Ligand source activities (1 row/activity)



Get vendors


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

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
155491018 180862 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 180862 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 7865 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 7865 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 7865 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 180862 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 180862 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 7865 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 7865 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 7865 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 180862 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 180862 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 180862 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 180862 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 101870 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 101870 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 7865 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 7865 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 7865 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 7865 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 7865 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 7865 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 180862 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 180862 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 180862 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 180862 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 84751 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 84751 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 175314 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 175314 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 7865 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 7865 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 7865 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 7865 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 7865 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 7865 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 71278 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 71278 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 100009 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 100009 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 84750 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 84750 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 196129 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 196129 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 185346 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 185346 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 196131 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 196131 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 180548 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 180548 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 185543 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 185543 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 196266 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 196266 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 195586 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 195586 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 196068 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 196068 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 177132 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 177132 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 200286 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 200286 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 185373 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 185373 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 185439 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 185439 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 179395 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 179395 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 185258 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 185258 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 70070 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 70070 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 185256 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 185256 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 185256 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 185256 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 185542 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 185542 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 185541 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 185541 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 185257 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 185257 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 195991 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 195991 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 195403 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 195403 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 194274 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 194274 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 145081 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 145081 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 92857 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 92857 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 195207 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 195207 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 194274 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 194274 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 175547 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 175547 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 194755 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 194755 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 199889 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 199889 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 92876 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 92876 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 92743 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 92743 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 92743 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 92743 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 195207 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 195207 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 14886 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 14886 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 104570 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 104570 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 175663 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 175663 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 175547 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 175547 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 144942 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 144942 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 195238 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 195238 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 7460 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 7460 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 7460 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 149038 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 149038 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 160308 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 160308 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 92857 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 92857 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 7461 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 7461 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 7461 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 182996 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 182996 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 194011 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 194011 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 102114 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 102114 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 104464 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 104464 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 10514 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 10514 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 10514 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 10514 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 10514 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 10514 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 104817 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 104817 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 77783 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 77783 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 104817 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 104817 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 194011 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 194011 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 194014 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 194014 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 194274 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 194274 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 200312 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 200312 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 145041 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 145041 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 144961 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 144961 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 14885 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 14885 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 145081 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 145081 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 25881 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 25881 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 194689 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 194689 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 14816 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 14816 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 144992 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 144992 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 14987 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 14987 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 81319 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 81319 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 26101 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 26101 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 160308 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 160308 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 92743 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 92743 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 160308 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 160308 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 81324 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 81324 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 175547 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 175547 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 175547 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 175547 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 77113 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 77113 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 80502 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 80502 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 14622 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 14622 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 84605 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 84605 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 195226 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 195226 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 77792 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 77792 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 154568 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 154568 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 194470 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 194470 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 159907 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 159907 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 159907 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 159907 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 65563 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 65563 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 86494 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 86494 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 91854 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 91854 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 91932 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 91932 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 91994 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 91994 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 92005 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 92005 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 149067 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 149067 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 168663 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 168663 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 173046 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 173046 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 173104 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 173104 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 173106 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 173106 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 148804 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 148804 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 66972 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 66972 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 66972 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 162152 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 162152 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 91823 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 91823 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 148690 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 148690 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 148845 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 148845 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 69347 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 69347 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 104247 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 104247 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 190766 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 190766 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 190766 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 190766 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 145652 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 145652 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 72202 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 72202 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 102211 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 102211 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 102212 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 102212 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 72569 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 72569 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 72570 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 72570 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 72573 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 72573 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 15116 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 15116 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 179228 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 179228 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 15147 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 15147 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 15148 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 15148 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 144369 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 144369 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 75730 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 75730 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 97069 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 97069 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 10514 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 10514 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 10514 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 80513 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 80513 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 81324 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 81324 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 75735 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 75735 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 26062 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 26062 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 104543 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 104543 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 72580 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 72580 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 14489 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 14489 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 102214 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 102214 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 190685 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 190685 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 179565 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 179565 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 92841 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 92841 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 25881 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 25881 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 15194 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 15194 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 104631 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 104631 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 82004 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 82004 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 128614 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 128614 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 66972 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 66972 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 66972 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 102351 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 102351 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 168127 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 168127 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 128612 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 128612 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 101471 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 101471 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 101471 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 101471 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 168348 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 168348 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 104706 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 104706 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 90352 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 90352 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 200205 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 200205 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 200350 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 200350 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 80501 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 80501 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 92841 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 92841 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 92790 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 92790 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 150145 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 150145 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 84424 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 84424 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 92790 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 92790 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 150145 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 150145 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 190657 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 190657 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 75711 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 75711 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 75729 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 75729 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 104385 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 104385 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 72198 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 72198 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 75722 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 75722 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 75724 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 75724 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 198824 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 198824 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 80511 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 80511 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 72207 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 72207 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 181362 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 181362 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 101836 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 101836 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 72562 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 72562 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 72574 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 72574 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 101418 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 101418 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 26100 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 26100 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 101418 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 101418 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 160026 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 160026 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 160026 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 160026 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 75731 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 75731 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 72583 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 72583 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 163568 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 163568 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 153605 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 153605 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 65653 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 65653 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 75720 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 75720 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 91772 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 91772 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 148889 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 148889 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 69342 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 69342 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 144099 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 144099 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 72189 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 72189 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 81314 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 81314 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 72551 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 72551 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 72571 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 72571 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 148796 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 148796 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 100424 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 100424 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 65651 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 65651 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 65652 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 65652 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 91792 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 91792 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 97463 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 97463 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 77783 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 77783 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 168210 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 168210 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 26101 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 26101 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 75718 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 75718 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 179474 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 179474 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 178262 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 178262 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 179740 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 179740 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 75706 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 75706 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 10547 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 10547 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 10547 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 148796 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 148796 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 8805 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 8805 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 8805 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 195014 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 195014 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 72219 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 72219 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 167916 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 167916 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 15075 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 15075 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 128628 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 128628 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 65650 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 65650 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 81978 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 81978 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 168309 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 168309 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 81988 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 81988 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 128484 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 128484 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 90345 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 90345 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 128631 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 128631 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 80495 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 80495 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 192815 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 192815 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 72575 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 72575 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 190612 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 190612 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 200350 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 200350 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 72204 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 72204 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 72218 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 72218 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 72518 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 72518 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 15021 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 15021 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 150353 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 150353 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 128618 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 128618 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 165333 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 165333 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 85009 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 85009 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 168189 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 168189 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 81975 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 81975 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 85009 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 85009 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 158697 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 158697 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 104817 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 104817 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 81327 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 81327 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 104817 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 104817 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 165083 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 165083 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 15193 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 15193 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 65246 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 65246 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 69335 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 69335 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 69341 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 69341 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 65244 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 65244 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 128613 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 128613 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 95397 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 95397 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 168275 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 168275 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 81986 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 81986 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 98749 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 98749 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 14675 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 14675 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 75735 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 75735 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 75733 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 75733 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 194837 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 194837 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 200205 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 200205 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 197873 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 197873 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 8805 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 8805 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 8805 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 72549 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 72549 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 92762 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 92762 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 92762 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 92762 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 92801 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 92801 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 153978 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 153978 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 75723 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 75723 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 192818 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 192818 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 91864 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 91864 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 150337 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 150337 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 101384 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 101384 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 168133 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 168133 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 101384 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 101384 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 168165 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 168165 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 96697 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 96697 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 194637 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 194637 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 194841 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 194841 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 195563 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 195563 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 196573 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 196573 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 102020 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 102020 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 174238 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 174238 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 72516 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 72516 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 92876 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 92876 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 92082 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 92082 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 195065 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 195065 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 145047 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 145047 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 65234 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 65234 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 84412 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 84412 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 194755 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 194755 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 161985 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 161985 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 65230 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 65230 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 7461 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 7461 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 7461 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 81316 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 81316 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 104465 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 104465 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 15232 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 15232 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 77794 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 77794 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 144993 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 144993 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 8805 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 8805 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 8805 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 80507 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 80507 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 77789 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 77789 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 72533 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 72533 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 72534 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 72534 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 72584 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 72584 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 92801 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 92801 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 66972 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 66972 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 66972 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 82004 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 82004 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 91857 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 91857 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 91906 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 91906 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 91889 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 91889 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 143329 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 143329 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 81987 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 81987 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 161626 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 161626 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 161626 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 161626 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 98757 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 98757 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 179430 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 179430 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 195225 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 195225 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 195241 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 195241 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 194653 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 194653 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 72200 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 72200 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 102277 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 102277 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 104211 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 104211 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 165333 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 165333 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 104631 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 104631 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 84576 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 84576 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 84576 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 84576 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 72214 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 72214 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 104647 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 104647 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 72577 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 72577 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 190658 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 190658 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 81814 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 81814 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 75712 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 75712 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 102039 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 102039 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 91578 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 91578 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 97549 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 97549 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 161658 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 161658 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 101383 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 101383 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 161658 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 161658 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 80512 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 80512 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 80580 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 80580 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 199344 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 199344 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 14987 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 14987 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 15117 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 15117 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 81328 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 81328 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 162317 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 162317 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 69317 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 69317 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 75721 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 75721 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 91981 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 91981 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 101383 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 101383 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 179228 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 179228 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 80497 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 80497 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 101870 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 101870 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 80481 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 80481 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 100547 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 100547 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 72199 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 72199 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 81977 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 81977 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 168136 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 168136 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 194638 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 194638 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 72195 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 72195 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 161627 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 161627 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 161627 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 161627 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 69340 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 69340 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 75702 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 75702 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 168117 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 168117 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 194720 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 194720 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 182246 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 182246 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 100516 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 100516 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 81996 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 81996 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 26062 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 26062 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 72216 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 72216 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 190611 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 190611 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 72586 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 72586 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 10514 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 10514 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 10514 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 149135 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 149135 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 10514 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 10514 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 10514 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 10514 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 10514 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 10514 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 194587 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 194587 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 75728 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 75728 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 81995 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 81995 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 90355 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 90355 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 72203 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 72203 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 72559 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 72559 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 101446 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 101446 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 149124 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 149124 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 101446 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 101446 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 149124 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 149124 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 97414 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 97414 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 81980 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 81980 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 101469 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 101469 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 101469 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 101469 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 194806 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 194806 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 101470 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 101470 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 161953 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 161953 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 101470 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 101470 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 177363 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 177363 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 81325 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 81325 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 14643 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 14643 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 168338 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 168338 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 87370 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 87370 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 194720 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 194720 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 195224 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 195224 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 77786 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 77786 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 25861 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 25861 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 72514 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 72514 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 92857 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 92857 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 104466 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 104466 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 92857 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 92857 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 77784 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 77784 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 65245 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 65245 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 65245 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 65245 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 19435 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 19435 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 19435 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 8805 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 8805 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 8805 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 81320 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 81320 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 93004 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 93004 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 160310 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 160310 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 101708 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 101708 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 93004 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 93004 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 160310 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 160310 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 162317 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 162317 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 104570 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 104570 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 14622 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 14622 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 81318 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 81318 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 8803 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 8803 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 8803 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 8803 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 92876 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 92876 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 77785 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 77785 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 8805 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 8805 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 8805 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 65245 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 65245 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 102215 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 102215 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 92876 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 92876 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 92817 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 92817 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 90342 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 90342 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 90356 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 90356 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 167916 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 167916 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 72566 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 72566 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 15117 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 15117 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 160485 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 160485 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 182246 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 182246 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 160485 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 160485 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 69335 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 69335 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 10547 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 10547 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 10547 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 165348 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 165348 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 151328 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 151328 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 91852 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 91852 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 175716 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 175716 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 81320 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 81320 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 81984 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 81984 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 72568 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 72568 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 189053 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 189053 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 128615 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 128615 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 97474 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 97474 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 80491 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 80491 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 81999 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 81999 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 108091 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 108091 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 161166 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 161166 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 90343 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 90343 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 80504 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 80504 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 81327 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 81327 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 81328 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 81328 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 189053 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 189053 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 72578 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 72578 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 180478 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 180478 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 177363 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 177363 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 168423 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 168423 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 180044 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 180044 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 72550 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 72550 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 72552 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 72552 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 72192 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 72192 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 72209 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 72209 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 75714 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 75714 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 104587 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 104587 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 72515 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 72515 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 148151 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 148151 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 148151 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 148151 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 148151 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 148151 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 128629 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 128629 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 81317 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 81317 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 75726 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 75726 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 69318 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 69318 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 104840 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 104840 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 82005 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 82005 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 162018 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 162018 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 100424 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 100424 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 81322 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 81322 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 72585 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 72585 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 176244 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 176244 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 75734 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 75734 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 82003 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 82003 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 194637 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 194637 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 86535 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 86535 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 168304 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 168304 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 100584 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 100584 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 86535 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 86535 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 180044 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 180044 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 168247 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 168247 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 65649 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 65649 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 86652 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 86652 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 176118 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 176118 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 90359 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 90359 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 75735 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 75735 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 80497 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 80497 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 181363 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 181363 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 72567 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 72567 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 92817 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 92817 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 80499 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 80499 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 81325 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 81325 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 8802 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 8802 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 8802 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 8802 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 8802 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 8802 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 179430 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 179430 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 84415 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 84415 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 182996 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 182996 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 104392 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 104392 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 81326 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 81326 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 72523 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 72523 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 180478 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 180478 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 69334 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 69334 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 86652 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 86652 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 91853 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 91853 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 144988 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 144988 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 190391 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 190391 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 149147 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 149147 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 166834 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 166834 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 175786 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 175786 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 72196 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 72196 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 104385 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 104385 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 81979 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 81979 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 81997 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 81997 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 149147 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 149147 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 81985 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 81985 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 146491 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 146491 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 146491 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 146491 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 90346 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 90346 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 104646 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 104646 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 162433 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 162433 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 195241 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 195241 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 69336 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 69336 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 81993 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 81993 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 90344 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 90344 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 25861 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 25861 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 102310 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 102310 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 168218 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 168218 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 69339 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 69339 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 69346 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 69346 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 128617 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 128617 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 72526 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 72526 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 102512 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 102512 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 75732 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 75732 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 168183 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 168183 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 194587 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 194587 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 80496 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 80496 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 152264 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 152264 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 195226 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 195226 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 195563 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 195563 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 102213 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 102213 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 194330 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 194330 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 80500 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 80500 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 104464 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 104464 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 160243 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 160243 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 194841 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 194841 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 81315 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 81315 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 190685 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 190685 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 162018 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 162018 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 77793 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 77793 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 84399 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 84399 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 65231 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 65231 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 77790 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 77790 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 84423 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 84423 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 82004 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 82004 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 86535 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 86535 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 75700 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 75700 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 69321 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 69321 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 91933 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 91933 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 150921 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 150921 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 168306 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 168306 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 84398 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 84398 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 194544 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 194544 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 100586 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 100586 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 161571 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 161571 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 72201 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 72201 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 72217 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 72217 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 81309 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 81309 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 14687 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 14687 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 75719 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 75719 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 173638 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 173638 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 10547 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 10547 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 10547 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 72211 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 72211 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 82002 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 82002 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 168312 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 168312 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 90337 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 90337 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 92082 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 92082 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 100584 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 100584 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 72208 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 72208 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 145719 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 145719 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 145719 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 145719 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 81990 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 81990 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 100547 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 100547 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 153978 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 153978 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 81982 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 81982 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 81992 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 81992 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 82000 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 82000 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 81991 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 81991 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 75735 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 75735 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 194638 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 194638 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 190657 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 190657 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 190658 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 190658 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 195711 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 195711 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 195724 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 195724 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 8802 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 8802 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 8802 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 81322 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 81322 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 162130 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 162130 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 65244 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 65244 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 69319 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 69319 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 195014 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 195014 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 81318 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 81318 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 26100 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 26100 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 65238 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 65238 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 90354 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 90354 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 75715 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 75715 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 91968 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 91968 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 143158 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 143158 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 168311 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 168311 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 128630 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 128630 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 14654 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 14654 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 81974 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 81974 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 104392 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 104392 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 168213 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 168213 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 179676 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 179676 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 75727 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 75727 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 102214 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 102214 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 81981 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 81981 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 75716 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 75716 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 161471 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 161471 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 161471 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 161471 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 90357 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 90357 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 69318 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 69318 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 72528 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 72528 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 69345 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 69345 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 14608 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 14608 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 72215 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 72215 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 81319 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 81319 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 72564 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 72564 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 93005 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 93005 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 93005 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 93005 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 75709 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 75709 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 90360 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 90360 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 97321 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 97321 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 128610 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 128610 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 100737 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 100737 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 194806 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 194806 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 179474 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 179474 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 190029 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 190029 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 75735 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 75735 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 192936 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 192936 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 72553 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 72553 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 72572 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 72572 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 72576 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 72576 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 72579 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 72579 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 80505 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 80505 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 77791 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 77791 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 145001 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 145001 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 194653 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 194653 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 77788 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 77788 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 102114 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 102114 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 92816 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 92816 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 92816 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 92816 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 69340 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 69340 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 8803 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 8803 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 8803 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 8803 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 160311 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 160311 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 90358 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 90358 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 10547 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 10547 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 10547 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 65653 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 65653 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 65653 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 65653 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 149130 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 149130 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 69337 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 69337 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 69348 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 69348 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 14470 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 14470 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 168330 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 168330 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 100586 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 100586 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 69320 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 69320 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 90336 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 90336 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 168414 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 168414 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 80506 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 80506 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 175757 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 175757 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 69338 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 69338 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 75736 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 75736 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 190766 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 190766 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 190766 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 190766 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 81983 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 81983 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 14751 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 14751 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 128611 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 128611 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 84513 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 84513 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 84513 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 84513 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 104657 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 104657 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 145997 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 145997 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 145997 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 145997 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 168324 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 168324 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 187875 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 187875 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 77113 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 77113 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 100516 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 100516 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 195224 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 195224 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 190391 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 190391 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 199344 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 199344 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 72517 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 72517 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 160311 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 160311 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 84413 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 84413 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 81323 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 81323 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 104303 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 104303 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 65246 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 65246 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 92802 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 92802 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 66972 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 66972 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 66972 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 66972 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 66972 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 66972 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 149418 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 149418 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 151451 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 151451 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 80508 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 80508 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 75701 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 75701 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 161166 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 161166 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 86679 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 86679 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 152532 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 152532 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 75713 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 75713 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 86304 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 86304 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 86679 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 86679 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 86304 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 86304 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 154568 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 154568 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 72527 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 72527 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 75703 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 75703 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 85667 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 85667 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 187875 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 187875 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 160485 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 160485 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 85667 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 85667 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 176615 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 176615 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 176615 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 176615 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 81323 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 81323 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 128616 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 128616 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 10169 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 10169 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 10169 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 80503 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 80503 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 14489 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 14489 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 15193 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 15193 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 65268 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 65268 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 72513 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 72513 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 92802 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 92802 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 145083 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 145083 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 162320 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 162320 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 77787 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 77787 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 162523 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 162523 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 80498 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 80498 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 69344 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 69344 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 75705 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 75705 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 75704 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 75704 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 75710 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 75710 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 81973 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 81973 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 75725 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 75725 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 193474 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 193474 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 81972 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 81972 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 87896 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 87896 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 87896 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 87896 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 75707 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 75707 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 75708 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 75708 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 101870 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 101870 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 75907 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 75907 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 90750 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 90750 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 75900 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 75900 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 75889 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 75889 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 75909 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 75909 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 75906 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 75906 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 82004 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 82004 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 75897 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 75897 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 75899 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 75899 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 75901 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 75901 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 75903 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 75903 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 75904 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 75904 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 75905 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 75905 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 75902 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 75902 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 75908 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 75908 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 75898 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 75898 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 17501 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 17501 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 17475 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 17475 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 17474 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 17474 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 17465 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 17465 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 17502 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 17502 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 17465 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 17465 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 75898 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 75898 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 75901 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 75901 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 90749 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 90749 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 90749 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 90749 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 90750 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 90750 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 75893 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 75893 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 75893 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 75893 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 17329 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 17329 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 17422 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 17422 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 17422 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 17422 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 17368 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 17368 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 195048 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 195048 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 195048 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 195048 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 195048 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 195048 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 17422 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 17422 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 161426 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 161426 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 17500 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 17500 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 17465 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 17465 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 75892 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 75892 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 161426 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 161426 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 108464 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 108464 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 75889 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 75889 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 75890 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 75890 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 201374 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 201374 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 201374 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 201374 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 201374 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 201374 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 17369 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 17369 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 17422 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 17422 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 17347 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 17347 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 17560 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 17560 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 17544 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 17544 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 75895 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 75895 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 75900 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 75900 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 108563 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 108563 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 108563 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 108563 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 108563 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 108563 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 201373 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 201373 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 101379 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 101379 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 101379 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 101379 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 17464 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 17464 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 17560 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 17560 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 17401 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 17401 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 17559 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 17559 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 75902 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 75902 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 75889 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 75889 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 75894 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 75894 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 108620 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 108620 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 75906 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 75906 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 75907 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 75907 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 17331 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 17331 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 108279 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 108279 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 108279 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 108279 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 75891 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 75891 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 17559 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 17559 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 17330 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 17330 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 17500 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 17500 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 75894 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 75894 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 108279 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 108279 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 75896 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 75896 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 201514 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 201514 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 201514 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 201514 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 108464 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 108464 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 75899 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 75899 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 17476 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 17476 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 17563 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 17563 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 17472 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 17472 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 17500 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 17500 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 101571 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 101571 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 101571 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 101571 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 108142 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 108142 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 108142 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 108142 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 108142 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 108142 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 196205 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 196205 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 201712 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 201712 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 17330 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 17330 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 17559 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 17559 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 17559 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 17559 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 17470 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 17470 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 17565 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 17565 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 17578 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 17578 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 75904 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 75904 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 75891 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 75891 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 108432 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 108432 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 108432 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 108432 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 169333 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 169333 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 108432 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 108432 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 201537 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 201537 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 201605 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 201605 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 201537 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 201537 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 201605 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 201605 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 201537 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 201537 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 201605 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 201605 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 108456 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 108456 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 108456 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 108456 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 108456 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 108456 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 17564 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 17564 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 10289 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 10289 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 10289 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 10289 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 10289 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 10289 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 17471 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 17471 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 17505 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 17505 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 10289 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 10289 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 10289 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 17578 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 17578 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 174931 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 174931 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 174931 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 174931 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 174931 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 174931 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 108538 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 108538 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 108538 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 108538 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 108538 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 108538 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 201552 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 201552 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 201552 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 201552 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 201552 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 201552 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 201552 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 201552 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 195069 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 195069 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 195069 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 195069 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 201498 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 201498 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 201498 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 201498 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 195069 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 195069 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 201498 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 201498 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 197987 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 197987 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 108661 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 108661 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 108661 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 108661 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 75909 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 75909 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 75897 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 75897 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 75905 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 75905 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 75890 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 75890 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 17500 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 17500 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 17329 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 17329 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 17518 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 17518 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 17518 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 17518 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 195407 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 195407 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 195407 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 195407 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 195407 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 195407 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 211064 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 211064 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 75896 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 75896 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 211064 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 211064 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 195933 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 195933 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 195933 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 195933 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 195933 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 195933 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 17547 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 17547 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 201326 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 201326 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 201326 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 201326 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 201326 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 201326 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 108353 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 108353 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 161651 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 161651 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 75892 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 75892 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 90750 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 90750 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 90753 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 90753 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 90753 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 90753 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 161651 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 161651 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 195494 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 195494 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 201632 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 201632 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 195494 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 195494 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 201632 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 201632 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 75895 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 75895 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 17530 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 17530 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 17544 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 17544 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 195494 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 195494 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 201632 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 201632 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 75903 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 75903 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 75908 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 75908 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 201485 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 201485 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 201485 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 201485 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 201485 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 201485 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 9912 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 8772 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 8772 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 8772 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 8772 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 7613 0 None -28 3 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
769 7613 0 None -28 3 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15207250
11192346 8805 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 8805 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 8805 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 8802 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 8802 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 8802 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 7640 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15207250
759 7654 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
759 7654 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9276730
759 7654 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9346309
11597 7461 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 7461 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 7461 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 7334 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 7334 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 7334 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 7657 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
770 7615 0 None -7 2 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
770 7615 0 None -7 2 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9276730
68764898 7459 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 7459 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 7459 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 7625 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10770925
771 7625 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
771 7625 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15207250
771 7625 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9276730
771 7625 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9346309
775 7637 0 None -316 2 Human 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15207250
10000456 10162 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 10162 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 10162 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 10749 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
10008367 8803 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 8803 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 8803 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 8803 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 8718 0 None 12 2 Human 8.3 pIC50 None 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9789057
5071702 10165 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 10165 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 9246 0 None - 1 Human 8.8 pIC50 None 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600978
486830 10774 0 None 6 5 Human 9.1 pIC50 None 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9287217
768 10774 0 None 6 5 Human 9.1 pIC50 None 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9287217


Get vendors


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

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

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

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
183790 10514 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 10514 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 10514 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 9911 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 9911 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 9911 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 9911 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 9911 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 10514 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 10514 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 10514 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 9911 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 9911 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 9911 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 9911 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 9911 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 116593 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 116593 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 116595 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 116595 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 102474 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 102474 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 7459 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 7459 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 7459 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 10514 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 10514 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 10514 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 117903 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 117903 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 188239 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 188239 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 14816 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 14816 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 116593 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 116593 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 194755 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 194755 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 15078 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 15078 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 177880 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 177880 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 128017 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 128017 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 92743 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 92743 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 128015 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 128015 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 14886 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 14886 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 116594 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 116594 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 8805 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 8805 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 8805 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 128015 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 128015 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 128012 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 128012 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 189539 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 189539 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 116591 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 116591 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 102049 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 102049 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 102245 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 102245 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 7460 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 7460 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 7460 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 7460 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 7460 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 7460 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 116588 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 116588 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 7459 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 7459 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 7459 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 7459 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 7459 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 7459 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 7461 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 7461 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 7461 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 14885 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 14885 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 15121 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 15121 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 14885 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 14885 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 150143 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 150143 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 14885 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 14885 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 128003 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 128003 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 84399 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 84399 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 178743 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 178743 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 26100 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 26100 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 194587 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 194587 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 116595 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 116595 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 101768 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 101768 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 162233 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 162233 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 162447 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 162447 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 14886 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 14886 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 14886 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 14886 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 77783 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 77783 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 128012 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 128012 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 116592 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 116592 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 7460 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 7460 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 7460 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 7460 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 7460 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 7460 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 128002 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 128002 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 84423 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 84423 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 116587 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 116587 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 116591 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 116591 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 116596 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 116596 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 194274 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 194274 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 14885 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 14885 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 116597 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 116597 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 195207 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 195207 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 195238 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 195238 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 188239 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 188239 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 173663 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 173663 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 92551 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 92551 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 160025 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 160025 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 92083 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 92083 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 7460 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 7460 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 7460 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 77113 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 77113 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 200312 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 200312 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 178384 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 178384 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 104666 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 104666 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 160243 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 160243 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 92082 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 92082 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 199889 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 199889 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 194274 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 194274 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 117899 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 117899 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 189053 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 189053 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 187694 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 187694 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 187872 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 187872 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 149038 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 149038 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 128013 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 128013 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 128010 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 128010 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 116585 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 116585 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 116585 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 116585 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 92827 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 92827 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 160308 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 160308 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 194637 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 194637 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 84415 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 84415 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 84424 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 84424 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 178234 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 178234 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 175547 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 175547 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 26100 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 26100 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 26101 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 26101 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 93357 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 93357 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 91675 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 91675 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 189053 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 189053 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 179740 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 179740 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 101886 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 101886 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 102376 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 102376 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 162122 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 162122 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 162177 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 162177 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 81981 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 81981 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 80506 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 80506 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 72195 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 72195 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 100158 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 100158 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 100567 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 100567 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 148853 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 148853 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 84682 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 84682 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 81317 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 81317 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 81326 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 81326 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 25861 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 25861 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 96601 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 96601 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 7659 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 7659 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 7659 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 200351 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 77787 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 77787 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 65231 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 65231 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 65249 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 65249 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 77792 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 77792 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 187875 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 187875 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 80477 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 80477 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 80486 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 80486 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 90351 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 90351 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 161704 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 161704 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 10169 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 10169 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 10169 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 10289 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 10289 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 10289 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 133137 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 133137 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 72191 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 72191 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 86494 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 86494 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 14654 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 14654 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 100735 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 100735 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 84827 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 84827 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 212602 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 212602 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 72389 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 72389 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 176201 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 176201 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 77891 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 77891 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 131153 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 131153 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 10547 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 10547 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 10547 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 84418 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 84418 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 155028 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 155028 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 25719 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 25719 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 133106 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 133106 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 187875 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 187875 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 27697 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 27697 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 80590 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 80590 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 122443 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 122443 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 81992 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 81992 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 133091 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 133091 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 97549 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 97549 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 97549 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 97549 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 21984 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 21984 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 93183 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 93183 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 85183 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 85183 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 98757 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 98757 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 29309 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 29309 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 117882 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 117882 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 137425 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 137425 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 136179 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 136179 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 84397 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 84397 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 80587 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 80587 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 144099 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 144099 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 65246 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 65246 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 81309 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 81309 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 81327 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 81327 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 104464 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 104464 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 100516 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 100516 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 117888 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 117888 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 65451 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 65451 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 69318 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 69318 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 65235 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 65235 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 65445 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 65445 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 65450 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 65450 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 112037 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 112037 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 72218 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 72218 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 100260 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 100260 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 100548 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 100548 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 100738 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 100738 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 161556 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 161556 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 30850 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 30850 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 93164 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 93164 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 161559 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 161559 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 146323 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 146323 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 148255 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 148255 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 176262 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 176262 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 72891 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 72891 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 73107 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 73107 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 72780 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 72780 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 73900 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 73900 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 7186 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 7186 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 7186 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 7186 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 7186 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 159980 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 159980 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 133098 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 133098 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 100765 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 100765 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 186738 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 186738 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 14987 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 14987 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 128616 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 128616 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 21981 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 21981 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 153605 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 153605 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 14643 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 14643 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 26315 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 26315 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 100248 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 100248 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 144250 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 144250 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 104587 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 104587 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 161871 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 161871 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 95848 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 95848 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 65254 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 65254 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 102214 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 102214 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 104465 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 104465 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 112006 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 112006 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 14751 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 14751 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 194805 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 194805 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 81976 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 81976 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 165840 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 165840 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 27258 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 27258 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 190766 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 190766 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 72513 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 72513 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 72515 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 72515 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 72516 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 72516 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 77284 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 77284 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 77114 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 77114 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 145652 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 145652 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 102020 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 102020 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 65452 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 65452 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 7659 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 7659 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 7659 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 187875 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 187875 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 65444 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 65444 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 195065 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 195065 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 190391 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 190391 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 7659 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 7659 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 7659 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 187875 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 187875 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 65458 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 65458 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 137407 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 137407 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 136188 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 136188 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 72521 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 72521 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 156625 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 156625 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 26021 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 26021 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 100323 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 100323 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 100501 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 100501 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 100742 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 100742 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 143144 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 143144 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 26865 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 26865 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 96600 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 96600 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 84751 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 84751 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 72194 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 72194 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 194470 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 194470 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 100312 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 100312 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 161824 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 161824 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 71541 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 71541 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 100953 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 100953 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 163621 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 163621 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 162130 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 162130 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 29386 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 29386 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 112018 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 112018 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 137431 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 137431 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 21983 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 21983 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 153606 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 153606 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 81974 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 81974 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 194331 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 194331 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 194543 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 194543 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 194332 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 194332 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 80588 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 80588 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 124378 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 124378 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 84422 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 84422 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 93181 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 93181 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 86562 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 86562 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 175073 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 175073 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 93157 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 93157 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 112029 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 112029 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 87205 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 87205 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 81308 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 81308 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 92802 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 92802 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 101062 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 101062 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 26437 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 26437 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 81814 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 81814 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 30737 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 30737 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 28187 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 28187 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 92905 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 92905 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 117881 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 117881 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 87925 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 87925 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 133092 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 133092 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 137401 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 137401 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 8805 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 8805 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 8805 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 72207 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 72207 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 72517 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 72517 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 72523 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 72523 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 72575 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 72575 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 86849 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 86849 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 92841 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 92841 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 84533 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 84533 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 93023 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 93023 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 93110 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 93110 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 65447 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 65447 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 69321 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 69321 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 154568 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 154568 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 128005 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 128005 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 194653 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 194653 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 92790 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 92790 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 150145 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 150145 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 65267 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 65267 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 65456 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 65456 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 75729 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 75729 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 137404 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 137404 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 137433 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 137433 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 93160 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 93160 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 77110 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 77110 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 65442 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 65442 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 100263 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 100263 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 173187 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 173187 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 100954 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 100954 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 92083 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 92083 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 112032 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 112032 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 100325 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 100325 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 72902 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 72902 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 84421 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 84421 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 14489 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 14489 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 27527 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 27527 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 75711 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 75711 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 145204 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 145204 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 92904 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 92904 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 69317 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 69317 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 190347 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 190347 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 75731 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 75731 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 84417 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 84417 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 104705 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 104705 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 29464 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 29464 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 133099 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 133099 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 117887 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 117887 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 137401 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 137401 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 136187 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 136187 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 176118 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 176118 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 77789 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 77789 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 92910 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 92910 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 165083 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 165083 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 117880 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 117880 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 160026 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 160026 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 194011 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 194011 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 175686 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 175686 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 65448 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 65448 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 65460 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 65460 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 72530 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 72530 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 161620 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 161620 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 85177 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 85177 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 133080 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 133080 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 72582 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 72582 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 100848 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 100848 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 73767 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 73767 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 199889 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 199889 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 15116 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 15116 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 133132 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 133132 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 161897 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 161897 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 133083 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 133083 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 81989 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 81989 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 92904 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 92904 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 133086 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 133086 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 145875 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 145875 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 133104 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 133104 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 124221 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 124221 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 137408 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 137408 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 93355 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 93355 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 93356 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 93356 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 72214 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 72214 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 72553 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 72553 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 148461 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 148461 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 186395 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 186395 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 187905 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 187905 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 65239 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 65239 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 92816 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 92816 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 175483 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 175483 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 100547 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 100547 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 127999 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 127999 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 95964 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 95964 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 153089 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 153089 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 65465 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 65465 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 69348 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 69348 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 92840 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 92840 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 69345 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 69345 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 69334 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 69334 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 69336 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 69336 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 187875 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 187875 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 137409 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 137409 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 93154 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 93154 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 144107 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 144107 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 100329 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 100329 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 100506 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 100506 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 161671 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 161671 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 84812 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 84812 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 123825 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 123825 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 93167 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 93167 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 72935 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 72935 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 73472 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 73472 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 73729 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 73729 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 73174 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 73174 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 100539 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 100539 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 100883 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 100883 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 84686 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 84686 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 100261 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 100261 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 15120 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 15120 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 112031 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 112031 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 133118 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 133118 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 93177 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 93177 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 195208 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 195208 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 104657 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 104657 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 133097 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 133097 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 190856 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 190856 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 200044 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 200044 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 102311 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 102311 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 200044 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 200044 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 80583 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 80583 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 128009 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 128009 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 187875 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 187875 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 136179 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 136179 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 136183 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 136183 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 93151 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 93151 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 81982 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 81982 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 90355 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 90355 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 72573 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 72573 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 84605 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 84605 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 190029 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 190029 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 148796 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 148796 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 92734 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 92734 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 160462 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 160462 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 117876 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 117876 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 117879 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 117879 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 197873 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 197873 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 133140 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 133140 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 161448 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 161448 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 80488 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 80488 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 87274 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 87274 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 100319 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 100319 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 100926 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 100926 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 100928 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 100928 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 87858 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 87858 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 144208 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 144208 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 133085 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 133085 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 133112 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 133112 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 133113 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 133113 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 133119 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 133119 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 72243 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 72243 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 195467 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 195467 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 117885 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 117885 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 31286 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 31286 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 102236 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 102236 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 175637 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 175637 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 102277 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 102277 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 190344 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 190344 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 97415 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 97415 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 97415 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 97415 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 144219 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 144219 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 93368 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 93368 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 8805 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 8805 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 8805 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 81984 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 81984 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 81997 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 81997 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 65246 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 65246 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 65267 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 65267 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 80489 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 80489 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 25812 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 25812 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 149137 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 149137 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 65449 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 65449 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 92875 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 92875 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 93004 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 93004 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 10547 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 10547 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 10547 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 65459 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 65459 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 65461 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 65461 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 148853 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 148853 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 133122 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 133122 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 69338 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 69338 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 133139 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 133139 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 136179 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 136179 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 93166 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 93166 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 81972 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 81972 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 90335 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 90335 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 72564 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 72564 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 100456 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 100456 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 161703 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 161703 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 124229 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 124229 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 7659 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 7659 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 7659 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 80586 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 80586 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 100511 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 100511 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 123342 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 123342 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 73473 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 73473 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 130679 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 130679 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 81987 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 81987 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 194690 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 194690 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 165333 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 165333 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 15009 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 15009 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 194302 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 194302 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 15008 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 15008 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 65233 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 65233 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 85009 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 85009 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 194302 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 194302 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 137410 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 137410 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 112012 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 112012 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 90342 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 90342 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 90354 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 90354 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 72579 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 72579 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 65228 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 65228 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 158105 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 158105 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 81311 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 81311 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 77783 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 77783 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 65266 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 65266 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 69335 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 69335 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 112019 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 112019 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 101870 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 101870 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 80476 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 80476 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 77298 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 77298 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 85009 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 85009 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 103479 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 103479 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 101870 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 101870 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 100892 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 100892 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 117895 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 117895 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 85009 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 85009 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 95397 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 95397 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 93150 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 93150 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 72190 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 72190 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 100774 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 100774 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 95397 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 95397 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 128612 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 128612 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 98756 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 98756 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 21982 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 21982 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 158657 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 158657 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 16552 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 133095 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 133095 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 173074 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 173074 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 26062 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 26062 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 92910 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 92910 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 137401 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 137401 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 200012 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 200012 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 200045 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 200045 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 74641 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 74641 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 15232 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 15232 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 93362 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 93362 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 93382 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 93382 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 75726 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 75726 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 80484 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 80484 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 80485 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 80485 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 90343 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 90343 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 72566 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 72566 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 72578 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 72578 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 92762 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 92762 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 175637 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 175637 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 102215 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 102215 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 100584 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 100584 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 153978 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 153978 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 80484 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 80484 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 65252 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 65252 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 69347 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 69347 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 133103 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 133103 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 112006 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 112006 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 75723 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 75723 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 90362 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 90362 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 72188 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 72188 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 100328 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 100328 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 100502 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 100502 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 117898 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 117898 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 101287 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 101287 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 73045 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 73045 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 130586 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 130586 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 87830 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 87830 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 93005 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 93005 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 194173 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 194173 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 194173 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 194173 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 133087 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 133087 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 179375 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 179375 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 136181 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 136181 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 101847 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 101847 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 161970 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 161970 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 189053 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 189053 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 117889 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 117889 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 195226 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 195226 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 80499 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 80499 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 25881 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 25881 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 116586 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 116586 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 128014 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 128014 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 128016 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 128016 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 25861 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 25861 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 25881 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 25881 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 175578 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 175578 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 101708 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 101708 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 77793 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 77793 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 190658 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 190658 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 195563 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 195563 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 80502 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 80502 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 128007 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 128007 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 128010 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 128010 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 153895 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 153895 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 116585 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 116585 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 77785 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 77785 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 148795 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 148795 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 8802 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 8802 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 8802 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 128007 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 128007 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 128014 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 128014 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 179474 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 179474 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 7461 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 7461 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 7461 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 84413 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 84413 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 65245 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 65245 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 65245 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 65245 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 187655 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 187655 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 26101 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 26101 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 64947 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 64947 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 194330 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 194330 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 93381 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 93381 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 144099 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 144099 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 186395 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 186395 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 137417 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 137417 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 136186 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 136186 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 101921 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 101921 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 102231 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 102231 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 162025 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 162025 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 93155 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 93155 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 80514 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 80514 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 72215 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 72215 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 159907 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 159907 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 92723 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 92723 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 92801 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 92801 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 92803 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 92803 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 102212 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 102212 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 104466 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 104466 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 100424 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 100424 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 128008 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 128008 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 153091 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 153091 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 173545 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 173545 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 69344 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 69344 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 93144 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 93144 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 93165 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 93165 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 72531 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 72531 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 72583 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 72583 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 100294 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 100294 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 173134 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 173134 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 161705 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 161705 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 96697 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 96697 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 96697 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 96697 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 96697 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 96697 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 100131 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 100131 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 100846 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 100846 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 29866 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 29866 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 87384 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 87384 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 104211 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 104211 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 159837 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 159837 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 152546 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 152546 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 152546 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 152546 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 162433 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 162433 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 72532 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 72532 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 93371 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 93371 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 112008 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 112008 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 7865 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 7865 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 7865 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 75734 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 75734 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 82002 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 82002 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 72196 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 72196 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 72534 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 72534 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 104385 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 104385 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 194837 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 194837 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 194458 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 194458 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 93163 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 93163 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 72212 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 72212 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 144163 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 144163 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 152267 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 152267 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 154409 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 154409 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 100775 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 100775 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 73985 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 73985 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 104816 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 104816 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 65229 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 65229 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 117901 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 117901 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 87630 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 87630 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 80579 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 80579 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 163419 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 163419 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 84576 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 84576 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 76154 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 76154 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 93358 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 93358 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 93361 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 93361 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 93147 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 93147 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 72216 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 72216 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 199413 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 199413 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 65250 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 65250 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 112001 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 112001 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 137416 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 137416 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 90339 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 90339 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 84576 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 84576 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 122027 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 122027 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 161407 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 161407 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 161407 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 161407 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 100811 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 100811 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 117886 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 117886 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 28513 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 28513 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 133121 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 133121 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 73840 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 73840 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 161599 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 161599 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 98749 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 98749 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 65247 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 65247 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 14608 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 14608 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 162018 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 162018 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 190824 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 190824 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 92904 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 92904 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 92839 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 92839 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 128008 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 128008 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 93375 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 93375 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 75727 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 75727 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 93153 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 93153 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 72584 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 72584 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 157090 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 157090 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 100586 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 100586 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 100693 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 100693 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 104392 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 104392 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 112033 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 112033 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 137418 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 137418 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 72561 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 72561 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 100682 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 100682 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 193988 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 193988 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 100740 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 100740 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 29388 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 29388 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 123518 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 123518 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 194453 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 194453 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 134066 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 134066 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 100771 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 100771 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 26245 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 26245 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 10514 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 10514 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 10514 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 146911 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 146911 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 160313 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 160313 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 86818 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 86818 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 65255 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 65255 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 93176 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 93176 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 133094 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 133094 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 194274 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 194274 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 162522 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 162522 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 200045 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 200045 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 97725 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 97725 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 97725 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 97725 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 93148 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 93148 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 136185 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 136185 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 80580 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 80580 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 161817 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 161817 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 65449 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 65449 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 80481 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 80481 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 80510 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 80510 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 72219 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 72219 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 161621 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 161621 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 102484 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 102484 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 73818 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 73818 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 80479 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 80479 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 104544 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 104544 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 128610 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 128610 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 195728 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 195728 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 86711 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 86711 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 214620 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 214620 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 93146 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 93146 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 144358 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 144358 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 128005 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 128005 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 75706 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 75706 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 75714 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 75714 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 72204 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 72204 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 72217 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 72217 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 87370 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 87370 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 84216 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 84216 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 176154 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 176154 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 69337 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 69337 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 133126 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 133126 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 90341 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 90341 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 100681 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 100681 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 100741 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 100741 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 133078 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 133078 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 133079 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 133079 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 133108 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 133108 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 133116 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 133116 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 65439 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 65439 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 144312 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 144312 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 100406 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 100406 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 82001 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 82001 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 194011 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 194011 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 81999 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 81999 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 162317 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 162317 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 160311 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 160311 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 176244 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 176244 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 100508 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 100508 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 27671 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 27671 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 72524 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 72524 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 100772 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 100772 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 178148 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 178148 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 93158 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 93158 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 144314 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 144314 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 137406 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 137406 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 101864 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 101864 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 81996 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 81996 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 104816 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 104816 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 93360 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 93360 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 10514 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 10514 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 10514 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 111998 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 111998 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 10514 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 10514 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 10514 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 10514 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 10514 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 10514 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 81986 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 81986 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 80493 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 80493 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 90346 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 90346 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 72200 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 72200 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 72527 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 72527 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 72551 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 72551 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 77299 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 77299 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 92905 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 92905 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 10514 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 10514 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 10514 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 117890 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 117890 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 10514 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 10514 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 10514 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 10514 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 10514 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 10514 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 195225 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 195225 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 65244 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 65244 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 65251 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 65251 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 193988 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 193988 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 75728 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 75728 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 90349 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 90349 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 123288 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 123288 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 15089 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 15089 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 133109 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 133109 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 133110 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 133110 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 133130 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 133130 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 133134 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 133134 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 160313 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 160313 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 112013 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 112013 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 80508 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 80508 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 72574 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 72574 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 145652 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 145652 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 190766 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 190766 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 149124 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 149124 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 65232 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 65232 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 65462 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 65462 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 69342 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 69342 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 92904 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 92904 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 10514 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 10514 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 10514 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 194451 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 194451 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 100587 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 100587 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 190766 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 190766 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 133141 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 133141 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 92578 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 92578 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 87207 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 87207 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 26254 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 26254 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 130755 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 130755 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 80591 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 80591 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 133144 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 133144 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 90347 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 90347 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 21977 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 21977 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 14754 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 14754 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 144058 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 144058 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 98750 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 98750 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 87925 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 87925 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 14687 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 14687 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 112003 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 112003 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 72552 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 72552 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 72576 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 72576 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 72577 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 72577 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 117882 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 117882 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 69339 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 69339 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 199937 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 199937 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 173638 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 173638 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 93173 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 93173 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 72491 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 72491 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 100358 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 100358 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 77287 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 77287 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 100891 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 100891 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 161781 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 161781 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 65256 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 65256 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 144212 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 144212 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 86818 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 86818 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 187655 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 187655 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 136182 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 136182 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 187694 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 187694 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 173657 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 173657 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 65245 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 65245 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 65245 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 65245 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 92735 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 92735 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 149035 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 149035 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 175663 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 175663 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 65245 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 65245 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 199889 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 199889 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 128018 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 128018 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 84412 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 84412 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 199344 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 199344 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 92857 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 92857 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 65230 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 65230 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 65463 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 65463 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 65268 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 65268 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 77784 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 77784 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 77794 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 77794 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 65457 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 65457 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 102114 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 102114 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 128004 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 128004 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 128013 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 128013 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 92856 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 92856 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 81324 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 81324 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 81328 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 81328 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 80491 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 80491 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 65268 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 65268 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 194841 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 194841 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 82004 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 82004 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 15090 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 15090 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 93004 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 93004 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 92810 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 92810 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 160310 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 160310 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 65446 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 65446 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 92856 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 92856 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 80497 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 80497 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 80497 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 80497 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 81322 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 81322 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 104817 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 104817 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 8802 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 8802 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 8802 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 194689 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 194689 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 8802 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 8802 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 8802 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 80501 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 80501 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 80511 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 80511 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 179228 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 179228 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 196573 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 196573 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 195224 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 195224 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 65245 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 65245 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 186303 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 186303 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 92876 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 92876 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 92829 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 92829 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 189053 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 189053 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 102473 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 102473 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 86535 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 86535 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 112034 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 112034 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 173638 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 173638 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 72568 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 72568 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 155026 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 155026 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 160485 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 160485 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 199937 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 199937 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 117897 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 117897 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 112016 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 112016 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 161953 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 161953 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 161262 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 161262 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 161262 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 161262 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 124081 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 124081 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 100540 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 100540 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 73416 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 73416 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 144166 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 144166 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 104778 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 104778 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 123868 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 123868 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 104817 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 104817 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 14622 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 14622 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 81312 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 81312 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 101904 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 101904 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 133111 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 133111 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 104647 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 104647 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 112011 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 112011 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 80475 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 80475 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 72206 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 72206 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 72585 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 72585 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 72586 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 72586 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 65248 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 65248 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 69320 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 69320 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 90338 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 90338 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 77286 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 77286 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 100247 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 100247 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 100009 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 100009 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 162082 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 162082 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 101223 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 101223 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 14856 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 14856 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 133107 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 133107 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 14490 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 14490 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 174248 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 174248 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 117884 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 117884 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 112011 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 112011 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 112010 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 112010 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 82003 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 82003 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 72203 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 72203 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 72528 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 72528 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 92904 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 92904 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 84575 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 84575 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 65443 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 65443 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 190611 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 190611 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 92828 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 92828 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 133081 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 133081 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 112016 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 112016 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 137419 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 137419 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 160727 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 160727 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 160727 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 160727 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 161187 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 161187 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 86815 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 86815 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 96696 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 96696 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 101870 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 101870 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 175490 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 175490 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 144100 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 144100 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 133136 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 133136 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 112034 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 112034 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 112013 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 112013 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 128006 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 128006 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 137434 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 137434 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 72520 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 72520 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 117892 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 117892 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 128631 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 128631 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 153433 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 153433 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 93175 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 93175 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 153433 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 153433 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 72931 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 72931 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 128000 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 128000 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 93174 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 93174 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 77301 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 77301 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 77116 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 77116 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 65253 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 65253 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 133090 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 133090 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 80577 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 80577 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 77112 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 77112 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 117894 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 117894 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 26940 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 26940 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 27118 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 27118 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 100813 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 100813 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 161180 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 161180 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 72967 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 72967 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 144334 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 144334 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 146036 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 146036 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 100099 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 100099 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 15147 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 15147 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 144028 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 144028 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 87908 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 87908 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 112008 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 112008 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 81985 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 81985 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 72192 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 72192 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 81304 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 81304 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 117902 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 117902 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 199413 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 199413 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 80478 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 80478 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 149124 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 149124 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 15021 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 15021 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 93180 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 93180 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 93364 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 93364 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 90353 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 90353 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 72211 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 72211 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 72533 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 72533 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 144248 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 144248 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 65242 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 65242 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 92836 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 92836 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 159980 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 159980 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 194458 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 194458 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 100321 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 100321 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 161908 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 161908 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 92192 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 92192 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 65441 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 65441 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 104507 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 104507 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 194205 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 194205 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 194205 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 194205 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 128618 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 128618 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 128617 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 128617 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 112003 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 112003 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 81975 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 81975 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 90356 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 90356 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 77281 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 77281 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 87830 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 87830 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 146911 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 146911 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 161166 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 161166 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 167916 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 167916 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 133125 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 133125 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 137413 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 137413 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 133932 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 133932 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 72519 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 72519 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 77111 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 77111 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 117900 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 117900 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 27542 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 27542 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 144102 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 144102 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 144206 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 144206 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 77285 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 77285 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 93383 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 93383 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 84416 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 84416 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 87896 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 87896 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 65455 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 65455 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 161557 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 161557 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 190766 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 190766 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 100773 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 100773 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 163568 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 163568 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 29942 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 29942 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 93373 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 93373 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 112036 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 112036 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 91674 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 91674 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 86535 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 86535 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 101836 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 101836 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 65266 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 65266 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 65454 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 65454 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 131225 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 131225 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 80474 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 80474 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 72193 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 72193 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 100204 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 100204 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 27525 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 27525 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 133102 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 133102 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 112033 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 112033 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 189053 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 189053 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 180862 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 180862 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 136184 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 136184 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 101881 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 101881 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 80495 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 80495 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 176118 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 176118 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 102482 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 102482 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 92817 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 92817 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 160021 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 160021 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 194274 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 194274 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 117877 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 117877 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 96112 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 96112 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 96656 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 96656 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 96697 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 96697 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 153115 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 153115 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 102211 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 102211 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 65453 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 65453 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 77786 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 77786 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 65464 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 65464 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 200350 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 200350 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 186303 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 186303 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 80513 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 80513 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 81323 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 81323 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 69319 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 69319 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 187872 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 187872 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 65234 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 65234 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 161985 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 161985 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 194500 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 194500 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 194386 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 194386 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 7459 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 7459 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 7459 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 80498 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 80498 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 80498 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 80498 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 128009 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 128009 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 190657 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 190657 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 77791 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 77791 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 128004 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 128004 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 93359 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 93359 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 137428 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 137428 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 101841 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 101841 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 162074 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 162074 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 80578 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 80578 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 100357 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 100357 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 93172 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 93172 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 86652 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 86652 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 100316 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 100316 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 161790 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 161790 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 104549 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 104549 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 176252 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 176252 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 168443 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 168443 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 73418 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 73418 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 137435 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 137435 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 137427 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 137427 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 93149 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 93149 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 112009 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 112009 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 112014 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 112014 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 65249 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 65249 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 80490 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 80490 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 90360 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 90360 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 101889 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 101889 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 69321 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 69321 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 128011 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 128011 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 200213 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 200213 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 133115 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 133115 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 75705 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 75705 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 112000 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 112000 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 112004 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 112004 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 72213 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 72213 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 161600 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 161600 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 124839 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 124839 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 71992 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 71992 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 77288 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 77288 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 73788 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 73788 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 104630 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 104630 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 104630 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 104630 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 128484 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 128484 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 104271 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 104271 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 200068 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 200068 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 200068 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 200068 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 87205 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 87205 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 149147 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 149147 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 102213 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 102213 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 194274 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 194274 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 21987 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 21987 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 73853 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 73853 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 74048 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 74048 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 146491 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 146491 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 100098 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 100098 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 97321 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 97321 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 80509 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 80509 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 72209 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 72209 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 133089 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 133089 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 133127 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 133127 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 97463 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 97463 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 100318 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 100318 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 129896 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 129896 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 162098 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 162098 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 146327 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 146327 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 144278 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 144278 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 97463 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 97463 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 90337 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 90337 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 72205 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 72205 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 72526 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 72526 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 102183 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 102183 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 148796 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 148796 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 179676 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 179676 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 80585 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 80585 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 86974 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 86974 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 93171 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 93171 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 97724 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 97724 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 97724 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 97724 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 15194 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 15194 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 133138 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 133138 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 81993 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 81993 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 112012 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 112012 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 93156 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 93156 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 182996 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 182996 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 90336 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 90336 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 72201 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 72201 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 162001 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 162001 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 162317 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 162317 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 103704 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 103704 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 148514 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 148514 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 84420 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 84420 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 65240 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 65240 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 133143 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 133143 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 74031 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 74031 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 15171 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 15171 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 144210 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 144210 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 101286 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 101286 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 73016 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 73016 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 195108 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 195108 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 65227 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 65227 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 65236 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 65236 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 133133 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 133133 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 65243 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 65243 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 15032 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 15032 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 145459 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 145459 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 65237 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 65237 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 199981 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 199981 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 128629 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 128629 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 19435 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 19435 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 19435 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 19435 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 19435 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 19435 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 87384 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 87384 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 26122 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 26122 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 100320 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 100320 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 148944 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 148944 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 133129 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 133129 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 137403 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 137403 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 155766 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 155766 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 155766 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 155766 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 133084 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 133084 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 176176 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 176176 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 176176 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 176176 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 100645 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 100645 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 26754 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 26754 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 87321 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 87321 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 161571 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 161571 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 72581 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 72581 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 101923 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 101923 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 104840 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 104840 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 80584 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 80584 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 90345 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 90345 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 93148 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 93148 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 133123 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 133123 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 100509 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 100509 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 75732 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 75732 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 93366 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 93366 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 93369 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 93369 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 91676 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 91676 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 137401 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 137401 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 137426 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 137426 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 152264 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 152264 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 8772 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 8772 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 8772 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 8772 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 81979 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 81979 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 80481 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 80481 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 80482 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 80482 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 90359 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 90359 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 72189 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 72189 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 72567 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 72567 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 72580 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 72580 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 116590 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 116590 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 102020 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 102020 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 92875 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 92875 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 65440 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 65440 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 92857 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 92857 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 80481 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 80481 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 152264 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 152264 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 104817 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 104817 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 8803 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 8803 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 8803 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 8803 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 104817 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 104817 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 82004 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 82004 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 116589 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 116589 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 77282 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 77282 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 150300 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 150300 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 8805 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 8805 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 8805 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 80503 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 80503 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 104303 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 104303 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 81325 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 81325 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 199989 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 199989 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 175483 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 175483 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 194014 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 194014 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 81320 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 81320 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 199889 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 199889 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 65238 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 65238 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 81316 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 81316 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 80500 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 80500 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 195014 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 195014 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 149136 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 149136 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 7666 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 7666 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 7666 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 7666 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 7666 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 7666 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 7666 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 7666 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 7666 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 7666 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 7666 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 7666 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 194014 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 194014 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 97474 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 97474 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 93374 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 93374 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 161841 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 161841 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 162035 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 162035 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 81983 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 81983 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 90344 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 90344 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 15031 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 15031 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 102237 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 102237 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 10514 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 10514 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 10514 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 96655 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 96655 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 27102 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 27102 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 130817 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 130817 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 72927 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 72927 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 15170 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 15170 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 81313 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 81313 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 25812 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 25812 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 194332 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 194332 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 194011 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 194011 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 84419 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 84419 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 133124 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 133124 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 72492 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 72492 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 72525 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 72525 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 100810 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 100810 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 92911 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 92911 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 81978 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 81978 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 72208 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 72208 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 158700 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 158700 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 161263 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 161263 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 84558 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 84558 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 131189 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 131189 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 97742 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 97742 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 97742 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 97742 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 145671 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 145671 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 133088 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 133088 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 84396 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 84396 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 93147 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 93147 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 65250 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 65250 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 72559 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 72559 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 162320 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 162320 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 72529 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 72529 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 100317 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 100317 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 104391 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 104391 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 90348 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 90348 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 77300 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 77300 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 10547 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 10547 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 10547 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 26122 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 26122 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 133076 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 133076 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 104186 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 104186 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 72490 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 72490 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 144129 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 144129 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 72549 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 72549 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 100507 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 100507 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 133114 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 133114 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 194500 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 194500 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 144290 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 144290 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 168028 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 168028 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 73897 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 73897 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 82006 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 82006 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 100736 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 100736 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 137414 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 137414 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 92904 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 92904 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 93363 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 93363 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 72562 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 72562 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 72570 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 72570 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 194386 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 194386 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 172520 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 172520 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 15171 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 15171 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 112005 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 112005 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 160724 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 160724 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 93170 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 93170 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 100326 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 100326 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 128001 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 128001 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 112001 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 112001 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 90358 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 90358 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 92817 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 92817 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 84750 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 84750 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 77295 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 77295 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 145719 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 145719 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 117883 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 117883 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 146116 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 146116 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 30015 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 30015 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 144214 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 144214 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 137412 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 137412 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 93162 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 93162 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 81988 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 81988 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 15117 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 15117 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 112007 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 112007 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 93161 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 93161 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 77283 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 77283 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 162523 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 162523 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 117878 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 117878 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 86968 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 86968 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 137436 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 137436 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 100847 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 100847 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 86746 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 86746 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 133101 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 133101 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 101885 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 101885 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 102239 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 102239 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 97474 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 97474 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 72514 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 72514 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 72569 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 72569 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 101851 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 101851 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 101890 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 101890 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 162092 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 162092 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 174238 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 174238 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 81318 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 81318 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 81319 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 81319 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 194011 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 194011 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 194806 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 194806 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 104543 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 104543 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 194720 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 194720 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 182996 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 182996 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 65244 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 65244 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 194638 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 194638 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 92904 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 92904 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 194806 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 194806 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 156702 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 156702 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 180044 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 180044 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 103704 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 103704 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 149135 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 149135 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 65452 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 65452 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 117887 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 117887 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 77113 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 77113 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 77115 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 77115 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 189539 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 189539 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 117891 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 117891 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 80496 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 80496 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 80507 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 80507 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 81314 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 81314 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 128006 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 128006 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 100314 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 100314 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 75714 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 75714 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 80192 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 80192 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 179431 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 179431 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 137415 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 137415 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 87829 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 87829 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 123702 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 123702 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 93148 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 93148 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 72199 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 72199 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 190030 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 190030 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 97069 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 97069 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 10547 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 10547 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 10547 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 104247 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 104247 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 144140 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 144140 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 136180 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 136180 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 112030 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 112030 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 97069 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 97069 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 90352 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 90352 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 101889 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 101889 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 117896 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 117896 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 127998 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 127998 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 112017 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 112017 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 72518 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 72518 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 92723 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 92723 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 194206 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 194206 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 175786 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 175786 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 173288 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 173288 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 194217 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 194217 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 194217 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 194217 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 98728 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 98728 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 98728 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 98728 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 75716 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 75716 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 111998 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 111998 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 81980 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 81980 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 81995 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 81995 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 80480 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 80480 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 161818 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 161818 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 92762 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 92762 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 194206 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 194206 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 104631 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 104631 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 123556 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 123556 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 134065 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 134065 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 80487 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 80487 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 80487 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 80487 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 73195 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 73195 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 137435 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 137435 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 87630 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 87630 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 162318 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 162318 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 100927 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 100927 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 98757 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 98757 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 97482 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 97482 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 26080 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 26080 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 112010 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 112010 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 80483 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 80483 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 81306 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 81306 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 100327 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 100327 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 100546 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 100546 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 148893 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 148893 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 92841 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 92841 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 133082 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 133082 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 90361 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 90361 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 72565 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 72565 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 30538 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 30538 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 97414 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 97414 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 65241 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 65241 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 81310 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 81310 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 100737 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 100737 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 97414 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 97414 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 71278 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 71278 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 86827 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 86827 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 95847 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 95847 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 15115 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 15115 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 72989 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 72989 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 144203 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 144203 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 75709 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 75709 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 137420 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 137420 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 35858 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 35858 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 86968 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 86968 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 93005 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 93005 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 65251 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 65251 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 100322 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 100322 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 145737 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 145737 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 112035 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 112035 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 81991 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 81991 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 69343 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 69343 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 95538 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 95538 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 112004 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 112004 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 82005 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 82005 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 144031 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 144031 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 87896 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 87896 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 80582 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 80582 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 166834 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 166834 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 100324 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 100324 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 131162 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 131162 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 93178 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 93178 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 93365 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 93365 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 93367 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 93367 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 93370 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 93370 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 136179 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 136179 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 102335 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 102335 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 65238 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 65238 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 80492 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 80492 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 72202 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 72202 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 72572 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 72572 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 194453 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 194453 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 80512 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 80512 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 77790 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 77790 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 158583 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 158583 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 69318 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 69318 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 80504 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 80504 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 26062 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 26062 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 157637 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 157637 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 104817 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 104817 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 92876 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 92876 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 92049 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 92049 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 186729 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 186729 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 92816 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 92816 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 190612 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 190612 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 161447 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 161447 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 194331 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 194331 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 77788 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 77788 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 194330 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 194330 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 84398 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 84398 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 200205 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 200205 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 72198 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 72198 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 175314 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 175314 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 144285 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 144285 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 146374 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 146374 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 73945 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 73945 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 100313 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 100313 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 137421 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 137421 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 111999 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 111999 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 90340 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 90340 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 137422 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 137422 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 72187 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 72187 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 72187 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 72187 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 81994 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 81994 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 80581 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 80581 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 100161 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 100161 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 93376 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 93376 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 77297 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 77297 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 87207 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 87207 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 87908 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 87908 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 145997 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 145997 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 145997 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 145997 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 96393 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 96393 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 100510 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 100510 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 87274 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 87274 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 158697 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 158697 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 104656 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 104656 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 8803 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 8803 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 8803 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 8803 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 158697 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 158697 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 92911 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 92911 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 149955 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 149955 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 137402 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 137402 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 73760 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 73760 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 73760 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 73760 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 131830 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 131830 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 144032 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 144032 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 194806 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 194806 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 137405 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 137405 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 65466 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 65466 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 75705 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 75705 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 100315 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 100315 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 14639 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 14639 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 84513 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 84513 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 175757 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 175757 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 128011 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 128011 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 93166 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 93166 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 133093 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 133093 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 133077 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 133077 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 194249 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 194249 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 97548 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 97548 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 97548 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 97548 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 199989 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 199989 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 194451 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 194451 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 111999 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 111999 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 194249 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 194249 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 112015 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 112015 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 145997 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 145997 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 100541 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 100541 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 123344 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 123344 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 90357 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 90357 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 112015 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 112015 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 81973 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 81973 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 84768 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 84768 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 130623 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 130623 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 100160 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 100160 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 87927 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 87927 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 104630 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 104630 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 102512 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 102512 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 104674 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 104674 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 65244 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 65244 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 77117 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 77117 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 93110 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 93110 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 90350 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 90350 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 100984 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 100984 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 104816 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 104816 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 128611 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 128611 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 73772 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 73772 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 93182 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 93182 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 81998 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 81998 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 93372 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 93372 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 137403 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 137403 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 137426 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 137426 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 160311 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 160311 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 146926 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 146926 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 175547 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 175547 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 195241 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 195241 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 69340 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 69340 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 179565 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 179565 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 149955 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 149955 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 65451 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 65451 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 65246 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 65246 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 19435 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 19435 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 19435 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 117888 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 117888 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 179430 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 179430 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 69341 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 69341 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 152532 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 152532 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 102281 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 102281 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 72197 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 72197 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 144248 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 144248 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 86849 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 86849 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 105425 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 105425 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 86827 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 86827 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 161650 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 161650 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 105425 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 105425 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 95963 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 95963 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 128628 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 128628 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 87696 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 87696 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 137423 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 137423 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 93145 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 93145 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 112000 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 112000 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 157090 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 157090 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 117893 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 117893 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 133117 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 133117 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 112009 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 112009 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 72550 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 72550 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 144232 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 144232 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 133096 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 133096 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 86679 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 86679 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 137429 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 137429 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 133128 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 133128 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 86679 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 86679 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 133135 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 133135 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 102310 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 102310 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 15075 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 15075 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 86304 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 86304 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 81305 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 81305 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 194346 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 194346 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 100955 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 100955 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 72210 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 72210 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 194346 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 194346 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 82000 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 82000 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 87829 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 87829 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 81303 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 81303 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 123585 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 123585 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 85667 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 85667 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 112037 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 112037 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 137430 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 137430 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 112036 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 112036 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 80494 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 80494 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 174107 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 174107 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 161700 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 161700 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 131241 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 131241 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 93179 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 93179 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 112035 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 112035 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 93159 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 93159 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 104646 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 104646 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 100503 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 100503 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 137426 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 137426 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 77117 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 77117 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 155286 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 155286 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 136181 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 136181 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 102288 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 102288 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 175670 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 175670 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 152532 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 152532 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 72571 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 72571 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 144099 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 144099 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 87370 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 87370 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 92802 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 92802 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 81315 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 81315 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 104570 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 104570 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 92818 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 92818 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 69346 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 69346 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 80505 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 80505 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 65248 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 65248 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 69317 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 69317 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 8803 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 8803 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 8803 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 8803 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 80498 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 80498 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 190685 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 190685 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 112030 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 112030 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 100407 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 100407 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 100588 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 100588 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 31100 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 31100 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 80589 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 80589 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 161907 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 161907 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 65226 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 65226 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 133100 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 133100 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 72563 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 72563 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 74640 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 74640 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 144240 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 144240 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 136179 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 136179 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 165333 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 165333 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 92840 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 92840 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 148679 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 148679 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 73771 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 73771 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 98455 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 98455 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 21978 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 21978 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 93152 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 93152 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 81307 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 81307 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 133105 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 133105 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 112005 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 112005 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 137437 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 137437 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 100809 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 100809 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 149137 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 149137 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 100725 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 100725 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 104252 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 104252 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 29880 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 29880 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 137424 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 137424 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 102351 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 102351 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 104706 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 104706 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 112014 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 112014 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 100504 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 100504 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 194544 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 194544 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 164462 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 164462 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 144046 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 144046 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 81990 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 81990 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 148461 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 148461 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 75708 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 75708 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 75707 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 75707 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 112007 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 112007 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 81977 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 81977 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 14755 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 14755 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 100505 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 100505 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 26364 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 26364 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 15193 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 15193 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 10755 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 10755 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 10755 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 10755 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 9327 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 9327 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 9327 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 180862 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 180862 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 179278 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 179278 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 180862 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 180862 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 179278 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 179278 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 9327 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 9327 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 9327 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 94604 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 94604 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 180992 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 180992 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 180992 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 180992 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 189053 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 189053 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 189053 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 189053 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 182248 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 182248 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 182008 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 182008 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 182008 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 182008 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 182248 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 182248 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 94603 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 94603 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 94605 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 94605 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 125474 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 125474 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 179740 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 179740 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 179740 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 179740 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 182060 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 182060 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 182060 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 182060 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 7865 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 7865 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 7865 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 176505 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 176505 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 125467 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 125467 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 7865 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 7865 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 7865 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 176505 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 176505 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 178262 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 178262 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 178262 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 178262 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 180982 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 180982 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 180982 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 180982 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 177346 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 177346 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 177346 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 177346 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 189053 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 189053 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 90750 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 90750 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 90751 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 90751 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 90753 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 90753 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 90767 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 90767 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 90750 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 90750 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 125482 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 125482 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 125484 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 125484 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 179104 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 179104 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 133139 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 133139 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 10289 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 10289 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 10289 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 10289 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 10289 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 10289 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 90756 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 90756 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 90757 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 90757 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 90759 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 90759 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 179583 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 179583 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 179583 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 179583 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 133080 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 133080 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 178984 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 178984 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 27903 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 27903 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 10514 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 10514 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 10514 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 178984 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 178984 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 133107 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 133107 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 133111 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 133111 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 125479 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 125479 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 179104 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 179104 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 133095 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 133095 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 125486 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 125486 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 133140 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 133140 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 10514 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 10514 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 10514 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 90770 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 90770 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 90771 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 90771 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 180233 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 180233 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 133097 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 133097 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 90755 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 90755 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 161426 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 161426 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 161651 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 161651 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 10289 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 10289 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 10289 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 125470 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 125470 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 125472 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 125472 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 125490 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 125490 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 180233 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 180233 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 133143 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 133143 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 10514 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 10514 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 10514 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 125497 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 125497 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 178134 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 178134 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 123102 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 123102 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 177657 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 177657 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 177657 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 177657 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 178134 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 178134 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 10514 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 10514 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 10514 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 168151 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 168151 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 125460 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 125460 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 125464 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 125464 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 177363 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 177363 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 133125 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 133125 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 177363 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 177363 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 177124 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 177124 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 177124 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 177124 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 7659 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 7659 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 7659 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 200351 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 90754 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 90754 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 177877 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 177877 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 27903 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 27903 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 178300 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 178300 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 180276 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 180276 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 181917 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 181917 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 180276 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 180276 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 181917 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 181917 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 178798 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 178798 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 178300 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 178300 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 90761 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 90761 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 133129 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 133129 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 10289 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 10289 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 10289 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 179006 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 179006 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 178798 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 178798 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 104271 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 104271 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 178552 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 178552 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 10289 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 10289 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 10289 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 10289 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 10289 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 10289 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 177877 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 177877 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 133122 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 133122 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 179006 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 179006 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 10514 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 10514 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 10514 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 178337 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 178337 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 178552 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 178552 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 10169 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 10169 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 10169 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 177618 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 177618 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 177618 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 177618 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 178337 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 178337 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 176905 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 176905 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 10514 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 10514 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 10514 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 10547 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 10547 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 10547 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 176905 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 176905 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 189750 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 189750 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 125496 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 125496 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 133091 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 133091 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 10169 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 10169 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 10169 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 177535 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 177535 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 168243 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 168243 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 125488 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 125488 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 125494 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 125494 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 10514 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 10514 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 10514 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 94602 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 94602 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 181915 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 181915 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 181915 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 181915 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 179714 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 179714 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 125461 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 125461 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 179714 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 179714 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 179060 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 179060 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 125468 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 125468 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 179060 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 179060 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 125492 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 125492 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 189053 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 189053 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 181830 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 181830 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 181830 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 181830 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 10514 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 10514 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 10514 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 179835 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 179835 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 177948 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 177948 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 177948 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 177948 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 27903 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 27903 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 177535 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 177535 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 133093 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 133093 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 10169 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 10169 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 10169 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 10289 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 10289 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 10289 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 125465 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 125465 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 133127 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 133127 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 10514 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 10514 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 10514 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 181066 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 181066 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 177629 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 177629 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 177908 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 177908 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 180105 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 180105 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 177629 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 177629 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 177908 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 177908 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 180105 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 180105 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 10169 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 10169 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 10169 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 189750 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 189750 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 181066 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 181066 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 176559 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 176559 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 176559 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 176559 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 180890 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 180890 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 10289 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 10289 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 10289 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 27903 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 27903 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 125471 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 125471 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 125485 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 125485 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 27903 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 27903 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 178866 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 178866 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 178866 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 178866 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 168239 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 168239 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 125493 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 125493 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 10289 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 10289 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 10289 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 90763 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 90763 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 90768 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 90768 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 109600 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 109600 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 90765 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 90765 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 109600 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 109600 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 10169 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 10169 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 10169 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 10289 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 10289 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 10289 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 10547 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 10547 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 10547 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 27903 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 27903 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 35858 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 35858 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 180890 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 180890 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 133087 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 133087 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 181181 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 181181 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 181181 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 181181 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 10514 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 10514 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 10514 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 123100 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 123100 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 133100 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 133100 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 133081 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 133081 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 10514 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 10514 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 10514 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 27903 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 27903 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 10547 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 10547 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 10547 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 179316 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 179316 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 144982 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 144982 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 133090 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 133090 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 125487 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 125487 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 179835 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 179835 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 178824 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 178824 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 179179 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 179179 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 180068 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 180068 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 178824 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 178824 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 180068 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 180068 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 179179 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 179179 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 189053 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 189053 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 187875 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 187875 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 182732 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 182732 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 133082 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 133082 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 27903 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 27903 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 179316 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 179316 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 133094 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 133094 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 125462 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 125462 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 189631 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 189631 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 133089 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 133089 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 90749 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 90749 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 90766 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 90766 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 189631 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 189631 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 176580 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 176580 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 10547 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 10547 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 10547 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 10547 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 10547 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 10547 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 10547 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 10547 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 10547 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 176580 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 176580 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 133076 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 133076 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 133103 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 133103 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 133133 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 133133 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 10547 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 10547 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 10547 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 179844 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 179844 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 179844 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 179844 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 133115 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 133115 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 125480 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 125480 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 90752 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 90752 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 211140 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 211140 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 189053 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 189053 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 182732 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 182732 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 177229 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 177229 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 177229 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 177229 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 10514 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 10514 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 10514 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 125469 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 125469 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 187875 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 187875 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 125489 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 125489 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 125463 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 125463 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 125495 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 125495 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 125466 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 125466 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 211140 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 211140 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 81972 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 81972 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 125483 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 125483 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 7186 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 7186 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 7186 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 7186 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 7186 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 133102 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 133102 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 10169 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 10169 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 10169 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 133104 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 133104 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 27903 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 27903 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 125477 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 125477 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 133128 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 133128 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 178750 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 178750 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 178240 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 178240 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 182246 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 182246 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 178240 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 178240 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 178750 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 178750 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 10289 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 10289 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 10289 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 194249 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 194249 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 10289 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 10289 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 10289 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 10289 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 10289 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 10289 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 90760 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 90760 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 90762 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 90762 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 10289 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 10289 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 10289 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 10289 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 10289 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 10289 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 90748 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 90748 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 90758 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 90758 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 177423 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 177423 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 177423 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 177423 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 10169 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 10169 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 10169 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 125478 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 125478 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 133136 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 133136 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 10289 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 10289 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 10289 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 180246 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 180246 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 180246 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 180246 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 10169 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 10169 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 10169 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 27903 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 27903 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 133088 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 133088 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 187875 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 187875 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 182246 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 182246 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 133141 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 133141 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 187875 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 187875 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 187875 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 187875 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 187875 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 187875 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 178429 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 178429 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 178429 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 178429 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 10514 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 10514 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 10514 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 133077 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 133077 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 10514 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 10514 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 10514 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 90764 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 90764 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 189962 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 189962 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 109600 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 109600 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 109600 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 109600 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 10169 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 10169 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 10169 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 176752 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 176752 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 123101 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 123101 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 176752 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 176752 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 181560 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 181560 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 133114 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 133114 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 181560 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 181560 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 10547 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 10547 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 10547 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 133137 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 133137 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 27903 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 27903 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 180956 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 180956 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 180956 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 180956 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 125473 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 125473 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 16552 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 10547 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 10547 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 10547 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 10289 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 10289 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 10289 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 123045 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 123045 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 125481 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 125481 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 27903 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 27903 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 133123 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 133123 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 10547 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 10547 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 10547 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 133126 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 133126 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 161651 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 161651 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 177566 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 177566 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 161651 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 161651 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 133101 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 133101 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 133124 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 133124 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 180478 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 180478 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 177566 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 177566 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 125491 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 125491 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 133105 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 133105 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 76154 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 76154 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 10169 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 10169 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 10169 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 189962 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 189962 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 180478 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 180478 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 10514 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 10514 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 10514 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 123103 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 123103 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 179318 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 179318 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 179318 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 179318 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 195728 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 195728 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 177962 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 177962 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 214620 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 214620 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 177962 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 177962 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 90356 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 90356 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 7659 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 7659 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 7659 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 9911 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 9911 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 9911 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 9911 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 9911 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 7460 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 7460 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 7460 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 8920 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 8920 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 8920 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 9836 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 9836 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 9836 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 7186 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 7186 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 7186 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 7186 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 7186 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 214620 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 214620 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 76154 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 76154 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 7865 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 7865 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 7865 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 8667 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 8667 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 8667 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 10547 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 10547 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 10547 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 10169 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 10169 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 10169 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 10289 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 10289 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 10289 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 10514 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 10514 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 10514 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 10514 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 10514 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 10514 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 10514 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 10514 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 10514 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