10.1021/ml200030q
CHEMBL1951776 71017 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cnccn3)CC2)C1 10.1021/ml200030q
162658125 181096 0 None - 1 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181096 0 None - 1 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
10184250 73702 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 10 4 4 3.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)C(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018365 73702 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 10 4 4 3.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)C(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
10186010 73711 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 513 10 4 4 4.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)c2ccccc2)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018375 73711 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 513 10 4 4 4.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)c2ccccc2)c(C)c1 10.1016/j.bmcl.2012.03.007
46241120 83576 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 481 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cccs3)CC2)C1 10.1021/ml300260s
CHEMBL2204258 83576 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 481 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cccs3)CC2)C1 10.1021/ml300260s
44442557 154925 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 10 4 4 3.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2(C)CC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL401010 154925 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 10 4 4 3.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2(C)CC2)c(C)c1 10.1016/j.bmcl.2007.07.028
781 3396 80 None - 1 Human 7.0 pIC50 = 7 Binding
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/acs.jmedchem.6b01309
9953769 3396 80 None - 1 Human 7.0 pIC50 = 7 Binding
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/acs.jmedchem.6b01309
CHEMBL134074 3396 80 None - 1 Human 7.0 pIC50 = 7 Binding
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/acs.jmedchem.6b01309
10436045 3516 4 None -85 13 Human 7.0 pIC50 = 7 Binding
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01309
782 3516 4 None -85 13 Human 7.0 pIC50 = 7 Binding
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01309
CHEMBL432713 3516 4 None -85 13 Human 7.0 pIC50 = 7 Binding
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01309
89823342 126359 0 None - 1 Human 7.0 pIC50 = 7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650405 126359 0 None - 1 Human 7.0 pIC50 = 7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
56680600 65417 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 501 6 2 5 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN(C2CC=C(c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829607 65417 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 501 6 2 5 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN(C2CC=C(c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
44413167 79719 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 447 8 2 3 4.2 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL211560 79719 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 447 8 2 3 4.2 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
46842232 7882 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 544 8 2 4 3.9 Cc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL1089965 7882 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 544 8 2 4 3.9 Cc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
10161975 93960 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 3 5 2.5 COC(=O)[C@@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248416 93960 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 3 5 2.5 COC(=O)[C@@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
11843945 78052 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 504 8 1 2 6.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCCN1CCCCC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL209975 78052 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 504 8 1 2 6.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCCN1CCCCC1)c1ccc(F)cc1 10.1021/jm060439n
5481702 205823 1 None - 0 Human 5.0 pIC50 = 5 Binding
Compound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR2 receptorCompound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR2 receptor
ChEMBL 556 8 0 4 5.3 CN(C[C@@H](CCN1CCC2(CC1)C[S+]([O-])c1ccccc12)c1cccc(Cl)c1)S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00639-9
CHEMBL83338 205823 1 None - 0 Human 5.0 pIC50 = 5 Binding
Compound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR2 receptorCompound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR2 receptor
ChEMBL 556 8 0 4 5.3 CN(C[C@@H](CCN1CCC2(CC1)C[S+]([O-])c1ccccc12)c1cccc(Cl)c1)S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00639-9
56672021 65615 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 433 5 2 5 3.0 C#C[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1833983 65615 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 433 5 2 5 3.0 C#C[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
44453208 169422 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 385 6 2 3 2.8 Cc1ccc(C(=O)NCC(=O)N[C@@H]2CCN(Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL442451 169422 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 385 6 2 3 2.8 Cc1ccc(C(=O)NCC(=O)N[C@@H]2CCN(Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2008.02.015
11329244 71116 11 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of C-C chemokine receptor type 2Inhibition of C-C chemokine receptor type 2
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1021/jm049530m
CHEMBL195433 71116 11 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of C-C chemokine receptor type 2Inhibition of C-C chemokine receptor type 2
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1021/jm049530m
11272103 124375 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of C-C chemokine receptor type 2Inhibition of C-C chemokine receptor type 2
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL363840 124375 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of C-C chemokine receptor type 2Inhibition of C-C chemokine receptor type 2
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
44353447 3775 0 None - 1 Human 4.0 pIC50 = 4 Binding
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/acs.jmedchem.6b01309
785 3775 0 None - 1 Human 4.0 pIC50 = 4 Binding
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/acs.jmedchem.6b01309
CHEMBL337246 3775 0 None - 1 Human 4.0 pIC50 = 4 Binding
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/acs.jmedchem.6b01309
11227368 77643 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 618 9 2 5 6.2 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C3CCCC3)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088383 77643 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 618 9 2 5 6.2 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C3CCCC3)cc2)C1 10.1016/j.bmcl.2012.08.002
25267730 148249 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 421 6 1 2 5.2 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)CC1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL393632 148249 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 421 6 1 2 5.2 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)CC1CCOCC1 10.1016/j.bmcl.2007.01.115
9885683 18947 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 369 3 1 4 3.9 O=C(O)c1cc2ccccc2n1S(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL128640 18947 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 369 3 1 4 3.9 O=C(O)c1cc2ccccc2n1S(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
89823584 126328 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 537 6 1 6 3.8 COc1ccc(N2C[C@@H]3C[C@H]2CN3C(=O)[C@@]23CCC[C@@H]2C[C@@H](N[C@H]2CCOC[C@H]2OC)C3)cc1C(F)(F)F nan
CHEMBL3650376 126328 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 537 6 1 6 3.8 COc1ccc(N2C[C@@H]3C[C@H]2CN3C(=O)[C@@]23CCC[C@@H]2C[C@@H](N[C@H]2CCOC[C@H]2OC)C3)cc1C(F)(F)F nan
162658125 181096 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181096 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
44353196 20925 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 343 3 1 4 4.2 Clc1ccc(Cn2c(-c3nn[nH]n3)cc3ccccc32)cc1Cl 10.1016/j.bmcl.2003.10.049
CHEMBL131087 20925 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 343 3 1 4 4.2 Clc1ccc(Cn2c(-c3nn[nH]n3)cc3ccccc32)cc1Cl 10.1016/j.bmcl.2003.10.049
10371682 73815 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 620 11 4 6 5.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)C1=O 10.1016/j.bmcl.2012.03.007
CHEMBL2018541 73815 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 620 11 4 6 5.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)C1=O 10.1016/j.bmcl.2012.03.007
22310939 115665 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2ccc(C(F)(F)F)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL335378 115665 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2ccc(C(F)(F)F)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
70681778 75217 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 367 4 1 4 2.6 N#Cc1cccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)c1 10.1016/j.bmcl.2012.04.118
CHEMBL2036768 75217 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 367 4 1 4 2.6 N#Cc1cccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)c1 10.1016/j.bmcl.2012.04.118
89823498 126313 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C)C1 nan
CHEMBL3650361 126313 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C)C1 nan
44439169 90774 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL239170 90774 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44439169 90774 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239170 90774 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
49863202 15212 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 550 12 1 4 7.6 CCN(CC)C(C)CCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL1210670 15212 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 550 12 1 4 7.6 CCN(CC)C(C)CCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
71518728 86408 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 481 4 1 5 3.7 COC1COCCC1N[C@@H]1C[C@H]2CCCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314065 86408 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 481 4 1 5 3.7 COC1COCCC1N[C@@H]1C[C@H]2CCCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
44414578 78408 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.2 C[C@](CCN1CCC(c2ccccc2)CC1)(CNCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL211106 78408 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.2 C[C@](CCN1CCC(c2ccccc2)CC1)(CNCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1021/jm060439n
11570431 91982 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241502 91982 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44353418 22537 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2cccc([N+](=O)[O-])c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL132584 22537 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2cccc([N+](=O)[O-])c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
71768830 111105 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxisAntagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxis
ChEMBL 485 4 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2SCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263261 111105 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxisAntagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxis
ChEMBL 485 4 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2SCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
57344302 130647 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 554 7 3 4 5.3 CC1(C)Cc2cc(/C=C/C(=O)N3CCC(C(NC4CCC(c5c[nH]c6ccccc56)CC4)C(N)=O)CC3)ccc2O1 nan
CHEMBL3681893 130647 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 554 7 3 4 5.3 CC1(C)Cc2cc(/C=C/C(=O)N3CCC(C(NC4CCC(c5c[nH]c6ccccc56)CC4)C(N)=O)CC3)ccc2O1 nan
72663455 129401 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671251 129401 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
11753664 77622 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 596 9 2 6 5.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088210 77622 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 596 9 2 6 5.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
10207639 73812 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 508 12 4 5 3.7 CCC[C@H](OC)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018538 73812 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 508 12 4 5 3.7 CCC[C@H](OC)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
44595711 137321 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752627 137321 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
53322810 58472 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683075 58472 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
11409228 74534 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 490 6 3 5 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccccn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029412 74534 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 490 6 3 5 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccccn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
70689914 74552 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 552 6 2 9 3.0 N#Cc1ccnc(N2CCC(C(=O)N3CC[C@H](N[C@H]4CC[C@@](O)(c5ccc(-c6ncccn6)cn5)CC4)C3)CC2)c1 10.1021/ml200199c
CHEMBL2029571 74552 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 552 6 2 9 3.0 N#Cc1ccnc(N2CCC(C(=O)N3CC[C@H](N[C@H]4CC[C@@](O)(c5ccc(-c6ncccn6)cn5)CC4)C3)CC2)c1 10.1021/ml200199c
44453440 97688 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271288 97688 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
10142792 93741 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247245 93741 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
71768689 111111 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 469 4 1 6 2.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263269 111111 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 469 4 1 6 2.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
53319664 58677 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 461 6 1 5 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684700 58677 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 461 6 1 5 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
23630215 62544 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782376 62544 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
53321482 58461 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683064 58461 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
53318314 58671 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 445 5 1 4 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCCC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684692 58671 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 445 5 1 4 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCCC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
53323654 58676 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 447 6 1 5 2.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684699 58676 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 447 6 1 5 2.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
72947191 105260 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 600 7 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)CCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115275 105260 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 600 7 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)CCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
49763574 65444 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 477 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](F)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829636 65444 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 477 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](F)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
44442532 93485 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 9 4 4 3.2 Cc1ccc(CNC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246213 93485 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 9 4 4 3.2 Cc1ccc(CNC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442594 93773 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(NCc3ccccc3)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247456 93773 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(NCc3ccccc3)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
10205937 93963 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 10 4 4 2.5 CCNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248419 93963 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 10 4 4 2.5 CCNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
10300282 154777 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 494 10 3 5 2.3 CON(C)C(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL400158 154777 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 494 10 3 5 2.3 CON(C)C(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
22310954 24078 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2cc(Cl)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL133839 24078 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2cc(Cl)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
71518897 86389 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 433 4 1 5 3.0 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(Cl)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313782 86389 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 433 4 1 5 3.0 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(Cl)cc3C2)C1 10.1016/j.bmcl.2012.10.069
44442571 154780 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 508 10 4 5 2.6 COc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
CHEMBL400160 154780 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 508 10 4 5 2.6 COc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
11843946 139545 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 490 7 1 2 6.1 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCCCC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL379624 139545 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 490 7 1 2 6.1 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCCCC1)c1ccc(F)cc1 10.1021/jm060439n
11844079 141477 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 580 9 1 2 7.9 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL384368 141477 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 580 9 1 2 7.9 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
23655877 169483 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 460 5 3 3 4.7 O=C(O)C(C1CCN(C(=O)Nc2ccccc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL443058 169483 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 460 5 3 3 4.7 O=C(O)C(C1CCN(C(=O)Nc2ccccc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
44395113 66117 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 546 8 1 5 5.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(Cl)cc3)c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL183966 66117 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 546 8 1 5 5.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(Cl)cc3)c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44395058 66333 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 385 7 0 3 4.8 c1ccc(C(CCN2CCCN(Cc3ccncc3)CC2)c2ccccc2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL185032 66333 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 385 7 0 3 4.8 c1ccc(C(CCN2CCCN(Cc3ccncc3)CC2)c2ccccc2)cc1 10.1016/j.bmcl.2004.08.008
18426192 66006 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 7 2 3 3.1 O=C(CNC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
CHEMBL183681 66006 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 7 2 3 3.1 O=C(CNC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
44395093 67126 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 384 8 1 3 4.1 O=C(CCCC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL187476 67126 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 384 8 1 3 4.1 O=C(CCCC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
176 398 66 None -3 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 398 66 None -3 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 398 66 None -3 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 398 66 None -3 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 398 66 None -3 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
44425322 153201 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 738 9 2 5 8.6 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)C3Cc4ccccc43)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL397717 153201 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 738 9 2 5 8.6 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)C3Cc4ccccc43)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
89823655 126320 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2C)C1 nan
CHEMBL3650368 126320 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2C)C1 nan
44444096 93990 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 6 0 3 6.1 COc1ccccc1C1CCN(CC2CCN(C(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL248617 93990 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 6 0 3 6.1 COc1ccccc1C1CCN(CC2CCN(C(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.07.065
44570713 179959 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 580 8 6 6 2.5 CNC(=O)NC1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.12.062
CHEMBL474665 179959 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 580 8 6 6 2.5 CNC(=O)NC1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.12.062
46830335 8215 8 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 565 8 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092238 8215 8 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 565 8 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
122181150 121838 0 None - 0 Mouse 5.0 pIC50 = 5.0 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 608 7 1 3 7.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
CHEMBL3589845 121838 0 None - 0 Mouse 5.0 pIC50 = 5.0 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 608 7 1 3 7.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
49863199 15209 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 528 9 1 4 7.1 O=C(CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1 10.1016/j.ejmech.2010.04.024
CHEMBL1210667 15209 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 528 9 1 4 7.1 O=C(CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1 10.1016/j.ejmech.2010.04.024
44439158 146827 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 542 10 1 4 7.5 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1 10.1016/j.bmcl.2006.10.060
CHEMBL392493 146827 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 542 10 1 4 7.5 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1 10.1016/j.bmcl.2006.10.060
46884818 7871 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089881 7871 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
22310877 19543 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 285 3 1 2 4.0 O=C(O)c1cc2ccccc2n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL129958 19543 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 285 3 1 2 4.0 O=C(O)c1cc2ccccc2n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2003.10.049
42632811 93473 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1cccc(NC(=O)c2ccc(Cl)c(Cl)c2)c1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL246104 93473 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1cccc(NC(=O)c2ccc(Cl)c(Cl)c2)c1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
127027628 137472 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cc(Cl)cc(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753826 137472 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cc(Cl)cc(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
44453373 97811 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 435 7 2 4 2.8 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271935 97811 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 435 7 2 4 2.8 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
44454793 155092 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
ChEMBL 515 4 0 3 7.0 C[C@H]1CN([C@@H]2CC[C@@]3(CCO[C@@H]3OCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.016
CHEMBL401890 155092 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
ChEMBL 515 4 0 3 7.0 C[C@H]1CN([C@@H]2CC[C@@]3(CCO[C@@H]3OCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.016
23656261 89073 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 485 6 2 3 5.1 Cc1ccc(/C=C/C(=O)N2CCC(C(C(=O)O)N3CCC(c4c[nH]c5ccccc45)CC3)CC2)cc1 10.1021/jm070902b
CHEMBL236510 89073 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 485 6 2 3 5.1 Cc1ccc(/C=C/C(=O)N2CCC(C(C(=O)O)N3CCC(c4c[nH]c5ccccc45)CC3)CC2)cc1 10.1021/jm070902b
53318855 58480 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 514 8 1 7 2.7 COCC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683083 58480 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 514 8 1 7 2.7 COCC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
44453409 95439 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257065 95439 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
44453441 97689 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 498 6 3 4 3.2 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL271289 97689 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 498 6 3 4 3.2 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
72946982 105229 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 602 6 1 7 3.8 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115103 105229 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 602 6 1 7 3.8 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
46842086 7979 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 544 8 2 4 3.9 Cc1cccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
CHEMBL1090548 7979 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 544 8 2 4 3.9 Cc1cccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
44580424 188026 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 494 8 4 5 4.0 CSc1ccc(CNC2CCCCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497576 188026 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 494 8 4 5 4.0 CSc1ccc(CNC2CCCCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
11502188 75201 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 398 4 1 3 3.9 CCN1CCC[C@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036752 75201 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 398 4 1 3 3.9 CCN1CCC[C@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
10184007 159061 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 7 3 3 4.6 Cc1cc(C)c(CN[C@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL409712 159061 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 7 3 3 4.6 Cc1cc(C)c(CN[C@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
22310971 20486 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2c(C(F)(F)F)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130724 20486 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2c(C(F)(F)F)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
22143196 183987 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL481790 183987 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
56671923 65739 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 471 6 3 4 4.5 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834631 65739 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 471 6 3 4 4.5 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
54755079 65741 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 528 8 4 5 3.5 NC(=O)Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cc1 10.1016/j.bmcl.2011.08.074
CHEMBL1834633 65741 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 528 8 4 5 3.5 NC(=O)Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cc1 10.1016/j.bmcl.2011.08.074
54754968 65742 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 502 7 3 6 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834634 65742 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 502 7 3 6 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
57400452 70509 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 9 3 5 3.6 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1946832 70509 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 9 3 5 3.6 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
57393347 70339 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 623 10 4 6 3.4 CCN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944777 70339 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 623 10 4 6 3.4 CCN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44416138 138874 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL378195 138874 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
9850318 95245 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL256154 95245 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
53324942 58678 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 469 6 1 5 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)c2ccccc2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684701 58678 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 469 6 1 5 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)c2ccccc2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
12093170 872 31 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.0c01137
9431 872 31 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.0c01137
CHEMBL4519152 872 31 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.0c01137
162658125 181096 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181096 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
53326225 58670 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 431 5 1 4 3.0 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684691 58670 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 431 5 1 4 3.0 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
44583283 188286 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 714 11 3 8 6.0 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL500175 188286 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 714 11 3 8 6.0 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2009.05.041
22143305 183612 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480228 183612 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
12093170 872 31 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.0c01137
9431 872 31 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.0c01137
CHEMBL4519152 872 31 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.0c01137
162658125 181096 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181096 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
53324943 58684 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 491 6 1 4 3.3 CC(CC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2F)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
CHEMBL1684707 58684 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 491 6 1 4 3.3 CC(CC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2F)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
57343818 130629 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 524 7 3 3 5.1 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCC3)CC1 nan
CHEMBL3681876 130629 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 524 7 3 3 5.1 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCC3)CC1 nan
86767127 129410 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 483 4 1 7 1.8 COC1COCCC1NC1CC2OC(=O)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671260 129410 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 483 4 1 7 1.8 COC1COCCC1NC1CC2OC(=O)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
56671924 65747 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 491 6 2 5 4.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C4CCCCC4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834639 65747 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 491 6 2 5 4.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C4CCCCC4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44441358 149846 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 427 5 1 3 4.5 C[N+](C)(Cc1ccc(NC(=O)C2=Cc3ccc(Cl)cc3OC2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL394897 149846 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 427 5 1 3 4.5 C[N+](C)(Cc1ccc(NC(=O)C2=Cc3ccc(Cl)cc3OC2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
52942863 19249 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 475 6 3 4 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)C2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
CHEMBL1290186 19249 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 475 6 3 4 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)C2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
44442581 93548 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 507 9 5 5 2.5 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1N 10.1016/j.bmcl.2007.07.028
CHEMBL246410 93548 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 507 9 5 5 2.5 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1N 10.1016/j.bmcl.2007.07.028
44442555 93726 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 11 4 4 3.6 CCC(C)(C)NC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247203 93726 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 11 4 4 3.6 CCC(C)(C)NC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
44442554 93967 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 11 4 4 3.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCC(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248423 93967 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 11 4 4 3.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCC(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
11844595 136366 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 604 7 1 2 8.0 C[C@@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@]12C=Cc1ccccc12 10.1021/jm060439n
CHEMBL373491 136366 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 604 7 1 2 8.0 C[C@@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@]12C=Cc1ccccc12 10.1021/jm060439n
44353395 20093 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 333 3 1 2 5.0 Cc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1Cl 10.1016/j.bmcl.2003.10.049
CHEMBL130403 20093 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 333 3 1 2 5.0 Cc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1Cl 10.1016/j.bmcl.2003.10.049
11635092 89825 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 5.8 O=C(O)C(C1CCN(C(=O)Nc2ccc(C(F)(F)F)cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237753 89825 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 5.8 O=C(O)C(C1CCN(C(=O)Nc2ccc(C(F)(F)F)cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
69212799 77976 3 None - 0 Human 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL2096789 77976 3 None - 0 Human 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
56677296 65420 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1ccc(C(F)(F)F)cc1)NC1CN([C@H]2CC[C@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829611 65420 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1ccc(C(F)(F)F)cc1)NC1CN([C@H]2CC[C@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
25256791 187691 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 494 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2010.02.072
CHEMBL495202 187691 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 494 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2010.02.072
10143025 93537 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 526 10 4 4 4.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)Nc2ccccc2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246397 93537 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 526 10 4 4 4.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)Nc2ccccc2)c(C)c1 10.1016/j.bmcl.2007.07.028
44444008 155045 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 478 9 1 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL401637 155045 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 478 9 1 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
44395194 64767 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 496 8 1 5 4.1 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL181918 64767 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 496 8 1 5 4.1 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
25008679 94178 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 454 7 1 3 5.2 COc1ccc(C2CCN(C[C@H]3CC[C@@H](NC(=O)/C=C/c4cc(F)cc(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249607 94178 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 454 7 1 3 5.2 COc1ccc(C2CCN(C[C@H]3CC[C@@H](NC(=O)/C=C/c4cc(F)cc(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
24801178 156842 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 481 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@@H]1NC(=O)c1ccc(Cl)cc1 10.1021/jm701488f
CHEMBL407145 156842 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 481 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@@H]1NC(=O)c1ccc(Cl)cc1 10.1021/jm701488f
44453329 155351 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 431 7 2 3 3.5 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL403281 155351 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 431 7 2 3 3.5 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
22310903 22614 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1cccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c12 10.1016/j.bmcl.2003.10.049
CHEMBL132662 22614 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1cccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c12 10.1016/j.bmcl.2003.10.049
76325121 105241 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 510 5 1 6 2.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115115 105241 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 510 5 1 6 2.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57344309 130653 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 485 7 3 4 4.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3cccnc32)CC1)C1CCN(C(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL3681899 130653 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 485 7 3 4 4.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3cccnc32)CC1)C1CCN(C(=O)/C=C/c2ccccc2)CC1 nan
49863201 15211 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 536 12 1 4 7.2 CCN(CC)CCCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL1210669 15211 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 536 12 1 4 7.2 CCN(CC)CCCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
11663995 146828 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 550 13 1 4 7.6 CCN(CC)CCCCNC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL392494 146828 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 550 13 1 4 7.6 CCN(CC)CCCCNC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
11567495 75199 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 398 4 1 3 3.9 CCN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036750 75199 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 398 4 1 3 3.9 CCN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
10052388 187552 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 520 7 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C2CC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494541 187552 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 520 7 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C2CC2)C1 10.1016/j.bmcl.2008.12.050
22143308 187764 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 509 9 5 6 2.8 CCSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL495717 187764 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 509 9 5 6 2.8 CCSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
44573609 187553 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 496 6 3 4 4.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2O)C1 10.1007/s00044-010-9501-4
CHEMBL494542 187553 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 496 6 3 4 4.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2O)C1 10.1007/s00044-010-9501-4
10256127 73813 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 520 10 4 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@H](NC(=O)c2cc(N)cc(C(F)(F)F)c2)C1=O 10.1016/j.bmcl.2012.03.007
CHEMBL2018539 73813 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 520 10 4 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@H](NC(=O)c2cc(N)cc(C(F)(F)F)c2)C1=O 10.1016/j.bmcl.2012.03.007
44353356 117600 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 395 4 1 2 6.4 O=C(O)c1cc2ccc(-c3ccccc3)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL340072 117600 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 395 4 1 2 6.4 O=C(O)c1cc2ccc(-c3ccccc3)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
11227383 77647 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 620 11 2 5 6.2 CC(C)CCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088387 77647 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 620 11 2 5 6.2 CC(C)CCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
71226374 86406 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 437 3 1 4 3.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCOCC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314061 86406 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 437 3 1 4 3.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCOCC1)C2 10.1016/j.bmcl.2012.10.069
44416066 79787 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 643 8 2 4 5.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)NS(=O)(=O)C(F)(F)F 10.1016/j.bmcl.2006.07.011
CHEMBL211923 79787 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 643 8 2 4 5.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)NS(=O)(=O)C(F)(F)F 10.1016/j.bmcl.2006.07.011
22310929 168294 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2cccc(F)c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL434059 168294 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2cccc(F)c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
71517402 86382 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 535 4 1 5 4.1 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](C(F)(F)F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313774 86382 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 535 4 1 5 4.1 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](C(F)(F)F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
72946204 105252 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 524 5 1 7 1.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C3COC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115267 105252 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 524 5 1 7 1.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C3COC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44415904 80430 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 514 9 1 2 7.0 CCC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL214641 80430 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 514 9 1 2 7.0 CCC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
11329328 74533 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 490 6 3 5 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3cccnc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029411 74533 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 490 6 3 5 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3cccnc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
44425630 86027 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230617 86027 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44444035 94287 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 460 9 2 3 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2ccc(O)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL250408 94287 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 460 9 2 3 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2ccc(O)cc2)CC1 10.1016/j.bmcl.2007.07.065
44353617 19665 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 334 3 2 3 4.3 Nc1ccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c2c1 10.1016/j.bmcl.2003.10.049
CHEMBL130065 19665 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 334 3 2 3 4.3 Nc1ccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c2c1 10.1016/j.bmcl.2003.10.049
57656942 75039 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 376 4 1 3 3.4 O=C(Nc1ccc(Cl)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2035000 75039 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 376 4 1 3 3.4 O=C(Nc1ccc(Cl)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
22310953 23965 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2cccc(C(F)(F)F)c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL133748 23965 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2cccc(C(F)(F)F)c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44353170 21415 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 318 3 1 2 4.1 NC(=O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL131493 21415 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 318 3 1 2 4.1 NC(=O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44425650 86130 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 570 9 1 2 8.3 CCCCCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231143 86130 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 570 9 1 2 8.3 CCCCCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
89853102 111104 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 552 5 1 8 3.5 COC1COCCC1N[C@@H]1C[C@H]2OC(c3nccs3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263260 111104 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 552 5 1 8 3.5 COC1COCCC1N[C@@H]1C[C@H]2OC(c3nccs3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
44415903 81150 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL215759 81150 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
89823502 126314 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2F)C1 nan
CHEMBL3650362 126314 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2F)C1 nan
56643545 130623 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681870 130623 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
11192346 2024 57 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity to rat CCR2Binding affinity to rat CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 2024 57 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity to rat CCR2Binding affinity to rat CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 2024 57 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity to rat CCR2Binding affinity to rat CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
46947816 65433 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cn3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829624 65433 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cn3)CC2)C1 10.1016/j.bmcl.2011.06.080
56664979 65743 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 529 6 2 7 4.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834635 65743 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 529 6 2 7 4.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
56671925 65749 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 481 7 2 7 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834640 65749 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 481 7 2 7 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56678508 65801 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834794 65801 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44415899 80074 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL213058 80074 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
44425641 86066 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230832 86066 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44413258 77758 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 446 8 1 2 5.5 CN(C)CCC[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL209063 77758 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 446 8 1 2 5.5 CN(C)CCC[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
44425315 86248 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 536 8 2 5 5.4 CC(=O)Nc1nc(C(CCN2CCCCC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL231252 86248 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 536 8 2 5 5.4 CC(=O)Nc1nc(C(CCN2CCCCC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425319 86335 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 727 10 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccn3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL231340 86335 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 727 10 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccn3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
53318315 58673 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 473 6 1 4 3.4 CC(CC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
CHEMBL1684695 58673 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 473 6 1 4 3.4 CC(CC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
54584109 62547 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 509 5 1 6 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782379 62547 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 509 5 1 6 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
10187492 147790 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 549 11 5 5 3.7 CCNc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H](CNCc1ccc(C)cc1C)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL393267 147790 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 549 11 5 5 3.7 CCNc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H](CNCc1ccc(C)cc1C)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
69285531 121227 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 441 8 2 3 4.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577935 121227 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 441 8 2 3 4.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
10152864 187874 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 543 8 3 6 3.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL496432 187874 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 543 8 3 6 3.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44425288 86015 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 570 8 2 5 6.4 Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230507 86015 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 570 8 2 5 6.4 Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425304 143367 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL389773 143367 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
53326721 58493 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 554 6 2 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(O)C(F)(F)F)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683189 58493 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 554 6 2 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(O)C(F)(F)F)C1 10.1016/j.bmcl.2011.01.015
53326901 58682 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 449 5 1 4 2.9 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684705 58682 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 449 5 1 4 2.9 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
57343820 68954 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 518 7 3 3 5.2 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(Cl)cc2)CC1 nan
CHEMBL1922816 68954 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 518 7 3 3 5.2 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(Cl)cc2)CC1 nan
57343819 130626 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(C(F)(F)F)cc2)CC1 nan
CHEMBL3681873 130626 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(C(F)(F)F)cc2)CC1 nan
57344311 130655 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 521 7 3 4 4.3 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681900 130655 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 521 7 3 4 4.3 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
71719764 86385 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 2 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313777 86385 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 2 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
57396832 70335 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 525 8 2 5 3.1 CN(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944773 70335 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 525 8 2 5 3.1 CN(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
53320968 58668 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 403 5 1 4 2.2 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684689 58668 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 403 5 1 4 2.2 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
44442553 93488 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 10 4 4 2.9 CCNC(=O)[C@@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)[C@@H](C)NCc1ccc(C)cc1C 10.1016/j.bmcl.2007.07.028
CHEMBL246221 93488 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 10 4 4 2.9 CCNC(=O)[C@@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)[C@@H](C)NCc1ccc(C)cc1C 10.1016/j.bmcl.2007.07.028
44442595 166408 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 577 12 5 5 4.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(NCC(C)C)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL427705 166408 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 577 12 5 5 4.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(NCC(C)C)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44444113 94179 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 7 1 3 5.3 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249608 94179 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 7 1 3 5.3 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11606411 85308 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125]hMCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125]hMCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
CHEMBL226066 85308 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125]hMCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125]hMCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
72946384 105255 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 546 5 1 8 2.5 COC1COCCC1N[C@@H]1C[C@H]2CN(c3ncccn3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115270 105255 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 546 5 1 8 2.5 COC1COCCC1N[C@@H]1C[C@H]2CN(c3ncccn3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44442583 93550 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 536 10 4 5 3.3 COc1cc(C)c(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1C 10.1016/j.bmcl.2007.07.028
CHEMBL246412 93550 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 536 10 4 5 3.3 COc1cc(C)c(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1C 10.1016/j.bmcl.2007.07.028
9890559 66128 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 462 8 0 4 4.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL184053 66128 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 462 8 0 4 4.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
11273475 77646 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 606 10 2 5 5.8 CC(C)Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088386 77646 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 606 10 2 5 5.8 CC(C)Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
46884898 7717 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1088874 7717 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
22310946 20755 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2c([N+](=O)[O-])cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130937 20755 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2c([N+](=O)[O-])cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
57344310 68936 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ncccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922794 68936 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ncccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
15518124 138426 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 402 5 1 3 5.5 CN(CCN1CCCCC1)c1ccc(-c2nc3cc(Cl)c(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2006.04.045
CHEMBL377432 138426 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 402 5 1 3 5.5 CN(CCN1CCCCC1)c1ccc(-c2nc3cc(Cl)c(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2006.04.045
44425649 86129 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 86129 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
54586021 62543 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 494 4 0 5 4.1 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N2CCC3COCCC32)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782375 62543 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 494 4 0 5 4.1 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N2CCC3COCCC32)C1 10.1016/j.bmcl.2011.01.034
44570779 183568 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 550 9 4 5 4.0 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480036 183568 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 550 9 4 5 4.0 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
57344299 68956 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 552 7 3 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(C(F)(F)F)cc2)CC1 nan
CHEMBL1922818 68956 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 552 7 3 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(C(F)(F)F)cc2)CC1 nan
11467577 77642 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 606 8 2 5 5.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C(C)(C)C)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088382 77642 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 606 8 2 5 5.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C(C)(C)C)cc2)C1 10.1016/j.bmcl.2012.08.002
44453536 97929 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 435 7 2 4 2.8 COc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272542 97929 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 435 7 2 4 2.8 COc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.02.015
22310899 22692 35 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 285 3 1 2 4.0 O=C(O)c1cc2ccccc2n1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2003.10.049
CHEMBL132725 22692 35 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 285 3 1 2 4.0 O=C(O)c1cc2ccccc2n1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2003.10.049
89823629 126321 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C)cc(C(F)(F)F)c2)C1 nan
CHEMBL3650369 126321 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C)cc(C(F)(F)F)c2)C1 nan
60148505 111110 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxisAntagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxis
ChEMBL 469 4 1 6 2.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263268 111110 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxisAntagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxis
ChEMBL 469 4 1 6 2.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
56643545 130623 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681870 130623 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
86767126 129409 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 545 5 1 6 4.1 COC1COCCC1NC1CC2OC(c3ccccc3)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671259 129409 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 545 5 1 6 4.1 COC1COCCC1NC1CC2OC(c3ccccc3)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
44415880 169339 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL441856 169339 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
57396998 71014 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cncnc3)CC2)C1 10.1021/ml200030q
CHEMBL1951773 71014 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cncnc3)CC2)C1 10.1021/ml200030q
44425320 86135 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 713 9 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3cccnc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL231149 86135 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 713 9 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3cccnc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
44453366 158304 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 451 6 5 6 1.7 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
CHEMBL408908 158304 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 451 6 5 6 1.7 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
71768794 111103 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 545 5 1 6 4.1 COC1COCCC1N[C@@H]1C[C@H]2OC(c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263259 111103 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 545 5 1 6 4.1 COC1COCCC1N[C@@H]1C[C@H]2OC(c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
44425286 153247 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397750 153247 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44593564 187232 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492564 187232 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
44425258 168907 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 2 6 6.1 CC(=O)Nc1nc(C(CCN2CCN(c3ccccc3C)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL438514 168907 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 2 6 6.1 CC(=O)Nc1nc(C(CCN2CCN(c3ccccc3C)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
53322299 58674 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 459 6 1 4 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CCC(F)(F)F)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684696 58674 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 459 6 1 4 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CCC(F)(F)F)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
53326226 58686 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 463 6 1 4 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC2CCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684709 58686 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 463 6 1 4 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC2CCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
56675301 65756 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 439 7 3 5 3.1 CCO[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834647 65756 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 439 7 3 5 3.1 CCO[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
44444110 154841 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4ccc(Cl)c(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL400483 154841 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4ccc(Cl)c(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11844469 78402 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.3 C[C@H]1CN(CC[C@H](CNCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@H]1c1ccccc1 10.1021/jm060439n
CHEMBL211092 78402 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.3 C[C@H]1CN(CC[C@H](CNCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@H]1c1ccccc1 10.1021/jm060439n
89823497 126302 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
CHEMBL3650350 126302 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
56676473 65808 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 489 6 2 7 3.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccn4C)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834850 65808 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 489 6 2 7 3.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccn4C)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44444106 94073 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 490 5 0 2 6.5 O=C(/C=C/c1cccc(C(F)(F)F)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL249010 94073 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 490 5 0 2 6.5 O=C(/C=C/c1cccc(C(F)(F)F)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
44395144 66993 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 7 2 3 3.2 Cc1cccc(C(=O)NCC(=O)NCC2CCCN2Cc2ccc(Cl)cc2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL186878 66993 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 7 2 3 3.2 Cc1cccc(C(=O)NCC(=O)NCC2CCCN2Cc2ccc(Cl)cc2)c1 10.1016/j.bmcl.2004.08.009
44593563 193110 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL522688 193110 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
46884856 8344 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 566 8 2 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092921 8344 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 566 8 2 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
89823512 126354 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 589 5 0 5 5.2 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 nan
CHEMBL3650400 126354 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 589 5 0 5 5.2 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 nan
10414966 155118 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ncccn3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL402010 155118 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ncccn3)CC2)C1 10.1016/j.bmcl.2007.12.029
89823482 126305 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2[C@H]3CC[C@@H]2CN(c2cc(C(F)(F)F)ccn2)C3)C1 nan
CHEMBL3650353 126305 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2[C@H]3CC[C@@H]2CN(c2cc(C(F)(F)F)ccn2)C3)C1 nan
70696469 75214 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 372 5 1 4 2.7 COc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1 10.1016/j.bmcl.2012.04.118
CHEMBL2036765 75214 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 372 5 1 4 2.7 COc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1 10.1016/j.bmcl.2012.04.118
44425649 86129 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 86129 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
89823499 126308 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cc(C)n2)C1 nan
CHEMBL3650356 126308 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cc(C)n2)C1 nan
44413230 139097 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 447 8 2 3 4.2 CN(C)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL378658 139097 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 447 8 2 3 4.2 CN(C)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
89823444 126326 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 523 6 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(OC(F)(F)F)c2)C1 nan
CHEMBL3650374 126326 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 523 6 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(OC(F)(F)F)c2)C1 nan
44353334 117443 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 319 3 1 2 4.7 O=C(O)c1cc2cc(Cl)ccc2n1Cc1ccccc1Cl 10.1016/j.bmcl.2003.10.049
CHEMBL339842 117443 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 319 3 1 2 4.7 O=C(O)c1cc2cc(Cl)ccc2n1Cc1ccccc1Cl 10.1016/j.bmcl.2003.10.049
57343917 130630 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 526 7 3 4 4.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCO3)CC1 nan
CHEMBL3681877 130630 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 526 7 3 4 4.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCO3)CC1 nan
54769305 86580 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 483 6 2 5 4.6 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315920 86580 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 483 6 2 5 4.6 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2012.12.017
68003962 86581 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 6 3.7 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315921 86581 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 6 3.7 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2012.12.017
49764446 65440 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 518 7 3 5 3.1 CN(C)c1cccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2011.06.080
CHEMBL1829631 65440 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 518 7 3 5 3.1 CN(C)c1cccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2011.06.080
54755560 65779 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 495 8 2 7 3.4 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(CC)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834721 65779 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 495 8 2 7 3.4 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(CC)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
44415922 141683 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL385540 141683 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
24794624 179616 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 492 6 3 6 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4742683 179616 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 492 6 3 6 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
162657824 181126 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 482 5 3 4 2.9 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(F)(F)F)c2)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4760566 181126 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 482 5 3 4 2.9 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(F)(F)F)c2)C1=O 10.1021/acsmedchemlett.1c00082
53326701 58465 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 497 6 1 5 3.9 CO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683068 58465 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 497 6 1 5 3.9 CO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
44425633 86041 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230721 86041 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44425648 168704 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 540 6 1 2 7.1 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL436796 168704 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 540 6 1 2 7.1 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44442590 93772 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247455 93772 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
11553489 121221 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 417 11 4 4 2.3 CCC[C@H](O)[C@H](CNCC(C)C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577929 121221 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 417 11 4 4 2.3 CCC[C@H](O)[C@H](CNCC(C)C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
11497533 89189 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 2 3 5.8 O=C(O)C(C1CCN(C(=O)/C=C/c2ccc(C(F)(F)F)cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL236722 89189 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 2 3 5.8 O=C(O)C(C1CCN(C(=O)/C=C/c2ccc(C(F)(F)F)cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
11541149 146311 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 541 6 3 4 4.9 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccc(O)cc23)CC1 10.1021/jm070902b
CHEMBL392097 146311 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 541 6 3 4 4.9 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccc(O)cc23)CC1 10.1021/jm070902b
53323664 58691 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 463 5 1 4 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684714 58691 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 463 5 1 4 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
54583187 62574 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 484 5 2 6 2.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2O)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782580 62574 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 484 5 2 6 2.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2O)C1 10.1016/j.bmcl.2011.01.034
44425639 86065 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 580 6 1 3 6.8 COCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230831 86065 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 580 6 1 3 6.8 COCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
54580190 62571 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 512 7 1 6 3.7 CCO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782577 62571 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 512 7 1 6 3.7 CCO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
54582215 62560 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782566 62560 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
54581190 62562 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782568 62562 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
162658125 181096 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181096 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
57344216 130631 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL3681878 130631 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cccc(C(F)(F)F)c2)CC1 nan
71517241 86379 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 485 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313771 86379 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 485 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
127025460 137329 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 437 4 1 3 5.1 C[C@H]1CC=C(C(=O)NS(=O)(=O)c2ccccc2)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752690 137329 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 437 4 1 3 5.1 C[C@H]1CC=C(C(=O)NS(=O)(=O)c2ccccc2)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
10165716 93554 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 538 10 4 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(SC(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246417 93554 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 538 10 4 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(SC(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442559 93731 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 532 10 4 4 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CCCCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247208 93731 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 532 10 4 4 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CCCCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
44442547 154892 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 11 3 4 3.2 CCNC(=O)[C@H](CCN(C)Cc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL400793 154892 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 11 3 4 3.2 CCNC(=O)[C@H](CCN(C)Cc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
9873546 78037 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 8 1 2 7.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL209899 78037 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 8 1 2 7.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
22310976 117047 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2c(Cl)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL339099 117047 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2c(Cl)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
71519050 86392 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 444 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc([N+](=O)[O-])cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313785 86392 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 444 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc([N+](=O)[O-])cc3C2)C1 10.1016/j.bmcl.2012.10.069
44395048 66161 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 495 8 3 6 2.9 NS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL184256 66161 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 495 8 3 6 2.9 NS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44395062 66698 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 512 8 2 6 3.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(F)cc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL185517 66698 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 512 8 2 6 3.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(F)cc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44395028 66955 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 528 8 2 6 4.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(Cl)cc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL186689 66955 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 528 8 2 6 4.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(Cl)cc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44395061 66400 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell; not determinedConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell; not determined
ChEMBL 510 8 3 7 3.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL185180 66400 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell; not determinedConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell; not determined
ChEMBL 510 8 3 7 3.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
9825735 93764 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 3 5 2.5 COC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247405 93764 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 3 5 2.5 COC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
44444032 94108 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 474 10 1 3 6.2 COc1ccc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249183 94108 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 474 10 1 3 6.2 COc1ccc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11844467 77911 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.4 CC(C[C@H](CNCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1)N1CCC(c2ccccc2)CC1 10.1021/jm060439n
CHEMBL209423 77911 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.4 CC(C[C@H](CNCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1)N1CCC(c2ccccc2)CC1 10.1021/jm060439n
44442540 93486 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 3 5 2.5 COC(=O)[C@@H](CNC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)NCc1ccc(C)cc1C 10.1016/j.bmcl.2007.07.028
CHEMBL246218 93486 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 3 5 2.5 COC(=O)[C@@H](CNC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)NCc1ccc(C)cc1C 10.1016/j.bmcl.2007.07.028
46886537 8348 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 511 8 1 5 3.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3ccccc3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1092940 8348 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 511 8 1 5 3.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3ccccc3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
76321527 105254 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 551 5 1 8 3.1 COC1COCCC1N[C@@H]1C[C@H]2CN(c3nccs3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115269 105254 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 551 5 1 8 3.1 COC1COCCC1N[C@@H]1C[C@H]2CN(c3nccs3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
89823389 126340 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 575 5 1 5 4.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 nan
CHEMBL3650388 126340 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 575 5 1 5 4.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 nan
71518407 86402 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 435 3 1 3 4.9 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCCC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314057 86402 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 435 3 1 3 4.9 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCCC1)C2 10.1016/j.bmcl.2012.10.069
10129107 188429 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 585 9 3 6 3.4 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)=O)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502248 188429 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 585 9 3 6 3.4 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)=O)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44453534 97881 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 451 7 3 5 2.5 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)ccc1O 10.1016/j.bmcl.2008.02.015
CHEMBL272331 97881 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 451 7 3 5 2.5 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)ccc1O 10.1016/j.bmcl.2008.02.015
89823621 126319 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)n2)C1 nan
CHEMBL3650367 126319 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)n2)C1 nan
22143349 184077 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 508 7 4 5 3.6 CSc1ccc(C(=O)NC2CCCCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL482387 184077 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 508 7 4 5 3.6 CSc1ccc(C(=O)NC2CCCCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
44573411 193265 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 464 6 2 2 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCC2)C1 10.1007/s00044-010-9501-4
CHEMBL523857 193265 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 464 6 2 2 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCC2)C1 10.1007/s00044-010-9501-4
44453620 95536 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 450 7 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc([N+](=O)[O-])cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257511 95536 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 450 7 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc([N+](=O)[O-])cc2)C1 10.1016/j.bmcl.2008.02.015
44573411 193265 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 464 6 2 2 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL523857 193265 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 464 6 2 2 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCC2)C1 10.1016/j.bmcl.2008.12.050
70681271 73808 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 550 13 5 5 3.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(=O)NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018533 73808 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 550 13 5 5 3.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(=O)NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
69286635 121231 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 469 9 2 3 4.9 CC(C)CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577939 121231 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 469 9 2 3 4.9 CC(C)CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
162658125 181096 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181096 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
72663455 129401 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671251 129401 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
86767122 129405 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 509 5 1 6 3.1 COC1COCCC1NC1CC2OC(C3CC3)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671255 129405 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 509 5 1 6 3.1 COC1COCCC1NC1CC2OC(C3CC3)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
71519226 86376 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 482 5 1 5 3.8 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(OC(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313768 86376 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 482 5 1 5 3.8 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(OC(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
11647276 75207 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 412 4 1 3 4.3 CC(C)N1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036758 75207 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 412 4 1 3 4.3 CC(C)N1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
46240584 83580 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 532 6 3 6 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nc4ccccc4s3)CC2)C1 10.1021/ml300260s
CHEMBL2204262 83580 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 532 6 3 6 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nc4ccccc4s3)CC2)C1 10.1021/ml300260s
56671795 65799 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 478 6 3 6 4.0 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834792 65799 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 478 6 3 6 4.0 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
54754967 77830 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 518 7 4 7 3.0 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL2092884 77830 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 518 7 4 7 3.0 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
22143241 183250 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 510 8 3 4 3.8 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL479642 183250 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 510 8 3 4 3.8 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.12.062
44425634 142018 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL387587 142018 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44425277 85959 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 674 10 2 5 8.1 O=C(Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)c1ccccc1 10.1016/j.bmcl.2006.10.059
CHEMBL230165 85959 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 674 10 2 5 8.1 O=C(Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)c1ccccc1 10.1016/j.bmcl.2006.10.059
44442592 153683 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 535 10 5 5 3.3 CNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL398134 153683 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 535 10 5 5 3.3 CNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
71768688 111099 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 469 4 1 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263255 111099 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 469 4 1 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
71768725 111102 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 509 5 1 6 3.1 COC1COCCC1N[C@@H]1C[C@H]2OC(C3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263258 111102 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 509 5 1 6 3.1 COC1COCCC1N[C@@H]1C[C@H]2OC(C3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
44571257 191094 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 518 9 3 4 4.3 CC(C)c1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL518772 191094 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 518 9 3 4 4.3 CC(C)c1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
71745103 126362 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650408 126362 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
11512375 154669 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 555 7 2 4 5.2 COc1ccc2[nH]cc(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1021/jm070902b
CHEMBL399617 154669 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 555 7 2 4 5.2 COc1ccc2[nH]cc(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1021/jm070902b
10227655 73713 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 480 9 5 5 2.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(C)(C)O)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018377 73713 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 480 9 5 5 2.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(C)(C)O)c(C)c1 10.1016/j.bmcl.2012.03.007
44415958 80499 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 578 7 1 2 8.0 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CCCCC1 10.1016/j.bmcl.2006.07.011
CHEMBL214747 80499 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 578 7 1 2 8.0 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CCCCC1 10.1016/j.bmcl.2006.07.011
44442575 93544 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 570 9 4 4 3.7 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL246405 93544 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 570 9 4 4 3.7 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
25010616 94151 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(C[C@@H]3CC[C@H](NC(=O)/C=C/c4cc(Cl)cc(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249413 94151 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(C[C@@H]3CC[C@H](NC(=O)/C=C/c4cc(Cl)cc(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
25007996 94153 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 454 7 1 3 5.2 COc1ccc(C2CCN(C[C@@H]3CC[C@H](NC(=O)/C=C/c4cc(F)cc(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249415 94153 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 454 7 1 3 5.2 COc1ccc(C2CCN(C[C@@H]3CC[C@H](NC(=O)/C=C/c4cc(F)cc(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11844209 81083 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 572 8 1 3 7.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccsc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL215515 81083 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 572 8 1 3 7.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccsc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
127028590 137430 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 284 2 1 1 4.2 C[C@@]1(c2cccc(C(F)(F)F)c2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
CHEMBL3753478 137430 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 284 2 1 1 4.2 C[C@@]1(c2cccc(C(F)(F)F)c2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
89823481 126307 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 582 5 1 5 5.4 O=C(O)c1cccc(C2CCN([C@@H]3C[C@H]4CCC[C@@]4(C(=O)N4C[C@@H]5C[C@H]4CN5c4cc(C(F)(F)F)ccn4)C3)CC2)c1 nan
CHEMBL3650355 126307 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 582 5 1 5 5.4 O=C(O)c1cccc(C2CCN([C@@H]3C[C@H]4CCC[C@@]4(C(=O)N4C[C@@H]5C[C@H]4CN5c4cc(C(F)(F)F)ccn4)C3)CC2)c1 nan
89823459 126334 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)cc2C(F)(F)F)C1 nan
CHEMBL3650382 126334 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)cc2C(F)(F)F)C1 nan
89823431 126335 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)c2C)C1 nan
CHEMBL3650383 126335 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)c2C)C1 nan
89823495 126341 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 498 5 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(Cl)c2C#N)C1 nan
CHEMBL3650389 126341 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 498 5 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(Cl)c2C#N)C1 nan
44395256 65469 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 492 8 1 5 4.2 Cc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.008
CHEMBL183001 65469 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 492 8 1 5 4.2 Cc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.008
44593554 188688 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CCC(NC(=O)OCc3ccccc3)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL504065 188688 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CCC(NC(=O)OCc3ccccc3)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
90656019 111108 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 546 5 1 7 1.6 COC1COCCC1N[C@@H]1C[C@H]2N(S(C)(=O)=O)CC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263266 111108 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 546 5 1 7 1.6 COC1COCCC1N[C@@H]1C[C@H]2N(S(C)(=O)=O)CC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
22310943 24514 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2ccc([N+](=O)[O-])cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL134230 24514 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2ccc([N+](=O)[O-])cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
10348168 95461 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 576 6 1 4 6.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccc(Cl)nn3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL257159 95461 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 576 6 1 4 6.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccc(Cl)nn3)CC2)C1 10.1016/j.bmcl.2007.12.029
44425317 168858 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 726 10 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL438128 168858 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 726 10 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
44453330 95502 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 483 6 2 3 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257316 95502 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 483 6 2 3 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
22143225 183565 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CCC(N)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480035 183565 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CCC(N)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
11620726 90640 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL238937 90640 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
11620726 90640 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238937 90640 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
127025448 137441 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 248 2 1 1 3.5 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(F)cc2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753563 137441 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 248 2 1 1 3.5 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(F)cc2)C1 10.1016/j.bmcl.2015.11.051
54768835 86593 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 7 3.6 Nc1cccnc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
CHEMBL2315933 86593 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 7 3.6 Nc1cccnc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
11192346 2024 57 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 2024 57 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 2024 57 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
57656657 75209 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(C(F)(F)F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036760 75209 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(C(F)(F)F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
57656641 75222 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 414 4 1 4 3.3 CC(C)N1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036775 75222 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 414 4 1 4 3.3 CC(C)N1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
53322810 58472 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683075 58472 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
53326721 58493 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 554 6 2 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(O)C(F)(F)F)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683189 58493 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 554 6 2 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(O)C(F)(F)F)C1 10.1016/j.bmcl.2011.01.015
10162844 73714 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 480 10 5 5 2.7 CC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018378 73714 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 480 10 5 5 2.7 CC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
52944966 19040 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 579 9 2 4 5.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1OCc1ccccc1 10.1016/j.bmcl.2010.10.020
CHEMBL1288324 19040 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 579 9 2 4 5.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1OCc1ccccc1 10.1016/j.bmcl.2010.10.020
44425316 142359 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 712 9 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL388869 142359 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 712 9 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
53320350 58675 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 463 6 1 5 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684697 58675 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 463 6 1 5 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
44425646 86100 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 528 6 1 2 7.1 CCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231038 86100 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 528 6 1 2 7.1 CCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44425653 86229 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231246 86229 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44353447 3775 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2007.07.028
785 3775 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2007.07.028
CHEMBL337246 3775 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2007.07.028
53326645 58685 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 477 6 1 4 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CCC(F)(F)F)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684708 58685 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 477 6 1 4 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CCC(F)(F)F)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
53324944 58687 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 457 5 1 4 3.0 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)c2ccccc2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684710 58687 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 457 5 1 4 3.0 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)c2ccccc2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
44425631 142075 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 564 5 1 2 7.6 CCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL388007 142075 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 564 5 1 2 7.6 CCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
89823661 126344 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 541 5 1 5 4.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
CHEMBL3650391 126344 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 541 5 1 5 4.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
54583185 62564 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ncn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782570 62564 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ncn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
89823581 126361 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650407 126361 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
72663455 129401 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671251 129401 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
71518574 86391 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313784 86391 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
11632418 75197 1 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036748 75197 1 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
46241720 83560 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 501 6 3 6 2.3 N#Cc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204242 83560 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 501 6 3 6 2.3 N#Cc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
135981707 65790 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 556 8 2 6 4.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNC3=NC(Cc4ccccc4)c4ccc(C(F)(F)F)cc43)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834783 65790 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 556 8 2 6 4.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNC3=NC(Cc4ccccc4)c4ccc(C(F)(F)F)cc43)C2)CC1 10.1016/j.bmcl.2011.08.074
44441359 93681 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 3 4.2 Cc1ccc2c(c1)OCC(C(=O)Nc1ccc(C[N+](C)(C)C3CCOCC3)cc1)=C2 10.1016/j.bmcl.2007.01.115
CHEMBL246933 93681 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 3 4.2 Cc1ccc2c(c1)OCC(C(=O)Nc1ccc(C[N+](C)(C)C3CCOCC3)cc1)=C2 10.1016/j.bmcl.2007.01.115
10206776 154924 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 10 4 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL401009 154924 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 10 4 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
22310896 117451 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2cc(C(F)(F)F)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL339851 117451 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2cc(C(F)(F)F)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
12093170 872 31 None - 1 Human 6.8 pIC50 = 6.8 Binding
Negative allosteric modulation of CCR2 (unknown origin)Negative allosteric modulation of CCR2 (unknown origin)
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.7b01844
9431 872 31 None - 1 Human 6.8 pIC50 = 6.8 Binding
Negative allosteric modulation of CCR2 (unknown origin)Negative allosteric modulation of CCR2 (unknown origin)
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.7b01844
CHEMBL4519152 872 31 None - 1 Human 6.8 pIC50 = 6.8 Binding
Negative allosteric modulation of CCR2 (unknown origin)Negative allosteric modulation of CCR2 (unknown origin)
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.7b01844
69315675 73811 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 621 14 5 5 5.1 CCC[C@H](O)[C@H](CN(Cc1ccc(C)cc1C)C(C)C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018537 73811 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 621 14 5 5 5.1 CCC[C@H](O)[C@H](CN(Cc1ccc(C)cc1C)C(C)C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
44442570 93736 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 556 9 4 4 3.4 CC(C)(C)NC(=O)[C@H](CNCc1ccc(Br)cc1)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247214 93736 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 556 9 4 4 3.4 CC(C)(C)NC(=O)[C@H](CNCc1ccc(Br)cc1)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
261407 116564 59 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 251 3 1 2 3.4 O=C(O)c1cc2ccccc2n1Cc1ccccc1 10.1016/j.bmcl.2003.10.049
CHEMBL336399 116564 59 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 251 3 1 2 3.4 O=C(O)c1cc2ccccc2n1Cc1ccccc1 10.1016/j.bmcl.2003.10.049
44395104 66699 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 476 9 3 5 3.7 Cc1csc(C(=O)NNC(=O)CN2CCC(NCCC(c3ccccc3)c3ccccc3)C2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL185518 66699 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 476 9 3 5 3.7 Cc1csc(C(=O)NNC(=O)CN2CCC(NCCC(c3ccccc3)c3ccccc3)C2)c1 10.1016/j.bmcl.2004.08.009
18426157 123901 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 6 2 3 3.2 Cc1cccc(C(=O)NCC(=O)NC2CCCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL362780 123901 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 6 2 3 3.2 Cc1cccc(C(=O)NCC(=O)NC2CCCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
57656887 75212 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 376 4 1 3 3.4 O=C(Nc1cccc(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036763 75212 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 376 4 1 3 3.4 O=C(Nc1cccc(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
10239671 187911 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 543 8 3 6 3.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL496632 187911 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 543 8 3 6 3.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2009.05.041
44416274 158554 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL409162 158554 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
46842085 8237 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 572 10 2 4 4.5 CCCc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL1092294 8237 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 572 10 2 4 4.5 CCCc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
44573450 187523 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 492 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCCC2)C1 10.1007/s00044-010-9501-4
CHEMBL494399 187523 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 492 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCCC2)C1 10.1007/s00044-010-9501-4
46842381 8236 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 558 9 2 4 4.1 CCc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL1092293 8236 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 558 9 2 4 4.1 CCc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
53324139 58459 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683062 58459 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2011.01.015
10346048 78234 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.04.045
CHEMBL210606 78234 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.04.045
44573450 187523 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 492 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494399 187523 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 492 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCCC2)C1 10.1016/j.bmcl.2008.12.050
57344217 130632 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 564 7 3 5 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)OC(F)(F)O3)CC1 nan
CHEMBL3681879 130632 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 564 7 3 5 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)OC(F)(F)O3)CC1 nan
72946775 105235 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 597 7 2 8 1.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCNC(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115109 105235 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 597 7 2 8 1.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCNC(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
46241717 83567 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 520 8 3 6 2.9 CCOc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204249 83567 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 520 8 3 6 2.9 CCOc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
46240484 83579 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 496 6 3 6 2.8 Cc1cnc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204261 83579 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 496 6 3 6 2.8 Cc1cnc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
56662695 65805 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 520 7 2 7 4.6 CCc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
CHEMBL1834798 65805 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 520 7 2 7 4.6 CCc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
11669935 58454 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 467 5 1 4 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683055 58454 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 467 5 1 4 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
44425276 151326 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 654 9 2 5 7.8 CC(C)(C)C(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL396101 151326 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 654 9 2 5 7.8 CC(C)(C)C(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
70689909 74536 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 496 6 3 6 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3nccs3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029414 74536 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 496 6 3 6 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3nccs3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
57402219 71008 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
CHEMBL1951766 71008 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
53321503 58492 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 516 8 1 6 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CCCF)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683188 58492 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 516 8 1 6 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CCCF)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
54585107 62561 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782567 62561 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
72946205 105242 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 508 5 1 6 2.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115116 105242 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 508 5 1 6 2.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44453327 95095 25 None - 0 Human 6.8 pIC50 = 6.8 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL255408 95095 25 None - 0 Human 6.8 pIC50 = 6.8 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
70691783 73701 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 12 4 4 3.9 CCCC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018364 73701 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 12 4 4 3.9 CCCC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
57402124 70523 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 511 8 3 5 2.8 CN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1947041 70523 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 511 8 3 5 2.8 CN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
10346048 78234 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.011
CHEMBL210606 78234 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.011
44441356 96704 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 471 5 1 3 4.6 C[N+](C)(Cc1ccc(NC(=O)C2=Cc3ccc(Br)cc3OC2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL264108 96704 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 471 5 1 3 4.6 C[N+](C)(Cc1ccc(NC(=O)C2=Cc3ccc(Br)cc3OC2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
44453327 95095 25 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL255408 95095 25 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
44444111 94117 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(Cl)cc(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249209 94117 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(Cl)cc(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
90656022 111118 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 510 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CC3CC2CN3c2cccc(C(F)(F)F)n2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263276 111118 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 510 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CC3CC2CN3c2cccc(C(F)(F)F)n2)C1 10.1016/j.bmcl.2014.03.036
10346048 78234 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL210606 78234 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1021/jm060439n
11670910 88622 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 524 6 2 3 4.6 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL235657 88622 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 524 6 2 3 4.6 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
71519225 86375 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 423 4 1 5 2.8 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(C#N)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313767 86375 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 423 4 1 5 2.8 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(C#N)cc3C2)C1 10.1016/j.bmcl.2012.10.069
49763568 65416 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829606 65416 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
44444007 93999 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 428 9 1 2 5.7 O=C(/C=C/c1ccc(F)cc1)NCCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL248641 93999 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 428 9 1 2 5.7 O=C(/C=C/c1ccc(F)cc1)NCCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
11670910 88622 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 524 6 2 3 4.6 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL235657 88622 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 524 6 2 3 4.6 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
122181146 121834 0 None - 0 Mouse 4.8 pIC50 = 4.8 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 544 7 1 4 5.7 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589841 121834 0 None - 0 Mouse 4.8 pIC50 = 4.8 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 544 7 1 4 5.7 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.02.019
44439159 91981 1 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 522 11 1 4 6.8 CN(C)CCCCNC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241501 91981 1 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 522 11 1 4 6.8 CN(C)CCCCNC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
49863200 15210 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 508 10 1 4 6.4 CN(C)CCCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL1210668 15210 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 508 10 1 4 6.4 CN(C)CCCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
25268803 151878 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 383 6 1 2 4.2 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2cccc(F)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL396571 151878 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 383 6 1 2 4.2 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2cccc(F)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL11359 9780 0 None -2 4 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL None None None None nan
89823461 126317 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 491 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(Cl)c2)C1 nan
CHEMBL3650365 126317 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 491 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(Cl)c2)C1 nan
44425247 166295 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 585 8 2 6 5.7 Cc1ccccc1N1CCN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(N)n2)CC1 10.1016/j.bmcl.2006.10.059
CHEMBL427110 166295 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 585 8 2 6 5.7 Cc1ccccc1N1CCN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(N)n2)CC1 10.1016/j.bmcl.2006.10.059
52943756 19290 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
CHEMBL1290412 19290 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
44425320 86135 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 713 9 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3cccnc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL231149 86135 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 713 9 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3cccnc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
56643545 130623 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681870 130623 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
44573537 193233 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 512 6 2 2 6.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2Cc3ccccc3C2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL523696 193233 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 512 6 2 2 6.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2Cc3ccccc3C2)C1 10.1016/j.bmcl.2008.12.050
44573538 193266 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 526 6 2 2 6.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc3C2)C1 10.1007/s00044-010-9501-4
CHEMBL523861 193266 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 526 6 2 2 6.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc3C2)C1 10.1007/s00044-010-9501-4
57392725 67866 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assayDisplacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assay
ChEMBL 467 9 2 3 5.6 O=C(NCCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2011.09.013
CHEMBL1910162 67866 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assayDisplacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assay
ChEMBL 467 9 2 3 5.6 O=C(NCCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2011.09.013
46885213 8460 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093802 8460 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
68004011 86587 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 530 7 3 8 3.1 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2012.12.017
CHEMBL2315927 86587 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 530 7 3 8 3.1 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2012.12.017
54769752 86607 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1nncc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2316210 86607 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1nncc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
57344296 68951 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
CHEMBL1922813 68951 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
10278257 73709 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 11 4 4 3.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CC(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018373 73709 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 11 4 4 3.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CC(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
10207590 73710 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 507 10 4 4 4.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CC(C)(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018374 73710 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 507 10 4 4 4.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CC(C)(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
71452241 83568 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 574 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OCC(F)(F)F)nc3)CC2)C1 10.1021/ml300260s
CHEMBL2204250 83568 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 574 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OCC(F)(F)F)nc3)CC2)C1 10.1021/ml300260s
56657929 65792 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 485 6 2 5 4.5 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccccc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834785 65792 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 485 6 2 5 4.5 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccccc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
56659197 65804 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 506 6 2 7 4.3 Cc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
CHEMBL1834797 65804 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 506 6 2 7 4.3 Cc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
44425637 85987 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230405 85987 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44425317 168858 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 726 10 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL438128 168858 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 726 10 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
508869 95440 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 446 7 3 4 3.1 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257066 95440 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 446 7 3 4 3.1 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
44442587 93809 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCc2ccccc2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247608 93809 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCc2ccccc2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442593 147200 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 549 11 5 5 3.7 CCNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL392814 147200 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 549 11 5 5 3.7 CCNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
10278257 73709 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 493 11 4 4 3.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CC(C)C)c(C)c1 10.1021/ml500505q
CHEMBL2018373 73709 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 493 11 4 4 3.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CC(C)C)c(C)c1 10.1021/ml500505q
53322812 58478 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 500 7 1 7 2.3 COC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683081 58478 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 500 7 1 7 2.3 COC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
54585109 62573 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 468 5 1 5 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782579 62573 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 468 5 1 5 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.034
89823606 126325 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
CHEMBL3650373 126325 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
72946982 105229 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 602 6 1 7 3.8 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115103 105229 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 602 6 1 7 3.8 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57344218 68948 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 484 7 3 3 4.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL1922806 68948 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 484 7 3 3 4.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2)CC1 nan
46241719 83587 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 494 6 3 5 2.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(F)nc3)CC2)C1 10.1021/ml300260s
CHEMBL2204270 83587 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 494 6 3 5 2.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(F)nc3)CC2)C1 10.1021/ml300260s
46241829 65414 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 476 6 3 5 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829603 65414 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 476 6 3 5 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.06.080
10165042 93553 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 522 10 4 5 3.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(OC(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246416 93553 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 522 10 4 5 3.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(OC(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442556 93727 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 522 11 5 5 2.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)CO)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247204 93727 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 522 11 5 5 2.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)CO)c(C)c1 10.1016/j.bmcl.2007.07.028
90656026 111121 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 527 7 1 7 2.4 COC1COCCC1N(CCCO)[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263281 111121 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 527 7 1 7 2.4 COC1COCCC1N(CCCO)[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
44444001 94512 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 450 8 1 2 5.5 O=C(/C=C/c1cc(F)c(F)c(F)c1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL251621 94512 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 450 8 1 2 5.5 O=C(/C=C/c1cc(F)c(F)c(F)c1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
23441058 66271 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 429 8 0 4 5.3 O=[N+]([O-])c1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL184688 66271 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 429 8 0 4 5.3 O=[N+]([O-])c1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44395160 123808 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 398 9 1 3 4.5 O=C(CCCC(=O)c1ccccc1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL362340 123808 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 398 9 1 3 4.5 O=C(CCCC(=O)c1ccccc1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
44415973 81055 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 536 8 1 2 7.0 C=CC[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215394 81055 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 536 8 1 2 7.0 C=CC[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44425654 86230 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231247 86230 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44573409 187394 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 450 6 2 2 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL493575 187394 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 450 6 2 2 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCC2)C1 10.1016/j.bmcl.2008.12.050
44573409 187394 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 450 6 2 2 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCC2)C1 10.1007/s00044-010-9501-4
CHEMBL493575 187394 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 450 6 2 2 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCC2)C1 10.1007/s00044-010-9501-4
89823470 126309 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)n2)C1 nan
CHEMBL3650357 126309 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)n2)C1 nan
10153373 172596 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 627 13 2 6 5.4 CCCN(CCC)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
CHEMBL448989 172596 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 627 13 2 6 5.4 CCCN(CCC)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
86767120 129403 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 468 4 1 5 2.9 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671253 129403 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 468 4 1 5 2.9 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 nan
44448915 95072 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 568 7 3 4 5.0 CC(=O)Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL255302 95072 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 568 7 3 4 5.0 CC(=O)Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
44449054 155191 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 553 6 2 3 5.6 O=C(/C=C/c1ccc(F)c(Br)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL402442 155191 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 553 6 2 3 5.6 O=C(/C=C/c1ccc(F)c(Br)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
162666730 182274 1 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182274 1 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
71768722 111112 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 468 4 1 5 2.9 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263270 111112 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 468 4 1 5 2.9 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
10239991 188447 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 585 10 3 6 4.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502516 188447 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 585 10 3 6 4.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
10120907 73724 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 577 12 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018388 73724 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 577 12 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCC1 10.1016/j.bmcl.2012.03.007
10007642 19109 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289203 19109 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
89844945 109809 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 518 7 1 6 2.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)n3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233179 109809 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 518 7 1 6 2.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)n3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
68767078 121236 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 457 7 1 5 5.0 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(Cl)cc23)C1=O 10.1021/ml500505q
CHEMBL3577944 121236 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 457 7 1 5 5.0 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(Cl)cc23)C1=O 10.1021/ml500505q
68768752 121238 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 463 5 1 5 4.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](C)C1 10.1021/ml500505q
CHEMBL3577947 121238 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 463 5 1 5 4.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](C)C1 10.1021/ml500505q
11756884 19089 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289083 19089 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
10007642 19109 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289203 19109 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
9986630 168799 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 641 9 2 5 6.9 CN(C)C(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL437552 168799 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 641 9 2 5 6.9 CN(C)C(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
11627639 94933 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL254355 94933 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
57396999 71018 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
CHEMBL1951777 71018 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
22143258 183879 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 522 9 3 5 3.9 CSc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481010 183879 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 522 9 3 5 3.9 CSc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44593555 188784 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL505722 188784 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
70691785 73727 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 606 12 6 6 2.9 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCNCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018391 73727 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 606 12 6 6 2.9 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCNCC1 10.1016/j.bmcl.2012.03.007
69285794 121229 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 455 9 2 3 4.6 CCCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577937 121229 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 455 9 2 3 4.6 CCCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
122178128 121232 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 503 9 2 3 5.1 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CCc2ccccc2)C1 10.1021/ml500505q
CHEMBL3577940 121232 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 503 9 2 3 5.1 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CCc2ccccc2)C1 10.1021/ml500505q
11555827 147117 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 555 7 2 4 5.2 COc1cccc2c(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c[nH]c12 10.1021/jm070902b
CHEMBL392748 147117 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 555 7 2 4 5.2 COc1cccc2c(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c[nH]c12 10.1021/jm070902b
42606792 109808 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 517 7 1 5 3.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233178 109808 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 517 7 1 5 3.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
57395218 71010 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnc3)CC2)C1 10.1021/ml200030q
CHEMBL1951769 71010 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnc3)CC2)C1 10.1021/ml200030q
44425279 142017 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL387583 142017 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
11527661 2021 30 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human CCR2-mediated Erk phosphorylationInhibition of human CCR2-mediated Erk phosphorylation
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
9045 2021 30 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human CCR2-mediated Erk phosphorylationInhibition of human CCR2-mediated Erk phosphorylation
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
CHEMBL1963131 2021 30 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human CCR2-mediated Erk phosphorylationInhibition of human CCR2-mediated Erk phosphorylation
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
69285794 121229 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 455 9 2 3 4.6 CCCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577937 121229 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 455 9 2 3 4.6 CCCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
68767078 121236 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 457 7 1 5 5.0 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(Cl)cc23)C1=O 10.1021/ml500505q
CHEMBL3577944 121236 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 457 7 1 5 5.0 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(Cl)cc23)C1=O 10.1021/ml500505q
44583282 172695 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 656 9 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCOCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL450231 172695 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 656 9 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCOCC2)cc1 10.1016/j.bmcl.2009.05.041
11597 674 5 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00082
23725180 674 5 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00082
CHEMBL4781426 674 5 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00082
11421840 77638 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 578 9 2 5 5.2 CCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088379 77638 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 578 9 2 5 5.2 CCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
50992246 58471 2 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683074 58471 2 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
50992246 58471 2 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to rat CCR2Binding affinity to rat CCR2
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683074 58471 2 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to rat CCR2Binding affinity to rat CCR2
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
24794656 180876 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 450 4 3 6 2.0 CC(=O)N[C@@H]1C[C@H](N)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4757452 180876 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 450 4 3 6 2.0 CC(=O)N[C@@H]1C[C@H](N)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
52941377 19329 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290637 19329 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
53326386 58173 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 465 5 1 6 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1681819 58173 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 465 5 1 6 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
44573608 187551 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 522 8 2 3 6.3 CCCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
CHEMBL494540 187551 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 522 8 2 3 6.3 CCCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
54771978 86606 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 505 6 3 7 3.8 O=C(CNc1nccc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2316209 86606 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 505 6 3 7 3.8 O=C(CNc1nccc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
44595711 137321 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of chemotaxis
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752627 137321 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of chemotaxis
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
24794624 179616 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 492 6 3 6 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4742683 179616 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 492 6 3 6 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
57400160 130639 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 3 5.6 O=C(O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681885 130639 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 3 5.6 O=C(O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
86767125 129408 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 511 6 1 6 3.5 CCCC1CC2(C(=O)N3CCc4ncc(C(F)(F)F)cc4C3)CC(NC3CCOCC3OC)CC2O1 nan
CHEMBL3671258 129408 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 511 6 1 6 3.5 CCCC1CC2(C(=O)N3CCc4ncc(C(F)(F)F)cc4C3)CC(NC3CCOCC3OC)CC2O1 nan
44449030 95146 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 543 6 2 3 6.1 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL255680 95146 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 543 6 2 3 6.1 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
44449174 95456 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 553 7 1 4 5.6 CC(=O)OCC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL257143 95456 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 553 7 1 4 5.6 CC(=O)OCC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
44448948 155246 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 569 7 2 5 4.9 COC(=O)c1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL402749 155246 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 569 7 2 5 4.9 COC(=O)c1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
71517242 86380 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 501 4 1 5 3.5 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](Cl)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313772 86380 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 501 4 1 5 3.5 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](Cl)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
11226430 73739 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 536 14 5 5 4.9 CCCNc1cc(NC(=O)CC(=O)N[C@@H](CNCc2ccc(C)cc2C)[C@@H](O)CCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018403 73739 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 536 14 5 5 4.9 CCCNc1cc(NC(=O)CC(=O)N[C@@H](CNCc2ccc(C)cc2C)[C@@H](O)CCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
49764322 65441 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 505 7 3 5 3.1 COc1ccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
CHEMBL1829632 65441 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 505 7 3 5 3.1 COc1ccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
11502371 153128 3 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL397647 153128 3 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
44425636 85948 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 590 6 1 2 8.0 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230078 85948 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 590 6 1 2 8.0 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44425629 86026 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230616 86026 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44425241 86028 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 570 8 2 5 6.4 Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230624 86028 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 570 8 2 5 6.4 Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44453407 95437 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 450 7 3 5 2.4 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257063 95437 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 450 7 3 5 2.4 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
44453442 97690 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 434 6 3 4 2.7 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271290 97690 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 434 6 3 4 2.7 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
44442599 93649 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL246804 93649 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
69285465 121230 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 457 9 2 4 3.5 COCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577938 121230 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 457 9 2 4 3.5 COCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
11699541 146313 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 543 6 2 3 5.3 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3cc(F)ccc23)CC1 10.1021/jm070902b
CHEMBL392098 146313 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 543 6 2 3 5.3 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3cc(F)ccc23)CC1 10.1021/jm070902b
11605867 166766 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 507 6 2 3 5.0 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL428378 166766 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 507 6 2 3 5.0 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
54582217 62570 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 512 7 1 6 3.7 CCO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782576 62570 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 512 7 1 6 3.7 CCO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
71517576 86369 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 497 5 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](OC)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313761 86369 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 497 5 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](OC)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
71518898 86390 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 477 4 1 5 3.1 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(Br)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313783 86390 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 477 4 1 5 3.1 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(Br)cc3C2)C1 10.1016/j.bmcl.2012.10.069
56675302 65757 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 451 8 3 5 3.3 C=CCO[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834648 65757 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 451 8 3 5 3.3 C=CCO[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56669631 65809 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 489 6 2 7 3.3 Cn1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)n1 10.1016/j.bmcl.2011.08.074
CHEMBL1834851 65809 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 489 6 2 7 3.3 Cn1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)n1 10.1016/j.bmcl.2011.08.074
25268081 93519 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 423 5 1 2 5.7 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCSCC1 10.1016/j.bmcl.2007.01.115
CHEMBL246313 93519 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 423 5 1 2 5.7 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCSCC1 10.1016/j.bmcl.2007.01.115
9934977 166355 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 482 7 3 4 3.7 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2006.04.045
CHEMBL427396 166355 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 482 7 3 4 3.7 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2006.04.045
44442560 154926 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 490 11 4 4 2.6 C=CCNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL401011 154926 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 490 11 4 4 2.6 C=CCNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
11548199 89922 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-mouse MCP1 from CCR2 in mouse WEHI265.1 cellsDisplacement of [125I]-mouse MCP1 from CCR2 in mouse WEHI265.1 cells
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237967 89922 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-mouse MCP1 from CCR2 in mouse WEHI265.1 cellsDisplacement of [125I]-mouse MCP1 from CCR2 in mouse WEHI265.1 cells
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
11548199 89922 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-mouse MCP1 from CCR2 in mouse peripheral blood monocytesDisplacement of [125I]-mouse MCP1 from CCR2 in mouse peripheral blood monocytes
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237967 89922 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-mouse MCP1 from CCR2 in mouse peripheral blood monocytesDisplacement of [125I]-mouse MCP1 from CCR2 in mouse peripheral blood monocytes
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
11548199 89922 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-rat MCP1 from rat CCR2 receptor in monocytesDisplacement of [125I]-rat MCP1 from rat CCR2 receptor in monocytes
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237967 89922 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-rat MCP1 from rat CCR2 receptor in monocytesDisplacement of [125I]-rat MCP1 from rat CCR2 receptor in monocytes
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
42632863 93356 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 373 5 1 2 4.3 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)cc2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL245497 93356 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 373 5 1 2 4.3 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)cc2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
44444104 94071 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 458 5 0 2 5.8 O=C(/C=C/c1ccc(F)c(F)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL249008 94071 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 458 5 0 2 5.8 O=C(/C=C/c1ccc(F)c(F)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
10957890 23094 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 310 3 1 3 3.9 N#Cc1cccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)c1 10.1016/j.bmcl.2003.10.049
CHEMBL133063 23094 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 310 3 1 3 3.9 N#Cc1cccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)c1 10.1016/j.bmcl.2003.10.049
44415992 80609 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215093 80609 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44453300 97436 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 451 7 2 4 3.5 CSc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL270005 97436 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 451 7 2 4 3.5 CSc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
44441382 153058 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 4.7 C[N+](C)(Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL397595 153058 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 4.7 C[N+](C)(Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
11706775 145768 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 564 13 1 4 7.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL391668 145768 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 564 13 1 4 7.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
11706775 145768 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 564 13 1 4 7.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL391668 145768 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 564 13 1 4 7.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44453562 155654 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 431 7 3 6 2.0 Nc1ccc([N+](=O)[O-])cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404837 155654 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 431 7 3 6 2.0 Nc1ccc([N+](=O)[O-])cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
56678640 65758 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 488 7 4 6 1.7 CS(=O)(=O)N[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834650 65758 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 488 7 4 6 1.7 CS(=O)(=O)N[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
54768836 86596 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 508 6 2 6 4.5 N#Cc1ccccc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
CHEMBL2315936 86596 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 508 6 2 6 4.5 N#Cc1ccccc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
72947193 105231 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 568 6 1 7 3.3 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115105 105231 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 568 6 1 7 3.3 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
10585 1079 1 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1079 1 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1079 1 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
57401954 68959 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)c(F)c2)CC1 nan
CHEMBL1922822 68959 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)c(F)c2)CC1 nan
57656871 75227 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 413 3 2 4 2.0 CCN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036780 75227 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 413 3 2 4 2.0 CCN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
49764447 65422 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829613 65422 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
54755801 65760 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 559 8 3 8 3.7 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834652 65760 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 559 8 3 8 3.7 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
24801525 97609 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 526 7 4 5 1.9 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL270906 97609 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 526 7 4 5 1.9 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
22143104 188058 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 483 7 5 5 2.3 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)NC1CNCCC1NCc1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497780 188058 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 483 7 5 5 2.3 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)NC1CNCCC1NCc1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.123
44573488 187679 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 482 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSC2)C1 10.1007/s00044-010-9501-4
CHEMBL495165 187679 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 482 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSC2)C1 10.1007/s00044-010-9501-4
71517575 86388 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 497 5 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](OC)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313780 86388 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 497 5 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](OC)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
49764700 65438 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 493 6 3 4 3.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829629 65438 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 493 6 3 4 3.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
127025461 137385 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 348 3 2 2 4.0 C[C@@]1(c2ccc(Cl)c(C(F)(F)F)c2)C[C@@H](CO)CC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
CHEMBL3753161 137385 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 348 3 2 2 4.0 C[C@@]1(c2ccc(Cl)c(C(F)(F)F)c2)C[C@@H](CO)CC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
11692057 145489 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 516 7 2 5 4.7 O=C(O)C(C1CCN(C(=O)/C=C/c2ccc([N+](=O)[O-])cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL391460 145489 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 516 7 2 5 4.7 O=C(O)C(C1CCN(C(=O)/C=C/c2ccc([N+](=O)[O-])cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
23656585 147631 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)[C@@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL393135 147631 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)[C@@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
44444009 94000 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 424 10 1 3 5.0 COc1ccc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248642 94000 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 424 10 1 3 5.0 COc1ccc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2007.07.065
23441036 67211 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 510 8 3 7 3.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(O)cc3)c3ccc(O)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL187856 67211 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 510 8 3 7 3.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(O)cc3)c3ccc(O)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
24801180 98040 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
CHEMBL273079 98040 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
11577400 58455 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 535 5 1 4 5.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683056 58455 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 535 5 1 4 5.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
71768899 111124 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 543 4 1 5 4.5 O=C(O)c1ccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4CCc5ncc(C(F)(F)F)cc5C4)C3)CC2)cc1 10.1016/j.bmcl.2014.03.036
CHEMBL3263284 111124 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 543 4 1 5 4.5 O=C(O)c1ccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4CCc5ncc(C(F)(F)F)cc5C4)C3)CC2)cc1 10.1016/j.bmcl.2014.03.036
44415927 80855 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 512 9 1 2 6.8 C=CC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215271 80855 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 512 9 1 2 6.8 C=CC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
11364218 73804 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 509 12 4 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)ccc1OC 10.1016/j.bmcl.2012.03.007
CHEMBL2018529 73804 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 509 12 4 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)ccc1OC 10.1016/j.bmcl.2012.03.007
24801179 156640 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 461 7 3 3 4.3 Cc1ccc(CN[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL406925 156640 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 461 7 3 3 4.3 Cc1ccc(CN[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
10458152 77801 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL209267 77801 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
4485 69379 118 None -1 8 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] nan
CHEMBL193 69379 118 None -1 8 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] nan
68003782 86583 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3ccns3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315923 86583 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3ccns3)CC2)C1 10.1016/j.bmcl.2012.12.017
68004010 86586 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 548 7 3 8 4.3 CC(C)c1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2012.12.017
CHEMBL2315926 86586 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 548 7 3 8 4.3 CC(C)c1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2012.12.017
71530223 86372 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 467 4 1 5 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313764 86372 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 467 4 1 5 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
49764196 65442 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 519 6 3 6 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829633 65442 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 519 6 3 6 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
44573487 192634 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 496 6 2 3 6.0 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL521697 192634 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 496 6 2 3 6.0 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSCC2)C1 10.1016/j.bmcl.2008.12.050
53320171 58476 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 512 7 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(C)C)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683079 58476 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 512 7 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(C)C)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
72948000 105224 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 601 6 2 6 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115099 105224 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 601 6 2 6 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
67774351 130638 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 521 7 3 3 5.5 O=C(O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681884 130638 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 521 7 3 3 5.5 O=C(O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
46241827 83564 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 520 7 3 6 2.8 COc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1C 10.1021/ml300260s
CHEMBL2204246 83564 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 520 7 3 6 2.8 COc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1C 10.1021/ml300260s
10458152 77801 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1021/jm060439n
CHEMBL209267 77801 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1021/jm060439n
44353396 115249 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 313 3 1 2 4.7 Cc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1C 10.1016/j.bmcl.2003.10.049
CHEMBL334766 115249 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 313 3 1 2 4.7 Cc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1C 10.1016/j.bmcl.2003.10.049
10203447 154628 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL399328 154628 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2012.03.007
10203447 154628 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL399328 154628 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2007.07.028
44444103 94036 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 470 5 0 2 6.4 Cc1ccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248814 94036 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 470 5 0 2 6.4 Cc1ccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2007.07.065
90656020 111109 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 602 6 1 7 3.9 COC1COCCC1N[C@@H]1C[C@H]2N(C(=O)OCc3ccccc3)CC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263267 111109 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 602 6 1 7 3.9 COC1COCCC1N[C@@H]1C[C@H]2N(C(=O)OCc3ccccc3)CC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
22310839 21741 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 397 4 1 4 4.1 CS(=O)(=O)c1ccc2c(c1)cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL131885 21741 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 397 4 1 4 4.1 CS(=O)(=O)c1ccc2c(c1)cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
89823443 126343 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2C#N)C1 nan
CHEMBL3650390 126343 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2C#N)C1 nan
44395097 67066 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 385 7 2 3 2.9 O=C(CCNC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL187237 67066 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 385 7 2 3 2.9 O=C(CCNC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
44442541 154820 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 10 4 4 2.5 CCNC(=O)[C@@H](CNC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)NCc1ccc(C)cc1C 10.1016/j.bmcl.2007.07.028
CHEMBL400382 154820 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 10 4 4 2.5 CCNC(=O)[C@@H](CNC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)NCc1ccc(C)cc1C 10.1016/j.bmcl.2007.07.028
44439155 91974 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 594 12 4 6 5.2 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241497 91974 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 594 12 4 6 5.2 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
53317526 58473 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 470 5 1 6 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683076 58473 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 470 5 1 6 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
46842235 7836 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 598 8 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089629 7836 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 598 8 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
44453298 155239 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 421 6 3 4 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL402723 155239 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 421 6 3 4 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
44570780 184045 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 508 7 4 5 3.0 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL482201 184045 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 508 7 4 5 3.0 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44425649 86129 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 86129 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44425305 86064 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 555 8 1 4 6.9 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H](CCN1CCC(c2ccccc2)CC1)c1cscn1 10.1016/j.bmcl.2006.10.059
CHEMBL230828 86064 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 555 8 1 4 6.9 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H](CCN1CCC(c2ccccc2)CC1)c1cscn1 10.1016/j.bmcl.2006.10.059
69285465 121230 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 457 9 2 4 3.5 COCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577938 121230 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 457 9 2 4 3.5 COCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
68003997 86600 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 530 6 3 8 3.6 N#Cc1cc(NCC(=O)NC2CN([C@H]3CC[C@@](O)(c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc2n1 10.1016/j.bmcl.2012.12.017
CHEMBL2315940 86600 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 530 6 3 8 3.6 N#Cc1cc(NCC(=O)NC2CN([C@H]3CC[C@@](O)(c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc2n1 10.1016/j.bmcl.2012.12.017
57344298 68952 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cccc(F)c2)CC1 nan
CHEMBL1922814 68952 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cccc(F)c2)CC1 nan
71517240 86378 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 485 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313770 86378 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 485 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
56659295 65810 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 503 7 2 7 4.2 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4noc5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834852 65810 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 503 7 2 7 4.2 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4noc5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44425318 150311 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 732 10 2 6 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3cccs3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL395289 150311 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 732 10 2 6 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3cccs3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
44442586 93811 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247621 93811 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442588 93918 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 577 12 5 5 4.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248188 93918 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 577 12 5 5 4.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
24801526 97616 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 541 7 5 6 1.5 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(S(N)(=O)=O)cc1 10.1021/jm701488f
CHEMBL270959 97616 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 541 7 5 6 1.5 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(S(N)(=O)=O)cc1 10.1021/jm701488f
72947413 105256 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 510 4 1 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115271 105256 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 510 4 1 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57344229 130640 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 3 6.5 O=C(O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3681886 130640 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 3 6.5 O=C(O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
54755562 65787 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 549 8 2 7 4.0 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(CC(F)(F)F)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834780 65787 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 549 8 2 7 4.0 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(CC(F)(F)F)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
25268440 93907 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 373 5 1 2 4.3 C[N+](C)(Cc1ccc(NC(=O)c2cccc(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL248153 93907 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 373 5 1 2 4.3 C[N+](C)(Cc1ccc(NC(=O)c2cccc(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
44573651 187209 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 6 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492376 187209 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 6 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(C)C)C1 10.1016/j.bmcl.2008.12.050
10276594 93965 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 464 9 4 4 2.1 CNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248420 93965 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 464 9 4 4 2.1 CNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
15290299 22616 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 319 3 1 2 4.7 O=C(O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL132664 22616 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 319 3 1 2 4.7 O=C(O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
22310883 116740 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 334 3 2 3 4.3 Nc1cccc2c1cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL337485 116740 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 334 3 2 3 4.3 Nc1cccc2c1cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44573699 187674 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 508 6 2 3 5.8 CC1COCC(C)C1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
CHEMBL495151 187674 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 508 6 2 3 5.8 CC1COCC(C)C1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
44395029 127288 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL365854 127288 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
44444002 93996 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 410 9 1 3 4.6 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248638 93996 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 410 9 1 3 4.6 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2007.07.065
22310869 19473 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1ccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c2c1 10.1016/j.bmcl.2003.10.049
CHEMBL129833 19473 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1ccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c2c1 10.1016/j.bmcl.2003.10.049
183790 3742 11 None - 2 Mouse 4.6 pIC50 = 4.6 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
783 3742 11 None - 2 Mouse 4.6 pIC50 = 4.6 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
CHEMBL1178786 3742 11 None - 2 Mouse 4.6 pIC50 = 4.6 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
44415939 140133 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 510 6 1 2 6.4 C[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL380190 140133 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 510 6 1 2 6.4 C[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44425638 153534 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 620 9 1 2 9.2 CCCCCCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL398001 153534 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 620 9 1 2 9.2 CCCCCCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44415996 80043 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 586 8 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)Cc1ccccc1 10.1016/j.bmcl.2006.07.011
CHEMBL212939 80043 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 586 8 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)Cc1ccccc1 10.1016/j.bmcl.2006.07.011
53317527 58481 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 526 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C2CCOC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683084 58481 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 526 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C2CCOC2)C1 10.1016/j.bmcl.2011.01.015
71518406 86401 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 421 3 1 3 4.5 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314056 86401 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 421 3 1 3 4.5 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCC1)C2 10.1016/j.bmcl.2012.10.069
89823349 126316 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C)c(C(F)(F)F)c2)C1 nan
CHEMBL3650364 126316 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C)c(C(F)(F)F)c2)C1 nan
44593562 187495 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
CHEMBL494191 187495 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
44453370 155743 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 385 6 2 3 2.8 Cc1cccc(C(=O)NCC(=O)N[C@@H]2CCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2008.02.015
CHEMBL405632 155743 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 385 6 2 3 2.8 Cc1cccc(C(=O)NCC(=O)N[C@@H]2CCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2008.02.015
44573538 193266 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 526 6 2 2 6.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc3C2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL523861 193266 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 526 6 2 2 6.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc3C2)C1 10.1016/j.bmcl.2008.12.050
11606167 90950 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 526 14 1 5 6.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(OC)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239359 90950 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 526 14 1 5 6.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(OC)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
11606167 90950 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 526 14 1 5 6.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(OC)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL239359 90950 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 526 14 1 5 6.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(OC)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
71519381 86373 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 467 4 1 5 3.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313765 86373 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 467 4 1 5 3.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
86767124 129407 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 483 4 1 6 2.7 COC1COCCC1NC1CC2OC(C)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671257 129407 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 483 4 1 6 2.7 COC1COCCC1NC1CC2OC(C)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
11489078 73805 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 509 12 4 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(OC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018530 73805 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 509 12 4 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(OC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
44447815 155038 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 592 6 2 5 6.0 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cc(Cl)ncn3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL401608 155038 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 592 6 2 5 6.0 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cc(Cl)ncn3)CC2)C1 10.1016/j.bmcl.2007.12.029
53320350 58675 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 463 6 1 5 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684697 58675 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 463 6 1 5 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
10162782 73706 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL2018370 73706 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
11180885 73735 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 594 12 5 6 5.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)ccc1NC(=O)OC(C)(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018399 73735 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 594 12 5 6 5.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)ccc1NC(=O)OC(C)(C)C 10.1016/j.bmcl.2012.03.007
49763575 65445 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 474 6 3 4 3.0 N[C@]1(c2ccccc2)CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
CHEMBL1829637 65445 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 474 6 3 4 3.0 N[C@]1(c2ccccc2)CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
44444112 154842 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 454 7 1 3 5.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(F)cc(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL400484 154842 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 454 7 1 3 5.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(F)cc(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
44449204 95709 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 581 8 3 3 5.4 CCNC(=O)NCC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL258252 95709 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 581 8 3 3 5.4 CCNC(=O)NCC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
44395222 67044 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 512 8 2 6 3.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL187126 67044 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 512 8 2 6 3.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
10279914 73704 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 527 11 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)Cc2ccccc2)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018368 73704 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 527 11 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)Cc2ccccc2)c(C)c1 10.1016/j.bmcl.2012.03.007
44453369 97768 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 405 6 2 3 3.1 O=C(CNC(=O)c1cccc(Cl)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL271726 97768 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 405 6 2 3 3.1 O=C(CNC(=O)c1cccc(Cl)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
122181144 121832 0 None - 0 Mouse 4.6 pIC50 = 4.6 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 514 6 1 3 5.7 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2015.02.019
CHEMBL3589839 121832 0 None - 0 Mouse 4.6 pIC50 = 4.6 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 514 6 1 3 5.7 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2015.02.019
8447 188949 84 None -12 13 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 188949 84 None -12 13 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
44415900 79936 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 589 8 2 4 4.7 CS(=O)(=O)NC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL212542 79936 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 589 8 2 4 4.7 CS(=O)(=O)NC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
3117 207841 103 None -2 16 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 207841 103 None -2 16 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
71517737 86371 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 1 6 2.9 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](N(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313763 86371 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 1 6 2.9 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](N(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
127027956 137580 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 294 2 1 1 4.8 Cc1ccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c2ccccc12 10.1016/j.bmcl.2015.11.051
CHEMBL3754764 137580 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 294 2 1 1 4.8 Cc1ccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c2ccccc12 10.1016/j.bmcl.2015.11.051
69285531 121227 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 441 8 2 3 4.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577935 121227 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 441 8 2 3 4.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
57344303 68931 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922789 68931 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
57344305 68939 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922797 68939 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
46944853 65430 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 490 7 2 5 3.4 COc1cc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)ccn1 10.1016/j.bmcl.2011.06.080
CHEMBL1829621 65430 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 490 7 2 5 3.4 COc1cc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)ccn1 10.1016/j.bmcl.2011.06.080
56677288 65443 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 517 6 3 5 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCC4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829634 65443 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 517 6 3 5 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCC4)CC2)C1 10.1016/j.bmcl.2011.06.080
44416157 80595 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CC[C@H](CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL215020 80595 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CC[C@H](CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
44413257 77441 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 464 8 1 3 5.4 CN(C)CCS[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL208685 77441 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 464 8 1 3 5.4 CN(C)CCS[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
11670968 169375 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 6.1 O=C(O)C(C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL442085 169375 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 6.1 O=C(O)C(C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
54585108 62563 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782569 62563 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
89823348 126348 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 575 5 1 5 4.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
CHEMBL3650395 126348 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 575 5 1 5 4.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
46241609 83566 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 506 7 3 6 2.5 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1021/ml300260s
CHEMBL2204248 83566 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 506 7 3 6 2.5 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1021/ml300260s
25268085 93906 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 417 5 1 2 4.5 C[N+](C)(Cc1ccc(NC(=O)c2cccc(Br)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL248151 93906 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 417 5 1 2 4.5 C[N+](C)(Cc1ccc(NC(=O)c2cccc(Br)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
10227556 93966 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 9 3 4 2.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)N(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248421 93966 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 9 3 4 2.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)N(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
89823555 126300 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@H]3C[C@@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650348 126300 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@H]3C[C@@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
89823534 126301 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@H]3C[C@@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650349 126301 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@H]3C[C@@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
89823347 126330 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ncccc2C(F)(F)F)C1 nan
CHEMBL3650378 126330 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ncccc2C(F)(F)F)C1 nan
89834736 126338 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.6 CO[C@@H]1COCC[C@H]1NC1C[C@H]2CCC[C@@]2(C(=O)N2[C@H]3CC[C@@H]2CN(c2cc(C(F)(F)F)ccn2)C3)C1 nan
CHEMBL3650386 126338 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.6 CO[C@@H]1COCC[C@H]1NC1C[C@H]2CCC[C@@]2(C(=O)N2[C@H]3CC[C@@H]2CN(c2cc(C(F)(F)F)ccn2)C3)C1 nan
53326900 58665 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 425 5 1 6 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C(C)C)(N2CCN(C(=O)OC(C)(C)C)CC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684682 58665 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 425 5 1 6 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C(C)C)(N2CCN(C(=O)OC(C)(C)C)CC2)C1 10.1016/j.bmcl.2011.01.052
127025447 137534 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 306 3 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cccc(-c3ccccc3)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3754334 137534 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 306 3 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cccc(-c3ccccc3)c2)C1 10.1016/j.bmcl.2015.11.051
42632888 93631 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 433 6 1 2 5.4 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL246725 93631 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 433 6 1 2 5.4 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
57656729 75226 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 414 3 1 4 2.4 CCN1CCOC(C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036779 75226 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 414 3 1 4 2.4 CCN1CCOC(C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44593564 187232 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492564 187232 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
70688149 75224 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 413 4 2 4 2.8 CC(C)N1CCN[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036777 75224 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 413 4 2 4 2.8 CC(C)N1CCN[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44453472 155538 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404259 155538 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
44425635 153532 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL398000 153532 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
10196988 169465 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 628 10 4 6 4.8 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL442929 169465 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 628 10 4 6 4.8 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
44442562 93733 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 9 3 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)N2CCCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247210 93733 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 9 3 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)N2CCCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
44353464 20899 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1c(Cl)c2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL131065 20899 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1c(Cl)c2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
56661559 65750 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 453 6 3 6 2.4 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(=O)O)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834641 65750 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 453 6 3 6 2.4 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(=O)O)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44444003 93997 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 460 9 1 3 5.8 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248639 93997 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 460 9 1 3 5.8 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
44395195 171369 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 490 10 3 5 4.1 Cc1csc(C(=O)NNC(=O)CN2CCCC2CNCCC(c2ccccc2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL446178 171369 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 490 10 3 5 4.1 Cc1csc(C(=O)NNC(=O)CN2CCCC2CNCCC(c2ccccc2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.009
71517403 86383 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 535 4 1 5 4.1 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](C(F)(F)F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313775 86383 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 535 4 1 5 4.1 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](C(F)(F)F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
127025728 137536 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 244 2 1 1 3.7 Cc1ccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)cc1 10.1016/j.bmcl.2015.11.051
CHEMBL3754349 137536 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 244 2 1 1 3.7 Cc1ccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)cc1 10.1016/j.bmcl.2015.11.051
67774360 130628 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 557 7 4 4 5.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL3681875 130628 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 557 7 4 4 5.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 nan
44453563 95089 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 430 6 2 4 2.7 N#Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL255385 95089 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 430 6 2 4 2.7 N#Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
57656869 75221 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 412 4 1 4 3.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@H]2CN(C3CC3)CCO2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036774 75221 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 412 4 1 4 3.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@H]2CN(C3CC3)CCO2)CC1 10.1016/j.bmcl.2012.04.118
24801180 98040 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
CHEMBL273079 98040 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
68004012 86585 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 520 6 3 8 3.5 Cc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2012.12.017
CHEMBL2315925 86585 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 520 6 3 8 3.5 Cc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2012.12.017
183790 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2020.112311
783 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2020.112311
CHEMBL1178786 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2020.112311
72947595 105221 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 511 4 2 6 1.5 COC1COCCC1N[C@@H]1C[C@H]2CN(C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115096 105221 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 511 4 2 6 1.5 COC1COCCC1N[C@@H]1C[C@H]2CN(C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
183790 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1007/s00044-010-9497-9
783 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1007/s00044-010-9497-9
CHEMBL1178786 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1007/s00044-010-9497-9
183790 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm300682j
783 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm300682j
CHEMBL1178786 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm300682j
57656640 75211 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 390 4 1 3 3.7 Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1Cl 10.1016/j.bmcl.2012.04.118
CHEMBL2036762 75211 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 390 4 1 3 3.7 Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1Cl 10.1016/j.bmcl.2012.04.118
10208946 73718 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 536 13 5 5 4.2 CCCC(O)(CCC)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018382 73718 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 536 13 5 5 4.2 CCCC(O)(CCC)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
46241718 83571 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 546 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OC4CCC4)nc3)CC2)C1 10.1021/ml300260s
CHEMBL2204253 83571 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 546 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OC4CCC4)nc3)CC2)C1 10.1021/ml300260s
49763931 65426 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 499 6 3 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc4[nH]cnc4c3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829617 65426 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 499 6 3 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc4[nH]cnc4c3)CC2)C1 10.1016/j.bmcl.2011.06.080
54754723 65753 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 467 8 2 6 3.4 CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834644 65753 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 467 8 2 6 3.4 CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
54755081 65777 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 467 7 3 6 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834719 65777 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 467 7 3 6 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
57396901 70524 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 525 9 3 5 3.2 CCN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1947042 70524 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 525 9 3 5 3.2 CCN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44425650 86130 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 570 9 1 2 8.3 CCCCCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231143 86130 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 570 9 1 2 8.3 CCCCCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
183790 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysisDisplacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysis
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
783 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysisDisplacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysis
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
CHEMBL1178786 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysisDisplacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysis
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
71768864 111113 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 485 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(OC(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263271 111113 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 485 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(OC(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
183790 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/acs.jmedchem.9b01701
783 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/acs.jmedchem.9b01701
CHEMBL1178786 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/acs.jmedchem.9b01701
183790 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Inhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cellsInhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm9906264
783 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Inhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cellsInhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm9906264
CHEMBL1178786 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Inhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cellsInhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm9906264
10175423 188446 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 614 10 4 6 4.4 CCNC(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502515 188446 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 614 10 4 6 4.4 CCNC(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
53325639 58470 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683073 58470 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
53321484 58477 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 510 7 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC2CC2)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683080 58477 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 510 7 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC2CC2)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
44573651 187209 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 508 6 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(C)C)C1 10.1007/s00044-010-9501-4
CHEMBL492376 187209 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 508 6 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(C)C)C1 10.1007/s00044-010-9501-4
57344297 68953 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2F)CC1 nan
CHEMBL1922815 68953 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2F)CC1 nan
46240381 83574 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 479 6 3 6 1.8 Cn1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)n1 10.1021/ml300260s
CHEMBL2204256 83574 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 479 6 3 6 1.8 Cn1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)n1 10.1021/ml300260s
44353223 116510 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 329 4 2 3 3.7 O=C(O)c1cccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)c1 10.1016/j.bmcl.2003.10.049
CHEMBL336143 116510 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 329 4 2 3 3.7 O=C(O)c1cccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)c1 10.1016/j.bmcl.2003.10.049
46886508 8317 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 620 8 3 6 6.2 CSc1ccc(CN[C@@H]2CCCC[C@@H]2N2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3NC(=O)OC(C)(C)C)C2=O)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1092739 8317 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 620 8 3 6 6.2 CSc1ccc(CN[C@@H]2CCCC[C@@H]2N2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3NC(=O)OC(C)(C)C)C2=O)cc1 10.1016/j.bmcl.2010.03.035
89823438 126331 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C(F)(F)F)cn2)C1 nan
CHEMBL3650379 126331 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C(F)(F)F)cn2)C1 nan
89823624 126332 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 474 5 1 6 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(Cl)c2)C1 nan
CHEMBL3650380 126332 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 474 5 1 6 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(Cl)c2)C1 nan
89823464 126352 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2C#N)C1 nan
CHEMBL3650399 126352 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2C#N)C1 nan
89823401 126356 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 512 5 0 6 3.7 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(Cl)c2C#N)C1 nan
CHEMBL3650402 126356 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 512 5 0 6 3.7 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(Cl)c2C#N)C1 nan
44425638 153534 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 620 9 1 2 9.2 CCCCCCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL398001 153534 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 620 9 1 2 9.2 CCCCCCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
72946381 105236 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 609 7 1 8 2.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115110 105236 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 609 7 1 8 2.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
68616341 73733 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 11 4 4 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018397 73733 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 11 4 4 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
56678507 65800 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834793 65800 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44416138 138874 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL378195 138874 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
22143196 183987 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481790 183987 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
44425642 142346 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL388675 142346 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
53325385 58458 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@H]2CCOC[C@@H]2C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683061 58458 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@H]2CCOC[C@@H]2C)C1 10.1016/j.bmcl.2011.01.015
53326242 58688 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 452 4 2 4 2.7 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)NC(C)(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684711 58688 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 452 4 2 4 2.7 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)NC(C)(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
54584164 62568 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nc(C(F)(F)F)cs3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782574 62568 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nc(C(F)(F)F)cs3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44425649 86129 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 86129 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
183790 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmcl.2008.12.050
783 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmcl.2008.12.050
CHEMBL1178786 3742 11 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmcl.2008.12.050
10323468 187672 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.7 CC1CC(N[C@@H]2CC[C@@](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C(C)C)C2)CCO1 10.1016/j.bmcl.2008.12.050
CHEMBL495149 187672 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.7 CC1CC(N[C@@H]2CC[C@@](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C(C)C)C2)CCO1 10.1016/j.bmcl.2008.12.050
10119551 93812 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 537 10 5 6 2.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(OC(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247622 93812 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 537 10 5 6 2.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(OC(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
22143196 183987 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL481790 183987 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
89823620 126363 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650409 126363 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
44425243 85803 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 610 8 2 7 6.2 Nc1nc(C(CCN2CCC(n3cnc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL229536 85803 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 610 8 2 7 6.2 Nc1nc(C(CCN2CCC(n3cnc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44416041 80432 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL214647 80432 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
22310991 19482 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1cccc2c1cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL129881 19482 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1cccc2c1cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44395138 123977 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 508 8 4 7 2.5 O=C(CN1CCCN(CCC(O)(c2ccccc2)c2cccc(O)c2)CC1)NNC(=O)c1cccs1 10.1016/j.bmcl.2004.08.008
CHEMBL362889 123977 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 508 8 4 7 2.5 O=C(CN1CCCN(CCC(O)(c2ccccc2)c2cccc(O)c2)CC1)NNC(=O)c1cccs1 10.1016/j.bmcl.2004.08.008
70683355 73816 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 620 11 4 6 5.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)C1=O 10.1016/j.bmcl.2012.03.007
CHEMBL2018542 73816 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 620 11 4 6 5.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)C1=O 10.1016/j.bmcl.2012.03.007
91754543 126366 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 465 4 1 4 4.1 O=C(N1CCN(c2ccc(C(F)(F)F)cc2)CC1)C12CCCC1CC(NC1CCOCC1)C2 nan
CHEMBL3650412 126366 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 465 4 1 4 4.1 O=C(N1CCN(c2ccc(C(F)(F)F)cc2)CC1)C12CCCC1CC(NC1CCOCC1)C2 nan
46241121 83572 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 466 6 3 6 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ncco3)CC2)C1 10.1021/ml300260s
CHEMBL2204254 83572 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 466 6 3 6 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ncco3)CC2)C1 10.1021/ml300260s
49863167 15205 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 561 9 2 6 5.6 COC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL1210603 15205 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 561 9 2 6 5.6 COC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
46886059 7982 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 565 7 1 5 4.0 CN(C)[C@@H]1CC[C@H](N2CCC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1090561 7982 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 565 7 1 5 4.0 CN(C)[C@@H]1CC[C@H](N2CCC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
127025446 137280 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.4 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752224 137280 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.4 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
44439156 91975 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 575 10 2 6 5.9 COC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241498 91975 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 575 10 2 6 5.9 COC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44415903 81150 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL215759 81150 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
46842084 7915 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 544 8 2 4 3.9 Cc1ccccc1C(=O)N1CCC(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
CHEMBL1090206 7915 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 544 8 2 4 3.9 Cc1ccccc1C(=O)N1CCC(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
72946387 105226 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 535 4 2 7 1.3 COC1COCCC1N[C@@H]1C[C@H]2CN(/C(N)=N\C#N)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115100 105226 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 535 4 2 7 1.3 COC1COCCC1N[C@@H]1C[C@H]2CN(/C(N)=N\C#N)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
54756038 65778 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 468 7 2 7 3.2 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3noc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834720 65778 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 468 7 2 7 3.2 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3noc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56683044 65802 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 521 6 3 8 3.4 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834795 65802 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 521 6 3 8 3.4 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
56659196 65803 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 522 8 3 8 3.4 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834796 65803 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 522 8 3 8 3.4 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
71768830 111105 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 485 4 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2SCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263261 111105 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 485 4 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2SCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
54582216 62565 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 500 6 1 8 2.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782571 62565 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 500 6 1 8 2.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44573486 193158 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 6 2 3 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOCC2)C1 10.1007/s00044-010-9501-4
CHEMBL523054 193158 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 6 2 3 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOCC2)C1 10.1007/s00044-010-9501-4
11721085 166859 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 565 13 2 5 7.4 CCN(CC)CCCC(C)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL428559 166859 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 565 13 2 5 7.4 CCN(CC)CCCC(C)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
71519055 86398 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 476 4 1 4 3.7 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(Br)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314053 86398 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 476 4 1 4 3.7 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(Br)cc3C2)C1 10.1016/j.bmcl.2012.10.069
56668306 65717 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 488 6 2 4 5.2 O=C(CSc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834580 65717 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 488 6 2 4 5.2 O=C(CSc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
44441396 93583 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 419 5 1 1 6.5 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCCCCC1 10.1016/j.bmcl.2007.01.115
CHEMBL246522 93583 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 419 5 1 1 6.5 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCCCCC1 10.1016/j.bmcl.2007.01.115
57402254 70512 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1946835 70512 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44444109 94116 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 504 6 0 2 7.2 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CCN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL249208 94116 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 504 6 0 2 7.2 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CCN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
44443996 155002 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 464 8 1 2 6.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL401387 155002 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 464 8 1 2 6.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
53322813 58482 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 547 7 1 7 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](Cc2cccnc2)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683085 58482 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 547 7 1 7 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](Cc2cccnc2)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
127028588 137434 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 250 2 1 1 3.8 C[C@@]1(c2cccc(Cl)c2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
CHEMBL3753509 137434 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 250 2 1 1 3.8 C[C@@]1(c2cccc(Cl)c2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
44415996 80043 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 586 8 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)Cc1ccccc1 10.1016/j.bmcl.2006.07.011
CHEMBL212939 80043 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 586 8 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)Cc1ccccc1 10.1016/j.bmcl.2006.07.011
24794656 180876 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 450 4 3 6 2.0 CC(=O)N[C@@H]1C[C@H](N)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4757452 180876 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 450 4 3 6 2.0 CC(=O)N[C@@H]1C[C@H](N)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
86767121 129404 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 438 3 1 4 3.3 O=C(N1CCc2ccc(C(F)(F)F)cc2C1)C12CCOC1CC(NC1CCOCC1)C2 nan
CHEMBL3671254 129404 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 438 3 1 4 3.3 O=C(N1CCc2ccc(C(F)(F)F)cc2C1)C12CCOC1CC(NC1CCOCC1)C2 nan
162656188 180915 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 429 5 3 5 1.4 CN[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
CHEMBL4757857 180915 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 429 5 3 5 1.4 CN[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
44447766 166878 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 558 6 1 2 7.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL428594 166878 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 558 6 1 2 7.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2007.12.029
50992246 58471 2 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683074 58471 2 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
50992246 58471 2 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1683074 58471 2 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
25110788 85960 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230166 85960 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425252 142257 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 652 9 2 7 6.6 CC(=O)Nc1nc(C(CCN2CCC(n3cnc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388486 142257 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 652 9 2 7 6.6 CC(=O)Nc1nc(C(CCN2CCC(n3cnc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425255 168884 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 650 8 2 5 7.2 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL438304 168884 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 650 8 2 5 7.2 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
50992246 58471 2 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683074 58471 2 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44593563 193110 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL522688 193110 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
68769802 121240 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 493 7 1 6 4.2 COC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
CHEMBL3577949 121240 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 493 7 1 6 4.2 COC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
11433008 77637 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 564 8 2 5 4.9 Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088378 77637 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 564 8 2 5 4.9 Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
44570781 192565 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 515 8 4 4 3.7 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc3[nH]ccc3c2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL521275 192565 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 515 8 4 4 3.7 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc3[nH]ccc3c2)C1 10.1016/j.bmcl.2008.12.062
44425645 86082 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230933 86082 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
53318853 58456 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683059 58456 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2011.01.015
53317041 58689 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 465 5 1 5 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC2CCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684712 58689 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 465 5 1 5 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC2CCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
53325460 58494 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 538 6 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(F)(F)F)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683190 58494 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 538 6 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(F)(F)F)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
57395217 71009 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccccn3)CC2)C1 10.1021/ml200030q
CHEMBL1951768 71009 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccccn3)CC2)C1 10.1021/ml200030q
57391767 71019 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 534 8 3 6 3.3 CCOc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
CHEMBL1951779 71019 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 534 8 3 6 3.3 CCOc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
53317028 58683 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 493 5 1 5 3.3 CC(OC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2F)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
CHEMBL1684706 58683 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 493 5 1 5 3.3 CC(OC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2F)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
25022597 95339 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1 10.1016/j.bmcl.2008.02.015
CHEMBL256629 95339 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1 10.1016/j.bmcl.2008.02.015
66768640 121226 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 515 13 6 5 2.6 CCC[C@H](O)[C@H](CNCC1CC1)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
CHEMBL3577934 121226 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 515 13 6 5 2.6 CCC[C@H](O)[C@H](CNCC1CC1)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
16066354 121235 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 567 9 3 4 5.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C1=O 10.1021/ml500505q
CHEMBL3577943 121235 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 567 9 3 4 5.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C1=O 10.1021/ml500505q
44425644 86081 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 514 5 1 2 6.7 CCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230932 86081 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 514 5 1 2 6.7 CCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
11353855 74549 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cc(C(F)(F)F)ccn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029568 74549 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cc(C(F)(F)F)ccn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
70689915 74553 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 611 6 3 9 3.3 O=C(N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1)C1(O)CCN(c2cc(C(F)(F)F)ccn2)CC1 10.1021/ml200199c
CHEMBL2029572 74553 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 611 6 3 9 3.3 O=C(N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1)C1(O)CCN(c2cc(C(F)(F)F)ccn2)CC1 10.1021/ml200199c
10117480 73716 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018380 73716 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
53325460 58494 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 538 6 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(F)(F)F)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683190 58494 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 538 6 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(F)(F)F)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
22143155 188062 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL497788 188062 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
57656833 75229 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036782 75229 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
46886538 8318 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 647 8 1 5 5.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1092748 8318 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 647 8 1 5 5.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
44425653 86229 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231246 86229 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44425272 86035 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 626 10 2 5 7.2 CCC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230684 86035 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 626 10 2 5 7.2 CCC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425290 153531 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397997 153531 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
53323653 58672 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 475 5 1 5 3.3 CC(OC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
CHEMBL1684694 58672 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 475 5 1 5 3.3 CC(OC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
44425644 86081 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 514 5 1 2 6.7 CCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230932 86081 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 514 5 1 2 6.7 CCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
10281316 73722 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1021/jm300682j
CHEMBL2018386 73722 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1021/jm300682j
10281316 73722 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1016/j.bmcl.2012.03.007
CHEMBL2018386 73722 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1016/j.bmcl.2012.03.007
11353843 74547 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 594 6 2 7 4.8 O=C(C1CCN(c2cccc(C(F)(F)F)c2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029566 74547 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 594 6 2 7 4.8 O=C(C1CCN(c2cccc(C(F)(F)F)c2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
24801690 98041 25 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
CHEMBL273083 98041 25 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
11527661 2021 30 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
9045 2021 30 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
CHEMBL1963131 2021 30 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
10218403 187910 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 557 9 3 6 3.5 CN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
CHEMBL496630 187910 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 557 9 3 6 3.5 CN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
11527661 2021 30 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9045 2021 30 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL1963131 2021 30 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
70683350 73726 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 607 12 5 6 3.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCOCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018390 73726 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 607 12 5 6 3.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCOCC1 10.1016/j.bmcl.2012.03.007
11179439 73736 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018400 73736 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
44583280 172449 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 640 9 3 6 4.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL447937 172449 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 640 9 3 6 4.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
44570714 189794 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 565 9 5 6 3.6 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL516224 189794 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 565 9 5 6 3.6 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
22143112 188445 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 594 11 5 6 3.7 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC)C1 10.1016/j.bmcl.2008.07.123
CHEMBL502513 188445 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 594 11 5 6 3.7 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC)C1 10.1016/j.bmcl.2008.07.123
50992246 58471 2 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683074 58471 2 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
24794585 179524 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 478 5 2 6 2.6 CC(=O)N[C@@H]1C[C@H](N(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4741305 179524 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 478 5 2 6 2.6 CC(=O)N[C@@H]1C[C@H](N(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
44425647 86101 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231039 86101 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44425273 86054 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 638 10 2 5 7.2 O=C(Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)C1CC1 10.1016/j.bmcl.2006.10.059
CHEMBL230794 86054 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 638 10 2 5 7.2 O=C(Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)C1CC1 10.1016/j.bmcl.2006.10.059
162666730 182274 1 None - 1 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182274 1 None - 1 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
44449031 95698 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 555 7 2 4 6.0 COc1ccc2c(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5ccc(Cl)c(Cl)c5)CC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL258204 95698 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 555 7 2 4 6.0 COc1ccc2c(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5ccc(Cl)c(Cl)c5)CC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2008.05.010
10323427 79760 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 in human monocytesBinding affinity to CCR2 in human monocytes
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2006.04.045
CHEMBL211775 79760 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 in human monocytesBinding affinity to CCR2 in human monocytes
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2006.04.045
72947411 105257 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 598 6 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115272 105257 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 598 6 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
11721085 166859 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 565 13 2 5 7.4 CCN(CC)CCCC(C)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL428559 166859 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 565 13 2 5 7.4 CCN(CC)CCCC(C)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
56671792 65794 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 472 6 3 5 3.9 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834787 65794 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 472 6 3 5 3.9 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.08.074
11640044 148247 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 405 5 1 1 6.2 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCCCC1 10.1016/j.bmcl.2007.01.115
CHEMBL393631 148247 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 405 5 1 1 6.2 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCCCC1 10.1016/j.bmcl.2007.01.115
44425308 153706 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL398150 153706 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44573486 193158 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL523054 193158 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOCC2)C1 10.1016/j.bmcl.2008.12.050
90656025 111120 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 483 4 0 6 2.7 COC1COCCC1N(C)[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263280 111120 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 483 4 0 6 2.7 COC1COCCC1N(C)[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
76335990 105239 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 482 4 1 6 2.1 COC1COCCC1N[C@@H]1C[C@H]2CN(C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115113 105239 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 482 4 1 6 2.1 COC1COCCC1N[C@@H]1C[C@H]2CN(C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44453535 155174 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 473 6 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2Cl)C1 10.1016/j.bmcl.2008.02.015
CHEMBL402322 155174 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 473 6 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2Cl)C1 10.1016/j.bmcl.2008.02.015
25033361 154483 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cell membraneDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cell membrane
ChEMBL 490 5 0 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL399045 154483 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cell membraneDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cell membrane
ChEMBL 490 5 0 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
25033361 154483 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 490 5 0 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL399045 154483 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 490 5 0 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
44353367 117303 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 344 3 1 3 4.6 N#Cc1c(C(=O)O)n(Cc2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2003.10.049
CHEMBL339670 117303 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 344 3 1 3 4.6 N#Cc1c(C(=O)O)n(Cc2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2003.10.049
44442542 93765 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 464 10 4 4 2.2 Cc1ccc(CNCC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247406 93765 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 464 10 4 4 2.2 Cc1ccc(CNCC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
10409097 66642 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 406 5 2 5 2.4 O=C(CN1CCCN(Cc2ccc(Cl)cc2)CC1)NNC(=O)c1cccs1 10.1016/j.bmcl.2004.08.008
CHEMBL185282 66642 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 406 5 2 5 2.4 O=C(CN1CCCN(Cc2ccc(Cl)cc2)CC1)NNC(=O)c1cccs1 10.1016/j.bmcl.2004.08.008
127027624 137388 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1cc(C)cc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1 10.1016/j.bmcl.2015.11.051
CHEMBL3753178 137388 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1cc(C)cc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1 10.1016/j.bmcl.2015.11.051
10277182 98002 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 7 2 3 4.6 Cc1ccc(CN(C)[C@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL272860 98002 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 7 2 3 4.6 Cc1ccc(CN(C)[C@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
22394337 117090 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 315 4 1 3 4.1 COc1cccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)c1 10.1016/j.bmcl.2003.10.049
CHEMBL339275 117090 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 315 4 1 3 4.1 COc1cccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)c1 10.1016/j.bmcl.2003.10.049
24801690 98041 25 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to CCR2 T292A mutantBinding affinity to CCR2 T292A mutant
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
CHEMBL273083 98041 25 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to CCR2 T292A mutantBinding affinity to CCR2 T292A mutant
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
46830336 7850 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 567 8 2 5 2.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089793 7850 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 567 8 2 5 2.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
11214277 74537 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 504 6 3 5 3.2 Cc1ccnc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1021/ml200199c
CHEMBL2029415 74537 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 504 6 3 5 3.2 Cc1ccnc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1021/ml200199c
44453268 95129 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 462 7 3 4 2.8 CC(=O)Nc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL255585 95129 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 462 7 3 4 2.8 CC(=O)Nc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
89823413 126333 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)ccc2C(F)(F)F)C1 nan
CHEMBL3650381 126333 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)ccc2C(F)(F)F)C1 nan
44453474 97871 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 512 6 3 4 2.6 Nc1ccc(I)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272284 97871 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 512 6 3 4 2.6 Nc1ccc(I)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
72946198 105234 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 624 7 1 8 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115108 105234 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 624 7 1 8 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
10299408 73700 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 11 4 4 3.5 CCC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018363 73700 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 11 4 4 3.5 CCC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
46946058 65432 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 504 7 2 6 2.8 CN(C)c1ncc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1016/j.bmcl.2011.06.080
CHEMBL1829623 65432 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 504 7 2 6 2.8 CN(C)c1ncc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1016/j.bmcl.2011.06.080
56683121 65811 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834853 65811 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
56676474 65812 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834854 65812 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
53322811 58474 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 484 6 1 6 3.1 CC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683077 58474 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 484 6 1 6 3.1 CC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
54583112 62546 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 513 6 0 7 3.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782378 62546 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 513 6 0 7 3.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
46240380 83563 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 519 7 3 6 2.5 CN(C)c1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204245 83563 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 519 7 3 6 2.5 CN(C)c1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
57393531 70511 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 9 3 5 3.6 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1946834 70511 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 9 3 5 3.6 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44442596 93472 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 593 11 5 6 3.8 CCOC(=O)Nc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246098 93472 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 593 11 5 6 3.8 CCOC(=O)Nc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
73351183 93234 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL2448120 93234 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
44453477 155303 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 419 6 2 3 3.1 Cc1cccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)c1 10.1016/j.bmcl.2008.02.015
CHEMBL402988 155303 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 419 6 2 3 3.1 Cc1cccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)c1 10.1016/j.bmcl.2008.02.015
44443989 94448 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 414 8 1 2 5.3 O=C(/C=C/c1ccc(F)cc1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL251217 94448 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 414 8 1 2 5.3 O=C(/C=C/c1ccc(F)cc1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
46886507 8084 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 594 9 4 6 5.7 CSc1ccc(CN[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1091266 8084 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 594 9 4 6 5.7 CSc1ccc(CN[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2010.03.035
89823576 126329 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 542 5 1 6 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ncc(C(F)(F)F)cc2Cl)C1 nan
CHEMBL3650377 126329 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 542 5 1 6 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ncc(C(F)(F)F)cc2Cl)C1 nan
46842233 7718 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1088875 7718 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
508741 167469 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 435 7 2 4 2.8 COc1cccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)c1 10.1016/j.bmcl.2008.02.015
CHEMBL429912 167469 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 435 7 2 4 2.8 COc1cccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)c1 10.1016/j.bmcl.2008.02.015
90656017 111107 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 468 4 2 6 1.9 COC1COCCC1N[C@@H]1C[C@H]2NCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263264 111107 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 468 4 2 6 1.9 COC1COCCC1N[C@@H]1C[C@H]2NCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
72946198 105234 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 624 7 1 8 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115108 105234 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 624 7 1 8 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
72946199 105233 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 610 6 1 8 3.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115107 105233 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 610 6 1 8 3.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57656854 75228 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 425 3 2 4 2.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C(=O)[C@H]2CN(C3CC3)CCN2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036781 75228 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 425 3 2 4 2.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C(=O)[C@H]2CN(C3CC3)CCN2)CC1 10.1016/j.bmcl.2012.04.118
46944854 65429 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 490 7 2 5 3.4 COc1cnccc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
CHEMBL1829620 65429 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 490 7 2 5 3.4 COc1cnccc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
54754724 65754 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 479 9 2 6 3.6 C=CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834645 65754 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 479 9 2 6 3.6 C=CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
44425649 86129 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 86129 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44413214 77800 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 421 4 1 5 4.9 Cc1ccc2c(c1)C1(CCN(CCc3coc(-c4ccc(F)cc4)n3)CC1)OC(=O)N2 10.1016/j.bmcl.2006.04.045
CHEMBL209263 77800 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 421 4 1 5 4.9 Cc1ccc2c(c1)C1(CCN(CCc3coc(-c4ccc(F)cc4)n3)CC1)OC(=O)N2 10.1016/j.bmcl.2006.04.045
53320349 58669 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 417 5 1 4 2.6 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684690 58669 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 417 5 1 4 2.6 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
44570717 183832 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 544 8 3 4 4.2 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL480620 183832 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 544 8 3 4 4.2 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.12.062
44425256 86053 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 631 9 2 6 5.9 CC(=O)Nc1nc(C(CCN2CCN(c3ccc(F)cc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230791 86053 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 631 9 2 6 5.9 CC(=O)Nc1nc(C(CCN2CCN(c3ccc(F)cc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
89823552 126303 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
CHEMBL3650351 126303 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
76335990 105239 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 482 4 1 6 2.1 COC1COCCC1N[C@@H]1C[C@H]2CN(C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115113 105239 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 482 4 1 6 2.1 COC1COCCC1N[C@@H]1C[C@H]2CN(C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57344229 130641 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 3 6.5 O=C(O)C(N[C@H]1CC[C@@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3681887 130641 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 3 6.5 O=C(O)C(N[C@H]1CC[C@@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
10137967 153948 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL398354 153948 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2012.03.007
10137967 153948 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL398354 153948 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2007.07.028
44444099 154408 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 6 0 3 6.1 COc1ccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL398844 154408 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 6 0 3 6.1 COc1ccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11844329 80040 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 592 7 1 2 7.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(CCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL212928 80040 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 592 7 1 2 7.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(CCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm060439n
23656584 89921 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 541 7 2 3 6.0 O=C(O)C(C1CCN(C(=O)CCc2ccc(Cl)c(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237966 89921 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 541 7 2 3 6.0 O=C(O)C(C1CCN(C(=O)CCc2ccc(Cl)c(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
44453327 95095 25 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL255408 95095 25 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2010.02.072
42632840 168711 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 364 5 1 3 3.6 C[N+](C)(Cc1ccc(NC(=O)c2cccc(C#N)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL436822 168711 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 364 5 1 3 3.6 C[N+](C)(Cc1ccc(NC(=O)c2cccc(C#N)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
127025730 137322 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1ccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)cc1C 10.1016/j.bmcl.2015.11.051
CHEMBL3752640 137322 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1ccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)cc1C 10.1016/j.bmcl.2015.11.051
89823462 126358 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 463 4 1 6 2.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)C1 nan
CHEMBL3650404 126358 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 463 4 1 6 2.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)C1 nan
72947411 105257 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 598 6 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115272 105257 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 598 6 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
72946381 105236 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 609 7 1 8 2.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115110 105236 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 609 7 1 8 2.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
69285563 121228 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 443 8 2 4 3.1 COC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577936 121228 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 443 8 2 4 3.1 COC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
67774071 130656 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 521 7 3 4 4.3 NC(=O)C(NC1CCC(c2c[nH]c3ncccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681901 130656 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 521 7 3 4 4.3 NC(=O)C(NC1CCC(c2c[nH]c3ncccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
54754844 65746 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 434 5 2 6 2.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C#N)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834638 65746 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 434 5 2 6 2.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C#N)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
71768831 111115 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 499 5 1 8 1.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263273 111115 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 499 5 1 8 1.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)C1 10.1016/j.bmcl.2014.03.036
122181238 121853 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 554 7 1 3 6.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)C1CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589952 121853 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 554 7 1 3 6.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)C1CC1 10.1016/j.bmc.2015.02.019
23655673 146655 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 539 6 1 4 5.3 COC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL392366 146655 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 539 6 1 4 5.3 COC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
71518405 86400 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 423 5 1 3 4.7 CCC(CC)N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314055 86400 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 423 5 1 3 4.7 CCC(CC)N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
23655673 146655 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 1 4 5.3 COC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL392366 146655 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 1 4 5.3 COC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
44395169 66157 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 476 9 3 5 3.7 Cc1csc(C(=O)NNC(=O)CNC2CCN(CCC(c3ccccc3)c3ccccc3)C2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL184240 66157 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 476 9 3 5 3.7 Cc1csc(C(=O)NNC(=O)CNC2CCN(CCC(c3ccccc3)c3ccccc3)C2)c1 10.1016/j.bmcl.2004.08.009
11690536 121222 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 431 12 4 4 2.7 CCC[C@H](O)[C@H](CNCCC(C)C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577930 121222 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 431 12 4 4 2.7 CCC[C@H](O)[C@H](CNCCC(C)C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
71519224 86399 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 466 4 1 4 3.9 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314054 86399 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 466 4 1 4 3.9 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
57400331 70526 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 551 9 3 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CC[C@@H](NC2CCC2)[C@@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
CHEMBL1947044 70526 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 551 9 3 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CC[C@@H](NC2CCC2)[C@@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
57403811 70341 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 651 10 3 6 4.1 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944779 70341 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 651 10 3 6 4.1 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
53326703 58479 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 514 8 1 7 2.7 CCOC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683082 58479 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 514 8 1 7 2.7 CCOC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
89823551 126312 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(C(F)(F)F)c2)C1 nan
CHEMBL3650360 126312 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(C(F)(F)F)c2)C1 nan
11215504 73802 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 594 12 5 6 5.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC(=O)OC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018527 73802 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 594 12 5 6 5.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC(=O)OC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
57398590 70337 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 565 8 2 5 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CC[C@@H](N2CCCCC2)[C@@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
CHEMBL1944775 70337 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 565 8 2 5 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CC[C@@H](N2CCCCC2)[C@@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
71768862 111117 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 511 5 1 8 1.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CC3CC2CN3c2ccnc(C(F)(F)F)n2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263275 111117 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 511 5 1 8 1.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CC3CC2CN3c2ccnc(C(F)(F)F)n2)C1 10.1016/j.bmcl.2014.03.036
22310924 20168 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2cccc(Cl)c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130467 20168 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2cccc(Cl)c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
22311000 20346 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2ccc(Cl)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130608 20346 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2ccc(Cl)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44444006 94038 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 446 9 1 3 4.9 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3cc(F)c(F)c(F)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248829 94038 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 446 9 1 3 4.9 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3cc(F)c(F)c(F)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
23656432 154401 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 549 6 1 5 5.2 CC(=O)n1cc(C2CCN(C(C(=O)O)C3CCN(C(=O)/C=C/c4cc(F)cc(F)c4)CC3)CC2)c2ccccc21 10.1021/jm070902b
CHEMBL398796 154401 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 549 6 1 5 5.2 CC(=O)n1cc(C2CCN(C(C(=O)O)C3CCN(C(=O)/C=C/c4cc(F)cc(F)c4)CC3)CC2)c2ccccc21 10.1021/jm070902b
44395137 66193 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 514 8 1 5 4.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(F)c3)c3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL184390 66193 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 514 8 1 5 4.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(F)c3)c3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
127028587 137556 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 250 2 1 1 3.8 C[C@@]1(c2ccc(Cl)cc2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
CHEMBL3754549 137556 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 250 2 1 1 3.8 C[C@@]1(c2ccc(Cl)cc2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
44413328 139258 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL378995 139258 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
25270182 93324 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 429 6 1 2 5.7 Cc1ccc(-c2cccc(C(=O)Nc3ccc(C[N+](C)(C)C4CCOCC4)cc3)c2)cc1 10.1016/j.bmcl.2007.01.115
CHEMBL245290 93324 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 429 6 1 2 5.7 Cc1ccc(-c2cccc(C(=O)Nc3ccc(C[N+](C)(C)C4CCOCC4)cc3)c2)cc1 10.1016/j.bmcl.2007.01.115
46885159 8375 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 545 8 2 5 2.4 Cc1ccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL1093153 8375 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 545 8 2 5 2.4 Cc1ccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
127027626 137250 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 266 2 1 1 3.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(F)c(F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3751926 137250 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 266 2 1 1 3.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(F)c(F)c2)C1 10.1016/j.bmcl.2015.11.051
44416015 81133 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215689 81133 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
72947193 105231 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 568 6 1 7 3.3 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115105 105231 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 568 6 1 7 3.3 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57656749 75210 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(Cl)c(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036761 75210 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(Cl)c(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
49763571 65418 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 459 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829609 65418 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 459 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
70687885 74529 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 473 6 2 3 4.4 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@H](c3ccccc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029407 74529 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 473 6 2 3 4.4 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@H](c3ccccc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
71768931 111125 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 544 4 1 5 4.9 O=C(O)c1cccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4COc5ccc(C(F)(F)F)cc5C4)C3)CC2)c1 10.1016/j.bmcl.2014.03.036
CHEMBL3263285 111125 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 544 4 1 5 4.9 O=C(O)c1cccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4COc5ccc(C(F)(F)F)cc5C4)C3)CC2)c1 10.1016/j.bmcl.2014.03.036
44573487 192634 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 496 6 2 3 6.0 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSCC2)C1 10.1007/s00044-010-9501-4
CHEMBL521697 192634 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 496 6 2 3 6.0 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSCC2)C1 10.1007/s00044-010-9501-4
10141379 73703 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 11 4 4 3.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)CC(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018366 73703 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 11 4 4 3.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)CC(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
44425642 142346 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL388675 142346 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
46885029 8249 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 545 8 2 5 2.4 Cc1cccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
CHEMBL1092343 8249 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 545 8 2 5 2.4 Cc1cccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
71518571 86405 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 485 3 1 5 3.1 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCS(=O)(=O)CC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314060 86405 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 485 3 1 5 3.1 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCS(=O)(=O)CC1)C2 10.1016/j.bmcl.2012.10.069
71552097 86589 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 7 3.6 Nc1cnccc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
CHEMBL2315929 86589 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 7 3.6 Nc1cnccc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
46240895 83578 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccns3)CC2)C1 10.1021/ml300260s
CHEMBL2204260 83578 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccns3)CC2)C1 10.1021/ml300260s
46927116 65437 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 4 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829628 65437 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 4 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
54755919 65759 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 516 6 2 7 4.5 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834651 65759 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 516 6 2 7 4.5 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
44612590 137470 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753813 137470 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
53326702 58468 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.2 COC[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683071 58468 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.2 COC[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
44425283 86061 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 648 10 2 6 6.2 CS(=O)(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230824 86061 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 648 10 2 6 6.2 CS(=O)(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425322 153201 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 738 9 2 5 8.6 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)C3Cc4ccccc43)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL397717 153201 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 738 9 2 5 8.6 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)C3Cc4ccccc43)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
44573488 187679 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 482 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL495165 187679 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 482 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSC2)C1 10.1016/j.bmcl.2008.12.050
44442577 93546 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 10 4 4 3.5 CCc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246407 93546 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 10 4 4 3.5 CCc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442578 155129 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 535 10 4 5 3.0 Cc1cc(N(C)C)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL402056 155129 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 535 10 4 5 3.0 Cc1cc(N(C)C)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
16720313 85417 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 498 5 1 2 6.4 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H]1CC[C@@H](N2CCC(c3ccccc3)CC2)C1 10.1021/jm070166b
CHEMBL226376 85417 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 498 5 1 2 6.4 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H]1CC[C@@H](N2CCC(c3ccccc3)CC2)C1 10.1021/jm070166b
53320967 58667 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 433 5 1 4 3.2 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684684 58667 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 433 5 1 4 3.2 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
24801344 97731 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 8 3 3 4.8 CC(C)c1ccc(CN[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL271537 97731 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 8 3 3 4.8 CC(C)c1ccc(CN[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
44573410 187426 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 7 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NCC2CCOCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL493779 187426 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 7 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NCC2CCOCC2)C1 10.1016/j.bmcl.2008.12.050
44573410 187426 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 7 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NCC2CCOCC2)C1 10.1007/s00044-010-9501-4
CHEMBL493779 187426 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 7 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NCC2CCOCC2)C1 10.1007/s00044-010-9501-4
122181153 121840 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 558 7 1 3 6.3 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
CHEMBL3589847 121840 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 558 7 1 3 6.3 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
122181151 121839 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 622 7 1 3 7.6 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589846 121839 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 622 7 1 3 7.6 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
72946387 105226 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 535 4 2 7 1.3 COC1COCCC1N[C@@H]1C[C@H]2CN(/C(N)=N\C#N)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115100 105226 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 535 4 2 7 1.3 COC1COCCC1N[C@@H]1C[C@H]2CN(/C(N)=N\C#N)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
11553070 75200 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 398 4 1 3 3.9 CCN1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036751 75200 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 398 4 1 3 3.9 CCN1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
46208367 83581 13 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1021/ml300260s
CHEMBL2204263 83581 13 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1021/ml300260s
10195882 70506 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 497 7 3 5 2.5 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
CHEMBL1946829 70506 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 497 7 3 5 2.5 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
44415973 81055 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 536 8 1 2 7.0 C=CC[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215394 81055 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 536 8 1 2 7.0 C=CC[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44415939 140133 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 510 6 1 2 6.4 C[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL380190 140133 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 510 6 1 2 6.4 C[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44442598 154387 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 5 5 1.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2N)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL398747 154387 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 5 5 1.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2N)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
24801522 161137 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 573 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(I)cc1 10.1021/jm701488f
CHEMBL411726 161137 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 573 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(I)cc1 10.1021/jm701488f
89823526 126347 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 538 4 0 4 5.7 O=C(N1C[C@@H]2C[C@H]1CN2c1cc(C(F)(F)F)ccn1)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
CHEMBL3650394 126347 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 538 4 0 4 5.7 O=C(N1C[C@@H]2C[C@H]1CN2c1cc(C(F)(F)F)ccn1)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
57344319 130635 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 491 6 4 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cccc(F)c2)CC1 nan
CHEMBL3681881 130635 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 491 6 4 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cccc(F)c2)CC1 nan
9889422 127154 3 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL365681 127154 3 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
54755193 65745 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 437 6 3 4 4.0 CC(C)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834637 65745 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 437 6 3 4 4.0 CC(C)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
57395061 70336 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 10 2 5 3.9 CCCN(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944774 70336 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 10 2 5 3.9 CCCN(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
71768897 111123 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 543 4 1 5 4.5 O=C(O)c1cccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4CCc5ncc(C(F)(F)F)cc5C4)C3)CC2)c1 10.1016/j.bmcl.2014.03.036
CHEMBL3263283 111123 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 543 4 1 5 4.5 O=C(O)c1cccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4CCc5ncc(C(F)(F)F)cc5C4)C3)CC2)c1 10.1016/j.bmcl.2014.03.036
44353197 20770 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 450 4 1 4 4.6 O=C(NS(=O)(=O)C(F)(F)F)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130947 20770 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 450 4 1 4 4.6 O=C(NS(=O)(=O)C(F)(F)F)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
127025729 137324 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1cccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1C 10.1016/j.bmcl.2015.11.051
CHEMBL3752652 137324 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1cccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1C 10.1016/j.bmcl.2015.11.051
127036934 137428 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 248 2 1 1 3.5 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cccc(F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753474 137428 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 248 2 1 1 3.5 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cccc(F)c2)C1 10.1016/j.bmcl.2015.11.051
57391797 70510 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 497 7 3 5 2.5 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1946833 70510 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 497 7 3 5 2.5 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
68004016 86608 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1nccc2ncc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2316211 86608 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1nccc2ncc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
11342351 77641 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 592 10 2 5 5.5 CCCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088381 77641 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 592 10 2 5 5.5 CCCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
44415898 81121 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL215654 81121 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
53320970 58681 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 435 5 1 4 2.5 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684704 58681 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 435 5 1 4 2.5 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
44442566 154778 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 10 4 4 3.2 CCc1ccccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL400159 154778 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 10 4 4 3.2 CCc1ccccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
22143196 183987 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL481790 183987 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
44444005 93998 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 428 9 1 3 4.8 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3cc(F)cc(F)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248640 93998 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 428 9 1 3 4.8 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3cc(F)cc(F)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
132572938 156789 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysisDisplacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysis
ChEMBL 551 8 1 4 6.4 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CN(CC(C)C)C3=O)cc1 10.1016/j.ejmech.2017.04.046
CHEMBL4070869 156789 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysisDisplacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysis
ChEMBL 551 8 1 4 6.4 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CN(CC(C)C)C3=O)cc1 10.1016/j.ejmech.2017.04.046
44353377 23170 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 397 4 1 4 4.1 CS(=O)(=O)c1cccc2c1cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL133111 23170 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 397 4 1 4 4.1 CS(=O)(=O)c1cccc2c1cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
71552260 86598 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 574 6 3 8 4.2 O=C(CNc1nc(C(F)(F)F)nc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315938 86598 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 574 6 3 8 4.2 O=C(CNc1nc(C(F)(F)F)nc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
72946013 105259 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 560 4 1 6 2.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)C#CC3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115274 105259 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 560 4 1 6 2.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)C#CC3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
76333441 84899 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H](NCCN1CCCCC1)c1ccsc1 10.1007/s00044-010-9497-9
CHEMBL2236473 84899 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H](NCCN1CCCCC1)c1ccsc1 10.1007/s00044-010-9497-9
10323427 79760 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2006.04.045
CHEMBL211775 79760 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2006.04.045
508877 95061 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 466 7 4 6 2.1 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
CHEMBL255209 95061 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 466 7 4 6 2.1 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
53321503 58492 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 516 8 1 6 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CCCF)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683188 58492 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 516 8 1 6 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CCCF)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
53321615 58680 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 451 5 1 4 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684703 58680 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 451 5 1 4 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
67772859 124447 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 535 7 2 4 5.6 COC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3639807 124447 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 535 7 2 4 5.6 COC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
10139782 73699 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 465 10 4 4 3.1 CC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018362 73699 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 465 10 4 4 3.1 CC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
49763569 65419 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 435 6 2 5 2.7 O=C(CNC(=O)c1ccccc1)NC1CN([C@H]2CC[C@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829610 65419 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 435 6 2 5 2.7 O=C(CNC(=O)c1ccccc1)NC1CN([C@H]2CC[C@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
25268436 93429 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 391 5 1 2 4.5 C[N+](C)(Cc1ccc(NC(=O)c2ccc(F)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL245896 93429 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 391 5 1 2 4.5 C[N+](C)(Cc1ccc(NC(=O)c2ccc(F)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
9885442 20753 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2cc([N+](=O)[O-])ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130936 20753 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2cc([N+](=O)[O-])ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
89823586 126324 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)n2)C1 nan
CHEMBL3650372 126324 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)n2)C1 nan
72947413 105256 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 510 4 1 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115271 105256 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 510 4 1 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
162666730 182274 1 None - 1 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182274 1 None - 1 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
155491018 174083 1 None - 1 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 174083 1 None - 1 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
86767123 129406 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 497 5 1 6 3.1 CCC1CC2(C(=O)N3CCc4ncc(C(F)(F)F)cc4C3)CC(NC3CCOCC3OC)CC2O1 nan
CHEMBL3671256 129406 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 497 5 1 6 3.1 CCC1CC2(C(=O)N3CCc4ncc(C(F)(F)F)cc4C3)CC(NC3CCOCC3OC)CC2O1 nan
11699149 95106 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL255478 95106 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
10304021 73720 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 594 12 5 6 4.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)OC(C)(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018384 73720 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 594 12 5 6 4.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)OC(C)(C)C 10.1016/j.bmcl.2012.03.007
44415880 169339 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL441856 169339 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
44447775 95707 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 558 6 1 2 7.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL258246 95707 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 558 6 1 2 7.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
44425643 86042 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230722 86042 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44425271 153242 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 598 10 2 5 6.4 O=CNc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397747 153242 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 598 10 2 5 6.4 O=CNc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44593562 187495 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 187495 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
71768755 111100 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 497 5 1 6 3.1 CCC1C[C@@]2(C(=O)N3CCc4ncc(C(F)(F)F)cc4C3)C[C@H](NC3CCOCC3OC)C[C@H]2O1 10.1016/j.bmcl.2014.03.036
CHEMBL3263256 111100 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 497 5 1 6 3.1 CCC1C[C@@]2(C(=O)N3CCc4ncc(C(F)(F)F)cc4C3)C[C@H](NC3CCOCC3OC)C[C@H]2O1 10.1016/j.bmcl.2014.03.036
11591956 89337 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 2 3 6.1 O=C(O)C(C1CCN(C(=O)/C=C/c2ccc(Cl)c(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL236930 89337 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 2 3 6.1 O=C(O)C(C1CCN(C(=O)/C=C/c2ccc(Cl)c(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
23656430 89881 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 540 6 3 4 4.8 Nc1ccc2[nH]cc(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1021/jm070902b
CHEMBL237806 89881 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 540 6 3 4 4.8 Nc1ccc2[nH]cc(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1021/jm070902b
11548199 89922 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237967 89922 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
23656431 146337 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 2 3 5.5 Cc1[nH]c2ccccc2c1C1CCN(C(C(=O)O)C2CCN(C(=O)/C=C/c3cc(F)c(F)c(F)c3)CC2)CC1 10.1021/jm070902b
CHEMBL392120 146337 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 2 3 5.5 Cc1[nH]c2ccccc2c1C1CCN(C(C(=O)O)C2CCN(C(=O)/C=C/c3cc(F)c(F)c(F)c3)CC2)CC1 10.1021/jm070902b
44453405 95436 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 469 6 4 5 2.6 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1Cl 10.1016/j.bmcl.2008.02.015
CHEMBL257062 95436 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 469 6 4 5 2.6 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1Cl 10.1016/j.bmcl.2008.02.015
53318316 58679 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 453 4 1 5 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684702 58679 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 453 4 1 5 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
57395219 71011 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncc3)CC2)C1 10.1021/ml200030q
CHEMBL1951770 71011 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncc3)CC2)C1 10.1021/ml200030q
53320973 58690 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 453 6 1 5 3.0 CC(C)COC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684713 58690 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 453 6 1 5 3.0 CC(C)COC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
44580590 193571 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL526859 193571 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
24794585 179524 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 478 5 2 6 2.6 CC(=O)N[C@@H]1C[C@H](N(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4741305 179524 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 478 5 2 6 2.6 CC(=O)N[C@@H]1C[C@H](N(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
11283842 73738 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 522 13 5 5 4.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018402 73738 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 522 13 5 5 4.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
11273379 74548 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029567 74548 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
54583111 62545 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 512 6 0 6 3.7 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782377 62545 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 512 6 0 6 3.7 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
24794583 181093 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 464 5 3 6 2.3 CN[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
CHEMBL4760098 181093 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 464 5 3 6 2.3 CN[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
53321616 58460 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683063 58460 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
25110716 155206 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
ChEMBL 515 4 0 3 7.0 C[C@H]1CN([C@@H]2CC[C@@]3(CCO[C@H]3OCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.016
CHEMBL402532 155206 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
ChEMBL 515 4 0 3 7.0 C[C@H]1CN([C@@H]2CC[C@@]3(CCO[C@H]3OCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.016
44573485 187721 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL495368 187721 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2008.12.050
44573452 187607 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOC2)C1 10.1007/s00044-010-9501-4
CHEMBL494770 187607 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOC2)C1 10.1007/s00044-010-9501-4
68764898 672 2 None - 3 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulationAntagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulation
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
9430 672 2 None - 3 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulationAntagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulation
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
CHEMBL3577945 672 2 None - 3 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulationAntagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulation
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
10281715 73723 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018387 73723 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
10281715 73723 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
CHEMBL2018387 73723 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
69286635 121231 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 469 9 2 3 4.9 CC(C)CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577939 121231 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 469 9 2 3 4.9 CC(C)CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
44571218 183878 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481009 183878 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
57398750 71016 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccnnc3)CC2)C1 10.1021/ml200030q
CHEMBL1951775 71016 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccnnc3)CC2)C1 10.1021/ml200030q
66768640 121226 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 515 13 6 5 2.6 CCC[C@H](O)[C@H](CNCC1CC1)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
CHEMBL3577934 121226 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 515 13 6 5 2.6 CCC[C@H](O)[C@H](CNCC1CC1)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
68004002 86584 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315924 86584 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
67774784 130650 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 4 5.3 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3681896 130650 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 4 5.3 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
11712754 95066 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 482 5 3 3 4.9 O=C(Nc1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL255266 95066 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 482 5 3 3 4.9 O=C(Nc1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11555541 155295 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 529 6 2 3 5.2 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL402955 155295 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 529 6 2 3 5.2 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11192300 73803 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 565 13 6 5 4.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC(=O)NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018528 73803 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 565 13 6 5 4.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC(=O)NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
11718088 93582 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 391 5 1 1 5.8 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCCC1 10.1016/j.bmcl.2007.01.115
CHEMBL246520 93582 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 391 5 1 1 5.8 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCCC1 10.1016/j.bmcl.2007.01.115
71519054 86397 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 432 4 1 4 3.6 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(Cl)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314052 86397 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 432 4 1 4 3.6 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(Cl)cc3C2)C1 10.1016/j.bmcl.2012.10.069
10436083 79877 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 501 8 2 3 5.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL212306 79877 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 501 8 2 3 5.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
44442565 93541 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 9 4 4 2.9 Cc1ccccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL246401 93541 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 9 4 4 2.9 Cc1ccccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
10299952 155011 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 488 10 4 4 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL401463 155011 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 488 10 4 4 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
24801343 97773 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 501 7 3 3 4.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(C(F)(F)F)cc1 10.1021/jm701488f
CHEMBL271752 97773 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 501 7 3 3 4.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(C(F)(F)F)cc1 10.1021/jm701488f
44395165 169473 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 508 9 2 6 3.4 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(CO)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL442966 169473 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 508 9 2 6 3.4 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(CO)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44444098 161664 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 6 0 3 6.1 COc1cccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2007.07.065
CHEMBL413084 161664 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 6 0 3 6.1 COc1cccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2007.07.065
44395129 66644 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 8 2 3 3.2 O=C(CCNC(=O)c1ccccc1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL185283 66644 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 8 2 3 3.2 O=C(CCNC(=O)c1ccccc1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
57344313 130657 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 503 7 3 4 4.1 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
CHEMBL3681902 130657 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 503 7 3 4 4.1 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
57344303 130649 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681895 130649 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
71517239 86374 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 COC1COCCC1N[C@H]1C[C@@H]2CCC[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313766 86374 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 COC1COCCC1N[C@H]1C[C@@H]2CCC[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
72946200 105232 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 570 7 1 8 2.2 COCCOC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115106 105232 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 570 7 1 8 2.2 COCCOC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
72946008 105237 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 625 7 1 9 1.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115111 105237 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 625 7 1 9 1.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
53321483 58475 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 498 7 1 6 3.5 CCC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683078 58475 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 498 7 1 6 3.5 CCC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
10279078 73715 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 508 11 5 5 3.5 CCC(O)(CC)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018379 73715 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 508 11 5 5 3.5 CCC(O)(CC)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
46240687 83585 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 528 7 3 7 3.2 CSc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204267 83585 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 528 7 3 7 3.2 CSc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
44447786 95114 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 584 7 2 3 7.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(C(=O)O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL255511 95114 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 584 7 2 3 7.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(C(=O)O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
54584109 62547 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 509 5 1 6 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782379 62547 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 509 5 1 6 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
69286108 121233 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 505 9 2 4 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](COc2ccccc2)C1 10.1021/ml500505q
CHEMBL3577941 121233 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 505 9 2 4 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](COc2ccccc2)C1 10.1021/ml500505q
10218812 193434 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 621 10 3 7 2.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NS(C)(=O)=O)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL526180 193434 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 621 10 3 7 2.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NS(C)(=O)=O)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
89823580 126337 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(Cl)c2)C1 nan
CHEMBL3650385 126337 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(Cl)c2)C1 nan
57344314 68930 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 553 7 2 4 5.7 COC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922788 68930 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 553 7 2 4 5.7 COC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
76314234 105223 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 553 5 2 6 2.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115098 105223 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 553 5 2 6 2.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
72945830 105227 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 526 4 1 7 2.2 COC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115101 105227 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 526 4 1 7 2.2 COC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
49764701 65439 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 500 6 3 5 2.9 N#Cc1cccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2011.06.080
CHEMBL1829630 65439 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 500 6 3 5 2.9 N#Cc1cccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2011.06.080
44442543 154821 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 11 4 4 2.9 CCNC(=O)[C@H](CCNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL400383 154821 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 11 4 4 2.9 CCNC(=O)[C@H](CCNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
22310945 118061 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1ccc2c(c1)cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL340450 118061 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1ccc2c(c1)cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44395186 65218 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 478 8 1 5 3.9 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL182598 65218 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 478 8 1 5 3.9 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
57397013 70513 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 343 4 3 3 1.8 N[C@H]1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2011.12.057
CHEMBL1946836 70513 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 343 4 3 3 1.8 N[C@H]1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2011.12.057
44395143 67014 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 406 6 3 5 2.3 Cc1csc(C(=O)NNC(=O)CNC2CCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL186984 67014 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 406 6 3 5 2.3 Cc1csc(C(=O)NNC(=O)CNC2CCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
24801345 97854 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 475 6 3 3 3.9 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL272167 97854 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 475 6 3 3 3.9 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
24801345 97854 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 6 3 3 3.9 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL272167 97854 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 6 3 3 3.9 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
122181152 121706 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 638 8 1 4 7.2 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3588870 121706 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 638 8 1 4 7.2 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
5353432 97495 89 None -1 3 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
CHEMBL270299 97495 89 None -1 3 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
44573569 193289 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 528 6 2 3 6.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOc3ccccc32)C1 10.1007/s00044-010-9501-4
CHEMBL524030 193289 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 528 6 2 3 6.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOc3ccccc32)C1 10.1007/s00044-010-9501-4
44573569 193289 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 528 6 2 3 6.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOc3ccccc32)C1 10.1016/j.bmcl.2008.12.050
CHEMBL524030 193289 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 528 6 2 3 6.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOc3ccccc32)C1 10.1016/j.bmcl.2008.12.050
44415904 80430 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 514 9 1 2 7.0 CCC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL214641 80430 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 514 9 1 2 7.0 CCC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44425306 142369 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388949 142369 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44453408 95438 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 436 6 4 5 2.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257064 95438 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 436 6 4 5 2.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
44593562 187495 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 187495 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
49863225 15215 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 609 13 5 7 4.4 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCNCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL1210728 15215 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 609 13 5 7 4.4 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCNCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44395136 67079 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 493 8 2 6 3.5 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(N)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL187284 67079 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 493 8 2 6 3.5 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(N)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
9842404 67274 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 371 6 2 3 2.5 O=C(CNC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL188170 67274 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 371 6 2 3 2.5 O=C(CNC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
44413147 139713 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccsc1 10.1016/j.bmcl.2006.04.045
CHEMBL379818 139713 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccsc1 10.1016/j.bmcl.2006.04.045
25269516 93323 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 353 5 1 2 4.0 Cc1cccc(C(=O)Nc2ccc(C[N+](C)(C)C3CCOCC3)cc2)c1 10.1016/j.bmcl.2007.01.115
CHEMBL245289 93323 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 353 5 1 2 4.0 Cc1cccc(C(=O)Nc2ccc(C[N+](C)(C)C3CCOCC3)cc2)c1 10.1016/j.bmcl.2007.01.115
44439166 90546 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 595 12 5 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238731 90546 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 595 12 5 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
11237256 73734 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018398 73734 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
46945254 65435 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 5 2.9 Nc1cccnc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
CHEMBL1829626 65435 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 5 2.9 Nc1cccnc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
89823575 126311 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2F)C1 nan
CHEMBL3650359 126311 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2F)C1 nan
89823628 126349 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 555 5 0 5 4.8 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
CHEMBL3650396 126349 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 555 5 0 5 4.8 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
11585168 90688 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL239143 90688 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44442573 93543 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 521 10 4 5 2.7 CN(C)c1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
CHEMBL246404 93543 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 521 10 4 5 2.7 CN(C)c1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
44395125 123118 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 409 7 0 3 5.3 N#Cc1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL361121 123118 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 409 7 0 3 5.3 N#Cc1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
508727 155319 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 389 6 2 3 2.6 O=C(CNC(=O)c1cccc(F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL403058 155319 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 389 6 2 3 2.6 O=C(CNC(=O)c1cccc(F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
44415945 139549 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 618 8 1 2 8.4 CC[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL379634 139549 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 618 8 1 2 8.4 CC[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
127028592 137500 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 284 2 1 1 4.4 C[C@@]1(c2ccc(Cl)c(Cl)c2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
CHEMBL3754037 137500 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 284 2 1 1 4.4 C[C@@]1(c2ccc(Cl)c(Cl)c2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
11585168 90688 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239143 90688 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
46241509 83562 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 506 7 3 6 2.5 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204244 83562 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 506 7 3 6 2.5 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
46945857 65431 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 461 6 2 5 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3cnccn3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829622 65431 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 461 6 2 5 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3cnccn3)CC2)C1 10.1016/j.bmcl.2011.06.080
54754722 65752 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 439 6 3 6 2.4 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](CO)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834643 65752 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 439 6 3 6 2.4 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](CO)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
10030247 95408 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccncn3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL256954 95408 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccncn3)CC2)C1 10.1016/j.bmcl.2007.12.029
44425634 142018 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL387587 142018 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
10240278 172897 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 654 10 4 6 5.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL451597 172897 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 654 10 4 6 5.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
69321774 73810 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 593 13 5 5 4.4 CCC[C@H](O)[C@H](CN(C)Cc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018536 73810 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 593 13 5 5 4.4 CCC[C@H](O)[C@H](CN(C)Cc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
11844471 80199 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 618 8 1 2 8.4 CCC1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CCC12C=Cc1ccccc12 10.1021/jm060439n
CHEMBL213648 80199 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 618 8 1 2 8.4 CCC1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CCC12C=Cc1ccccc12 10.1021/jm060439n
71519053 86396 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 416 4 1 4 3.1 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314051 86396 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 416 4 1 4 3.1 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
11570045 90949 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2ccc(Cl)cc2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL239358 90949 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2ccc(Cl)cc2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
11570045 90949 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2ccc(Cl)cc2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239358 90949 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2ccc(Cl)cc2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
46885028 8422 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 545 8 2 5 2.4 Cc1ccccc1C(=O)N1CCN(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
CHEMBL1093470 8422 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 545 8 2 5 2.4 Cc1ccccc1C(=O)N1CCN(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
89823601 126360 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650406 126360 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
70696470 75218 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 367 4 1 4 2.6 N#Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1 10.1016/j.bmcl.2012.04.118
CHEMBL2036769 75218 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 367 4 1 4 2.6 N#Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1 10.1016/j.bmcl.2012.04.118
72946775 105235 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 597 7 2 8 1.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCNC(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115109 105235 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 597 7 2 8 1.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCNC(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
71517401 86381 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 501 4 1 5 3.5 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](Cl)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313773 86381 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 501 4 1 5 3.5 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](Cl)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
51039119 176217 33 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CCL2 from mouse CCR2Displacement of [125I]-CCL2 from mouse CCR2
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
CHEMBL4594419 176217 33 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CCL2 from mouse CCR2Displacement of [125I]-CCL2 from mouse CCR2
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
46241826 83561 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 490 6 3 5 2.8 Cc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204243 83561 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 490 6 3 5 2.8 Cc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
56667036 65427 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 460 6 2 4 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829618 65427 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 460 6 2 4 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.06.080
44447789 155222 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 600 7 3 4 6.2 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(C(=O)O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL402624 155222 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 600 7 3 4 6.2 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(C(=O)O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
44453472 155538 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2b in HEK293 cellsDisplacement of [125I]MCP1 from human CCR2b in HEK293 cells
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404259 155538 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2b in HEK293 cellsDisplacement of [125I]MCP1 from human CCR2b in HEK293 cells
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
44425640 96929 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 576 5 1 2 7.6 C[C@H]1CN(C2CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL266017 96929 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 576 5 1 2 7.6 C[C@H]1CN(C2CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
11844470 141736 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 604 7 1 2 8.0 CC1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CCC12C=Cc1ccccc12 10.1021/jm060439n
CHEMBL385824 141736 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 604 7 1 2 8.0 CC1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CCC12C=Cc1ccccc12 10.1021/jm060439n
11456448 77645 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 640 10 2 5 6.2 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(Cc3ccccc3)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088385 77645 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 640 10 2 5 6.2 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(Cc3ccccc3)cc2)C1 10.1016/j.bmcl.2012.08.002
53321427 58466 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.3 CCO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683069 58466 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.3 CCO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
89823598 126365 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650410 126365 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
44395094 67257 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 528 8 2 6 4.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(Cl)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL188075 67257 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 528 8 2 6 4.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(Cl)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
46886057 8399 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 639 9 1 6 5.5 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2N2CCC(C)(NC(=O)c3cccc(C(F)(F)F)c3)C2=O)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1093319 8399 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 639 9 1 6 5.5 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2N2CCC(C)(NC(=O)c3cccc(C(F)(F)F)c3)C2=O)cc1 10.1016/j.bmcl.2010.03.035
44612589 137432 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 332 2 1 1 5.1 C[C@@H]1CC=C(C(=O)O)[C@@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753491 137432 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 332 2 1 1 5.1 C[C@@H]1CC=C(C(=O)O)[C@@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
44444000 94511 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 464 8 1 2 6.4 O=C(/C=C/c1cc(Cl)cc(Cl)c1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL251620 94511 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 464 8 1 2 6.4 O=C(/C=C/c1cc(Cl)cc(Cl)c1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
44395254 66242 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 564 10 1 7 4.1 CN(C)c1ccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccc(N(C)C)cc2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL184582 66242 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 564 10 1 7 4.1 CN(C)c1ccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccc(N(C)C)cc2)cc1 10.1016/j.bmcl.2004.08.008
10153431 188329 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 643 9 3 7 5.7 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL500786 188329 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 643 9 3 7 5.7 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2009.05.041
11641253 58453 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 464 5 1 3 5.3 CC(C)[C@]1(C(=O)N2CC=C(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683054 58453 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 464 5 1 3 5.3 CC(C)[C@]1(C(=O)N2CC=C(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
53324140 58462 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683065 58462 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
89823656 126355 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
CHEMBL3650401 126355 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
53318854 58469 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.2 COC[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683072 58469 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.2 COC[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
9852285 8260 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 634 7 3 6 5.8 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2N2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3NC(=O)OC(C)(C)C)C2=O)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1092434 8260 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 634 7 3 6 5.8 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2N2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3NC(=O)OC(C)(C)C)C2=O)cc1 10.1016/j.bmcl.2010.03.035
44415942 138681 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 534 8 2 3 5.7 CC(O)C(CCN1CCC(c2ccc(F)cc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL377819 138681 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 534 8 2 3 5.7 CC(O)C(CCN1CCC(c2ccc(F)cc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
53326700 58463 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683066 58463 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
22143314 193202 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 522 8 3 5 3.1 CSc1ccc(CNC2CCN(C(C)=O)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL523403 193202 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 522 8 3 5 3.1 CSc1ccc(CNC2CCN(C(C)=O)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.07.123
122181236 121851 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 588 8 1 4 6.3 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589950 121851 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 588 8 1 4 6.3 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
44593561 12663 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1007/s00044-010-9501-4
CHEMBL1187238 12663 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1007/s00044-010-9501-4
CHEMBL494580 12663 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1007/s00044-010-9501-4
44593561 12663 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL1187238 12663 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494580 12663 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
44415992 80609 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215093 80609 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
52950180 19350 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 545 10 2 4 5.1 CCCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290754 19350 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 545 10 2 4 5.1 CCCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
44442576 93545 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 522 10 4 5 2.9 COc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246406 93545 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 522 10 4 5 2.9 COc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44423285 142166 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 536 4 1 2 7.0 C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm070166b
CHEMBL388380 142166 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 536 4 1 2 7.0 C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm070166b
89823445 126351 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
CHEMBL3650398 126351 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
57344295 130625 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3681872 130625 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
23656067 148987 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 481 5 1 2 5.7 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL394228 148987 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 481 5 1 2 5.7 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
23656067 148987 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 481 5 1 2 5.7 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1021/jm070902b
CHEMBL394228 148987 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 481 5 1 2 5.7 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1021/jm070902b
86698131 126306 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 582 5 1 5 5.4 O=C(O)c1cccc(C2CCN([C@H]3C[C@H]4CCC[C@@]4(C(=O)N4C[C@@H]5C[C@H]4CN5c4cc(C(F)(F)F)ccn4)C3)CC2)c1 nan
CHEMBL3650354 126306 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 582 5 1 5 5.4 O=C(O)c1cccc(C2CCN([C@H]3C[C@H]4CCC[C@@]4(C(=O)N4C[C@@H]5C[C@H]4CN5c4cc(C(F)(F)F)ccn4)C3)CC2)c1 nan
44439160 169397 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 580 11 4 6 4.9 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL442254 169397 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 580 11 4 6 4.9 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44439160 169397 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 580 11 4 6 4.9 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL442254 169397 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 580 11 4 6 4.9 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
25267738 93870 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 339 5 1 2 3.7 C[N+](C)(Cc1ccc(NC(=O)c2ccccc2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL247949 93870 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 339 5 1 2 3.7 C[N+](C)(Cc1ccc(NC(=O)c2ccccc2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
22311005 19982 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 458 5 1 4 5.1 O=C(NS(=O)(=O)c1ccccc1)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130318 19982 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 458 5 1 4 5.1 O=C(NS(=O)(=O)c1ccccc1)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44415864 80546 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 554 7 2 3 6.0 CC(O)C(CCN1CC[C@@]2(C=Cc3ccccc32)[C@@H](C)C1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL214825 80546 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 554 7 2 3 6.0 CC(O)C(CCN1CC[C@@]2(C=Cc3ccccc32)[C@@H](C)C1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
10164316 154792 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 9 4 4 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL400196 154792 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 9 4 4 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
56683120 65807 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 476 6 2 7 3.5 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ncco4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834849 65807 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 476 6 2 7 3.5 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ncco4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44449229 95148 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 538 7 1 3 5.6 CN(C)CC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL255687 95148 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 538 7 1 3 5.6 CN(C)CC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
44453134 98064 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 455 7 2 4 3.4 O=C(CNC(=O)c1cccc(OC(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL273195 98064 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 455 7 2 4 3.4 O=C(CNC(=O)c1cccc(OC(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
11155781 73809 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 476 10 4 4 4.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)Cc1nc2c(C(F)(F)F)cccc2[nH]1 10.1016/j.bmcl.2012.03.007
CHEMBL2018534 73809 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 476 10 4 4 4.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)Cc1nc2c(C(F)(F)F)cccc2[nH]1 10.1016/j.bmcl.2012.03.007
46241610 83570 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 548 7 3 6 3.6 CC(C)(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204252 83570 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 548 7 3 6 3.6 CC(C)(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
71519381 86373 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 467 4 1 5 3.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL2313765 86373 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 467 4 1 5 3.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
89823417 126345 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 498 5 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C#N)c2)C1 nan
CHEMBL3650392 126345 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 498 5 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C#N)c2)C1 nan
44442563 93734 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 9 3 5 2.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)N2CCOCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247211 93734 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 9 3 5 2.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)N2CCOCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
57344221 68957 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 568 8 3 4 5.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL1922819 68957 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 568 8 3 4 5.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(OC(F)(F)F)cc2)CC1 nan
54772203 86591 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 484 6 2 6 4.0 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315931 86591 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 484 6 2 6 4.0 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2012.12.017
54771980 86594 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 484 6 2 6 4.0 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccn3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315934 86594 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 484 6 2 6 4.0 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccn3)CC2)C1 10.1016/j.bmcl.2012.12.017
71190126 84901 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1007/s00044-010-9497-9
CHEMBL2236475 84901 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1007/s00044-010-9497-9
56643545 130623 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681870 130623 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
57344303 130648 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681894 130648 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
11591776 145486 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 525 6 2 3 5.2 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL391459 145486 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 525 6 2 3 5.2 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
11185 1991 42 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 10.1021/jm300682j
25134303 1991 42 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 10.1021/jm300682j
CHEMBL2178573 1991 42 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 10.1021/jm300682j
DB16066 1991 42 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 10.1021/jm300682j
11598084 75204 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 474 6 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036755 75204 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 474 6 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
10162782 73706 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018370 73706 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
70691784 73707 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 12 4 4 3.9 CCCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018371 73707 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 12 4 4 3.9 CCCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
46241010 83584 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 540 8 3 7 3.3 CC(C)Oc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204266 83584 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 540 8 3 7 3.3 CC(C)Oc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
49763568 65415 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829605 65415 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
56657930 65793 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 528 7 2 6 4.6 CN(C)c1cccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)c1 10.1016/j.bmcl.2011.08.074
CHEMBL1834786 65793 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 528 7 2 6 4.6 CN(C)c1cccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)c1 10.1016/j.bmcl.2011.08.074
56683116 65806 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 534 7 2 7 5.1 CC(C)c1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
CHEMBL1834799 65806 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 534 7 2 7 5.1 CC(C)c1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
89845031 109813 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 533 8 1 6 2.8 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(OC(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233183 109813 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 533 8 1 6 2.8 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(OC(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
9850318 95245 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL256154 95245 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
44425646 86100 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 528 6 1 2 7.1 CCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231038 86100 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 528 6 1 2 7.1 CCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
53317027 58666 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 435 4 1 5 3.2 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684683 58666 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 435 4 1 5 3.2 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
44425645 86082 0 None - 0 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230933 86082 0 None - 0 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
10162782 73706 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL2018370 73706 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
11591776 145486 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL391459 145486 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
24801690 98041 25 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL273083 98041 25 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
10008367 2022 50 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
777 2022 50 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL1289316 2022 50 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL2426341 2022 50 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
24801690 98041 25 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
CHEMBL273083 98041 25 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
57656833 75229 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Inhibition of MCP1-induced CCR2-mediated chemotaxis in human THP-1 cellsInhibition of MCP1-induced CCR2-mediated chemotaxis in human THP-1 cells
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036782 75229 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Inhibition of MCP1-induced CCR2-mediated chemotaxis in human THP-1 cellsInhibition of MCP1-induced CCR2-mediated chemotaxis in human THP-1 cells
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
68767109 109812 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 531 7 1 5 3.3 Cc1ccc(C(=O)N[C@H]2CCN([C@H]3CC[C@@H](N(C)C(C)C)C[C@H]3CS(C)(=O)=O)C2=O)cc1C(F)(F)F 10.1016/j.bmcl.2014.02.013
CHEMBL3233182 109812 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 531 7 1 5 3.3 Cc1ccc(C(=O)N[C@H]2CCN([C@H]3CC[C@@H](N(C)C(C)C)C[C@H]3CS(C)(=O)=O)C2=O)cc1C(F)(F)F 10.1016/j.bmcl.2014.02.013
57400451 70507 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 9 3 5 3.6 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
CHEMBL1946830 70507 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 9 3 5 3.6 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
44425249 143522 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL389888 143522 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
11192346 2024 57 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 2024 57 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 2024 57 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
10165625 73728 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 536 13 5 5 4.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018392 73728 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 536 13 5 5 4.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)C 10.1016/j.bmcl.2012.03.007
44453365 97527 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 465 7 4 6 2.0 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
CHEMBL270435 97527 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 465 7 4 6 2.0 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
11227168 74550 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2nccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029569 74550 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2nccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
44573650 193210 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 564 6 3 4 5.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(O)C(F)(F)F)C1 10.1007/s00044-010-9501-4
CHEMBL523503 193210 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 564 6 3 4 5.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(O)C(F)(F)F)C1 10.1007/s00044-010-9501-4
44425648 168704 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 540 6 1 2 7.1 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL436796 168704 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 540 6 1 2 7.1 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44573649 187235 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 548 6 2 3 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C(F)(F)F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492569 187235 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 548 6 2 3 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C(F)(F)F)C1 10.1016/j.bmcl.2008.12.050
67011331 74545 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 557 7 3 7 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncco4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029424 74545 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 557 7 3 7 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncco4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
44593563 193110 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL522688 193110 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
53324304 58464 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 497 6 1 5 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683067 58464 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 497 6 1 5 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
11387511 74541 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ccncc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029419 74541 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ccncc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
10167417 73725 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 591 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018389 73725 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 591 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCCC1 10.1016/j.bmcl.2012.03.007
44583281 188235 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 626 9 3 6 4.5 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL499467 188235 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 626 9 3 6 4.5 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)cc1 10.1016/j.bmcl.2009.05.041
44425310 142358 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 651 8 3 5 6.8 CNC(=O)Nc1nc([C@@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388868 142358 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 651 8 3 5 6.8 CNC(=O)Nc1nc([C@@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
11285792 879 34 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at CCR2 assessed as inhibition of CCL2 bindingAntagonist activity at CCR2 assessed as inhibition of CCL2 binding
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm300682j
801 879 34 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at CCR2 assessed as inhibition of CCL2 bindingAntagonist activity at CCR2 assessed as inhibition of CCL2 binding
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm300682j
CHEMBL2110727 879 34 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at CCR2 assessed as inhibition of CCL2 bindingAntagonist activity at CCR2 assessed as inhibition of CCL2 binding
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm300682j
DB11758 879 34 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at CCR2 assessed as inhibition of CCL2 bindingAntagonist activity at CCR2 assessed as inhibition of CCL2 binding
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm300682j
11285792 879 34 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP-1 from CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from CCR2b expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
801 879 34 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP-1 from CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from CCR2b expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
CHEMBL2110727 879 34 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP-1 from CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from CCR2b expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
DB11758 879 34 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP-1 from CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from CCR2b expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
11285792 879 34 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/acs.jmedchem.9b01701
801 879 34 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/acs.jmedchem.9b01701
CHEMBL2110727 879 34 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/acs.jmedchem.9b01701
DB11758 879 34 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/acs.jmedchem.9b01701
44573649 187235 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 548 6 2 3 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C(F)(F)F)C1 10.1007/s00044-010-9501-4
CHEMBL492569 187235 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 548 6 2 3 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C(F)(F)F)C1 10.1007/s00044-010-9501-4
11534473 90699 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 594 14 1 5 8.0 CCN(CC)CCCC(NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)C(C)C 10.1016/j.ejmech.2010.04.024
CHEMBL239144 90699 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 594 14 1 5 8.0 CCN(CC)CCCC(NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)C(C)C 10.1016/j.ejmech.2010.04.024
71552261 86599 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 573 6 3 7 4.8 O=C(CNc1cc(C(F)(F)F)nc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315939 86599 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 573 6 3 7 4.8 O=C(CNc1cc(C(F)(F)F)nc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
11526729 155062 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 541 7 2 4 5.1 COc1ccc2c(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL401744 155062 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 541 7 2 4 5.1 COc1ccc2c(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2008.05.010
44448776 155256 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 572 6 3 5 5.7 COC(=O)c1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)Nc5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL402801 155256 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 572 6 3 5 5.7 COC(=O)c1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)Nc5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
57656825 75208 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 394 4 1 3 3.5 O=C(Nc1ccc(F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036759 75208 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 394 4 1 3 3.5 O=C(Nc1ccc(F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
46241608 83569 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 534 8 3 6 3.2 CC(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204251 83569 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 534 8 3 6 3.2 CC(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
46886482 8259 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 608 8 4 6 5.4 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1092433 8259 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 608 8 4 6 5.4 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2010.03.035
10482463 95462 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccnn3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL257160 95462 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccnn3)CC2)C1 10.1016/j.bmcl.2007.12.029
183790 3742 11 None -6 2 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysisDisplacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysis
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
783 3742 11 None -6 2 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysisDisplacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysis
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
CHEMBL1178786 3742 11 None -6 2 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysisDisplacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysis
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
11671120 89880 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 543 6 2 3 5.3 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070902b
CHEMBL237805 89880 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 543 6 2 3 5.3 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070902b
22310995 20330 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 334 3 2 3 4.3 Nc1ccc2c(c1)cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130598 20330 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 334 3 2 3 4.3 Nc1ccc2c(c1)cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
17866152 124039 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 507 9 2 6 4.0 CNc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.008
CHEMBL363059 124039 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 507 9 2 6 4.0 CNc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.008
44395239 66153 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 412 9 1 3 4.7 O=C(CCCC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
CHEMBL184220 66153 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 412 9 1 3 4.7 O=C(CCCC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
46886056 8398 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 607 10 1 5 5.2 CCCN(C(C)C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1093318 8398 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 607 10 1 5 5.2 CCCN(C(C)C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
11466237 74538 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 504 6 3 5 3.2 Cc1cccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)n1 10.1021/ml200199c
CHEMBL2029416 74538 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 504 6 3 5 3.2 Cc1cccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)n1 10.1021/ml200199c
52944966 19040 0 None - 0 Mouse 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 579 9 2 4 5.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1OCc1ccccc1 10.1016/j.bmcl.2010.10.020
CHEMBL1288324 19040 0 None - 0 Mouse 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 579 9 2 4 5.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1OCc1ccccc1 10.1016/j.bmcl.2010.10.020
44573609 187553 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 496 6 3 4 4.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2O)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494542 187553 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 496 6 3 4 4.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2O)C1 10.1016/j.bmcl.2008.12.050
44593564 187232 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1007/s00044-010-9501-4
CHEMBL492564 187232 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1007/s00044-010-9501-4
11296618 77644 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 632 9 2 6 6.3 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(-c3cccs3)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088384 77644 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 632 9 2 6 6.3 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(-c3cccs3)cc2)C1 10.1016/j.bmcl.2012.08.002
89823450 126346 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 562 4 0 4 6.2 N#Cc1ccc(C(F)(F)F)cc1N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
CHEMBL3650393 126346 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 562 4 0 4 6.2 N#Cc1ccc(C(F)(F)F)cc1N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
56678497 65718 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 472 6 2 4 4.5 O=C(COc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834581 65718 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 472 6 2 4 4.5 O=C(COc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
54754845 65751 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 452 6 3 6 1.8 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(N)=O)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834642 65751 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 452 6 3 6 1.8 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(N)=O)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44444102 94035 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 5 1 3 5.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CN2CCC(c3ccc(O)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL248813 94035 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 5 1 3 5.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CN2CCC(c3ccc(O)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
44425321 86136 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 740 10 2 5 9.0 CC(C(=O)Nc1nc(C(CCN2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)c1ccccc1 10.1016/j.bmcl.2006.10.059
CHEMBL231150 86136 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 740 10 2 5 9.0 CC(C(=O)Nc1nc(C(CCN2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)c1ccccc1 10.1016/j.bmcl.2006.10.059
11582651 75203 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 424 5 1 3 4.3 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CC3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036754 75203 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 424 5 1 3 4.3 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CC3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
46944855 65434 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccncc3O)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829625 65434 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccncc3O)CC2)C1 10.1016/j.bmcl.2011.06.080
44439170 151921 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 608 16 1 5 8.6 CCCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL396622 151921 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 608 16 1 5 8.6 CCCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44444107 154484 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 500 5 0 2 6.2 O=C(/C=C/c1ccc(Br)cc1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL399046 154484 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 500 5 0 2 6.2 O=C(/C=C/c1ccc(Br)cc1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
44413311 77783 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 473 8 2 3 4.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(NCCN1CCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL209171 77783 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 473 8 2 3 4.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(NCCN1CCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
89823456 124411 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)cc(C(F)(F)F)c2)C1 nan
CHEMBL3639492 124411 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)cc(C(F)(F)F)c2)C1 nan
11605985 90967 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 514 13 1 4 6.8 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239569 90967 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 514 13 1 4 6.8 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
11605985 90967 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 514 13 1 4 6.8 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL239569 90967 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 514 13 1 4 6.8 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44416070 138893 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 623 8 4 4 4.0 O=C1NCC(C(=O)NC(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)N1 10.1016/j.bmcl.2006.07.011
CHEMBL378258 138893 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 623 8 4 4 4.0 O=C1NCC(C(=O)NC(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)N1 10.1016/j.bmcl.2006.07.011
89823427 126310 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ncn2)C1 nan
CHEMBL3650358 126310 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ncn2)C1 nan
11296325 77621 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 596 9 2 6 5.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3ccc(C(F)(F)F)cc3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088209 77621 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 596 9 2 6 5.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3ccc(C(F)(F)F)cc3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
71530223 86372 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313764 86372 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
53320171 58476 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 512 7 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(C)C)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683079 58476 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 512 7 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(C)C)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
54756156 65785 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 507 9 2 7 3.6 C=CCn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(=O)OCC)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834779 65785 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 507 9 2 7 3.6 C=CCn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(=O)OCC)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44453325 155541 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 466 7 4 6 2.1 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1O 10.1016/j.bmcl.2008.02.015
CHEMBL404269 155541 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 466 7 4 6 2.1 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1O 10.1016/j.bmcl.2008.02.015
56675300 65755 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 411 5 4 5 2.1 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](O)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834646 65755 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 411 5 4 5 2.1 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](O)CC2)C1 10.1016/j.bmcl.2011.08.074
44442572 93542 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 10 4 4 3.2 CCc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
CHEMBL246403 93542 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 10 4 4 3.2 CCc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
24801342 97615 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 517 8 3 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(OC(F)(F)F)cc1 10.1021/jm701488f
CHEMBL270957 97615 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 517 8 3 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(OC(F)(F)F)cc1 10.1021/jm701488f
46240582 83573 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 479 6 3 6 1.8 Cn1ccnc1[C@]1(O)CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1021/ml300260s
CHEMBL2204255 83573 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 479 6 3 6 1.8 Cn1ccnc1[C@]1(O)CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1021/ml300260s
57403877 70525 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 10 3 5 3.6 CCCN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1947043 70525 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 10 3 5 3.6 CCCN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44353447 3775 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2008.02.015
785 3775 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2008.02.015
CHEMBL337246 3775 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2008.02.015
52950180 19350 0 None - 0 Mouse 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 545 10 2 4 5.1 CCCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290754 19350 0 None - 0 Mouse 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 545 10 2 4 5.1 CCCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
89823537 126298 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650346 126298 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
10115566 97411 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 461 7 3 3 4.3 Cc1ccc(CN[C@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL269898 97411 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 461 7 3 3 4.3 Cc1ccc(CN[C@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
56681842 65716 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 472 5 2 4 3.9 O=C(Cn1[nH]c2ccc(C(F)(F)F)cc2c1=O)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834579 65716 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 472 5 2 4 3.9 O=C(Cn1[nH]c2ccc(C(F)(F)F)cc2c1=O)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
127025159 137351 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 375 3 1 3 3.7 C[C@H]1CC=C(C(=O)NS(C)(=O)=O)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752915 137351 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 375 3 1 3 3.7 C[C@H]1CC=C(C(=O)NS(C)(=O)=O)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
56661444 65775 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 614 6 3 8 5.1 CC(C)(C)NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834717 65775 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 614 6 3 8 5.1 CC(C)(C)NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
23405932 93732 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 532 10 4 4 3.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCC(F)(F)F)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247209 93732 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 532 10 4 4 3.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCC(F)(F)F)c(C)c1 10.1016/j.bmcl.2007.07.028
89823506 126336 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
CHEMBL3650384 126336 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
44573485 187721 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2)C1 10.1007/s00044-010-9501-4
CHEMBL495368 187721 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2)C1 10.1007/s00044-010-9501-4
127036603 137512 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1ccc(C)c([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1 10.1016/j.bmcl.2015.11.051
CHEMBL3754155 137512 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1ccc(C)c([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1 10.1016/j.bmcl.2015.11.051
24801346 161249 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 461 6 3 3 3.6 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL411935 161249 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 461 6 3 3 3.6 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
508749 67123 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 413 7 2 3 3.4 Cc1cccc(C(=O)NCC(=O)NCC2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL187469 67123 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 413 7 2 3 3.4 Cc1cccc(C(=O)NCC(=O)NCC2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2004.08.009
57656701 75231 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 413 2 1 4 1.9 CN1CCN(C)C(C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036784 75231 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 413 2 1 4 1.9 CN1CCN(C)C(C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
10225909 93961 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 451 9 4 4 2.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248417 93961 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 451 9 4 4 2.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)O)c(C)c1 10.1016/j.bmcl.2007.07.028
57344222 130636 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 545 8 4 5 4.8 CCOC(=O)c1ccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)cc1 nan
CHEMBL3681882 130636 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 545 8 4 5 4.8 CCOC(=O)c1ccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)cc1 nan
44425649 86129 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 86129 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
68004146 86588 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 530 7 3 8 3.1 COc1cccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)n1 10.1016/j.bmcl.2012.12.017
CHEMBL2315928 86588 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 530 7 3 8 3.1 COc1cccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)n1 10.1016/j.bmcl.2012.12.017
54756045 65788 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 510 7 3 8 2.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C(N)=O)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834781 65788 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 510 7 3 8 2.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C(N)=O)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56671793 65796 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 486 6 2 6 3.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cccnc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834789 65796 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 486 6 2 6 3.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cccnc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44573452 187607 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494770 187607 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOC2)C1 10.1016/j.bmcl.2008.12.050
10427222 165741 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2cc(F)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL424638 165741 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2cc(F)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
46886057 8399 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 639 9 1 6 5.5 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2N2CCC(C)(NC(=O)c3cccc(C(F)(F)F)c3)C2=O)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1093319 8399 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 639 9 1 6 5.5 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2N2CCC(C)(NC(=O)c3cccc(C(F)(F)F)c3)C2=O)cc1 10.1016/j.bmcl.2010.03.035
72945827 105228 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 588 5 1 7 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)Oc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115102 105228 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 588 5 1 7 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)Oc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44442531 153945 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 10 4 4 2.5 CCNC(=O)[C@@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL398353 153945 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 10 4 4 2.5 CCNC(=O)[C@@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
71519052 86395 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 457 6 1 6 3.1 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(OC(C)C)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314050 86395 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 457 6 1 6 3.1 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(OC(C)C)cc3C2)C1 10.1016/j.bmcl.2012.10.069
44442584 93551 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 534 12 4 4 4.0 CCCCc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
CHEMBL246413 93551 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 534 12 4 4 4.0 CCCCc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
11590644 121223 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 457 11 4 4 3.3 CCC[C@H](O)[C@H](CNCC1CCCCC1)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577931 121223 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 457 11 4 4 3.3 CCC[C@H](O)[C@H](CNCC1CCCCC1)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
72948000 105224 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 601 6 2 6 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115099 105224 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 601 6 2 6 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
46240585 83583 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 524 7 3 6 3.6 CC(C)c1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204265 83583 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 524 7 3 6 3.6 CC(C)c1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
44425643 86042 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230722 86042 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
70697571 77975 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL2096788 77975 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
57398651 70520 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 385 6 3 3 2.9 CC(C)N[C@H]1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2011.12.057
CHEMBL1947039 70520 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 385 6 3 3 2.9 CC(C)N[C@H]1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2011.12.057
44416273 138941 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 496 6 1 2 6.2 O=C(CCCN1CCC2(C=Cc3ccccc32)CC1)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL378449 138941 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 496 6 1 2 6.2 O=C(CCCN1CCC2(C=Cc3ccccc32)CC1)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
90656015 111106 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 501 4 1 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2[S+]([O-])CC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263262 111106 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 501 4 1 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2[S+]([O-])CC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
44413344 139338 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 489 8 2 4 4.0 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(NCCN1CCOCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL379278 139338 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 489 8 2 4 4.0 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(NCCN1CCOCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
44353369 23243 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 315 4 1 3 4.1 COc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1 10.1016/j.bmcl.2003.10.049
CHEMBL133168 23243 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 315 4 1 3 4.1 COc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1 10.1016/j.bmcl.2003.10.049
44612708 137436 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@@H]1CC=C(C(=O)O)[C@@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753526 137436 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@@H]1CC=C(C(=O)O)[C@@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
57344219 130634 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 545 8 4 5 4.8 CCOC(=O)c1cccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)c1 nan
CHEMBL3681880 130634 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 545 8 4 5 4.8 CCOC(=O)c1cccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)c1 nan
71517574 86387 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 483 4 2 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313779 86387 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 483 4 2 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
57656921 75213 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 420 4 1 3 3.5 O=C(Nc1ccc(Br)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036764 75213 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 420 4 1 3 3.5 O=C(Nc1ccc(Br)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
46842383 8345 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 530 8 2 4 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092929 8345 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 530 8 2 4 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
72946010 105230 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 582 5 1 7 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115104 105230 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 582 5 1 7 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
71517573 86386 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 483 4 2 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313778 86386 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 483 4 2 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
57393530 70508 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 497 7 3 5 2.5 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1946831 70508 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 497 7 3 5 2.5 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44453372 155744 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 433 7 2 3 3.4 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL405633 155744 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 433 7 2 3 3.4 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
71768798 111101 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 497 4 1 6 3.1 COC1COCCC1N[C@@H]1C[C@H]2OC(C)(C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263257 111101 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 497 4 1 6 3.1 COC1COCCC1N[C@@H]1C[C@H]2OC(C)(C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
9851741 80193 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 604 7 1 2 8.0 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@]12C=Cc1ccccc12 10.1021/jm060439n
CHEMBL213601 80193 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 604 7 1 2 8.0 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@]12C=Cc1ccccc12 10.1021/jm060439n
67774475 130658 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 488 6 4 4 4.3 Cc1cccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5cccnc45)CC3)C(N)=O)CC2)c1 nan
CHEMBL3681903 130658 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 488 6 4 4 4.3 Cc1cccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5cccnc45)CC3)C(N)=O)CC2)c1 nan
44444105 94072 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 482 7 0 4 5.5 COc1ccc(/C=C/C(=O)N2CCC(CN3CCC(c4ccc(Cl)cc4)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.07.065
CHEMBL249009 94072 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 482 7 0 4 5.5 COc1ccc(/C=C/C(=O)N2CCC(CN3CCC(c4ccc(Cl)cc4)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.07.065
44413158 79971 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 437 8 2 4 3.8 CN(C)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccco1 10.1016/j.bmcl.2006.04.045
CHEMBL212674 79971 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 437 8 2 4 3.8 CN(C)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccco1 10.1016/j.bmcl.2006.04.045
89823541 126323 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)c2)C1 nan
CHEMBL3650371 126323 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)c2)C1 nan
11699524 95110 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 541 7 2 4 5.1 COc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL255499 95110 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 541 7 2 4 5.1 COc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
11605635 95464 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 493 6 2 3 4.9 O=C(/C=C/c1ccc(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL257173 95464 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 493 6 2 3 4.9 O=C(/C=C/c1ccc(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11534473 90699 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 594 14 1 5 8.0 CCN(CC)CCCC(NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)C(C)C 10.1016/j.bmcl.2006.10.060
CHEMBL239144 90699 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 594 14 1 5 8.0 CCN(CC)CCCC(NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)C(C)C 10.1016/j.bmcl.2006.10.060
54754969 65740 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 515 6 3 6 4.2 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834632 65740 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 515 6 3 6 4.2 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
56675205 65795 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 486 6 3 5 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834788 65795 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 486 6 3 5 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44447783 95076 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 556 6 2 3 7.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL255312 95076 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 556 6 2 3 7.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
10325032 95115 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 541 6 1 3 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL255513 95115 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 541 6 1 3 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
44447782 155313 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 570 7 1 3 7.4 COc1cccc(C2CCN([C@@H]3CC[C@@](C(=O)NCc4cc(C(F)(F)F)cc(C(F)(F)F)c4)(C(C)C)C3)CC2)c1 10.1016/j.bmcl.2007.12.029
CHEMBL403033 155313 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 570 7 1 3 7.4 COc1cccc(C2CCN([C@@H]3CC[C@@](C(=O)NCc4cc(C(F)(F)F)cc(C(F)(F)F)c4)(C(C)C)C3)CC2)c1 10.1016/j.bmcl.2007.12.029
10392978 167459 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 558 6 2 5 5.3 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL429849 167459 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 558 6 2 5 5.3 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
11421712 74543 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cnccn4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029421 74543 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cnccn4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
11365166 74544 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 573 7 3 7 4.0 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4nccs4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029423 74544 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 573 7 3 7 4.0 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4nccs4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
44593564 187232 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492564 187232 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
22143293 188027 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497577 188027 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
44453368 97767 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 449 6 4 5 2.3 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
CHEMBL271725 97767 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 449 6 4 5 2.3 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
22143309 187941 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL496959 187941 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
51039119 176217 33 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-CCL2 from CCR2 in human PBMC cellsDisplacement of [125I]-CCL2 from CCR2 in human PBMC cells
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
CHEMBL4594419 176217 33 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-CCL2 from CCR2 in human PBMC cellsDisplacement of [125I]-CCL2 from CCR2 in human PBMC cells
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
53325639 58470 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683073 58470 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
44580591 187859 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 551 9 4 6 3.1 CCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL496344 187859 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 551 9 4 6 3.1 CCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
44425649 86129 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 86129 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
22143293 188027 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497577 188027 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
11700079 149923 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 618 8 3 5 4.5 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1021/jm070902b
CHEMBL394955 149923 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 618 8 3 5 4.5 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1021/jm070902b
10129343 173265 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 642 11 3 6 5.2 CCN(CC)C(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL452509 173265 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 642 11 3 6 5.2 CCN(CC)C(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
44425640 96929 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 576 5 1 2 7.6 C[C@H]1CN(C2CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL266017 96929 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 576 5 1 2 7.6 C[C@H]1CN(C2CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44425309 142357 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388867 142357 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
53324942 58678 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 469 6 1 5 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)c2ccccc2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684701 58678 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 469 6 1 5 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)c2ccccc2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
60148505 111110 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 469 4 1 6 2.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263268 111110 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 469 4 1 6 2.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
57335017 70338 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944776 70338 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
57391591 70340 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 637 10 4 6 3.8 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944778 70340 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 637 10 4 6 3.8 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
162668957 182760 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 495 5 3 7 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(C)(C)C)nc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4790208 182760 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 495 5 3 7 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(C)(C)C)nc23)C1=O 10.1021/acsmedchemlett.1c00082
71768900 111114 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 470 4 1 6 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2COc3ccc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263272 111114 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 470 4 1 6 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2COc3ccc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
10209478 73721 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 551 12 6 5 3.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC 10.1016/j.bmcl.2012.03.007
CHEMBL2018385 73721 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 551 12 6 5 3.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC 10.1016/j.bmcl.2012.03.007
10300284 73732 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018396 73732 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
11752457 74539 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1021/ml200199c
CHEMBL2029417 74539 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1021/ml200199c
69285563 121228 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 443 8 2 4 3.1 COC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577936 121228 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 443 8 2 4 3.1 COC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
44442561 93539 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 11 4 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCC2CC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246399 93539 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 11 4 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCC2CC2)c(C)c1 10.1016/j.bmcl.2007.07.028
57344305 68939 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922797 68939 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
10207591 73417 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 507 10 4 4 4.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)CC(C)(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2016596 73417 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 507 10 4 4 4.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)CC(C)(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
44571216 172652 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 757 11 5 8 6.3 CSc1ccc(C(=O)NC2CCC(NC(=O)OCc3ccccc3)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL449674 172652 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 757 11 5 8 6.3 CSc1ccc(C(=O)NC2CCC(NC(=O)OCc3ccccc3)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2008.12.062
67772854 130637 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 7 3 5 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)OCCO3)CC1 nan
CHEMBL3681883 130637 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 7 3 5 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)OCCO3)CC1 nan
44415957 81054 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 510 6 1 2 6.4 C[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215391 81054 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 510 6 1 2 6.4 C[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
22310876 116924 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 396 4 1 4 3.7 CS(=O)(=O)NC(=O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL338495 116924 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 396 4 1 4 3.7 CS(=O)(=O)NC(=O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
71519381 86373 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313765 86373 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
49763804 65425 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 528 7 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(N4CCCC4)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829616 65425 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 528 7 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(N4CCCC4)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
44571258 183251 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 544 8 3 4 4.5 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL479643 183251 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 544 8 3 4 4.5 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2008.12.062
44439163 90294 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL238518 90294 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44353447 3775 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
785 3775 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
CHEMBL337246 3775 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
44453234 97471 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 489 7 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL270182 97471 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 489 7 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1 10.1016/j.bmcl.2008.02.015
127025462 137362 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 404 4 1 2 5.9 CC(C)(C)OC[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753005 137362 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 404 4 1 2 5.9 CC(C)(C)OC[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
86767119 129402 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 439 3 1 5 2.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)C12CCOC1CC(NC1CCOCC1)C2 nan
CHEMBL3671252 129402 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 439 3 1 5 2.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)C12CCOC1CC(NC1CCOCC1)C2 nan
76314242 105253 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 544 5 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115268 105253 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 544 5 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44439163 90294 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238518 90294 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
46240482 83577 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1 10.1021/ml300260s
CHEMBL2204259 83577 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1 10.1021/ml300260s
44447786 95114 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 584 7 2 3 7.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(C(=O)O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL255511 95114 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 584 7 2 3 7.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(C(=O)O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
71768721 111119 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 439 3 1 5 2.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCO[C@@H]1C[C@@H](NC1CCOCC1)C2 10.1016/j.bmcl.2014.03.036
CHEMBL3263279 111119 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 439 3 1 5 2.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCO[C@@H]1C[C@@H](NC1CCOCC1)C2 10.1016/j.bmcl.2014.03.036
122178127 121220 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 541 12 4 4 4.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CCc2ccccc2)c(C)c1 10.1021/ml500505q
CHEMBL3577928 121220 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 541 12 4 4 4.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CCc2ccccc2)c(C)c1 10.1021/ml500505q
72946202 105240 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 496 5 1 6 2.5 CCN1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115114 105240 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 496 5 1 6 2.5 CCN1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
54755083 65744 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 488 6 3 6 3.1 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](n3ccccc3=O)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834636 65744 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 488 6 3 6 3.1 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](n3ccccc3=O)CC2)C1 10.1016/j.bmcl.2011.08.074
44425636 85948 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 590 6 1 2 8.0 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230078 85948 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 590 6 1 2 8.0 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44573412 187427 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 478 6 2 2 6.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCC2)C1 10.1007/s00044-010-9501-4
CHEMBL493780 187427 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 478 6 2 2 6.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCC2)C1 10.1007/s00044-010-9501-4
44453565 169007 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2Cl)C1 10.1016/j.bmcl.2008.02.015
CHEMBL439252 169007 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2Cl)C1 10.1016/j.bmcl.2008.02.015
10138789 166509 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 450 9 4 4 1.8 Cc1ccc(CNC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL427875 166509 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 450 9 4 4 1.8 Cc1ccc(CNC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
44573535 187438 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 528 6 2 4 4.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCS(=O)(=O)CC2)C1 10.1007/s00044-010-9501-4
CHEMBL493843 187438 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 528 6 2 4 4.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCS(=O)(=O)CC2)C1 10.1007/s00044-010-9501-4
44573535 187438 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 528 6 2 4 4.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCS(=O)(=O)CC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL493843 187438 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 528 6 2 4 4.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCS(=O)(=O)CC2)C1 10.1016/j.bmcl.2008.12.050
11563597 91953 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 632 13 1 4 8.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL241462 91953 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 632 13 1 4 8.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
11563597 91953 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 632 13 1 4 8.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241462 91953 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 632 13 1 4 8.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
57344315 68941 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 530 8 2 5 3.9 COc1ccc(C2CCC(NC(C(N)=O)C3CCN(C(=O)/C=C/c4cc(F)c(F)c(F)c4)CC3)CC2)cn1 nan
CHEMBL1922799 68941 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 530 8 2 5 3.9 COc1ccc(C2CCC(NC(C(N)=O)C3CCN(C(=O)/C=C/c4cc(F)c(F)c(F)c4)CC3)CC2)cn1 nan
72947595 105221 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 511 4 2 6 1.5 COC1COCCC1N[C@@H]1C[C@H]2CN(C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115096 105221 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 511 4 2 6 1.5 COC1COCCC1N[C@@H]1C[C@H]2CN(C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57656713 75205 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 488 7 1 3 5.5 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036756 75205 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 488 7 1 3 5.5 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
11711078 75220 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 400 4 1 4 2.9 CCN1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036773 75220 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 400 4 1 4 2.9 CCN1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
10183362 73705 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 465 10 4 4 3.1 CC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018369 73705 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 465 10 4 4 3.1 CC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
10392559 155039 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccnnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL401609 155039 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccnnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
44425637 85987 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230405 85987 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44573412 187427 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 478 6 2 2 6.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL493780 187427 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 478 6 2 2 6.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCC2)C1 10.1016/j.bmcl.2008.12.050
24801523 97855 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 493 7 3 4 4.0 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL272168 97855 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 493 7 3 4 4.0 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
22310972 116778 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 395 4 1 2 6.4 O=C(O)c1cc2c(-c3ccccc3)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL337720 116778 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 395 4 1 2 6.4 O=C(O)c1cc2c(-c3ccccc3)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44395092 127287 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 522 8 4 7 2.9 Cc1csc(C(=O)NNC(=O)CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)c1 10.1016/j.bmcl.2004.08.008
CHEMBL365853 127287 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 522 8 4 7 2.9 Cc1csc(C(=O)NNC(=O)CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)c1 10.1016/j.bmcl.2004.08.008
10208555 73712 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 527 11 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)Cc2ccccc2)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018376 73712 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 527 11 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)Cc2ccccc2)c(C)c1 10.1016/j.bmcl.2012.03.007
10208555 73712 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 527 11 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)Cc2ccccc2)c(C)c1 10.1021/ml500505q
CHEMBL2018376 73712 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 527 11 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)Cc2ccccc2)c(C)c1 10.1021/ml500505q
44395201 66421 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 413 8 2 3 3.5 O=C(CCNC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
CHEMBL185190 66421 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 413 8 2 3 3.5 O=C(CCNC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
57344313 130657 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 503 7 3 4 4.1 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
CHEMBL3681902 130657 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 503 7 3 4 4.1 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
44415927 80855 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 512 9 1 2 6.8 C=CC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215271 80855 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 512 9 1 2 6.8 C=CC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44453473 155539 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 464 6 3 4 2.8 Nc1ccc(Br)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404260 155539 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 464 6 3 4 2.8 Nc1ccc(Br)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
25008678 94152 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(C[C@H]3CC[C@@H](NC(=O)/C=C/c4cc(Cl)cc(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249414 94152 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(C[C@H]3CC[C@@H](NC(=O)/C=C/c4cc(Cl)cc(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11570431 91982 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL241502 91982 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44439173 90707 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 650 13 1 4 8.8 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.10.060
CHEMBL239145 90707 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 650 13 1 4 8.8 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.10.060
52947417 19308 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN(C2CCN(c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
CHEMBL1290522 19308 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN(C2CCN(c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
72946199 105233 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 610 6 1 8 3.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115107 105233 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 610 6 1 8 3.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
10206007 73708 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 10 4 4 3.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)C(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018372 73708 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 10 4 4 3.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)C(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
11237168 74531 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 489 6 3 4 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccccc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029409 74531 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 489 6 3 4 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccccc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
10302973 93552 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 556 10 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246415 93552 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 556 10 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442589 93771 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 607 11 5 6 4.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247439 93771 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 607 11 5 6 4.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44423281 142115 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 498 5 1 2 6.4 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C1CCC(N2CCC(c3ccccc3)CC2)C1 10.1021/jm070166b
CHEMBL388308 142115 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 498 5 1 2 6.4 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C1CCC(N2CCC(c3ccccc3)CC2)C1 10.1021/jm070166b
44425641 86066 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230832 86066 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
86698129 126304 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 0 6 3.6 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650352 126304 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 0 6 3.6 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
46240481 83586 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 477 6 3 6 1.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncnc3)CC2)C1 10.1021/ml300260s
CHEMBL2204269 83586 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 477 6 3 6 1.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncnc3)CC2)C1 10.1021/ml300260s
56668313 65791 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 535 8 2 7 4.5 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C4CCCC4)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834784 65791 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 535 8 2 7 4.5 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C4CCCC4)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
44353370 23766 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 330 4 1 4 3.9 O=C(O)c1cc2cc(Cl)ccc2n1Cc1cccc([N+](=O)[O-])c1 10.1016/j.bmcl.2003.10.049
CHEMBL133569 23766 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 330 4 1 4 3.9 O=C(O)c1cc2cc(Cl)ccc2n1Cc1cccc([N+](=O)[O-])c1 10.1016/j.bmcl.2003.10.049
11678573 90639 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 566 13 1 5 7.4 CCN(CC)CCCC(C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238936 90639 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 566 13 1 5 7.4 CCN(CC)CCCC(C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
53324141 58467 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.3 CCO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683070 58467 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.3 CCO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
11340816 74535 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 491 6 3 6 2.2 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ncccn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029413 74535 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 491 6 3 6 2.2 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ncccn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
10182382 93962 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 450 9 4 4 1.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248418 93962 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 450 9 4 4 1.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
11678573 90639 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 566 13 1 5 7.4 CCN(CC)CCCC(C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL238936 90639 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 566 13 1 5 7.4 CCN(CC)CCCC(C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44395055 64504 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 6 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL181432 64504 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 6 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
44415995 80052 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 621 7 1 3 6.7 CC(=O)N1CCCC(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2006.07.011
CHEMBL212972 80052 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 621 7 1 3 6.7 CC(=O)N1CCCC(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2006.07.011
23656260 89072 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 501 7 2 4 4.8 COc1ccc(/C=C/C(=O)N2CCC(C(C(=O)O)N3CCC(c4c[nH]c5ccccc45)CC3)CC2)cc1 10.1021/jm070902b
CHEMBL236509 89072 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 501 7 2 4 4.8 COc1ccc(/C=C/C(=O)N2CCC(C(C(=O)O)N3CCC(c4c[nH]c5ccccc45)CC3)CC2)cc1 10.1021/jm070902b
46842382 8343 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092920 8343 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
508744 66215 1 None - 0 Human 4.2 pIC50 = 4.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 385 7 2 3 2.9 O=C(CNC(=O)c1ccccc1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL184474 66215 1 None - 0 Human 4.2 pIC50 = 4.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 385 7 2 3 2.9 O=C(CNC(=O)c1ccccc1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
127025160 137425 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 429 3 1 3 4.6 C[C@H]1CC=C(C(=O)NS(=O)(=O)C(F)(F)F)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753428 137425 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 429 3 1 3 4.6 C[C@H]1CC=C(C(=O)NS(=O)(=O)C(F)(F)F)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
57344316 68934 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 554 7 4 4 5.0 O=C(NO)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922792 68934 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 554 7 4 4 5.0 O=C(NO)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
57344230 130642 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 491 6 4 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(F)cc2)CC1 nan
CHEMBL3681888 130642 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 491 6 4 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(F)cc2)CC1 nan
11080 29085 79 None -1 6 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL1381098 29085 79 None -1 6 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
9851741 80193 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 604 7 1 2 8.0 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL213601 80193 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 604 7 1 2 8.0 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
44425654 86230 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231247 86230 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
53321484 58477 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 510 7 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC2CC2)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683080 58477 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 510 7 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC2CC2)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
44442580 93547 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 537 10 4 6 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.07.028
CHEMBL246409 93547 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 537 10 4 6 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.07.028
44413310 138959 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 475 10 2 3 5.0 CCN(CC)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL378517 138959 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 475 10 2 3 5.0 CCN(CC)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
72948004 105258 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 578 5 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/C(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115273 105258 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 578 5 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/C(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57656719 75216 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 410 4 1 3 3.7 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036767 75216 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 410 4 1 3 3.7 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
54580189 62569 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 505 6 1 8 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nc(C(F)(F)F)ns3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782575 62569 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 505 6 1 8 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nc(C(F)(F)F)ns3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
23656433 88763 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 6.1 O=C(O)C(C1CCN(C(=O)Nc2cccc(Cl)c2Cl)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL236269 88763 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 6.1 O=C(O)C(C1CCN(C(=O)Nc2cccc(Cl)c2Cl)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
72945830 105227 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 526 4 1 7 2.2 COC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115101 105227 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 526 4 1 7 2.2 COC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
67220645 75230 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 399 2 2 4 1.6 CN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036783 75230 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 399 2 2 4 1.6 CN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
127027955 137253 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 278 2 1 1 4.3 Cc1cc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)ccc1Cl 10.1016/j.bmcl.2015.11.051
CHEMBL3751958 137253 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 278 2 1 1 4.3 Cc1cc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)ccc1Cl 10.1016/j.bmcl.2015.11.051
44415898 81121 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL215654 81121 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
11478362 73807 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 547 11 4 4 5.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018532 73807 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 547 11 4 4 5.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
44453592 160055 24 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 405 6 2 3 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL410829 160055 24 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 405 6 2 3 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2)C1 10.1016/j.bmcl.2008.02.015
44442582 93549 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 536 10 4 5 3.3 COc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1C 10.1016/j.bmcl.2007.07.028
CHEMBL246411 93549 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 536 10 4 5 3.3 COc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1C 10.1016/j.bmcl.2007.07.028
9952114 124384 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 385 6 2 3 2.8 Cc1cccc(C(=O)NCC(=O)NC2CCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL363908 124384 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 385 6 2 3 2.8 Cc1cccc(C(=O)NCC(=O)NC2CCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
71518408 86403 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 449 3 1 3 5.2 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCCCC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314058 86403 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 449 3 1 3 5.2 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCCCC1)C2 10.1016/j.bmcl.2012.10.069
54772206 86590 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 514 7 2 7 4.0 COc1cnccc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
CHEMBL2315930 86590 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 514 7 2 7 4.0 COc1cnccc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
54772204 86592 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 500 6 3 7 3.7 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc(O)cn3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315932 86592 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 500 6 3 7 3.7 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc(O)cn3)CC2)C1 10.1016/j.bmcl.2012.12.017
54772205 86595 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 6 4.3 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3O)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315935 86595 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 6 4.3 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3O)CC2)C1 10.1016/j.bmcl.2012.12.017
72663455 129401 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671251 129401 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
11599317 95560 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 555 7 2 4 6.0 COc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL257628 95560 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 555 7 2 4 6.0 COc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
53324304 58464 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 497 6 1 5 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683067 58464 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 497 6 1 5 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
10228435 73717 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.1 CCC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018381 73717 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.1 CCC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
46927117 65428 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 490 7 2 5 3.4 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1016/j.bmcl.2011.06.080
CHEMBL1829619 65428 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 490 7 2 5 3.4 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1016/j.bmcl.2011.06.080
56661451 65798 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 500 6 2 6 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834791 65798 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 500 6 2 6 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44573699 187674 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 6 2 3 5.8 CC1COCC(C)C1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL495151 187674 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 6 2 3 5.8 CC1COCC(C)C1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
11306757 73737 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 508 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018401 73737 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 508 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
57391765 71015 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnn3)CC2)C1 10.1021/ml200030q
CHEMBL1951774 71015 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnn3)CC2)C1 10.1021/ml200030q
44425244 151804 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 594 7 2 5 6.6 Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL396517 151804 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 594 7 2 5 6.6 Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
23630215 62544 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782376 62544 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
10120067 73729 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 550 12 5 5 4.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018393 73729 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 550 12 5 5 4.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)(C)C 10.1016/j.bmcl.2012.03.007
52943756 19290 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
CHEMBL1290412 19290 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
44425274 150858 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 640 10 2 5 7.4 CC(C)C(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL395721 150858 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 640 10 2 5 7.4 CC(C)C(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
24801690 98041 25 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
CHEMBL273083 98041 25 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
44425647 86101 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231039 86101 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44423282 85274 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 522 4 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H]1CC[C@@H](N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm070166b
CHEMBL226017 85274 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 522 4 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H]1CC[C@@H](N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm070166b
162648673 179950 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 522 6 3 7 3.4 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(OC(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4746510 179950 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 522 6 3 7 3.4 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(OC(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
44425633 86041 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230721 86041 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44570718 183833 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 533 9 4 5 3.2 CC(=O)Nc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480621 183833 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 533 9 4 5 3.2 CC(=O)Nc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
11621035 154668 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 559 6 2 3 5.8 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3cc(Cl)ccc23)CC1 10.1021/jm070902b
CHEMBL399616 154668 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 559 6 2 3 5.8 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3cc(Cl)ccc23)CC1 10.1021/jm070902b
10052388 187552 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 520 7 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C2CC2)C1 10.1007/s00044-010-9501-4
CHEMBL494541 187552 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 520 7 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C2CC2)C1 10.1007/s00044-010-9501-4
57391768 71013 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncn3)CC2)C1 10.1021/ml200030q
CHEMBL1951772 71013 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncn3)CC2)C1 10.1021/ml200030q
44573608 187551 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 522 8 2 3 6.3 CCCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494540 187551 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 522 8 2 3 6.3 CCCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
11180383 77623 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 550 8 2 5 4.6 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088211 77623 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 550 8 2 5 4.6 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
22143294 193426 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 551 11 4 6 3.9 CCCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL526091 193426 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 551 11 4 6 3.9 CCCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
49763686 65424 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 7 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(C(=O)O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829615 65424 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 7 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(C(=O)O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
508750 168535 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 467 7 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
CHEMBL435499 168535 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 467 7 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
127028586 137507 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 264 2 1 1 4.0 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)cc2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3754119 137507 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 264 2 1 1 4.0 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)cc2)C1 10.1016/j.bmcl.2015.11.051
11844468 139596 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.3 C[C@@H]1CN(CC[C@H](CNCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@H]1c1ccccc1 10.1021/jm060439n
CHEMBL379742 139596 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.3 C[C@@H]1CN(CC[C@H](CNCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@H]1c1ccccc1 10.1021/jm060439n
44395088 67171 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 514 8 1 5 4.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL187701 67171 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 514 8 1 5 4.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
10209102 93538 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 540 11 4 4 3.6 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCc2ccccc2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246398 93538 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 540 11 4 4 3.6 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCc2ccccc2)c(C)c1 10.1016/j.bmcl.2007.07.028
57344320 130643 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 527 6 4 3 5.0 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681889 130643 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 527 6 4 3 5.0 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cc(F)c(F)c(F)c2)CC1 nan
72948001 105222 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 525 4 2 6 1.8 CNC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115097 105222 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 525 4 2 6 1.8 CNC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
46241611 83565 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 506 7 3 6 2.5 COc1cccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)n1 10.1021/ml300260s
CHEMBL2204247 83565 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 506 7 3 6 2.5 COc1cccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)n1 10.1021/ml300260s
57344232 130644 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 519 7 4 4 5.3 CSc1cccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)c1 nan
CHEMBL3681890 130644 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 519 7 4 4 5.3 CSc1cccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)c1 nan
44395126 65413 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 494 8 2 6 3.6 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL182958 65413 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 494 8 2 6 3.6 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44395126 65413 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 494 8 2 6 3.6 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL182958 65413 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 494 8 2 6 3.6 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.009
57656915 75219 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 342 4 1 3 2.7 O=C(Nc1ccccc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036772 75219 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 342 4 1 3 2.7 O=C(Nc1ccccc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
11341950 73806 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 557 11 4 4 4.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(Br)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018531 73806 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 557 11 4 4 4.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(Br)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
42632836 93386 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2cc(Cl)cc(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL245696 93386 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2cc(Cl)cc(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
68004094 86601 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 505 6 3 7 3.8 O=C(CNc1ccnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315941 86601 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 505 6 3 7 3.8 O=C(CNc1ccnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
57396900 70522 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 399 6 2 3 3.2 CC(C)N(C)[C@H]1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2011.12.057
CHEMBL1947040 70522 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 399 6 2 3 3.2 CC(C)N(C)[C@H]1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2011.12.057
44416041 80432 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL214647 80432 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
44416015 81133 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215689 81133 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44413144 139219 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.011
CHEMBL378784 139219 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.011
44413144 139219 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL378784 139219 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1021/jm060439n
23656434 89618 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 6.1 O=C(O)C(C1CCN(C(=O)Nc2cc(Cl)cc(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237538 89618 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 6.1 O=C(O)C(C1CCN(C(=O)Nc2cc(Cl)cc(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
44442569 93735 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 556 10 4 6 2.0 CC(C)(C)NC(=O)[C@H](CNCc1ccc(S(C)(=O)=O)cc1)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247213 93735 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 556 10 4 6 2.0 CC(C)(C)NC(=O)[C@H](CNCc1ccc(S(C)(=O)=O)cc1)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
44415958 80499 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 578 7 1 2 8.0 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CCCCC1 10.1016/j.bmcl.2006.07.011
CHEMBL214747 80499 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 578 7 1 2 8.0 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CCCCC1 10.1016/j.bmcl.2006.07.011
11563451 151918 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL396621 151918 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44453533 97880 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 420 6 3 4 2.7 Nc1ccc(Cl)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272330 97880 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 420 6 3 4 2.7 Nc1ccc(Cl)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
10008367 2022 50 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of rat CCR2Inhibition of rat CCR2
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
777 2022 50 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of rat CCR2Inhibition of rat CCR2
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL1289316 2022 50 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of rat CCR2Inhibition of rat CCR2
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL2426341 2022 50 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of rat CCR2Inhibition of rat CCR2
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
11563451 151918 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL396621 151918 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44425321 86136 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 740 10 2 5 9.0 CC(C(=O)Nc1nc(C(CCN2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)c1ccccc1 10.1016/j.bmcl.2006.10.059
CHEMBL231150 86136 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 740 10 2 5 9.0 CC(C(=O)Nc1nc(C(CCN2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)c1ccccc1 10.1016/j.bmcl.2006.10.059
44425651 143177 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 530 6 1 3 6.0 COCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL389610 143177 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 530 6 1 3 6.0 COCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
56643545 130624 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681871 130624 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
10025168 66986 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 420 5 2 5 2.7 Cc1csc(C(=O)NNC(=O)CN2CCCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2004.08.008
CHEMBL186855 66986 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 420 5 2 5 2.7 Cc1csc(C(=O)NNC(=O)CN2CCCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2004.08.008
10025168 66986 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 420 5 2 5 2.7 Cc1csc(C(=O)NNC(=O)CN2CCCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL186855 66986 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 420 5 2 5 2.7 Cc1csc(C(=O)NNC(=O)CN2CCCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2004.08.009
44395036 125052 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 7 2 3 3.2 O=C(CCNC(=O)c1ccccc1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL364405 125052 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 7 2 3 3.2 O=C(CCNC(=O)c1ccccc1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
127027625 137254 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 366 2 1 1 5.4 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3751959 137254 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 366 2 1 1 5.4 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
22143293 188027 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497577 188027 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
57343816 130627 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 552 7 3 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL3681874 130627 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 552 7 3 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cccc(C(F)(F)F)c2)CC1 nan
53320974 58692 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 464 4 1 4 2.8 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)N2CCCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684715 58692 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 464 4 1 4 2.8 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)N2CCCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
57344314 68930 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 553 7 2 4 5.7 COC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922788 68930 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 553 7 2 4 5.7 COC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
44442564 93540 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 9 4 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
CHEMBL246400 93540 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 9 4 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
46842236 7867 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 598 8 2 4 4.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089849 7867 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 598 8 2 4 4.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2010.02.072
44413411 77738 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 501 8 2 3 5.4 CC1CCN(CCN[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1 10.1016/j.bmcl.2006.04.045
CHEMBL209002 77738 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 501 8 2 3 5.4 CC1CCN(CCN[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1 10.1016/j.bmcl.2006.04.045
44453507 168978 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 531 7 2 3 5.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2-c2ccc3ccccc3c2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL439062 168978 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 531 7 2 3 5.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2-c2ccc3ccccc3c2)C1 10.1016/j.bmcl.2008.02.015
69286108 121233 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 505 9 2 4 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](COc2ccccc2)C1 10.1021/ml500505q
CHEMBL3577941 121233 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 505 9 2 4 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](COc2ccccc2)C1 10.1021/ml500505q
71518574 86391 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313784 86391 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
89823496 126315 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 3.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2)C1 nan
CHEMBL3650363 126315 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 3.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2)C1 nan
89823439 126299 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650347 126299 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
44573568 187470 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 512 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc32)C1 10.1007/s00044-010-9501-4
CHEMBL494019 187470 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 512 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc32)C1 10.1007/s00044-010-9501-4
44439164 90773 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 610 13 4 7 5.1 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239169 90773 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 610 13 4 7 5.1 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44439164 90773 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 610 13 4 7 5.1 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL239169 90773 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 610 13 4 7 5.1 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44573650 193210 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 564 6 3 4 5.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(O)C(F)(F)F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL523503 193210 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 564 6 3 4 5.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(O)C(F)(F)F)C1 10.1016/j.bmcl.2008.12.050
10323468 187672 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 6 2 3 5.7 CC1CC(N[C@@H]2CC[C@@](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C(C)C)C2)CCO1 10.1007/s00044-010-9501-4
CHEMBL495149 187672 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 6 2 3 5.7 CC1CC(N[C@@H]2CC[C@@](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C(C)C)C2)CCO1 10.1007/s00044-010-9501-4
72948001 105222 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 525 4 2 6 1.8 CNC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115097 105222 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 525 4 2 6 1.8 CNC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44573568 187470 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 512 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494019 187470 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 512 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.bmcl.2008.12.050
72947593 105238 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 468 4 2 6 1.7 COC1COCCC1N[C@@H]1C[C@H]2CNC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115112 105238 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 468 4 2 6 1.7 COC1COCCC1N[C@@H]1C[C@H]2CNC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44413144 139219 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2006.04.045
CHEMBL378784 139219 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2006.04.045
44442544 93766 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 10 4 4 3.6 Cc1ccc(CNCC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247407 93766 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 10 4 4 3.6 Cc1ccc(CNCC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44353190 116566 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1c(C(=O)O)n(Cc2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2003.10.049
CHEMBL336421 116566 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1c(C(=O)O)n(Cc2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2003.10.049
46240785 83582 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 510 7 3 6 3.1 CCc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204264 83582 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 510 7 3 6 3.1 CCc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
72947593 105238 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 468 4 2 6 1.7 COC1COCCC1N[C@@H]1C[C@H]2CNC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115112 105238 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 468 4 2 6 1.7 COC1COCCC1N[C@@H]1C[C@H]2CNC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
70692344 75198 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 370 3 2 3 3.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(CC2CCCNC2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036749 75198 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 370 3 2 3 3.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(CC2CCCNC2)CC1 10.1016/j.bmcl.2012.04.118
11844083 77993 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 581 8 1 3 6.9 CC1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CCN1c1ccccc1 10.1021/jm060439n
CHEMBL209696 77993 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 581 8 1 3 6.9 CC1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CCN1c1ccccc1 10.1021/jm060439n
44395238 123845 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 406 6 3 5 2.3 Cc1csc(C(=O)NNC(=O)CN2CCC(NCc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL362536 123845 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 406 6 3 5 2.3 Cc1csc(C(=O)NNC(=O)CN2CCC(NCc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
42632830 93385 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)cc2Cl)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL245694 93385 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)cc2Cl)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
44416156 81152 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 657 8 1 4 6.1 CS(=O)(=O)N1CCCC(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2006.07.011
CHEMBL215768 81152 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 657 8 1 4 6.1 CS(=O)(=O)N1CCCC(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2006.07.011
24801345 97854 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 475 6 3 3 3.9 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL272167 97854 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 475 6 3 3 3.9 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
44453171 95737 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 449 6 2 3 3.2 O=C(CNC(=O)c1cccc(Br)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL258364 95737 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 449 6 2 3 3.2 O=C(CNC(=O)c1cccc(Br)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
10300705 97898 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 501 7 3 3 5.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@@H]1NCc1ccc(Cl)cc1Cl 10.1021/jm701488f
CHEMBL272407 97898 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 501 7 3 3 5.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@@H]1NCc1ccc(Cl)cc1Cl 10.1021/jm701488f
53325639 58470 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683073 58470 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
57402059 70342 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944780 70342 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44425319 86335 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 727 10 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccn3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL231340 86335 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 727 10 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccn3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
46241011 83575 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 483 6 3 7 1.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nncs3)CC2)C1 10.1021/ml300260s
CHEMBL2204257 83575 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 483 6 3 7 1.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nncs3)CC2)C1 10.1021/ml300260s
44444114 94209 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 460 6 1 2 5.4 O=C(/C=C/c1cc(F)cc(F)c1)NC1CCC(CN2CCC(c3ccc(F)c(F)c3)CC2)C1 10.1016/j.bmcl.2007.07.065
CHEMBL249811 94209 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 460 6 1 2 5.4 O=C(/C=C/c1cc(F)cc(F)c1)NC1CCC(CN2CCC(c3ccc(F)c(F)c3)CC2)C1 10.1016/j.bmcl.2007.07.065
24801180 98040 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
CHEMBL273079 98040 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
122181145 121833 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 528 6 1 3 6.1 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589840 121833 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 528 6 1 3 6.1 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)O1 10.1016/j.bmc.2015.02.019
44395232 66998 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 508 9 1 6 3.9 COc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.008
CHEMBL186913 66998 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 508 9 1 6 3.9 COc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.008
71518727 86407 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 451 3 1 4 4.1 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCCC[C@@H]1C[C@@H](NC1CCOCC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314064 86407 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 451 3 1 4 4.1 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCCC[C@@H]1C[C@@H](NC1CCOCC1)C2 10.1016/j.bmcl.2012.10.069
57656808 75223 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 399 4 2 4 2.4 CCN1CCNC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036776 75223 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 399 4 2 4 2.4 CCN1CCNC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
54768838 86597 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 520 6 3 8 3.5 Cc1nc(NCC(=O)NC2CN([C@H]3CC[C@@](O)(c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc2n1 10.1016/j.bmcl.2012.12.017
CHEMBL2315937 86597 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 520 6 3 8 3.5 Cc1nc(NCC(=O)NC2CN([C@H]3CC[C@@](O)(c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc2n1 10.1016/j.bmcl.2012.12.017
57344295 130625 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3681872 130625 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
57344303 130648 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681894 130648 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
44425635 153532 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL398000 153532 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44413076 140148 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 475 9 1 3 5.0 CN(C)CCCN(C)[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL380258 140148 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 475 9 1 3 5.0 CN(C)CCCN(C)[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
44425652 168768 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL437359 168768 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
10312346 188462 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 614 9 3 6 4.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502795 188462 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 614 9 3 6 4.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N(C)C)cc1 10.1016/j.bmcl.2009.05.041
50991056 62566 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782572 62566 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
10218843 172786 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 633 11 3 6 5.1 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NCc3ccccc3)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL451340 172786 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 633 11 3 6 5.1 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NCc3ccccc3)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44425651 143177 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 530 6 1 3 6.0 COCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL389610 143177 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 530 6 1 3 6.0 COCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
53319664 58677 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 461 6 1 5 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684700 58677 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 461 6 1 5 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
53322810 58472 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683075 58472 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44593561 12663 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL1187238 12663 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494580 12663 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
71768689 111111 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxisAntagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxis
ChEMBL 469 4 1 6 2.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263269 111111 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxisAntagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxis
ChEMBL 469 4 1 6 2.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
22143346 172651 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 634 11 4 6 4.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL449672 172651 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 634 11 4 6 4.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)C1 10.1016/j.bmcl.2008.07.123
54580188 62567 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ncc(C(F)(F)F)s3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782573 62567 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ncc(C(F)(F)F)s3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
11606702 145754 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 580 14 1 5 7.8 CCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL391662 145754 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 580 14 1 5 7.8 CCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44449175 95506 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 552 7 2 3 5.2 CC(=O)NCC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL257351 95506 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 552 7 2 3 5.2 CC(=O)NCC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
49763685 65423 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 517 7 2 5 3.7 COC(=O)c1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
CHEMBL1829614 65423 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 517 7 2 5 3.7 COC(=O)c1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
44612590 137470 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753813 137470 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
44415899 80074 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL213058 80074 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
11844212 98649 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 590 7 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.011
CHEMBL277279 98649 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 590 7 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.011
44415995 80052 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 621 7 1 3 6.7 CC(=O)N1CCCC(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2006.07.011
CHEMBL212972 80052 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 621 7 1 3 6.7 CC(=O)N1CCCC(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2006.07.011
25007995 154871 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 7 1 3 5.3 COc1ccc(C2CCN(C[C@@H]3CC[C@H](NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL400680 154871 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 7 1 3 5.3 COc1ccc(C2CCN(C[C@@H]3CC[C@H](NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11844212 98649 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 590 7 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL277279 98649 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 590 7 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm060439n
11662833 89188 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 471 6 2 3 4.8 O=C(O)C(C1CCN(C(=O)/C=C/c2ccccc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL236721 89188 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 471 6 2 3 4.8 O=C(O)C(C1CCN(C(=O)/C=C/c2ccccc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
122181235 121850 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 572 7 1 3 6.7 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589949 121850 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 572 7 1 3 6.7 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
44416125 80921 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 569 7 2 4 5.5 COC(=O)NC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215333 80921 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 569 7 2 4 5.5 COC(=O)NC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
57344300 130645 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 509 6 4 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(F)c(F)c2)CC1 nan
CHEMBL3681891 130645 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 509 6 4 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(F)c(F)c2)CC1 nan
71517577 86370 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 1 6 2.9 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](N(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313762 86370 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 1 6 2.9 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](N(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
76314234 105223 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 553 5 2 6 2.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115098 105223 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 553 5 2 6 2.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44425318 150311 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 732 10 2 6 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3cccs3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL395289 150311 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 732 10 2 6 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3cccs3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
90656021 111116 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 511 5 1 8 1.6 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CC3CC2CN3c2nccc(C(F)(F)F)n2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263274 111116 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 511 5 1 8 1.6 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CC3CC2CN3c2nccc(C(F)(F)F)n2)C1 10.1016/j.bmcl.2014.03.036
89823460 126339 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)cc(C(F)(F)F)c2)C1 nan
CHEMBL3650387 126339 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)cc(C(F)(F)F)c2)C1 nan
72946200 105232 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 570 7 1 8 2.2 COCCOC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115106 105232 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 570 7 1 8 2.2 COCCOC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
56668309 65776 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 558 6 3 8 3.6 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834718 65776 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 558 6 3 8 3.6 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
127028591 137454 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 244 2 1 1 3.8 Cc1ccc([C@]2(C)CCCC=C2C(=O)O)cc1C 10.1016/j.bmcl.2015.11.051
CHEMBL3753683 137454 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 244 2 1 1 3.8 Cc1ccc([C@]2(C)CCCC=C2C(=O)O)cc1C 10.1016/j.bmcl.2015.11.051
89823691 126318 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 526 5 1 6 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)c2F)C1 nan
CHEMBL3650366 126318 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 526 5 1 6 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)c2F)C1 nan
11843812 79904 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL212423 79904 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
57344307 130651 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccncc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681897 130651 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccncc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
89823344 126350 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 589 5 0 5 5.2 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
CHEMBL3650397 126350 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 589 5 0 5 5.2 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
11843812 79904 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1021/jm060439n
CHEMBL212423 79904 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1021/jm060439n
89823453 126357 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 464 3 0 5 3.2 O=C(N1C[C@@H]2C[C@H]1CN2c1cc(C(F)(F)F)ccn1)[C@@]12CCC[C@@H]1C[C@@H](N1CCOCC1)C2 nan
CHEMBL3650403 126357 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 464 3 0 5 3.2 O=C(N1C[C@@H]2C[C@H]1CN2c1cc(C(F)(F)F)ccn1)[C@@]12CCC[C@@H]1C[C@@H](N1CCOCC1)C2 nan
508729 95535 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 416 7 2 5 2.4 O=C(CNC(=O)c1cccc([N+](=O)[O-])c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257510 95535 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 416 7 2 5 2.4 O=C(CNC(=O)c1cccc([N+](=O)[O-])c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
46884855 8303 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092656 8303 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2010.02.072
44413399 79529 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 501 8 2 3 5.5 CC1CCCCN1CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL211404 79529 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 501 8 2 3 5.5 CC1CCCCN1CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
70687886 74530 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 487 6 1 3 4.7 CN([C@H]1CC[C@@H](c2ccccc2)CC1)[C@H]1CCN(C(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1021/ml200199c
CHEMBL2029408 74530 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 487 6 1 3 4.7 CN([C@H]1CC[C@@H](c2ccccc2)CC1)[C@H]1CCN(C(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1021/ml200199c
44573451 187567 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 466 6 2 3 4.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOC2)C1 10.1007/s00044-010-9501-4
CHEMBL494591 187567 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 466 6 2 3 4.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOC2)C1 10.1007/s00044-010-9501-4
25008849 94180 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 7 1 3 5.3 COc1ccc(C2CCN(C[C@H]3CC[C@@H](NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249609 94180 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 7 1 3 5.3 COc1ccc(C2CCN(C[C@H]3CC[C@@H](NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
46945255 65436 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 5 2.9 Nc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1016/j.bmcl.2011.06.080
CHEMBL1829627 65436 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 5 2.9 Nc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1016/j.bmcl.2011.06.080
44573451 187567 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 466 6 2 3 4.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494591 187567 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 466 6 2 3 4.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOC2)C1 10.1016/j.bmcl.2008.12.050
11690139 75225 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 412 3 1 3 3.4 CCN1CCC[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036778 75225 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 412 3 1 3 3.4 CCN1CCC[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44415957 81054 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 510 6 1 2 6.4 C[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215391 81054 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 510 6 1 2 6.4 C[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
70683619 74528 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 473 6 2 3 4.4 O=C(NCC(=O)N1CC[C@@H](N[C@H]2CC[C@@H](c3ccccc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029406 74528 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 473 6 2 3 4.4 O=C(NCC(=O)N1CC[C@@H](N[C@H]2CC[C@@H](c3ccccc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
22310850 116807 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 395 4 1 2 6.4 O=C(O)c1cc2cc(-c3ccccc3)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL337857 116807 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 395 4 1 2 6.4 O=C(O)c1cc2cc(-c3ccccc3)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44413137 78892 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1cccs1 10.1016/j.bmcl.2006.04.045
CHEMBL211292 78892 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1cccs1 10.1016/j.bmcl.2006.04.045
72947191 105260 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 600 7 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)CCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115275 105260 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 600 7 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)CCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
67774197 130652 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 4 5.3 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3681898 130652 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 4 5.3 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
72946013 105259 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 560 4 1 6 2.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)C#CC3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115274 105259 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 560 4 1 6 2.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)C#CC3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
10207542 73719 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 506 9 5 5 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C2(O)CCCC2)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018383 73719 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 506 9 5 5 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C2(O)CCCC2)c(C)c1 10.1016/j.bmcl.2012.03.007
24801524 167328 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 525 7 3 5 2.7 CS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL429425 167328 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 525 7 3 5 2.7 CS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
22268768 154921 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 507 10 5 5 2.4 CCNC(=O)C(C)(CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2007.07.028
CHEMBL400968 154921 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 507 10 5 5 2.4 CCNC(=O)C(C)(CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2007.07.028
44395066 124463 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 398 8 1 3 4.5 O=C(CCCC(=O)c1ccccc1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL363994 124463 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 398 8 1 3 4.5 O=C(CCCC(=O)c1ccccc1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
71518570 86404 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 453 3 1 4 4.4 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCSCC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314059 86404 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 453 3 1 4 4.4 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCSCC1)C2 10.1016/j.bmcl.2012.10.069
72948004 105258 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 578 5 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/C(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115273 105258 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 578 5 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/C(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
71716742 86384 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 2 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313776 86384 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 2 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
44453471 97870 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 470 7 3 5 2.9 Nc1ccc(OC(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272283 97870 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 470 7 3 5 2.9 Nc1ccc(OC(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
10228205 93728 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 490 10 4 4 2.6 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247205 93728 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 490 10 4 4 2.6 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CC2)c(C)c1 10.1016/j.bmcl.2007.07.028
57344303 130648 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681894 130648 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
57402059 70342 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944780 70342 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
25268795 148507 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 421 6 1 2 4.7 C[N+](C)(Cc1ccc(CNC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL393835 148507 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 421 6 1 2 4.7 C[N+](C)(Cc1ccc(CNC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
86767120 129403 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 468 4 1 5 2.9 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671253 129403 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 468 4 1 5 2.9 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 nan
44449081 95513 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 535 6 2 3 5.4 O=C(/C=C/c1cccc(Br)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL257385 95513 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 535 6 2 3 5.4 O=C(/C=C/c1cccc(Br)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11634928 168891 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 514 5 3 3 6.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL438353 168891 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 514 5 3 3 6.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11606702 145754 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 580 14 1 5 7.8 CCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL391662 145754 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 580 14 1 5 7.8 CCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
56671794 65797 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 516 7 2 7 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834790 65797 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 516 7 2 7 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44595711 137321 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752627 137321 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
44416157 80595 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CC[C@H](CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL215020 80595 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CC[C@H](CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
44425630 86027 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230617 86027 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
11330529 74540 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cccnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029418 74540 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cccnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
24801689 97794 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 651 9 5 6 3.5 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)cc1 10.1021/jm701488f
CHEMBL271828 97794 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 651 9 5 6 3.5 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)cc1 10.1021/jm701488f
44425242 86043 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 588 8 2 5 6.6 Nc1nc(C(CCN2CCC(c3ccc(F)cc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230727 86043 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 588 8 2 5 6.6 Nc1nc(C(CCN2CCC(c3ccc(F)cc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
54583186 62572 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 496 6 1 5 4.3 CCC1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782578 62572 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 496 6 1 5 4.3 CCC1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
10232019 73730 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 584 14 5 5 5.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NCc1ccccc1 10.1016/j.bmcl.2012.03.007
CHEMBL2018394 73730 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 584 14 5 5 5.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NCc1ccccc1 10.1016/j.bmcl.2012.03.007
53322811 58474 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 484 6 1 6 3.1 CC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683077 58474 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 484 6 1 6 3.1 CC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
54586021 62543 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 494 4 0 5 4.1 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N2CCC3COCCC32)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782375 62543 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 494 4 0 5 4.1 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N2CCC3COCCC32)C1 10.1016/j.bmcl.2011.01.034
10008367 2022 50 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
777 2022 50 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL1289316 2022 50 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL2426341 2022 50 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
10281715 73723 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
CHEMBL2018387 73723 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
22143146 183906 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481202 183906 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
76314242 105253 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 544 5 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115268 105253 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 544 5 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
11633080 93632 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 417 5 1 1 6.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CC2CCC1C2 10.1016/j.bmcl.2007.01.115
CHEMBL246728 93632 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 417 5 1 1 6.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CC2CCC1C2 10.1016/j.bmcl.2007.01.115
44442591 93813 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 631 11 5 5 4.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247635 93813 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 631 11 5 5 4.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
22310914 24328 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2ccc(F)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL134072 24328 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2ccc(F)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
10459336 73814 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 520 10 4 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2N)C1=O 10.1016/j.bmcl.2012.03.007
CHEMBL2018540 73814 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 520 10 4 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2N)C1=O 10.1016/j.bmcl.2012.03.007
44442574 155128 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 517 9 4 5 2.8 Cc1cc(C#N)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL402055 155128 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 517 9 4 5 2.8 Cc1cc(C#N)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
11634118 58452 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 466 5 1 3 5.4 CC(C)[C@]1(C(=O)N2CCC(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683053 58452 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 466 5 1 3 5.4 CC(C)[C@]1(C(=O)N2CCC(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
89823507 126322 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(F)cc(C(F)(F)F)c2)C1 nan
CHEMBL3650370 126322 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(F)cc(C(F)(F)F)c2)C1 nan
56678506 65789 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 545 8 2 9 2.2 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(S(C)(=O)=O)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834782 65789 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 545 8 2 9 2.2 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(S(C)(=O)=O)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
57401421 67865 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assayDisplacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assay
ChEMBL 486 6 1 3 5.1 O=C(NCCCN1CCC(c2ccc(F)cc2)CC1)C1=Cc2cc(Br)ccc2OCC1 10.1016/j.bmcl.2011.09.013
CHEMBL1910161 67865 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assayDisplacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assay
ChEMBL 486 6 1 3 5.1 O=C(NCCCN1CCC(c2ccc(F)cc2)CC1)C1=Cc2cc(Br)ccc2OCC1 10.1016/j.bmcl.2011.09.013
127025445 137462 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 244 2 1 1 3.7 Cc1cccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1 10.1016/j.bmcl.2015.11.051
CHEMBL3753719 137462 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 244 2 1 1 3.7 Cc1cccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1 10.1016/j.bmcl.2015.11.051
72663455 129401 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671251 129401 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
44416274 158554 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL409162 158554 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
44425639 86065 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 580 6 1 3 6.8 COCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230831 86065 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 580 6 1 3 6.8 COCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
11843813 141901 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 8 1 2 7.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H](CCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL386865 141901 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 8 1 2 7.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H](CCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
44395079 66997 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 530 8 2 6 3.9 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cc(F)cc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL186899 66997 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 530 8 2 6 3.9 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cc(F)cc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44439157 91680 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 597 10 2 5 7.8 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccc2c(n1)NCCC2 10.1016/j.bmcl.2006.10.060
CHEMBL240853 91680 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 597 10 2 5 7.8 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccc2c(n1)NCCC2 10.1016/j.bmcl.2006.10.060
49863168 15206 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 583 9 2 5 7.4 O=C(CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccc2c(n1)NCCC2 10.1016/j.ejmech.2010.04.024
CHEMBL1210604 15206 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 583 9 2 5 7.4 O=C(CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccc2c(n1)NCCC2 10.1016/j.ejmech.2010.04.024
71519227 86377 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 503 4 1 5 3.6 COC1COCCC1N[C@@H]1C[C@H]2CC(F)(F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313769 86377 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 503 4 1 5 3.6 COC1COCCC1N[C@@H]1C[C@H]2CC(F)(F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
11318368 74532 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 520 7 3 6 2.9 COc1ccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200199c
CHEMBL2029410 74532 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 520 7 3 6 2.9 COc1ccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200199c
89823428 126327 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 514 5 1 7 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nc(C(F)(F)F)cs2)C1 nan
CHEMBL3650375 126327 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 514 5 1 7 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nc(C(F)(F)F)cs2)C1 nan
72945827 105228 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 588 5 1 7 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)Oc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115102 105228 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 588 5 1 7 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)Oc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57391487 130659 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 540 7 3 4 4.6 NC(=O)C(N[C@H]1CC[C@H](C2CNc3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681904 130659 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 540 7 3 4 4.6 NC(=O)C(N[C@H]1CC[C@H](C2CNc3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
44444100 94034 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 499 6 0 3 6.2 CN(C)c1ccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248812 94034 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 499 6 0 3 6.2 CN(C)c1ccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2007.07.065
44425316 142359 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 712 9 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL388869 142359 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 712 9 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
25268442 93950 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 369 6 1 3 3.7 COc1cccc(C(=O)Nc2ccc(C[N+](C)(C)C3CCOCC3)cc2)c1 10.1016/j.bmcl.2007.01.115
CHEMBL248358 93950 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 369 6 1 3 3.7 COc1cccc(C(=O)Nc2ccc(C[N+](C)(C)C3CCOCC3)cc2)c1 10.1016/j.bmcl.2007.01.115
508870 97476 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 488 6 3 4 3.7 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2Cl)C1 10.1016/j.bmcl.2008.02.015
CHEMBL270205 97476 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 488 6 3 4 3.7 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2Cl)C1 10.1016/j.bmcl.2008.02.015
22310992 23108 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 363 4 2 3 4.4 O=C(O)c1c(C(=O)O)n(Cc2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2003.10.049
CHEMBL133075 23108 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 363 4 2 3 4.4 O=C(O)c1c(C(=O)O)n(Cc2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2003.10.049
57344301 130646 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 540 7 3 4 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCCO3)CC1 nan
CHEMBL3681892 130646 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 540 7 3 4 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCCO3)CC1 nan
508742 95576 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 423 6 2 3 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257702 95576 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 423 6 2 3 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2008.02.015
44453538 97930 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 419 6 2 3 3.1 Cc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272543 97930 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 419 6 2 3 3.1 Cc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.02.015
72946008 105237 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 625 7 1 9 1.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115111 105237 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 625 7 1 9 1.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
10278862 93729 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 10 4 4 3.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247206 93729 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 10 4 4 3.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
22143200 187765 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 480 8 4 5 2.8 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL495718 187765 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 480 8 4 5 2.8 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.07.123
9956260 157683 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
CHEMBL408172 157683 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
127025444 137268 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 230 2 1 1 3.4 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccccc2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752110 137268 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 230 2 1 1 3.4 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccccc2)C1 10.1016/j.bmcl.2015.11.051
57656938 75215 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 410 4 1 3 3.7 O=C(Nc1cccc(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036766 75215 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 410 4 1 3 3.7 O=C(Nc1cccc(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
44415922 141683 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL385540 141683 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
57344318 68933 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 566 7 2 3 5.6 CN(C)C(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922791 68933 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 566 7 2 3 5.6 CN(C)C(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
57344317 68932 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 552 7 3 3 5.3 CNC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922790 68932 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 552 7 3 3 5.3 CNC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
72946010 105230 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 582 5 1 7 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115104 105230 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 582 5 1 7 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
11510932 75202 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 460 5 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(Cc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036753 75202 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 460 5 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(Cc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
46886061 7983 1 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 593 8 1 6 3.9 CC(C)N(C)[C@@H]1CC[C@H](N2C(=O)C[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1090562 7983 1 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 593 8 1 6 3.9 CC(C)N(C)[C@@H]1CC[C@H](N2C(=O)C[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
44442558 93730 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 518 10 4 4 3.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CCCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247207 93730 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 518 10 4 4 3.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CCCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
22310965 19592 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2c(F)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130008 19592 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2c(F)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
46885027 8421 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 531 8 2 5 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093469 8421 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 531 8 2 5 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
10343454 3983 29 None 34 2 Human 10.0 pKd = 10 Binding
Binding affinity to CCR2 (unknown origin) assessed as dissociation constantBinding affinity to CCR2 (unknown origin) assessed as dissociation constant
ChEMBL 444 5 1 4 4.3 Clc1ccc(c(c1)C(=O)c1cc[n+](cc1)[O-])NS(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.6b01309
9046 3983 29 None 34 2 Human 10.0 pKd = 10 Binding
Binding affinity to CCR2 (unknown origin) assessed as dissociation constantBinding affinity to CCR2 (unknown origin) assessed as dissociation constant
ChEMBL 444 5 1 4 4.3 Clc1ccc(c(c1)C(=O)c1cc[n+](cc1)[O-])NS(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.6b01309
CHEMBL2178578 3983 29 None 34 2 Human 10.0 pKd = 10 Binding
Binding affinity to CCR2 (unknown origin) assessed as dissociation constantBinding affinity to CCR2 (unknown origin) assessed as dissociation constant
ChEMBL 444 5 1 4 4.3 Clc1ccc(c(c1)C(=O)c1cc[n+](cc1)[O-])NS(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.6b01309
DB15250 3983 29 None 34 2 Human 10.0 pKd = 10 Binding
Binding affinity to CCR2 (unknown origin) assessed as dissociation constantBinding affinity to CCR2 (unknown origin) assessed as dissociation constant
ChEMBL 444 5 1 4 4.3 Clc1ccc(c(c1)C(=O)c1cc[n+](cc1)[O-])NS(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.6b01309
11180808 2549 52 None - 1 Human 9.3 pKd = 9.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F 10.1016/j.ejmech.2015.01.063
9048 2549 52 None - 1 Human 9.3 pKd = 9.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F 10.1016/j.ejmech.2015.01.063
CHEMBL3305901 2549 52 None - 1 Human 9.3 pKd = 9.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F 10.1016/j.ejmech.2015.01.063
155491018 174083 1 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 174083 1 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
53389902 172499 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.8 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)c(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4483373 172499 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.8 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)c(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155491018 174083 1 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 174083 1 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
53389902 172499 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.8 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)c(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4483373 172499 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.8 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)c(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
11180808 2549 52 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F 10.1016/j.ejmech.2015.01.063
9048 2549 52 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F 10.1016/j.ejmech.2015.01.063
CHEMBL3305901 2549 52 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F 10.1016/j.ejmech.2015.01.063
71717723 87829 0 None 51 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 525 7 2 7 4.3 CO[C@@H]1COCC[C@@H]1NC1CCN(C(=O)c2nc(CF)nc(Nc3ccc(Cl)c(Cl)c3)c2C)CC1 10.1021/ml400055e
CHEMBL2338392 87829 0 None 51 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 525 7 2 7 4.3 CO[C@@H]1COCC[C@@H]1NC1CCN(C(=O)c2nc(CF)nc(Nc3ccc(Cl)c(Cl)c3)c2C)CC1 10.1021/ml400055e
155554273 174213 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4548396 174213 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.9b00742
155554273 174213 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4548396 174213 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.9b00742
162666730 182274 1 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182274 1 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
162666730 182274 1 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182274 1 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
155554106 175469 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Br)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4577171 175469 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Br)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155562719 175229 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 407 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(I)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4571719 175229 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 407 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(I)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155562719 175229 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 407 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(I)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4571719 175229 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 407 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(I)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155554106 175469 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Br)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4577171 175469 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Br)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
71718331 87828 0 None 208 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 663 8 2 8 5.7 Cc1c(NC[C@H]2CCC[C@@H](c3ccc(C(F)(F)F)cc3)O2)nc(C2CCOCC2)nc1C(=O)N1CCC(N[C@H]2CCOC[C@H]2F)CC1 10.1021/ml400055e
CHEMBL2338391 87828 0 None 208 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 663 8 2 8 5.7 Cc1c(NC[C@H]2CCC[C@@H](c3ccc(C(F)(F)F)cc3)O2)nc(C2CCOCC2)nc1C(=O)N1CCC(N[C@H]2CCOC[C@H]2F)CC1 10.1021/ml400055e
71719547 87830 0 None 50 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 660 8 2 9 5.8 Cc1cc(-c2nc(NC[C@H]3CCC[C@@H](c4ccc(C(F)(F)F)cc4)O3)c(C)c(C(=O)N3CCC(N[C@@H]4CCOC[C@@H]4F)CC3)n2)no1 10.1021/ml400055e
CHEMBL2338393 87830 0 None 50 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 660 8 2 9 5.8 Cc1cc(-c2nc(NC[C@H]3CCC[C@@H](c4ccc(C(F)(F)F)cc4)O3)c(C)c(C(=O)N3CCC(N[C@@H]4CCOC[C@@H]4F)CC3)n2)no1 10.1021/ml400055e
118734584 118696 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 530 6 1 4 6.1 COc1cc2c(cc1OC)C(N[C@@H]1CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C1)CC2 10.1016/j.ejmech.2015.01.063
CHEMBL3417124 118696 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 530 6 1 4 6.1 COc1cc2c(cc1OC)C(N[C@@H]1CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C1)CC2 10.1016/j.ejmech.2015.01.063
53389845 172961 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4517518 172961 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
53389845 172961 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4517518 172961 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155563012 175281 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Br)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4572833 175281 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Br)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155563012 175281 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Br)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4572833 175281 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Br)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
10585 1079 1 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1079 1 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1079 1 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
155513284 169726 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 343 3 2 5 2.9 Nc1nc2[nH]c(C3CCCC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4438407 169726 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 343 3 2 5 2.9 Nc1nc2[nH]c(C3CCCC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
118734578 118689 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 504 4 1 2 6.7 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(Cl)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417117 118689 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 504 4 1 2 6.7 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(Cl)ccc32)C1 10.1016/j.ejmech.2015.01.063
10585 1079 1 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1079 1 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1079 1 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
155513284 169726 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 343 3 2 5 2.9 Nc1nc2[nH]c(C3CCCC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4438407 169726 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 343 3 2 5 2.9 Nc1nc2[nH]c(C3CCCC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
53389660 171483 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12 10.1021/acs.jmedchem.9b00742
CHEMBL4463626 171483 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12 10.1021/acs.jmedchem.9b00742
53389660 171483 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12 10.1021/acs.jmedchem.9b00742
CHEMBL4463626 171483 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12 10.1021/acs.jmedchem.9b00742
155553917 174203 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4548107 174203 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155553917 174203 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4548107 174203 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
53389637 170567 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 3 2 5 2.4 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4450273 170567 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 3 2 5 2.4 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
53389637 170567 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 3 2 5 2.4 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4450273 170567 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 3 2 5 2.4 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
162666730 182274 1 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182274 1 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
15985912 83975 0 None 2 3 Human 8.0 pKi = 8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207081 83975 0 None 2 3 Human 8.0 pKi = 8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71461438 83976 0 None 100 3 Human 8.0 pKi = 8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cnnc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207082 83976 0 None 100 3 Human 8.0 pKi = 8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cnnc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71214709 83978 0 None 14 2 Human 8.0 pKi = 8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207084 83978 0 None 14 2 Human 8.0 pKi = 8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71450658 83992 0 None 15 3 Human 8.0 pKi = 8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.7 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207098 83992 0 None 15 3 Human 8.0 pKi = 8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.7 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
15985912 83975 0 None 2 3 Human 8.0 pKi = 8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207081 83975 0 None 2 3 Human 8.0 pKi = 8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
118734680 118704 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 547 5 1 3 7.1 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(-c4cccnc4)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417225 118704 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 547 5 1 3 7.1 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(-c4cccnc4)ccc32)C1 10.1016/j.ejmech.2015.01.063
118734682 118706 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 591 7 1 4 7.5 CCOc1cncc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c1 10.1016/j.ejmech.2015.01.063
CHEMBL3417227 118706 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 591 7 1 4 7.5 CCOc1cncc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c1 10.1016/j.ejmech.2015.01.063
12093167 172325 33 None 1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 351 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4475389 172325 33 None 1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 351 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823581 126361 0 None - 1 Human 8.0 pKi = 8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650407 126361 0 None - 1 Human 8.0 pKi = 8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
10436045 3516 4 None -85 13 Human 7.0 pKi = 7 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3516 4 None -85 13 Human 7.0 pKi = 7 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3516 4 None -85 13 Human 7.0 pKi = 7 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
10436045 3516 4 None -85 13 Human 7.0 pKi = 7 Binding
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01309
782 3516 4 None -85 13 Human 7.0 pKi = 7 Binding
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01309
CHEMBL432713 3516 4 None -85 13 Human 7.0 pKi = 7 Binding
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01309
71461439 83981 0 None 10 3 Human 7.0 pKi = 7 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.020
CHEMBL2207087 83981 0 None 10 3 Human 7.0 pKi = 7 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.020
71452487 83982 0 None 12 3 Human 7.0 pKi = 7 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207088 83982 0 None 12 3 Human 7.0 pKi = 7 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(Cl)c1 10.1016/j.bmcl.2012.09.020
71454247 83984 0 None 15 2 Human 7.0 pKi = 7 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 366 5 1 5 2.9 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(F)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207090 83984 0 None 15 2 Human 7.0 pKi = 7 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 366 5 1 5 2.9 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(F)c1 10.1016/j.bmcl.2012.09.020
155539148 172804 0 None -3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 4.1 CCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4513770 172804 0 None -3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 4.1 CCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
155539148 172804 0 None -3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 4.1 CCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4513770 172804 0 None -3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 4.1 CCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823497 126302 0 None - 1 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
CHEMBL3650350 126302 0 None - 1 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
155536512 172205 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
CHEMBL4473756 172205 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
3013430 21131 1 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21131 1 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
183790 3742 11 None -6 2 Human 7.0 pKi = 7.0 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3742 11 None -6 2 Human 7.0 pKi = 7.0 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3742 11 None -6 2 Human 7.0 pKi = 7.0 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
155536512 172205 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
CHEMBL4473756 172205 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
89823576 126329 0 None - 1 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 542 5 1 6 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ncc(C(F)(F)F)cc2Cl)C1 nan
CHEMBL3650377 126329 0 None - 1 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 542 5 1 6 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ncc(C(F)(F)F)cc2Cl)C1 nan
89823413 126333 0 None - 1 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)ccc2C(F)(F)F)C1 nan
CHEMBL3650381 126333 0 None - 1 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)ccc2C(F)(F)F)C1 nan
118734676 118701 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 571 5 1 3 7.6 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(-c4ccc(C#N)cc4)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417221 118701 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 571 5 1 3 7.6 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(-c4ccc(C#N)cc4)ccc32)C1 10.1016/j.ejmech.2015.01.063
12093167 172325 33 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 351 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4475389 172325 33 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 351 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823461 126317 0 None - 1 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 491 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(Cl)c2)C1 nan
CHEMBL3650365 126317 0 None - 1 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 491 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(Cl)c2)C1 nan
118734684 118708 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 595 6 1 4 7.3 COc1cc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c(F)cn1 10.1016/j.ejmech.2015.01.063
CHEMBL3417229 118708 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 595 6 1 4 7.3 COc1cc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c(F)cn1 10.1016/j.ejmech.2015.01.063
71745103 126362 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650408 126362 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
183790 3742 11 None -6 2 Human 7.9 pKi = 7.9 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3742 11 None -6 2 Human 7.9 pKi = 7.9 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3742 11 None -6 2 Human 7.9 pKi = 7.9 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
71454248 83995 0 None 25 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
CHEMBL2207100 83995 0 None 25 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
71214976 83996 0 None 79 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.5 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207101 83996 0 None 79 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.5 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
155545321 173454 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4529401 173454 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
89823621 126319 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)n2)C1 nan
CHEMBL3650367 126319 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)n2)C1 nan
71463165 83980 0 None 6 2 Human 5.9 pKi = 5.9 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 348 5 1 5 2.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccccc1 10.1016/j.bmcl.2012.09.020
CHEMBL2207086 83980 0 None 6 2 Human 5.9 pKi = 5.9 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 348 5 1 5 2.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccccc1 10.1016/j.bmcl.2012.09.020
9870980 154647 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL399472 154647 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
25110660 154872 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL400698 154872 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
10436045 3516 4 None -85 13 Human 6.9 pKi = 6.9 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3516 4 None -85 13 Human 6.9 pKi = 6.9 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3516 4 None -85 13 Human 6.9 pKi = 6.9 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
118734580 118692 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 538 4 1 2 7.1 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(C(F)(F)F)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417120 118692 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 538 4 1 2 7.1 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(C(F)(F)F)ccc32)C1 10.1016/j.ejmech.2015.01.063
118734582 118694 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 495 4 1 3 5.9 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3ccc(C#N)cc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417122 118694 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 495 4 1 3 5.9 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3ccc(C#N)cc32)C1 10.1016/j.ejmech.2015.01.063
118734688 118712 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 592 5 1 3 7.4 COc1cc2c(cc1Br)C(C)CC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417233 118712 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 592 5 1 3 7.4 COc1cc2c(cc1Br)C(C)CC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
155545321 173454 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4529401 173454 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
89823598 126365 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650410 126365 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
183790 3742 11 None -6 2 Human 5.9 pKi = 5.9 Binding
Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3742 11 None -6 2 Human 5.9 pKi = 5.9 Binding
Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3742 11 None -6 2 Human 5.9 pKi = 5.9 Binding
Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
118734694 118719 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@@H]2C[C@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417240 118719 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@@H]2C[C@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
9902578 171355 0 None -4 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 5 1 3 4.5 CCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4461627 171355 0 None -4 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 5 1 3 4.5 CCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
118723411 116324 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 503 6 3 4 4.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(C2CCC(c3ccc(O)cc3)CC2)CC1 10.1016/j.bmcl.2014.10.060
CHEMBL3359300 116324 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 503 6 3 4 4.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(C2CCC(c3ccc(O)cc3)CC2)CC1 10.1016/j.bmcl.2014.10.060
155523645 170878 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3Cl)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4454297 170878 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3Cl)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155523645 170878 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3Cl)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4454297 170878 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3Cl)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
9902578 171355 0 None -4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 5 1 3 4.5 CCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4461627 171355 0 None -4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 5 1 3 4.5 CCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
183790 3742 11 None -6 2 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3742 11 None -6 2 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3742 11 None -6 2 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
54597147 161372 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 594 5 0 7 3.3 Cc1c(C(=O)N2CCC(N3CCC(N(C)S(C)(=O)=O)CC3)CC2)ncnc1N1CCc2ccc(C(F)(F)F)cc2C1 10.1016/j.bmc.2018.05.027
CHEMBL4126162 161372 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 594 5 0 7 3.3 Cc1c(C(=O)N2CCC(N3CCC(N(C)S(C)(=O)=O)CC3)CC2)ncnc1N1CCc2ccc(C(F)(F)F)cc2C1 10.1016/j.bmc.2018.05.027
118734571 118682 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 500 5 1 4 5.2 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417110 118682 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 500 5 1 4 5.2 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.ejmech.2015.01.063
118734575 118686 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 495 4 1 3 5.9 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3c(C#N)cccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417114 118686 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 495 4 1 3 5.9 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3c(C#N)cccc32)C1 10.1016/j.ejmech.2015.01.063
155521447 170584 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4450561 170584 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
89823526 126347 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 538 4 0 4 5.7 O=C(N1C[C@@H]2C[C@H]1CN2c1cc(C(F)(F)F)ccn1)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
CHEMBL3650394 126347 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 538 4 0 4 5.7 O=C(N1C[C@@H]2C[C@H]1CN2c1cc(C(F)(F)F)ccn1)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
155521447 170584 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4450561 170584 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
155518928 170345 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
CHEMBL4447263 170345 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
155518928 170345 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
CHEMBL4447263 170345 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
12093170 872 31 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.6b01309
9431 872 31 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.6b01309
CHEMBL4519152 872 31 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.6b01309
CHEMBL5268600 193572 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C2CCC(O)(c3ccc4c(c3)OCO4)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/acs.jmedchem.6b01309
71214710 83979 0 None 39 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.6 Cn1nnnc1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207085 83979 0 None 39 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.6 Cn1nnnc1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
10293022 171098 12 None 1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 377 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4457687 171098 12 None 1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 377 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
3013430 21131 1 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21131 1 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
155530253 171521 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 365 3 2 5 3.2 Cc1ccc(-c2[nH]c3nc(N)nn3c(=O)c2Cc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.9b00742
CHEMBL4464168 171521 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 365 3 2 5 3.2 Cc1ccc(-c2[nH]c3nc(N)nn3c(=O)c2Cc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.9b00742
155545804 173497 0 None -5 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 6 1 3 4.9 CCCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4530510 173497 0 None -5 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 6 1 3 4.9 CCCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10132885 175138 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 3 1 3 4.7 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4569870 175138 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 3 1 3 4.7 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
155545804 173497 0 None -5 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 6 1 3 4.9 CCCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4530510 173497 0 None -5 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 6 1 3 4.9 CCCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10132885 175138 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 3 1 3 4.7 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4569870 175138 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 3 1 3 4.7 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
155535265 172019 0 None -8 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 339 4 1 3 4.1 Cc1ccc(N2C(=O)C(O)=C(C(=O)C3CC3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4471583 172019 0 None -8 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 339 4 1 3 4.1 Cc1ccc(N2C(=O)C(O)=C(C(=O)C3CC3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
155530253 171521 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 365 3 2 5 3.2 Cc1ccc(-c2[nH]c3nc(N)nn3c(=O)c2Cc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.9b00742
CHEMBL4464168 171521 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 365 3 2 5 3.2 Cc1ccc(-c2[nH]c3nc(N)nn3c(=O)c2Cc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.9b00742
71456007 83986 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 373 5 1 6 2.7 N#Cc1cccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207092 83986 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 373 5 1 6 2.7 N#Cc1cccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)c1 10.1016/j.bmcl.2012.09.020
89823445 126351 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
CHEMBL3650398 126351 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
10436045 3516 4 None -85 13 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3516 4 None -85 13 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3516 4 None -85 13 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
53389980 172227 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 289 2 2 5 1.6 Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4474089 172227 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 289 2 2 5 1.6 Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155535265 172019 0 None -8 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 339 4 1 3 4.1 Cc1ccc(N2C(=O)C(O)=C(C(=O)C3CC3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4471583 172019 0 None -8 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 339 4 1 3 4.1 Cc1ccc(N2C(=O)C(O)=C(C(=O)C3CC3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
5353432 97495 89 None -1 3 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
CHEMBL270299 97495 89 None -1 3 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
9924108 171773 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4467708 171773 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCCC1 10.1021/acs.jmedchem.8b00605
10436045 3516 4 None -85 13 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3516 4 None -85 13 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3516 4 None -85 13 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
10436045 3516 4 None -85 13 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3516 4 None -85 13 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3516 4 None -85 13 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
10293022 171098 12 None 1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 377 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4457687 171098 12 None 1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 377 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823661 126344 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 541 5 1 5 4.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
CHEMBL3650391 126344 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 541 5 1 5 4.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
53389980 172227 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 289 2 2 5 1.6 Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4474089 172227 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 289 2 2 5 1.6 Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
183790 3742 11 None -6 2 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3742 11 None -6 2 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3742 11 None -6 2 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
22335694 171558 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4464639 171558 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9924108 171773 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4467708 171773 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCCC1 10.1021/acs.jmedchem.8b00605
781 3396 80 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3396 80 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3396 80 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
155522874 170839 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 373 8 2 5 3.8 CCCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4453718 170839 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 373 8 2 5 3.8 CCCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155522874 170839 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 373 8 2 5 3.8 CCCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4453718 170839 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 373 8 2 5 3.8 CCCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
22335694 171558 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4464639 171558 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9902204 170126 12 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4443909 170126 12 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
183790 3742 11 None -6 2 Human 6.7 pKi = 6.7 Binding
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3742 11 None -6 2 Human 6.7 pKi = 6.7 Binding
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3742 11 None -6 2 Human 6.7 pKi = 6.7 Binding
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
44353447 3775 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3775 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3775 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
9902204 170126 12 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4443909 170126 12 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
162671727 182971 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 601 10 3 5 5.6 C=CC(=O)NCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4793148 182971 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 601 10 3 5 5.6 C=CC(=O)NCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
118734693 118718 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@@H]2C[C@@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417239 118718 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@@H]2C[C@@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
89823498 126313 0 None - 1 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C)C1 nan
CHEMBL3650361 126313 0 None - 1 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C)C1 nan
781 3396 80 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/acs.jmedchem.6b01309
9953769 3396 80 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/acs.jmedchem.6b01309
CHEMBL134074 3396 80 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/acs.jmedchem.6b01309
3794409 170756 7 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4452558 170756 7 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.8b00605
76167595 161464 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 493 6 2 7 3.8 COC1COCCC1NC1CCN(C(=O)c2ncnc(Nc3ccc(Cl)c(Cl)c3)c2C)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4127538 161464 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 493 6 2 7 3.8 COC1COCCC1NC1CCN(C(=O)c2ncnc(Nc3ccc(Cl)c(Cl)c3)c2C)CC1 10.1016/j.bmc.2018.05.027
118734686 118710 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC1CC(N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c2ccc(Br)cc21 10.1016/j.ejmech.2015.01.063
CHEMBL3417231 118710 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC1CC(N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c2ccc(Br)cc21 10.1016/j.ejmech.2015.01.063
118734691 118716 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@H]2C[C@@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417237 118716 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@H]2C[C@@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
183790 3742 11 None -6 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometryDisplacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometry
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
783 3742 11 None -6 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometryDisplacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometry
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
CHEMBL1178786 3742 11 None -6 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometryDisplacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometry
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
71718930 87827 0 None 75 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 601 5 1 7 4.4 CO[C@@H]1COCC[C@@H]1NC1CCN(C(=O)c2nc(C(F)(F)F)nc(N3CCc4cc(C(F)(F)F)ccc4C3)c2C)CC1 10.1021/ml400055e
CHEMBL2338390 87827 0 None 75 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 601 5 1 7 4.4 CO[C@@H]1COCC[C@@H]1NC1CCN(C(=O)c2nc(C(F)(F)F)nc(N3CCc4cc(C(F)(F)F)ccc4C3)c2C)CC1 10.1021/ml400055e
155551912 175136 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 439 3 2 5 3.2 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Br)cc(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4569807 175136 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 439 3 2 5 3.2 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Br)cc(Br)c1 10.1021/acs.jmedchem.9b00742
155551912 175136 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 439 3 2 5 3.2 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Br)cc(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4569807 175136 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 439 3 2 5 3.2 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Br)cc(Br)c1 10.1021/acs.jmedchem.9b00742
155540798 172935 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)cc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4516788 172935 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)cc(Cl)c1 10.1021/acs.jmedchem.9b00742
118734572 118683 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 470 4 1 2 6.1 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417111 118683 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 470 4 1 2 6.1 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.ejmech.2015.01.063
155540798 172935 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)cc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4516788 172935 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)cc(Cl)c1 10.1021/acs.jmedchem.9b00742
53389710 172281 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 331 5 2 5 2.6 CCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4474757 172281 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 331 5 2 5 2.6 CCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
71576618 118690 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 548 4 1 2 6.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417118 118690 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 548 4 1 2 6.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
53389710 172281 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 331 5 2 5 2.6 CCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4474757 172281 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 331 5 2 5 2.6 CCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
73334813 118714 17 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 548 4 1 2 6.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@@H]2CCc3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417235 118714 17 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 548 4 1 2 6.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@@H]2CCc3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
162666730 182274 1 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182274 1 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
155560784 175051 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4567816 175051 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
155560784 175051 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4567816 175051 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
183790 3742 11 None -6 2 Human 8.6 pKi = 8.6 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3742 11 None -6 2 Human 8.6 pKi = 8.6 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3742 11 None -6 2 Human 8.6 pKi = 8.6 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
155541801 173056 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4519409 173056 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155527193 171169 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
CHEMBL4458846 171169 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
155527193 171169 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
CHEMBL4458846 171169 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
3013430 21131 1 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21131 1 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
3794409 170756 7 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4452558 170756 7 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.8b00605
89823496 126315 0 None - 1 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 3.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2)C1 nan
CHEMBL3650363 126315 0 None - 1 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 3.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2)C1 nan
781 3396 80 None - 1 Human 6.7 pKi = 6.7 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3396 80 None - 1 Human 6.7 pKi = 6.7 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3396 80 None - 1 Human 6.7 pKi = 6.7 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
10436045 3516 4 None -85 13 Human 5.7 pKi = 5.7 Binding
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3516 4 None -85 13 Human 5.7 pKi = 5.7 Binding
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3516 4 None -85 13 Human 5.7 pKi = 5.7 Binding
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
118734576 118687 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 486 4 2 3 5.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3c(O)cccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417115 118687 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 486 4 2 3 5.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3c(O)cccc32)C1 10.1016/j.ejmech.2015.01.063
89823628 126349 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 555 5 0 5 4.8 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
CHEMBL3650396 126349 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 555 5 0 5 4.8 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
183790 3742 11 None -6 2 Human 7.7 pKi = 7.7 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3742 11 None -6 2 Human 7.7 pKi = 7.7 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3742 11 None -6 2 Human 7.7 pKi = 7.7 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
155550777 174287 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 7 2 5 3.4 CCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4549837 174287 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 7 2 5 3.4 CCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
3796276 170850 7 None -2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Br)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4453953 170850 7 None -2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Br)cc1 10.1021/acs.jmedchem.8b00605
155526680 171129 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 467 3 1 3 4.8 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
CHEMBL4458295 171129 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 467 3 1 3 4.8 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
12093162 173326 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 329 4 1 4 3.4 COc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4526524 173326 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 329 4 1 4 3.4 COc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
3796276 170850 7 None -2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Br)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4453953 170850 7 None -2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Br)cc1 10.1021/acs.jmedchem.8b00605
155526680 171129 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 467 3 1 3 4.8 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
CHEMBL4458295 171129 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 467 3 1 3 4.8 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
12093162 173326 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 329 4 1 4 3.4 COc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4526524 173326 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 329 4 1 4 3.4 COc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
781 3396 80 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3396 80 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3396 80 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
162671727 182971 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 601 10 3 5 5.6 C=CC(=O)NCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4793148 182971 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 601 10 3 5 5.6 C=CC(=O)NCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
155550777 174287 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 7 2 5 3.4 CCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4549837 174287 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 7 2 5 3.4 CCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155513605 169780 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.9b00742
CHEMBL4439033 169780 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.9b00742
155513605 169780 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.9b00742
CHEMBL4439033 169780 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.9b00742
155553131 174111 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 2.9 Nc1nc2[nH]c(-c3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4545333 174111 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 2.9 Nc1nc2[nH]c(-c3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
10436045 3516 4 None -85 13 Human 6.6 pKi = 6.6 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3516 4 None -85 13 Human 6.6 pKi = 6.6 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3516 4 None -85 13 Human 6.6 pKi = 6.6 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
3013430 21131 1 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21131 1 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
118734581 118693 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 484 4 1 2 6.4 Cc1ccc2c(c1)C(N[C@@H]1CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C1)CC2 10.1016/j.ejmech.2015.01.063
CHEMBL3417121 118693 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 484 4 1 2 6.4 Cc1ccc2c(c1)C(N[C@@H]1CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C1)CC2 10.1016/j.ejmech.2015.01.063
118734683 118707 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 577 6 1 4 7.1 COc1cc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)ccn1 10.1016/j.ejmech.2015.01.063
CHEMBL3417228 118707 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 577 6 1 4 7.1 COc1cc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)ccn1 10.1016/j.ejmech.2015.01.063
3013430 21131 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21131 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
9967465 172087 11 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2cccc(Cl)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4472384 172087 11 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2cccc(Cl)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9967465 172087 11 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2cccc(Cl)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4472384 172087 11 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2cccc(Cl)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
68070944 161460 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 582 8 1 7 4.1 CCS(=O)(=O)N(C)C1CCN(C2CCN(C(=O)c3ncnc(NCc4ccc(Cl)c(Cl)c4)c3C)CC2)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4127496 161460 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 582 8 1 7 4.1 CCS(=O)(=O)N(C)C1CCN(C2CCN(C(=O)c3ncnc(NCc4ccc(Cl)c(Cl)c4)c3C)CC2)CC1 10.1016/j.bmc.2018.05.027
118734690 118715 3 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 548 4 1 2 6.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@H]2CCc3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417236 118715 3 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 548 4 1 2 6.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@H]2CCc3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
10436045 3516 4 None -85 13 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3516 4 None -85 13 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3516 4 None -85 13 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
71450657 83988 0 None 15 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2012.09.020
CHEMBL2207094 83988 0 None 15 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2012.09.020
15604497 83993 0 None 39 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 432 5 1 7 3.0 Cn1nnnc1Cc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207099 83993 0 None 39 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 432 5 1 7 3.0 Cn1nnnc1Cc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
44309012 102823 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
CHEMBL305470 102823 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
71463166 83990 0 None 7 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 390 5 1 8 2.3 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc2nonc12 10.1016/j.bmcl.2012.09.020
CHEMBL2207096 83990 0 None 7 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 390 5 1 8 2.3 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc2nonc12 10.1016/j.bmcl.2012.09.020
44309012 102823 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
CHEMBL305470 102823 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
781 3396 80 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3396 80 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3396 80 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
10436045 3516 4 None -85 13 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3516 4 None -85 13 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3516 4 None -85 13 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
44353447 3775 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3775 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3775 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
3013430 21131 1 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21131 1 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
11080 29085 79 None -1 6 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL1381098 29085 79 None -1 6 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
155553131 174111 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 2.9 Nc1nc2[nH]c(-c3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4545333 174111 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 2.9 Nc1nc2[nH]c(-c3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
89823470 126309 0 None - 1 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)n2)C1 nan
CHEMBL3650357 126309 0 None - 1 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)n2)C1 nan
12093163 174402 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2cccc(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4552420 174402 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2cccc(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
12093163 174402 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2cccc(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4552420 174402 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2cccc(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
183790 3742 11 None -6 2 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3742 11 None -6 2 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3742 11 None -6 2 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
118723406 116322 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 501 6 2 3 5.1 Cc1cccc(C2CCC(N3CCC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)CC3)CC2)c1 10.1016/j.bmcl.2014.10.060
CHEMBL3359295 116322 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 501 6 2 3 5.1 Cc1cccc(C2CCC(N3CCC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)CC3)CC2)c1 10.1016/j.bmcl.2014.10.060
89823507 126322 0 None - 1 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(F)cc(C(F)(F)F)c2)C1 nan
CHEMBL3650370 126322 0 None - 1 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(F)cc(C(F)(F)F)c2)C1 nan
89823552 126303 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
CHEMBL3650351 126303 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
183790 3742 11 None -6 2 Human 7.5 pKi = 7.5 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3742 11 None -6 2 Human 7.5 pKi = 7.5 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3742 11 None -6 2 Human 7.5 pKi = 7.5 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
3013430 21131 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21131 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
44353447 3775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
155540563 172537 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2cccc(C(F)(F)F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4483756 172537 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2cccc(C(F)(F)F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9949615 138204 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 335 3 2 3 4.4 O=C(O)c1cc2cc(O)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2006.04.045
CHEMBL376981 138204 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 335 3 2 3 4.4 O=C(O)c1cc2cc(O)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2006.04.045
89823551 126312 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(C(F)(F)F)c2)C1 nan
CHEMBL3650360 126312 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(C(F)(F)F)c2)C1 nan
118734685 118709 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 484 4 1 2 6.6 CC1CC(N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c2ccccc21 10.1016/j.ejmech.2015.01.063
CHEMBL3417230 118709 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 484 4 1 2 6.6 CC1CC(N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c2ccccc21 10.1016/j.ejmech.2015.01.063
155541801 173056 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4519409 173056 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155535293 172045 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
CHEMBL4471792 172045 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
53389636 172400 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 4 2 5 2.2 CCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4476551 172400 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 4 2 5 2.2 CCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155543260 173289 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 314 3 1 4 2.8 Cc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4525646 173289 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 314 3 1 4 2.8 Cc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155535293 172045 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
CHEMBL4471792 172045 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
155543260 173289 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 314 3 1 4 2.8 Cc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4525646 173289 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 314 3 1 4 2.8 Cc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
53389636 172400 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 4 2 5 2.2 CCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4476551 172400 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 4 2 5 2.2 CCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
162666730 182274 1 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182274 1 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
162658125 181096 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181096 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
53389641 175953 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 303 3 2 5 1.8 CCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4588111 175953 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 303 3 2 5 1.8 CCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
86698129 126304 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 0 6 3.6 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650352 126304 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 0 6 3.6 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
3013430 21131 1 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21131 1 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
155540563 172537 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2cccc(C(F)(F)F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4483756 172537 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2cccc(C(F)(F)F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823349 126316 0 None - 1 Human 6.5 pKi = 6.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C)c(C(F)(F)F)c2)C1 nan
CHEMBL3650364 126316 0 None - 1 Human 6.5 pKi = 6.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C)c(C(F)(F)F)c2)C1 nan
118734573 118684 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 484 4 1 2 6.4 Cc1cccc2c1CCC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417112 118684 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 484 4 1 2 6.4 Cc1cccc2c1CCC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
162671079 182852 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.4 O=C(NCCN=C=S)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4791522 182852 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.4 O=C(NCCN=C=S)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
89823575 126311 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2F)C1 nan
CHEMBL3650359 126311 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2F)C1 nan
15985914 83974 0 None 8 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207080 83974 0 None 8 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71461440 83991 0 None 31 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 400 5 1 5 3.6 O=S(=O)(Nc1cc(F)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207097 83991 0 None 31 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 400 5 1 5 3.6 O=S(=O)(Nc1cc(F)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
162671079 182852 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.4 O=C(NCCN=C=S)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4791522 182852 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.4 O=C(NCCN=C=S)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
155513751 169801 0 None -7 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 4 1 3 4.3 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4439354 169801 0 None -7 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 4 1 3 4.3 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
44353447 3775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
44353447 3775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
44353447 3775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/acs.jmedchem.6b01309
785 3775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/acs.jmedchem.6b01309
CHEMBL337246 3775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/acs.jmedchem.6b01309
155513751 169801 0 None -7 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 4 1 3 4.3 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4439354 169801 0 None -7 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 4 1 3 4.3 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
89823537 126298 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650346 126298 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
89823606 126325 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
CHEMBL3650373 126325 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
89823656 126355 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
CHEMBL3650401 126355 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
44353447 3775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
9967349 173065 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4519533 173065 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9967349 173065 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4519533 173065 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823580 126337 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(Cl)c2)C1 nan
CHEMBL3650385 126337 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(Cl)c2)C1 nan
118734678 118702 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 576 6 1 3 7.7 COc1cccc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c1 10.1016/j.ejmech.2015.01.063
CHEMBL3417223 118702 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 576 6 1 3 7.7 COc1cccc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c1 10.1016/j.ejmech.2015.01.063
71214725 83977 0 None 15 3 Human 7.4 pKi = 7.4 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cncn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207083 83977 0 None 15 3 Human 7.4 pKi = 7.4 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cncn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
10257042 204361 0 None 12 7 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL71707 204361 0 None 12 7 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
162666730 182274 1 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182274 1 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
53389641 175953 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 303 3 2 5 1.8 CCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4588111 175953 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 303 3 2 5 1.8 CCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155520385 170450 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(F)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4448714 170450 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(F)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155520385 170450 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(F)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4448714 170450 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(F)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
183790 3742 11 None -6 2 Human 8.4 pKi = 8.4 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3742 11 None -6 2 Human 8.4 pKi = 8.4 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3742 11 None -6 2 Human 8.4 pKi = 8.4 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
118734579 118691 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 596 4 1 2 6.7 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(I)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417119 118691 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 596 4 1 2 6.7 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(I)ccc32)C1 10.1016/j.ejmech.2015.01.063
162658125 181096 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181096 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
118734687 118711 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 578 5 1 3 6.8 COc1cc2c(cc1Br)CCC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417232 118711 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 578 5 1 3 6.8 COc1cc2c(cc1Br)CCC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
118734574 118685 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 485 4 2 3 5.6 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3c(N)cccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417113 118685 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 485 4 2 3 5.6 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3c(N)cccc32)C1 10.1016/j.ejmech.2015.01.063
118734692 118717 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@H]2C[C@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417238 118717 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@H]2C[C@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
118734577 118688 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 488 4 1 2 6.2 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(F)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417116 118688 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 488 4 1 2 6.2 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(F)ccc32)C1 10.1016/j.ejmech.2015.01.063
10257042 204361 0 None 12 7 Human 7.4 pKi = 7.4 Binding
Binding affinity for C-C chemokine receptor type 2B was determinedBinding affinity for C-C chemokine receptor type 2B was determined
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL71707 204361 0 None 12 7 Human 7.4 pKi = 7.4 Binding
Binding affinity for C-C chemokine receptor type 2B was determinedBinding affinity for C-C chemokine receptor type 2B was determined
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
11632418 75197 1 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human HEK cell membraneDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human HEK cell membrane
ChEMBL 384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036748 75197 1 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human HEK cell membraneDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human HEK cell membrane
ChEMBL 384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
118734681 118705 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 577 6 1 4 7.1 COc1cncc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c1 10.1016/j.ejmech.2015.01.063
CHEMBL3417226 118705 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 577 6 1 4 7.1 COc1cncc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c1 10.1016/j.ejmech.2015.01.063
176 398 66 None -3 31 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 398 66 None -3 31 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 398 66 None -3 31 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 398 66 None -3 31 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 398 66 None -3 31 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
89823586 126324 0 None - 1 Human 6.4 pKi = 6.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)n2)C1 nan
CHEMBL3650372 126324 0 None - 1 Human 6.4 pKi = 6.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)n2)C1 nan
781 3396 80 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3396 80 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3396 80 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
89823444 126326 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 523 6 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(OC(F)(F)F)c2)C1 nan
CHEMBL3650374 126326 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 523 6 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(OC(F)(F)F)c2)C1 nan
3013430 21131 1 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21131 1 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
118734671 118699 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 530 6 1 4 6.1 COc1ccc(OC)c2c1CCC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417216 118699 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 530 6 1 4 6.1 COc1ccc(OC)c2c1CCC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
89823344 126350 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 589 5 0 5 5.2 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
CHEMBL3650397 126350 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 589 5 0 5 5.2 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
155534565 171971 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 281 3 2 5 1.5 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4470785 171971 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 281 3 2 5 1.5 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155529754 171461 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.5 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(C(F)(F)F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4463383 171461 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.5 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(C(F)(F)F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
10111333 175467 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4577133 175467 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
155529754 171461 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.5 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(C(F)(F)F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4463383 171461 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.5 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(C(F)(F)F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155534565 171971 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 281 3 2 5 1.5 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4470785 171971 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 281 3 2 5 1.5 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
10436045 3516 4 None -85 13 Human 7.3 pKi = 7.3 Binding
Binding affinity at C-C chemokine receptor type 2 was determinedBinding affinity at C-C chemokine receptor type 2 was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3516 4 None -85 13 Human 7.3 pKi = 7.3 Binding
Binding affinity at C-C chemokine receptor type 2 was determinedBinding affinity at C-C chemokine receptor type 2 was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3516 4 None -85 13 Human 7.3 pKi = 7.3 Binding
Binding affinity at C-C chemokine receptor type 2 was determinedBinding affinity at C-C chemokine receptor type 2 was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
44573568 187470 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 512 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL494019 187470 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 512 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.ejmech.2015.01.063
10436045 3516 4 None -85 13 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2006.04.045
782 3516 4 None -85 13 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2006.04.045
CHEMBL432713 3516 4 None -85 13 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2006.04.045
10436045 3516 4 None -85 13 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
782 3516 4 None -85 13 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
CHEMBL432713 3516 4 None -85 13 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
71457815 83985 0 None 19 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 3.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207091 83985 0 None 19 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 3.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
71452488 83987 0 None 19 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 388 5 1 6 3.5 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
CHEMBL2207093 83987 0 None 19 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 388 5 1 6 3.5 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
10436045 3516 4 None -85 13 Human 7.3 pKi = 7.3 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3516 4 None -85 13 Human 7.3 pKi = 7.3 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3516 4 None -85 13 Human 7.3 pKi = 7.3 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
10436045 3516 4 None -85 13 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
782 3516 4 None -85 13 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
CHEMBL432713 3516 4 None -85 13 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
15985981 83973 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 443 5 1 4 5.0 Cc1cc(C)n(Cc2ccc(C(F)(F)F)cc2NS(=O)(=O)c2ccc(Cl)cc2)n1 10.1016/j.bmcl.2012.09.020
CHEMBL2207079 83973 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 443 5 1 4 5.0 Cc1cc(C)n(Cc2ccc(C(F)(F)F)cc2NS(=O)(=O)c2ccc(Cl)cc2)n1 10.1016/j.bmcl.2012.09.020
71454246 83983 0 None 1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 376 5 1 5 3.4 Cc1ccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)cc1C 10.1016/j.bmcl.2012.09.020
CHEMBL2207089 83983 0 None 1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 376 5 1 5 3.4 Cc1ccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)cc1C 10.1016/j.bmcl.2012.09.020
155522058 170644 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 379 5 2 5 3.0 Nc1nc2[nH]c(CCc3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4451290 170644 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 379 5 2 5 3.0 Nc1nc2[nH]c(CCc3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155522058 170644 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 379 5 2 5 3.0 Nc1nc2[nH]c(CCc3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4451290 170644 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 379 5 2 5 3.0 Nc1nc2[nH]c(CCc3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
781 3396 80 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3396 80 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3396 80 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
118734675 118700 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 571 5 1 3 7.6 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(-c4cccc(C#N)c4)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417220 118700 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 571 5 1 3 7.6 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(-c4cccc(C#N)c4)ccc32)C1 10.1016/j.ejmech.2015.01.063
89823462 126358 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 463 4 1 6 2.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)C1 nan
CHEMBL3650404 126358 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 463 4 1 6 2.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)C1 nan
10436045 3516 4 None -85 13 Human 6.3 pKi = 6.3 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3516 4 None -85 13 Human 6.3 pKi = 6.3 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3516 4 None -85 13 Human 6.3 pKi = 6.3 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
22335665 173467 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4529804 173467 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
22335665 173467 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4529804 173467 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
781 3396 80 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3396 80 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3396 80 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
3013430 21131 1 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21131 1 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
89823427 126310 0 None - 1 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ncn2)C1 nan
CHEMBL3650358 126310 0 None - 1 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ncn2)C1 nan
162658125 181096 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181096 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
10111333 175467 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4577133 175467 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823620 126363 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650409 126363 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
162658125 181096 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181096 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
162658125 181096 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181096 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
162658125 181096 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181096 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
155531561 171650 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 6 2 5 3.2 CCC(CC)Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4466027 171650 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 6 2 5 3.2 CCC(CC)Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155531561 171650 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 6 2 5 3.2 CCC(CC)Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4466027 171650 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 6 2 5 3.2 CCC(CC)Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
183790 3742 11 None -6 2 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3742 11 None -6 2 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3742 11 None -6 2 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
89823439 126299 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650347 126299 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
183790 3742 11 None -6 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/acs.jmedchem.6b01309
783 3742 11 None -6 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/acs.jmedchem.6b01309
CHEMBL1178786 3742 11 None -6 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/acs.jmedchem.6b01309
71456008 83989 0 None 25 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 404 5 1 6 4.0 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1csc2ccccc12 10.1016/j.bmcl.2012.09.020
CHEMBL2207095 83989 0 None 25 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 404 5 1 6 4.0 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1csc2ccccc12 10.1016/j.bmcl.2012.09.020
162672927 183183 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 733 11 3 7 6.4 O=C(NCCNC(=O)c1ccc(S(=O)(=O)F)cc1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4795646 183183 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 733 11 3 7 6.4 O=C(NCCNC(=O)c1ccc(S(=O)(=O)F)cc1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
44309012 102823 0 None - 1 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
CHEMBL305470 102823 0 None - 1 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
44309012 102823 0 None - 1 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
CHEMBL305470 102823 0 None - 1 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
781 3396 80 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3396 80 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3396 80 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9967166 169973 11 None 2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 3.9 CCc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4441958 169973 11 None 2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 3.9 CCc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
118723408 116323 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 517 7 2 4 4.8 COc1cccc(C2CCC(N3CCC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)CC3)CC2)c1 10.1016/j.bmcl.2014.10.060
CHEMBL3359297 116323 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 517 7 2 4 4.8 COc1cccc(C2CCC(N3CCC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)CC3)CC2)c1 10.1016/j.bmcl.2014.10.060
9967166 169973 11 None 2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 3.9 CCc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4441958 169973 11 None 2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 3.9 CCc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
155559153 174781 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 457 4 1 3 5.6 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)c1ccccc1 10.1021/acs.jmedchem.8b00605
CHEMBL4561618 174781 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 457 4 1 3 5.6 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)c1ccccc1 10.1021/acs.jmedchem.8b00605
89823506 126336 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
CHEMBL3650384 126336 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
155559153 174781 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 457 4 1 3 5.6 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)c1ccccc1 10.1021/acs.jmedchem.8b00605
CHEMBL4561618 174781 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 457 4 1 3 5.6 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)c1ccccc1 10.1021/acs.jmedchem.8b00605
44353447 3775 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3775 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3775 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
89823342 126359 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650405 126359 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
3013430 21131 1 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21131 1 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
155553573 174177 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 345 6 2 5 3.0 CCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4547381 174177 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 345 6 2 5 3.0 CCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155553573 174177 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 345 6 2 5 3.0 CCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4547381 174177 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 345 6 2 5 3.0 CCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
118734583 118695 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 504 4 1 2 6.7 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3ccc(Cl)cc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417123 118695 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 504 4 1 2 6.7 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3ccc(Cl)cc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL11359 9780 0 None -2 4 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL None None None None nan
44353447 3775 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3775 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3775 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
10436045 3516 4 None -85 13 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3516 4 None -85 13 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3516 4 None -85 13 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
118723021 116267 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 487 6 2 3 4.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(C2CCC(c3ccccc3)CC2)CC1 10.1016/j.bmcl.2014.10.060
CHEMBL3358698 116267 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 487 6 2 3 4.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(C2CCC(c3ccccc3)CC2)CC1 10.1016/j.bmcl.2014.10.060
118734679 118703 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 576 6 1 3 7.7 COc1ccc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)cc1 10.1016/j.ejmech.2015.01.063
CHEMBL3417224 118703 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 576 6 1 3 7.7 COc1ccc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)cc1 10.1016/j.ejmech.2015.01.063
3013430 21131 1 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21131 1 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
89823417 126345 0 None - 1 Human 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 498 5 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C#N)c2)C1 nan
CHEMBL3650392 126345 0 None - 1 Human 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 498 5 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C#N)c2)C1 nan
44353447 3775 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3775 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3775 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
89823348 126348 0 None - 1 Human 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 575 5 1 5 4.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
CHEMBL3650395 126348 0 None - 1 Human 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 575 5 1 5 4.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
25110660 154872 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL400698 154872 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
9857981 170787 11 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4453024 170787 11 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
25110660 154872 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL400698 154872 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
89823541 126323 0 None - 1 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)c2)C1 nan
CHEMBL3650371 126323 0 None - 1 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)c2)C1 nan
89823450 126346 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 562 4 0 4 6.2 N#Cc1ccc(C(F)(F)F)cc1N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
CHEMBL3650393 126346 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 562 4 0 4 6.2 N#Cc1ccc(C(F)(F)F)cc1N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
22725647 173699 0 None 3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4535696 173699 0 None 3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9857981 170787 11 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4453024 170787 11 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
118734689 118713 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 606 6 1 3 7.8 CCC1CC(N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c2cc(OC)c(Br)cc21 10.1016/j.ejmech.2015.01.063
CHEMBL3417234 118713 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 606 6 1 3 7.8 CCC1CC(N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c2cc(OC)c(Br)cc21 10.1016/j.ejmech.2015.01.063
89823428 126327 0 None - 1 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 514 5 1 7 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nc(C(F)(F)F)cs2)C1 nan
CHEMBL3650375 126327 0 None - 1 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 514 5 1 7 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nc(C(F)(F)F)cs2)C1 nan
4485 69379 118 None -1 8 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] nan
CHEMBL193 69379 118 None -1 8 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] nan
781 3396 80 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3396 80 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3396 80 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
162672927 183183 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 733 11 3 7 6.4 O=C(NCCNC(=O)c1ccc(S(=O)(=O)F)cc1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4795646 183183 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 733 11 3 7 6.4 O=C(NCCNC(=O)c1ccc(S(=O)(=O)F)cc1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
22725647 173699 0 None 3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4535696 173699 0 None 3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
183790 3742 11 None -6 2 Human 8.0 pKi = 8.0 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3742 11 None -6 2 Human 8.0 pKi = 8.0 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3742 11 None -6 2 Human 8.0 pKi = 8.0 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
118723412 116325 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 531 6 2 5 4.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(C2CCC(c3ccc4c(c3)OCO4)CC2)CC1 10.1016/j.bmcl.2014.10.060
CHEMBL3359301 116325 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 531 6 2 5 4.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(C2CCC(c3ccc4c(c3)OCO4)CC2)CC1 10.1016/j.bmcl.2014.10.060
10133557 172539 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2ccc(C(F)(F)F)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4483771 172539 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2ccc(C(F)(F)F)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10133557 172539 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2ccc(C(F)(F)F)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4483771 172539 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2ccc(C(F)(F)F)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
8447 188949 84 None -12 13 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 188949 84 None -12 13 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
9945265 171183 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4459033 171183 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCC1 10.1021/acs.jmedchem.8b00605
3117 207841 103 None -2 16 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 207841 103 None -2 16 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
9945265 171183 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4459033 171183 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCC1 10.1021/acs.jmedchem.8b00605
46208367 83581 13 None - 1 Mouse 5.0 pKi = 5.0 Binding
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1021/ml300260s
CHEMBL2204263 83581 13 None - 1 Mouse 5.0 pKi = 5.0 Binding
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1021/ml300260s
12093170 872 31 None - 1 Human 5.3 pIC50 < 5.3 Binding
Antagonism of <sup>125</sup>I-MCP-1 binding to THP-1 cellsAntagonism of <sup>125</sup>I-MCP-1 binding to THP-1 cells
Guide to Pharmacology 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C None
9431 872 31 None - 1 Human 5.3 pIC50 < 5.3 Binding
Antagonism of <sup>125</sup>I-MCP-1 binding to THP-1 cellsAntagonism of <sup>125</sup>I-MCP-1 binding to THP-1 cells
Guide to Pharmacology 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C None
CHEMBL4519152 872 31 None - 1 Human 5.3 pIC50 < 5.3 Binding
Antagonism of <sup>125</sup>I-MCP-1 binding to THP-1 cellsAntagonism of <sup>125</sup>I-MCP-1 binding to THP-1 cells
Guide to Pharmacology 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C None
4410 3137 106 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
65015 3137 106 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
844 3137 106 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
CHEMBL18442 3137 106 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
DB06809 3137 106 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
11598 673 9 None - 1 Human 9.0 pIC50 = 9.0 Binding
Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.
Guide to Pharmacology 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 30891130
23725177 673 9 None - 1 Human 9.0 pIC50 = 9.0 Binding
Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.
Guide to Pharmacology 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 30891130
CHEMBL4442783 673 9 None - 1 Human 9.0 pIC50 = 9.0 Binding
Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.
Guide to Pharmacology 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 30891130
10586 2139 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Measuring antagonism of <sup>125</sup>I-MCP-1binding to human CCR2 expressed by CHO cells in a competition binding assay.Measuring antagonism of <sup>125</sup>I-MCP-1binding to human CCR2 expressed by CHO cells in a competition binding assay.
Guide to Pharmacology 379 5 1 6 4.3 CC[C@@H](n1c(=S)[nH]c(c1C(=O)OC)c1ccno1)c1ccc(c(c1)F)F 18599682
11617815 2139 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Measuring antagonism of <sup>125</sup>I-MCP-1binding to human CCR2 expressed by CHO cells in a competition binding assay.Measuring antagonism of <sup>125</sup>I-MCP-1binding to human CCR2 expressed by CHO cells in a competition binding assay.
Guide to Pharmacology 379 5 1 6 4.3 CC[C@@H](n1c(=S)[nH]c(c1C(=O)OC)c1ccno1)c1ccc(c(c1)F)F 18599682
CHEMBL5290248 2139 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Measuring antagonism of <sup>125</sup>I-MCP-1binding to human CCR2 expressed by CHO cells in a competition binding assay.Measuring antagonism of <sup>125</sup>I-MCP-1binding to human CCR2 expressed by CHO cells in a competition binding assay.
Guide to Pharmacology 379 5 1 6 4.3 CC[C@@H](n1c(=S)[nH]c(c1C(=O)OC)c1ccno1)c1ccc(c(c1)F)F 18599682
46198579 3062 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.
Guide to Pharmacology 511 6 1 7 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1C[C@@H]2C[C@H]1CN2c1ncnc(c1)C(F)(F)F None
9979 3062 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.
Guide to Pharmacology 511 6 1 7 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1C[C@@H]2C[C@H]1CN2c1ncnc(c1)C(F)(F)F None
DB14955 3062 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.
Guide to Pharmacology 511 6 1 7 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1C[C@@H]2C[C@H]1CN2c1ncnc(c1)C(F)(F)F None
176 398 66 None -3 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 398 66 None -3 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 398 66 None -3 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 398 66 None -3 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 398 66 None -3 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
3117 207841 103 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
CHEMBL964 207841 103 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
4485 69379 118 None -1 8 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] None
CHEMBL193 69379 118 None -1 8 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] None
10585 1079 1 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity determined from a radioligand binding assay, measuring displacement of [<sup>3</sup>H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.Binding affinity determined from a radioligand binding assay, measuring displacement of [<sup>3</sup>H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.
Guide to Pharmacology 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 31742400
145996522 1079 1 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity determined from a radioligand binding assay, measuring displacement of [<sup>3</sup>H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.Binding affinity determined from a radioligand binding assay, measuring displacement of [<sup>3</sup>H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.
Guide to Pharmacology 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 31742400
CHEMBL4531005 1079 1 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity determined from a radioligand binding assay, measuring displacement of [<sup>3</sup>H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.Binding affinity determined from a radioligand binding assay, measuring displacement of [<sup>3</sup>H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.
Guide to Pharmacology 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 31742400
11560568 1886 0 None - 1 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 6 4 6 1.7 OCC(CNc1cccc(c1)C1=C(C(=O)NC1=O)c1cn(c2c1cc(F)cc2)C)O None
3502 1886 0 None - 1 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 6 4 6 1.7 OCC(CNc1cccc(c1)C1=C(C(=O)NC1=O)c1cn(c2c1cc(F)cc2)C)O None
CHEMBL1082152 1886 0 None - 1 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 6 4 6 1.7 OCC(CNc1cccc(c1)C1=C(C(=O)NC1=O)c1cn(c2c1cc(F)cc2)C)O None
44353447 3775 0 None - 1 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 12954060
785 3775 0 None - 1 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 12954060
CHEMBL337246 3775 0 None - 1 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 12954060
781 3396 80 None - 1 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 12954060
9953769 3396 80 None - 1 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 12954060
CHEMBL134074 3396 80 None - 1 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 12954060
10436045 3516 4 None -85 13 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 12954060
782 3516 4 None -85 13 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 12954060
CHEMBL432713 3516 4 None -85 13 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 12954060
183790 3742 11 None -6 2 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 12954060
783 3742 11 None -6 2 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 12954060
CHEMBL1178786 3742 11 None -6 2 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 12954060
183790 3742 11 None -6 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10318947
183790 3742 11 None -6 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 12954060
783 3742 11 None -6 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10318947
783 3742 11 None -6 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 12954060
CHEMBL1178786 3742 11 None -6 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10318947
CHEMBL1178786 3742 11 None -6 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 12954060