Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Unit Assay Type Assay Description Mol
weight
Rot
Bonds
H don H acc LogP Smiles
CHEMBL4544504 ccr2_human Human Yes 7.9 EC50 = 12.3 nM Funct
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)
395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1
CHEMBL4531005 ccr2_human Human Yes 7.9 EC50 = 12.9 nM Funct
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)
351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C
CHEMBL4544504 ccr2_human Human Yes 7.9 EC50 = 13 nM Funct
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)
395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1
CHEMBL4531005 ccr2_human Human Yes 7.9 EC50 = 13 nM Funct
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)
351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C
CHEMBL4544504 ccr2_human Human Yes 6.9 EC50 = 134.9 nM Funct
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)
395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1
CHEMBL4544504 ccr2_human Human Yes 6.8 EC50 = 148 nM Funct
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)
395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1
CHEMBL255408 ccr2_human Human Yes 7.7 EC50 = 20 nM Funct
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1
CHEMBL4531005 ccr2_human Human Yes 7.6 EC50 = 25.1 nM Funct
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)
351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C
CHEMBL4531005 ccr2_human Human Yes 7.6 EC50 = 26 nM Funct
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)
351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C
CHEMBL4544504 ccr2_human Human Yes 7.5 EC50 = 29.5 nM Funct
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)
395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1
CHEMBL4544504 ccr2_human Human Yes 7.5 EC50 = 32 nM Funct
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)
395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1
CHEMBL2096789 ccr2_human Human Yes 6.4 EC50 = 360 nM Funct
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCN(Cc2ccc(Cl)cc2)C1
CHEMBL435499 ccr2_human Human Yes 7.4 EC50 = 40 nM Funct
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
467 7 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCN(Cc2ccc(Cl)cc2)CC1
CHEMBL4531005 ccr2_human Human Yes 7.3 EC50 = 53.7 nM Funct
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)
351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C
CHEMBL4531005 ccr2_human Human Yes 7.3 EC50 = 56 nM Funct
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)
351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C
CHEMBL181432 ccr2_human Human No 6.2 EC50 = 610 nM Funct
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
453 6 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCCN(Cc2ccc(Cl)cc2)C1
CHEMBL2448120 ccr2_human Human No 6.2 EC50 = 630 nM Funct
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@@H]1CCCN1Cc1ccc(Cl)cc1
CHEMBL2096788 ccr2_human Human No 6.1 EC50 = 810 nM Funct
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@H]1CCCN1Cc1ccc(Cl)cc1
CHEMBL1178786 ccr2_human Human Yes 10.5 IC50 = 0.0 nM Bind
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C
CHEMBL18442 ccr2_human Human Yes 10.4 IC50 = 0.0 nM Bind
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1
CHEMBL1178786 ccr2_human Human Yes 10.1 IC50 = 0.1 nM Bind
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C
CHEMBL18442 ccr2_human Human Yes 10.1 IC50 = 0.1 nM Bind
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1
CHEMBL494191 ccr2_human Human No 10.0 IC50 = 0.1 nM Funct
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
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
CHEMBL3770912 ccr2_human Human No 9.9 IC50 = 0.1 nM Funct
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
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
CHEMBL230933 ccr2_human Human No 9.8 IC50 = 0.2 nM Funct
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
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
CHEMBL502247 ccr2_human Human No 9.7 IC50 = 0.2 nM Funct
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
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
CHEMBL3233186 ccr2_human Human No 9.7 IC50 = 0.2 nM Bind
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
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
CHEMBL3233188 ccr2_human Human No 9.7 IC50 = 0.2 nM Bind
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
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
CHEMBL494191 ccr2_human Human No 9.7 IC50 = 0.2 nM Funct
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
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
CHEMBL258205 ccr2_human Human No 9.7 IC50 = 0.2 nM Bind
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
525 6 2 3 6.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1
CHEMBL437359 ccr2_human Human No 9.6 IC50 = 0.2 nM Funct
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
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
CHEMBL3577945 ccr2_human Human No 9.6 IC50 = 0.2 nM Bind
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
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
CHEMBL1178786 ccr2_human Human Yes 9.6 IC50 = 0.3 nM Bind
Displacement of [125I]MCP1 from CCR2 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2 expressed in CHOK1 cells
495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C
CHEMBL3263286 ccr2_human Human No 9.6 IC50 = 0.3 nM Bind
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
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
CHEMBL497202 ccr2_human Human No 9.5 IC50 = 0.3 nM Funct
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
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
CHEMBL4764460 ccr2_human Human No 9.5 IC50 = 0.3 nM Bind
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
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
CHEMBL522688 ccr2_human Human No 9.5 IC50 = 0.3 nM Funct
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
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
CHEMBL1090893 ccr2_human Human No 9.5 IC50 = 0.3 nM Bind
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
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
CHEMBL231039 ccr2_human Human No 9.5 IC50 = 0.3 nM Funct
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
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
CHEMBL3233186 ccr2_human Human No 9.5 IC50 = 0.3 nM Bind
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
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
CHEMBL497202 ccr2_human Human No 9.4 IC50 = 0.4 nM Bind
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
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
CHEMBL1092678 ccr2_human Human No 9.4 IC50 = 0.4 nM Bind
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
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
CHEMBL4457723 ccr2_human Human No 9.4 IC50 = 0.4 nM Bind
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
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
CHEMBL3577948 ccr2_human Human No 9.4 IC50 = 0.4 nM Bind
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
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
CHEMBL230281 ccr2_human Human No 9.4 IC50 = 0.4 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL230281 ccr2_human Human No 9.4 IC50 = 0.4 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL230281 ccr2_human Human No 9.4 IC50 = 0.4 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
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
CHEMBL3577946 ccr2_human Human No 9.3 IC50 = 0.5 nM Bind
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
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
CHEMBL502247 ccr2_human Human No 9.3 IC50 = 0.5 nM Funct
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
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
CHEMBL1091605 ccr2_human Human No 9.3 IC50 = 0.5 nM Funct
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
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
CHEMBL1091605 ccr2_human Human No 9.3 IC50 = 0.5 nM Bind
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
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
CHEMBL271828 ccr2_human Human No 9.3 IC50 = 0.5 nM Funct
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
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
CHEMBL3233187 ccr2_human Human No 9.3 IC50 = 0.5 nM Bind
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
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
CHEMBL2029422 ccr2_human Human No 9.3 IC50 = 0.5 nM Bind
Inhibition of CCR2-mediated Erk phosphorylationInhibition of CCR2-mediated Erk phosphorylation
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
CHEMBL3577946 ccr2_human Human No 9.3 IC50 = 0.5 nM Bind
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
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
CHEMBL3577942 ccr2_human Human No 9.2 IC50 = 0.6 nM Bind
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
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
CHEMBL4790208 ccr2_human Human No 9.2 IC50 = 0.6 nM Bind
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
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
CHEMBL3233184 ccr2_human Human No 9.2 IC50 = 0.6 nM Bind
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
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
CHEMBL256301 ccr2_human Human No 9.2 IC50 = 0.6 nM Bind
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
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
CHEMBL257191 ccr2_human Human No 9.2 IC50 = 0.6 nM Bind
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
493 6 2 3 4.9 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1
CHEMBL438304 ccr2_human Human No 9.2 IC50 = 0.6 nM Funct
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
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
CHEMBL437359 ccr2_human Human No 9.2 IC50 = 0.6 nM Funct
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
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
CHEMBL3769444 ccr2_human Human No 9.2 IC50 = 0.7 nM Funct
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
428 2 2 6 1.9 Cc1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)(C)C)CCN3)CC2)sc1Cl
CHEMBL4442783 ccr2_human Human Yes 9.2 IC50 = 0.7 nM Bind
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
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
CHEMBL502793 ccr2_human Human No 9.2 IC50 = 0.7 nM Funct
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
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
CHEMBL4442783 ccr2_human Human Yes 9.2 IC50 = 0.7 nM Bind
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
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
CHEMBL3233181 ccr2_human Human No 9.2 IC50 = 0.7 nM Bind
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
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
CHEMBL3577945 ccr2_human Human No 9.2 IC50 = 0.7 nM Bind
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
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
CHEMBL388487 ccr2_human Human No 9.2 IC50 = 0.7 nM Funct
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
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
CHEMBL397996 ccr2_human Human No 9.2 IC50 = 0.7 nM Funct
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
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
CHEMBL3577945 ccr2_human Human No 9.2 IC50 = 0.7 nM Bind
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
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
CHEMBL230933 ccr2_human Human No 9.2 IC50 = 0.7 nM Funct
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
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
CHEMBL4781426 ccr2_human Human Yes 9.1 IC50 = 0.8 nM Bind
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
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
CHEMBL492564 ccr2_human Human No 9.1 IC50 = 0.8 nM Funct
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
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
CHEMBL1091604 ccr2_human Human No 9.1 IC50 = 0.8 nM Bind
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
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
CHEMBL1092941 ccr2_human Human No 9.1 IC50 = 0.8 nM Bind
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
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
CHEMBL1091604 ccr2_human Human No 9.1 IC50 = 0.8 nM Bind
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
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
CHEMBL389771 ccr2_human Human No 9.1 IC50 = 0.8 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
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
CHEMBL1091604 ccr2_human Human No 9.1 IC50 = 0.8 nM Bind
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
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
CHEMBL3577933 ccr2_human Human No 9.1 IC50 = 0.8 nM Bind
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
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
CHEMBL256629 ccr2_human Human No 9.1 IC50 = 0.8 nM Funct
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
448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1
CHEMBL271288 ccr2_human Human No 9.1 IC50 = 0.9 nM Funct
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
448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1
CHEMBL2088212 ccr2_human Human No 9.1 IC50 = 0.9 nM Bind
Binding affinity to CCR2Binding affinity to CCR2
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
CHEMBL4470701 ccr2_human Human No 9.1 IC50 = 0.9 nM Bind
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
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
CHEMBL1178786 ccr2_human Human Yes 9.0 IC50 = 1.0 nM Funct
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
495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C
CHEMBL1178786 ccr2_human Human Yes 9.0 IC50 = 1.0 nM Funct
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
495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C
CHEMBL1290636 ccr2_human Human No 9.0 IC50 = 1.0 nM Bind
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
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
CHEMBL495924 ccr2_human Human No 9.0 IC50 = 1.0 nM Bind
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
509 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1
CHEMBL3233188 ccr2_human Human No 9.0 IC50 = 1.0 nM Bind
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
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
CHEMBL273083 ccr2_human Human Yes 9.0 IC50 = 1 nM Funct
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
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
CHEMBL1951766 ccr2_human Human No 9.0 IC50 = 1 nM Funct
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
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
CHEMBL273083 ccr2_human Human Yes 9.0 IC50 = 1 nM Funct
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
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
CHEMBL492564 ccr2_human Human No 9.0 IC50 = 1 nM Funct
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
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
CHEMBL492569 ccr2_human Human No 9.0 IC50 = 1 nM Funct
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
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
CHEMBL494191 ccr2_human Human No 9.0 IC50 = 1 nM Funct
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
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
CHEMBL254772 ccr2_human Human No 9.0 IC50 = 1 nM Bind
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
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
CHEMBL403889 ccr2_human Human No 9.0 IC50 = 1 nM Bind
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
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
CHEMBL404904 ccr2_human Human No 9.0 IC50 = 1 nM Bind
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
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
CHEMBL1091605 ccr2_human Human No 9.0 IC50 = 1 nM Bind
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
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
CHEMBL1091605 ccr2_human Human No 9.0 IC50 = 1 nM Bind
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
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
CHEMBL1951766 ccr2_human Human No 9.0 IC50 = 1 nM Bind
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
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
CHEMBL3577942 ccr2_human Human No 9.0 IC50 = 1 nM Bind
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
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
CHEMBL526752 ccr2_human Human No 9.0 IC50 = 1.1 nM Funct
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
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
CHEMBL3770530 ccr2_human Human No 9.0 IC50 = 1.1 nM Funct
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
420 3 2 6 1.8 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C4CC4)cs3)CC2)C1
CHEMBL3233185 ccr2_human Human No 9.0 IC50 = 1.1 nM Bind
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
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
CHEMBL4442783 ccr2_human Human Yes 9.0 IC50 = 1.1 nM Bind
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
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
CHEMBL4442783 ccr2_human Human Yes 9.0 IC50 = 1.1 nM Bind
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
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
CHEMBL3577932 ccr2_human Human No 9.0 IC50 = 1.1 nM Bind
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
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
CHEMBL3769610 ccr2_human Human No 8.9 IC50 = 1.2 nM Funct
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
442 4 2 6 2.3 CC(C)c1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)C)CCN3)CC2)sc1Cl
CHEMBL2088388 ccr2_human Human No 8.9 IC50 = 1.2 nM Bind
Binding affinity to CCR2Binding affinity to CCR2
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
CHEMBL3233180 ccr2_human Human No 8.9 IC50 = 1.2 nM Bind
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
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
CHEMBL3233184 ccr2_human Human No 8.9 IC50 = 1.2 nM Bind
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
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
CHEMBL3233189 ccr2_human Human No 8.9 IC50 = 1.2 nM Bind
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
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
CHEMBL494191 ccr2_human Human No 8.9 IC50 = 1.2 nM Bind
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
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
CHEMBL1091604 ccr2_human Human No 8.9 IC50 = 1.3 nM Bind
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
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
CHEMBL1091604 ccr2_human Human No 8.9 IC50 = 1.3 nM Funct
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
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
CHEMBL3770912 ccr2_rat Rat No 8.9 IC50 = 1.3 nM Funct
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
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
CHEMBL3233190 ccr2_human Human No 8.9 IC50 = 1.3 nM Bind
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
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
CHEMBL502247 ccr2_human Human No 8.9 IC50 = 1.3 nM Bind
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
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
CHEMBL502793 ccr2_human Human No 8.9 IC50 = 1.3 nM Bind
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
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
CHEMBL4764460 ccr2_human Human No 8.9 IC50 = 1.3 nM Bind
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
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
CHEMBL428602 ccr2_human Human No 8.9 IC50 = 1.3 nM Bind
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
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
CHEMBL229316 ccr2_human Human No 8.9 IC50 = 1.3 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
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
CHEMBL397749 ccr2_human Human No 8.9 IC50 = 1.3 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
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
CHEMBL226066 ccr2_human Human No 8.9 IC50 = 1.3 nM Bind
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
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
CHEMBL1289203 ccr2_human Human No 8.9 IC50 = 1.4 nM Funct
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
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
CHEMBL1944776 ccr2_human Human No 8.9 IC50 = 1.4 nM Bind
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
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
CHEMBL526752 ccr2_human Human No 8.9 IC50 = 1.4 nM Bind
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
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
CHEMBL4465351 ccr2_human Human No 8.9 IC50 = 1.4 nM Bind
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
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
CHEMBL272369 ccr2_human Human Yes 8.9 IC50 = 1.4 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
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
CHEMBL397948 ccr2_human Human No 8.9 IC50 = 1.4 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
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
CHEMBL226065 ccr2_human Human No 8.9 IC50 = 1.4 nM Bind
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
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
CHEMBL522688 ccr2_human Human No 8.8 IC50 = 1.5 nM Bind
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
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
CHEMBL496630 ccr2_human Human No 8.8 IC50 = 1.5 nM Funct
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
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
CHEMBL494191 ccr2_human Human No 8.8 IC50 = 1.5 nM Bind
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
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
CHEMBL3263282 ccr2_human Human No 8.8 IC50 = 1.5 nM Bind
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
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
CHEMBL4783861 ccr2_human Human No 8.8 IC50 = 1.6 nM Bind
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
589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1
CHEMBL1090893 ccr2_human Human No 8.8 IC50 = 1.6 nM Funct
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
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
CHEMBL4757857 ccr2_human Human No 8.8 IC50 = 1.6 nM Bind
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
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
CHEMBL4760098 ccr2_human Human No 8.8 IC50 = 1.7 nM Bind
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
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
CHEMBL3769984 ccr2_human Human No 8.8 IC50 = 1.7 nM Funct
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
428 4 2 6 1.7 CCc1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)C)CCN3)CC2)sc1Cl
CHEMBL1092238 ccr2_human Human Yes 8.8 IC50 = 1.7 nM Funct
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
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
CHEMBL388487 ccr2_human Human No 8.8 IC50 = 1.7 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
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
CHEMBL3577943 ccr2_human Human No 8.8 IC50 = 1.7 nM Bind
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
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
CHEMBL3577940 ccr2_human Human No 8.7 IC50 = 1.8 nM Bind
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
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
CHEMBL2029423 ccr2_human Human No 8.7 IC50 = 1.8 nM Funct
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
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
CHEMBL1290637 ccr2_human Human No 8.7 IC50 = 1.8 nM Funct
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
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
CHEMBL397996 ccr2_human Human No 8.7 IC50 = 1.8 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL3233178 ccr2_human Human No 8.7 IC50 = 1.8 nM Bind
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
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
CHEMBL3233178 ccr2_human Human No 8.7 IC50 = 1.8 nM Bind
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
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
CHEMBL230790 ccr2_human Human No 8.7 IC50 = 1.8 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
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
CHEMBL397996 ccr2_human Human No 8.7 IC50 = 1.8 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
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
CHEMBL496343 ccr2_human Human No 8.7 IC50 = 1.8 nM Bind
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
523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1
CHEMBL230281 ccr2_human Human No 8.7 IC50 = 1.8 nM Funct
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
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
CHEMBL397996 ccr2_human Human No 8.7 IC50 = 1.8 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL2029568 ccr2_human Human No 8.7 IC50 = 1.9 nM Funct
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
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
CHEMBL437359 ccr2_human Human No 8.7 IC50 = 1.9 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL2088380 ccr2_human Human No 8.7 IC50 = 1.9 nM Bind
Binding affinity to CCR2Binding affinity to CCR2
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
CHEMBL2088389 ccr2_human Human No 8.7 IC50 = 1.9 nM Bind
Binding affinity to CCR2Binding affinity to CCR2
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
CHEMBL4463290 ccr2_human Human No 8.7 IC50 = 1.9 nM Bind
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
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
CHEMBL437359 ccr2_human Human No 8.7 IC50 = 1.9 nM Bind
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
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
CHEMBL1290636 ccr2_mouse Mouse No 8.7 IC50 = 1.9 nM Bind
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
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
CHEMBL1290637 ccr2_mouse Mouse No 8.7 IC50 = 1.9 nM Bind
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
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
CHEMBL437359 ccr2_human Human No 8.7 IC50 = 1.9 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL2315922 ccr2_human Human No 8.0 IC50 = 10 nM Bind
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
506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1
CHEMBL1944776 ccr2_human Human No 8.0 IC50 = 10 nM Funct
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
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
CHEMBL2018391 ccr2_human Human No 8.0 IC50 = 10 nM Funct
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
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
CHEMBL1089793 ccr2_human Human No 8.0 IC50 = 10 nM Funct
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
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
CHEMBL2236474 ccr2_human Human No 8.0 IC50 = 10 nM Bind
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
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
CHEMBL4783861 ccr2_human Human No 8.0 IC50 = 10 nM Bind
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
589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1
CHEMBL2092884 ccr2_human Human No 8.0 IC50 = 10 nM Funct
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
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
CHEMBL4517518 ccr2_human Human No 8.0 IC50 = 10 nM Bind
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
315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1
CHEMBL255500 ccr2_human Human No 8.0 IC50 = 10 nM Bind
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
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
CHEMBL257768 ccr2_human Human No 8.0 IC50 = 10 nM Bind
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
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
CHEMBL403250 ccr2_human Human No 8.0 IC50 = 10 nM Bind
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
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
CHEMBL403581 ccr2_human Human No 8.0 IC50 = 10 nM Bind
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
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
CHEMBL2036757 ccr2_human Human No 8.0 IC50 = 10 nM Bind
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
410 4 1 3 4.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1
CHEMBL2018395 ccr2_human Human No 8.0 IC50 = 10 nM Bind
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
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
CHEMBL1829612 ccr2_human Human No 8.0 IC50 = 10 nM Bind
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
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
CHEMBL245686 ccr2_human Human No 8.0 IC50 = 10 nM Bind
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
509 7 1 2 6.8 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cc1)C1CCOCC1
CHEMBL247537 ccr2_human Human No 8.0 IC50 = 10 nM Bind
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
455 7 1 2 6.1 Cc1ccc(-c2ccc(/C=C/C(=O)Nc3ccc(C[N+](C)(C)C4CCOCC4)cc3)cc2)cc1
CHEMBL388007 ccr2_human Human No 8.0 IC50 = 10 nM Bind
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
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
CHEMBL209411 ccr2_human Human No 8.0 IC50 = 10 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
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
CHEMBL2029420 ccr2_human Human No 8.0 IC50 = 10 nM Bind
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
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
CHEMBL2029570 ccr2_human Human No 8.0 IC50 = 10 nM Bind
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
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
CHEMBL1289083 ccr2_mouse Mouse No 8.0 IC50 = 10 nM Bind
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
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
CHEMBL237754 ccr2_human Human No 8.0 IC50 = 10 nM Bind
Inhibition of human CCR2Inhibition of human CCR2
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
CHEMBL1951771 ccr2_human Human No 8.0 IC50 = 10.3 nM Bind
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
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
CHEMBL502516 ccr2_human Human No 8.0 IC50 = 10.4 nM Funct
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
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
CHEMBL1951776 ccr2_human Human No 8.0 IC50 = 10.4 nM Funct
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
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
CHEMBL1683060 ccr2_human Human No 8.0 IC50 = 10.5 nM Bind
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
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
CHEMBL1683078 ccr2_human Human No 8.0 IC50 = 10.6 nM Bind
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
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
CHEMBL1951776 ccr2_human Human No 8.0 IC50 = 10.9 nM Bind
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
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
CHEMBL393267 ccr2_human Human No 7.0 IC50 = 100 nM Funct
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
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
CHEMBL495202 ccr2_human Human No 7.0 IC50 = 100 nM Funct
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
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
CHEMBL397647 ccr2_human Human No 7.0 IC50 = 100 nM Funct
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
407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1
CHEMBL397647 ccr2_human Human No 7.0 IC50 = 100 nM Funct
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
407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1
CHEMBL4760108 ccr2_human Human No 7.0 IC50 = 100 nM Bind
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
471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1
CHEMBL2018365 ccr2_human Human No 7.0 IC50 = 100 nM Bind
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
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
CHEMBL2018375 ccr2_human Human No 7.0 IC50 = 100 nM Bind
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
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
CHEMBL2204258 ccr2_human Human No 7.0 IC50 = 100 nM Bind
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
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
CHEMBL401010 ccr2_human Human No 7.0 IC50 = 100 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL3650405 ccr2_human Human No 7.0 IC50 = 100 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL1687955 ccr2_human Human No 6.0 IC50 = 1000 nM Funct
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
342 4 2 5 3.2 CC(C)Oc1cccc(NC(=O)NC(=O)c2ccc3c(c2)OCO3)c1
CHEMBL211560 ccr2_human Human No 6.0 IC50 = 1000 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL1829607 ccr2_human Human No 6.0 IC50 = 1000 nM Bind
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
501 6 2 5 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN(C2CC=C(c3ccc4c(c3)OCO4)CC2)C1
CHEMBL211560 ccr2_human Human No 6.0 IC50 = 1000 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
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
CHEMBL1089965 ccr2_human Human No 6.0 IC50 = 1000 nM Bind
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
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
CHEMBL248416 ccr2_human Human No 6.0 IC50 = 1000 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
465 9 3 5 2.5 COC(=O)[C@@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1
CHEMBL224510 ccr2_human Human No 6.0 IC50 = 1000 nM Funct
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
342 4 2 3 3.9 Fc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1F
CHEMBL225166 ccr2_human Human No 6.0 IC50 = 1000 nM Funct
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
312 4 2 4 3.7 c1cc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cs1
CHEMBL225582 ccr2_human Human No 6.0 IC50 = 1000 nM Funct
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
307 4 1 3 3.6 c1ccc(CN2CCCC(Oc3ccc4[nH]ncc4c3)C2)cc1
CHEMBL225637 ccr2_human Human No 6.0 IC50 = 1000 nM Funct
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
336 5 2 4 3.6 COc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1
CHEMBL388516 ccr2_human Human No 6.0 IC50 = 1000 nM Funct
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
320 4 2 3 3.9 Cc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1
CHEMBL415061 ccr2_human Human No 6.0 IC50 = 1000 nM Funct
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
334 4 2 3 3.4 O=C(Nc1ccc2[nH]ncc2c1)C1CCCN(Cc2ccccc2)C1
CHEMBL426925 ccr2_human Human No 6.0 IC50 = 1000 nM Funct
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
340 4 2 3 4.3 Clc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1
CHEMBL427245 ccr2_human Human No 6.0 IC50 = 1000 nM Funct
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
326 4 2 3 3.9 Clc1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)cc1
CHEMBL427254 ccr2_human Human No 6.0 IC50 = 1000 nM Funct
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
321 4 3 4 3.2 Nc1ccccc1CN1CCCC(Nc2ccc3[nH]ncc3c2)C1
CHEMBL387625 ccr2_human Human Yes 6.0 IC50 = 1000 nM Funct
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
318 4 2 4 3.5 Nc1cccc(CN2CC[C@@H](Nc3cccc4cnccc34)C2)c1
CHEMBL209975 ccr2_human Human No 6.0 IC50 = 1000 nM Bind
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
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
CHEMBL1688889 ccr2_rat Rat No 5.0 IC50 = 10000 nM Funct
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
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
CHEMBL1739922 ccr2_rat Rat No 5.0 IC50 = 10000 nM Funct
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
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
CHEMBL403424 ccr2_human Human No 5.0 IC50 = 10000 nM Funct
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
453 7 2 3 3.9 O=C(CCNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1
CHEMBL83338 ccr2_human Human Yes 5.0 IC50 = 10000 nM Bind
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
556 8 0 4 5.3 CN(C[C@@H](CCN1CCC2(CC1)C[S+]([O-])c1ccccc12)c1cccc(Cl)c1)S(=O)(=O)c1ccccc1
CHEMBL1833983 ccr2_human Human No 5.0 IC50 = 10000 nM Bind
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
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
CHEMBL442451 ccr2_human Human No 5.0 IC50 = 10000 nM Bind
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
385 6 2 3 2.8 Cc1ccc(C(=O)NCC(=O)N[C@@H]2CCN(Cc3ccc(Cl)cc3)C2)cc1
CHEMBL195433 ccr2_human Human Yes 5.0 IC50 = 10000 nM Bind
Inhibition of C-C chemokine receptor type 2Inhibition of C-C chemokine receptor type 2
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
CHEMBL363840 ccr2_human Human No 5.0 IC50 = 10000 nM Bind
Inhibition of C-C chemokine receptor type 2Inhibition of C-C chemokine receptor type 2
505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1
CHEMBL224166 ccr2_human Human No 5.0 IC50 = 10000 nM Funct
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
295 4 3 3 3.0 c1c[nH]c(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1
CHEMBL386937 ccr2_human Human No 5.0 IC50 = 10000 nM Funct
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
292 4 2 3 3.2 c1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)cc1
CHEMBL387954 ccr2_human Human Yes 5.0 IC50 = 10000 nM Funct
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
339 4 1 3 4.2 Fc1cccc(F)c1CN1CCC(Nc2cccc3cnccc23)C1
CHEMBL1782579 ccr2_human Human No 7.0 IC50 = 101 nM Funct
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
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
CHEMBL2088383 ccr2_human Human No 7.0 IC50 = 102 nM Bind
Binding affinity to CCR2Binding affinity to CCR2
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
CHEMBL393632 ccr2_human Human No 6.0 IC50 = 1020 nM Bind
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
421 6 1 2 5.2 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)CC1CCOCC1
CHEMBL128640 ccr2_human Human No 6.0 IC50 = 1020 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
369 3 1 4 3.9 O=C(O)c1cc2ccccc2n1S(=O)(=O)c1ccc(Cl)c(Cl)c1
CHEMBL3650376 ccr2_human Human No 6.0 IC50 = 1020 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL4760108 ccr2_human Human No 7.0 IC50 = 103 nM Bind
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
471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1
CHEMBL270182 ccr2_human Human No 7.0 IC50 = 103 nM Funct
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
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
CHEMBL131087 ccr2_human Human No 6.0 IC50 = 1030 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
343 3 1 4 4.2 Clc1ccc(Cn2c(-c3nn[nH]n3)cc3ccccc32)cc1Cl
CHEMBL2018541 ccr2_human Human No 6.0 IC50 = 1040 nM Bind
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
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
CHEMBL335378 ccr2_human Human No 6.0 IC50 = 1050 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
387 3 1 2 5.7 O=C(O)c1cc2ccc(C(F)(F)F)cc2n1Cc1ccc(Cl)c(Cl)c1
CHEMBL2036768 ccr2_human Human No 6.0 IC50 = 1055 nM Bind
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
367 4 1 4 2.6 N#Cc1cccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)c1
CHEMBL3650361 ccr2_human Human No 7.0 IC50 = 106 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL239170 ccr2_human Human No 7.0 IC50 = 106.9 nM Bind
Inhibition of CCR2Inhibition of CCR2
622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1
CHEMBL239170 ccr2_human Human No 7.0 IC50 = 107 nM Bind
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
622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1
CHEMBL1210670 ccr2_human Human No 7.0 IC50 = 107.9 nM Bind
Inhibition of CCR2Inhibition of CCR2
550 12 1 4 7.6 CCN(CC)C(C)CCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1
CHEMBL2314065 ccr2_human Human No 6.0 IC50 = 1070 nM Bind
Binding affinity to human CCR2Binding affinity to human CCR2
481 4 1 5 3.7 COC1COCCC1N[C@@H]1C[C@H]2CCCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1
CHEMBL211106 ccr2_human Human No 6.0 IC50 = 1070 nM Bind
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
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
CHEMBL241502 ccr2_human Human No 7.0 IC50 = 108 nM Bind
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
564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1
CHEMBL132584 ccr2_human Human No 5.0 IC50 = 10840 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
364 4 1 4 4.6 O=C(O)c1cc2cccc([N+](=O)[O-])c2n1Cc1ccc(Cl)c(Cl)c1
CHEMBL481790 ccr2_human Human No 7.0 IC50 = 109 nM Funct
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1
CHEMBL481790 ccr2_human Human No 7.0 IC50 = 109 nM Funct
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
509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1
CHEMBL3263261 ccr2_human Human No 7.0 IC50 = 109 nM Bind
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
485 4 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2SCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1
CHEMBL3681893 ccr2_human Human No 6.0 IC50 = 1098 nM Bind
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 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.).
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
CHEMBL378195 ccr2_human Human No 8.0 IC50 = 11 nM Funct
Activity at CCR2b by calcium flux based FLIPR assay in CHO cellsActivity at CCR2b by calcium flux based FLIPR assay in CHO cells
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
CHEMBL1829619 ccr2_human Human No 8.0 IC50 = 11 nM Funct
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
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
CHEMBL257062 ccr2_human Human No 8.0 IC50 = 11 nM Funct
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
469 6 4 5 2.6 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1Cl
CHEMBL257063 ccr2_human Human No 8.0 IC50 = 11 nM Funct
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
450 7 3 5 2.4 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1
CHEMBL1834788 ccr2_human Human No 8.0 IC50 = 11 nM Funct
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
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
CHEMBL1834789 ccr2_human Human No 8.0 IC50 = 11 nM Funct
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
486 6 2 6 3.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cccnc4)CC3)C2)c2cc(C(F)(F)F)ccc21
CHEMBL1834792 ccr2_human Human No 8.0 IC50 = 11 nM Funct
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
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
CHEMBL1092921 ccr2_human Human No 8.0 IC50 = 11 nM Funct
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
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
CHEMBL3671251 ccr2_human Human No 8.0 IC50 = 11 nM Bind
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.
469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1
CHEMBL2088210 ccr2_human Human No 8.0 IC50 = 11 nM Bind
Binding affinity to CCR2Binding affinity to CCR2
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
CHEMBL2018538 ccr2_human Human No 8.0 IC50 = 11 nM Bind
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
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
CHEMBL3752627 ccr2_human Human No 8.0 IC50 = 11 nM Bind
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
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
CHEMBL1683075 ccr2_human Human No 8.0 IC50 = 11 nM Bind
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
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
CHEMBL2029412 ccr2_human Human No 8.0 IC50 = 11 nM Bind
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
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
CHEMBL2029571 ccr2_human Human No 8.0 IC50 = 11 nM Bind
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
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
CHEMBL271288 ccr2_human Human No 8.0 IC50 = 11 nM Bind
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1
CHEMBL247245 ccr2_human Human No 8.0 IC50 = 11 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL3263269 ccr2_human Human No 8.0 IC50 = 11 nM Bind
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
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
CHEMBL1684700 ccr2_human Human No 8.0 IC50 = 11.1 nM Bind
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
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
CHEMBL1782376 ccr2_human Human No 8.0 IC50 = 11.2 nM Bind
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
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
CHEMBL1683064 ccr2_human Human No 7.9 IC50 = 11.5 nM Bind
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
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
CHEMBL1684692 ccr2_human Human No 7.9 IC50 = 11.6 nM Bind
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
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
CHEMBL1684699 ccr2_human Human No 7.9 IC50 = 11.7 nM Bind
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
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
CHEMBL447937 ccr2_human Human No 7.9 IC50 = 11.8 nM Funct
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
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
CHEMBL1093153 ccr2_human Human No 7.0 IC50 = 110 nM Funct
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
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
CHEMBL3115275 ccr2_human Human No 7.0 IC50 = 110 nM Bind
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
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
CHEMBL1829636 ccr2_human Human No 7.0 IC50 = 110 nM Bind
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
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
CHEMBL246213 ccr2_human Human No 7.0 IC50 = 110 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL247456 ccr2_human Human No 7.0 IC50 = 110 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL248419 ccr2_human Human No 7.0 IC50 = 110 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
478 10 4 4 2.5 CCNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1
CHEMBL400158 ccr2_human Human No 7.0 IC50 = 110 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL133839 ccr2_human Human No 7.0 IC50 = 110 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
353 3 1 2 5.3 O=C(O)c1cc2cc(Cl)ccc2n1Cc1ccc(Cl)c(Cl)c1
CHEMBL1093154 ccr2_human Human No 6.0 IC50 = 1100 nM Funct
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
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
CHEMBL2313782 ccr2_human Human No 6.0 IC50 = 1100 nM Bind
Binding affinity to human CCR2Binding affinity to human CCR2
433 4 1 5 3.0 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(Cl)cc3C2)C1
CHEMBL400160 ccr2_human Human No 6.0 IC50 = 1100 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL379624 ccr2_human Human No 6.0 IC50 = 1100 nM Bind
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
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
CHEMBL384368 ccr2_human Human No 6.0 IC50 = 1100 nM Bind
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
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
CHEMBL443058 ccr2_human Human No 6.0 IC50 = 1100 nM Bind
Inhibition of human CCR2Inhibition of human CCR2
460 5 3 3 4.7 O=C(O)C(C1CCN(C(=O)Nc2ccccc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1
CHEMBL183966 ccr2_human Human No 5.0 IC50 = 11000 nM Bind
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
546 8 1 5 5.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(Cl)cc3)c3ccc(Cl)cc3)CC2)cc1
CHEMBL185032 ccr2_human Human No 5.0 IC50 = 11000 nM Bind
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
385 7 0 3 4.8 c1ccc(C(CCN2CCCN(Cc3ccncc3)CC2)c2ccccc2)cc1
CHEMBL183681 ccr2_human Human No 5.0 IC50 = 11000 nM Bind
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
399 7 2 3 3.1 O=C(CNC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1
CHEMBL187476 ccr2_human Human No 5.0 IC50 = 11000 nM Bind
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
384 8 1 3 4.1 O=C(CCCC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1
CHEMBL375556 ccr2_human Human Yes 5.0 IC50 = 11000 nM Funct
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
337 4 1 3 4.6 Clc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1
CHEMBL633 ccr2_human Human Yes 5.0 IC50 = 11086 nM Bind
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2
CHEMBL397717 ccr2_mouse Mouse No 7.0 IC50 = 111 nM Bind
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
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
CHEMBL3650368 ccr2_human Human No 6.0 IC50 = 1110 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL248617 ccr2_human Human No 5.0 IC50 = 11100 nM Bind
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
486 6 0 3 6.1 COc1ccccc1C1CCN(CC2CCN(C(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)CC1
CHEMBL474665 ccr2_human Human No 7.0 IC50 = 112 nM Bind
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
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
CHEMBL1092238 ccr2_human Human Yes 6.0 IC50 = 1120 nM Bind
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
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
CHEMBL3589845 ccr2_mouse Mouse No 5.0 IC50 = 11200 nM Bind
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
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
CHEMBL1210667 ccr2_human Human No 6.0 IC50 = 1122.0 nM Bind
Inhibition of CCR2Inhibition of CCR2
528 9 1 4 7.1 O=C(CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1
CHEMBL392493 ccr2_human Human No 6.0 IC50 = 1123 nM Bind
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
542 10 1 4 7.5 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1
CHEMBL1089881 ccr2_human Human No 6.0 IC50 = 1130 nM Bind
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
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
CHEMBL129958 ccr2_human Human No 6.0 IC50 = 1130 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
285 3 1 2 4.0 O=C(O)c1cc2ccccc2n1Cc1cccc(Cl)c1
CHEMBL246104 ccr2_human Human No 5.0 IC50 = 11350 nM Bind
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
407 5 1 2 5.0 C[N+](C)(Cc1cccc(NC(=O)c2ccc(Cl)c(Cl)c2)c1)C1CCOCC1
CHEMBL3753826 ccr2_human Human No 6.9 IC50 = 114 nM Bind
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
298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cc(Cl)cc(Cl)c2)C1
CHEMBL271935 ccr2_human Human No 6.9 IC50 = 114 nM Bind
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
435 7 2 4 2.8 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1
CHEMBL401890 ccr2_human Human No 6.9 IC50 = 115 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
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
CHEMBL236510 ccr2_human Human No 6.9 IC50 = 115 nM Bind
Inhibition of human CCR2Inhibition of human CCR2
485 6 2 3 5.1 Cc1ccc(/C=C/C(=O)N2CCC(C(C(=O)O)N3CCC(c4c[nH]c5ccccc45)CC3)CC2)cc1
CHEMBL1683083 ccr2_human Human No 6.9 IC50 = 116 nM Bind
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
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
CHEMBL257065 ccr2_human Human No 6.9 IC50 = 116 nM Bind
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1
CHEMBL271289 ccr2_human Human No 6.9 IC50 = 116 nM Bind
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
498 6 3 4 3.2 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1
CHEMBL1922817 ccr2_human Human No 4.9 IC50 = 11600 nM Funct
Antagonist activity at human CCR2Antagonist activity at human CCR2
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
CHEMBL238518 ccr2_human Human No 6.9 IC50 = 118 nM Funct
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
596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1
CHEMBL3115103 ccr2_human Human No 6.9 IC50 = 118 nM Bind
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
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
CHEMBL1090548 ccr2_human Human No 5.9 IC50 = 1180 nM Bind
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
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
CHEMBL497576 ccr2_human Human No 5.9 IC50 = 1180 nM Bind
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
494 8 4 5 4.0 CSc1ccc(CNC2CCCCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1
CHEMBL2036752 ccr2_human Human No 5.9 IC50 = 1184 nM Bind
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
398 4 1 3 3.9 CCN1CCC[C@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1
CHEMBL409712 ccr2_human Human No 5.9 IC50 = 1190 nM Bind
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
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
CHEMBL130724 ccr2_human Human No 5.9 IC50 = 1190 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
387 3 1 2 5.7 O=C(O)c1cc2c(C(F)(F)F)cccc2n1Cc1ccc(Cl)c(Cl)c1
CHEMBL1178786 ccr2_human Human Yes 7.9 IC50 = 12 nM Funct
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
495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C
CHEMBL2018402 ccr2_human Human No 7.9 IC50 = 12 nM Funct
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
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
CHEMBL2029568 ccr2_human Human No 7.9 IC50 = 12 nM Funct
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
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
CHEMBL1922823 ccr2_human Human No 7.9 IC50 = 12 nM Funct
Antagonist activity at human CCR2Antagonist activity at human CCR2
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
CHEMBL1290412 ccr2_human Human No 7.9 IC50 = 12 nM Funct
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
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
CHEMBL271725 ccr2_human Human No 7.9 IC50 = 12 nM Funct
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
449 6 4 5 2.3 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N
CHEMBL1834799 ccr2_human Human No 7.9 IC50 = 12 nM Funct
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
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
CHEMBL1088874 ccr2_human Human No 7.9 IC50 = 12 nM Funct
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
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
CHEMBL481790 ccr2_human Human No 7.9 IC50 = 12 nM Bind
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1
CHEMBL1834631 ccr2_human Human No 7.9 IC50 = 12 nM Bind
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
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
CHEMBL1834633 ccr2_human Human No 7.9 IC50 = 12 nM Bind
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
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
CHEMBL1834634 ccr2_human Human No 7.9 IC50 = 12 nM Bind
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
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
CHEMBL1946832 ccr2_human Human No 7.9 IC50 = 12 nM Bind
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
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
CHEMBL1944777 ccr2_human Human No 7.9 IC50 = 12 nM Bind
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
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
CHEMBL378195 ccr2_human Human No 7.9 IC50 = 12 nM Bind
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
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
CHEMBL256154 ccr2_human Human No 7.9 IC50 = 12 nM Bind
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
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
CHEMBL1684701 ccr2_human Human No 7.9 IC50 = 12 nM Bind
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
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
CHEMBL4519152 ccr2_human Human Yes 7.9 IC50 = 12 nM Bind
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
351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C
CHEMBL4760108 ccr2_human Human No 7.9 IC50 = 12 nM Bind
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
471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1
CHEMBL1684691 ccr2_human Human No 7.9 IC50 = 12.2 nM Bind
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
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
CHEMBL257065 ccr2_human Human No 7.9 IC50 = 12.4 nM Funct
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
419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1
CHEMBL500175 ccr2_human Human No 7.9 IC50 = 12.5 nM Bind
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
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
CHEMBL480228 ccr2_human Human No 7.9 IC50 = 12.5 nM Bind
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1
CHEMBL4519152 ccr2_human Human Yes 7.9 IC50 = 12.6 nM Bind
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
351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C
CHEMBL4760108 ccr2_human Human No 7.9 IC50 = 12.6 nM Bind
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
471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1
CHEMBL481202 ccr2_human Human No 7.9 IC50 = 12.6 nM Funct
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
490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1
CHEMBL451340 ccr2_human Human No 7.9 IC50 = 12.7 nM Funct
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
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
CHEMBL1684707 ccr2_human Human No 7.9 IC50 = 12.8 nM Bind
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
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
CHEMBL230832 ccr2_human Human No 7.9 IC50 = 12.9 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL1289203 ccr2_mouse Mouse No 7.9 IC50 = 12.9 nM Funct
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
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
CHEMBL1093470 ccr2_human Human No 6.9 IC50 = 120 nM Funct
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
545 8 2 5 2.4 Cc1ccccc1C(=O)N1CCN(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1
CHEMBL3681876 ccr2_human Human No 6.9 IC50 = 120 nM Bind
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 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.).
524 7 3 3 5.1 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCC3)CC1
CHEMBL3671260 ccr2_human Human No 6.9 IC50 = 120 nM Bind
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.
483 4 1 7 1.8 COC1COCCC1NC1CC2OC(=O)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1
CHEMBL1834639 ccr2_human Human No 6.9 IC50 = 120 nM Bind
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
491 6 2 5 4.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C4CCCCC4)CC3)C2)c2cc(C(F)(F)F)ccc21
CHEMBL394897 ccr2_human Human No 6.9 IC50 = 120 nM Bind
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
427 5 1 3 4.5 C[N+](C)(Cc1ccc(NC(=O)C2=Cc3ccc(Cl)cc3OC2)cc1)C1CCOCC1
CHEMBL1290186 ccr2_human Human No 6.9 IC50 = 120 nM Bind
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
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
CHEMBL246410 ccr2_human Human No 6.9 IC50 = 120 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL247203 ccr2_human Human No 6.9 IC50 = 120 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL248423 ccr2_human Human No 6.9 IC50 = 120 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL373491 ccr2_human Human No 6.9 IC50 = 120 nM Bind
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
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
CHEMBL130403 ccr2_human Human No 6.9 IC50 = 120 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
333 3 1 2 5.0 Cc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1Cl
CHEMBL237753 ccr2_human Human No 6.9 IC50 = 120 nM Bind
Inhibition of human CCR2Inhibition of human CCR2
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
CHEMBL272168 ccr2_human Human No 5.9 IC50 = 1200 nM Funct
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
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
CHEMBL2036782 ccr2_mouse Mouse No 5.9 IC50 = 1200 nM Funct
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
427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1
CHEMBL2096789 ccr2_human Human Yes 5.9 IC50 = 1200 nM Bind
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCN(Cc2ccc(Cl)cc2)C1
CHEMBL1829611 ccr2_human Human No 5.9 IC50 = 1200 nM Bind
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
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
CHEMBL495202 ccr2_human Human No 5.9 IC50 = 1200 nM Bind
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
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
CHEMBL246397 ccr2_human Human No 5.9 IC50 = 1200 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL401637 ccr2_human Human No 5.9 IC50 = 1200 nM Bind
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
478 9 1 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2ccc(Cl)cc2)CC1
CHEMBL3589843 ccr2_human Human No 4.9 IC50 = 12000 nM Funct
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
478 6 1 3 5.2 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(F)cc(C(F)(F)F)c3)CC2)O1
CHEMBL1688889 ccr2_mouse Mouse No 4.9 IC50 = 12000 nM Funct
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
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
CHEMBL1739922 ccr2_mouse Mouse No 4.9 IC50 = 12000 nM Funct
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
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
CHEMBL181918 ccr2_human Human No 4.9 IC50 = 12000 nM Bind
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
496 8 1 5 4.1 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(F)c3)CC2)cc1
CHEMBL249607 ccr2_human Human No 4.9 IC50 = 12000 nM Bind
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
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
CHEMBL407145 ccr2_human Human No 4.9 IC50 = 12000 nM Bind
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
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
CHEMBL257702 ccr2_human Human Yes 6.9 IC50 = 121 nM Funct
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
423 6 2 3 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(F)cc2)C1
CHEMBL403281 ccr2_human Human No 6.9 IC50 = 121 nM Bind
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
431 7 2 3 3.5 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1
CHEMBL132662 ccr2_human Human No 5.9 IC50 = 1210 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
349 4 1 3 4.7 COc1cccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c12
CHEMBL3115115 ccr2_human Human No 5.9 IC50 = 1215 nM Bind
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
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
CHEMBL3681899 ccr2_human Human No 6.9 IC50 = 122 nM Bind
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 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.).
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
CHEMBL1210669 ccr2_human Human No 5.9 IC50 = 1224.6 nM Bind
Inhibition of CCR2Inhibition of CCR2
536 12 1 4 7.2 CCN(CC)CCCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1
CHEMBL392494 ccr2_human Human No 5.9 IC50 = 1225 nM Bind
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
550 13 1 4 7.6 CCN(CC)CCCCNC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1
CHEMBL2036750 ccr2_human Human No 6.9 IC50 = 123 nM Bind
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
398 4 1 3 3.9 CCN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1
CHEMBL494541 ccr2_human Human No 6.9 IC50 = 123 nM Bind
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
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
CHEMBL495717 ccr2_human Human No 6.9 IC50 = 123 nM Bind
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
509 9 5 6 2.8 CCSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1
CHEMBL494542 ccr2_human Human No 6.9 IC50 = 123.0 nM Bind
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
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
CHEMBL2018539 ccr2_human Human No 5.9 IC50 = 1230 nM Bind
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
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
CHEMBL340072 ccr2_human Human No 4.9 IC50 = 12300 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
395 4 1 2 6.4 O=C(O)c1cc2ccc(-c3ccccc3)cc2n1Cc1ccc(Cl)c(Cl)c1
CHEMBL4125866 ccr2_human Human No 4.9 IC50 = 12330 nM Funct
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
489 6 1 5 4.1 CC(=O)N1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1
CHEMBL3589841 ccr2_human Human No 5.9 IC50 = 1240 nM Funct
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
544 7 1 4 5.7 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1
CHEMBL2088387 ccr2_human Human No 6.9 IC50 = 125 nM Bind
Binding affinity to CCR2Binding affinity to CCR2
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
CHEMBL2314061 ccr2_human Human No 6.9 IC50 = 125 nM Bind
Binding affinity to human CCR2Binding affinity to human CCR2
437 3 1 4 3.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCOCC1)C2
CHEMBL211923 ccr2_human Human No 6.9 IC50 = 125 nM Bind
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
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
CHEMBL434059 ccr2_human Human No 6.9 IC50 = 125 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
337 3 1 2 4.8 O=C(O)c1cc2cccc(F)c2n1Cc1ccc(Cl)c(Cl)c1
CHEMBL252815 ccr2_human Human No 6.9 IC50 = 125.9 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
514 9 1 2 7.0 CCCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1
CHEMBL2313774 ccr2_human Human No 5.9 IC50 = 1258 nM Bind
Binding affinity to human CCR2Binding affinity to human CCR2
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
CHEMBL252815 ccr2_human Human No 6.9 IC50 = 126 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
514 9 1 2 7.0 CCCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1
CHEMBL3115267 ccr2_human Human No 6.9 IC50 = 126 nM Bind
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
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
CHEMBL214641 ccr2_human Human No 6.9 IC50 = 126 nM Bind
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
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
CHEMBL2029411 ccr2_human Human No 6.9 IC50 = 126 nM Bind
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
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
CHEMBL230617 ccr2_mouse Mouse No 6.9 IC50 = 126 nM Bind
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
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
CHEMBL250408 ccr2_human Human No 4.9 IC50 = 12600 nM Bind
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
460 9 2 3 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2ccc(O)cc2)CC1
CHEMBL130065 ccr2_human Human No 4.9 IC50 = 12600 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
334 3 2 3 4.3 Nc1ccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c2c1
CHEMBL4128975 ccr2_human Human No 5.9 IC50 = 1261 nM Funct
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
446 6 1 4 5.4 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCCCC1
CHEMBL272543 ccr2_human Human No 6.9 IC50 = 127 nM Funct
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
419 6 2 3 3.1 Cc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1
CHEMBL2035000 ccr2_human Human No 6.9 IC50 = 127 nM Bind
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
376 4 1 3 3.4 O=C(Nc1ccc(Cl)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1
CHEMBL133748 ccr2_human Human No 5.9 IC50 = 1270 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
387 3 1 2 5.7 O=C(O)c1cc2cccc(C(F)(F)F)c2n1Cc1ccc(Cl)c(Cl)c1
CHEMBL131493 ccr2_human Human No 4.9 IC50 = 12700 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
318 3 1 2 4.1 NC(=O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1
CHEMBL231143 ccr2_mouse Mouse No 6.9 IC50 = 128 nM Bind
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
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
CHEMBL3263260 ccr2_human Human No 5.9 IC50 = 1280 nM Bind
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
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
CHEMBL215759 ccr2_human Human No 6.9 IC50 = 129 nM Bind
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
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
CHEMBL3650362 ccr2_human Human No 5.9 IC50 = 1290 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL2204259 ccr2_human Human No 7.9 IC50 = 13 nM Funct
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
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
CHEMBL526091 ccr2_human Human No 7.9 IC50 = 13 nM Funct
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
551 11 4 6 3.9 CCCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1
CHEMBL526859 ccr2_human Human No 7.9 IC50 = 13 nM Funct
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
565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1
CHEMBL2018390 ccr2_human Human No 7.9 IC50 = 13 nM Funct
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
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
CHEMBL230832 ccr2_human Human No 7.9 IC50 = 13 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL3681870 ccr2_human Human No 7.9 IC50 = 13 nM Bind
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 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.).
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
CHEMBL2029422 ccr2_rat Rat No 7.9 IC50 = 13 nM Bind
Binding affinity to rat CCR2Binding affinity to rat CCR2
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
CHEMBL1829624 ccr2_human Human No 7.9 IC50 = 13 nM Bind
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
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
CHEMBL1834635 ccr2_human Human No 7.9 IC50 = 13 nM Bind
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
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
CHEMBL1834640 ccr2_human Human No 7.9 IC50 = 13 nM Bind
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
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
CHEMBL1834794 ccr2_human Human No 7.9 IC50 = 13 nM Bind
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
492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21
CHEMBL213058 ccr2_human Human No 7.9 IC50 = 13 nM Bind
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
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
CHEMBL230832 ccr2_human Human No 7.9 IC50 = 13 nM Bind
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
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
CHEMBL209063 ccr2_human Human No 7.9 IC50 = 13 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
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
CHEMBL231252 ccr2_human Human No 7.9 IC50 = 13 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
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
CHEMBL231340 ccr2_human Human No 7.9 IC50 = 13 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
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
CHEMBL1684695 ccr2_human Human No 7.9 IC50 = 13 nM Bind
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
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
CHEMBL1782379 ccr2_human Human No 7.9 IC50 = 13 nM Bind
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
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
CHEMBL393267 ccr2_human Human No 7.9 IC50 = 13 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL3577935 ccr2_human Human No 7.9 IC50 = 13 nM Bind
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
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
CHEMBL496432 ccr2_human Human No 7.9 IC50 = 13.1 nM Bind
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
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
CHEMBL230507 ccr2_human Human No 7.9 IC50 = 13.2 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL389773 ccr2_human Human No 7.9 IC50 = 13.2 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL2088389 ccr2_human Human No 7.9 IC50 = 13.3 nM Funct
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
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
CHEMBL230507 ccr2_human Human No 7.9 IC50 = 13.3 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL389773 ccr2_human Human No 7.9 IC50 = 13.3 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL230507 ccr2_human Human No 7.9 IC50 = 13.3 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
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
CHEMBL389773 ccr2_human Human No 7.9 IC50 = 13.3 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
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
CHEMBL481009 ccr2_human Human No 7.9 IC50 = 13.5 nM Funct
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
523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1
CHEMBL1683189 ccr2_human Human No 7.9 IC50 = 13.5 nM Bind
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
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
CHEMBL1684705 ccr2_human Human No 7.9 IC50 = 13.9 nM Bind
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
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
CHEMBL1922794 ccr2_human Human No 6.9 IC50 = 130 nM Funct
Antagonist activity at human CCR2Antagonist activity at human CCR2
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
CHEMBL1922816 ccr2_human Human No 6.9 IC50 = 130 nM Funct
Antagonist activity at human CCR2Antagonist activity at human CCR2
518 7 3 3 5.2 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(Cl)cc2)CC1
CHEMBL270906 ccr2_human Human No 6.9 IC50 = 130 nM Funct
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
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
CHEMBL1922816 ccr2_human Human No 6.9 IC50 = 130 nM Bind
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 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.).
518 7 3 3 5.2 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(Cl)cc2)CC1
CHEMBL3681873 ccr2_human Human No 6.9 IC50 = 130 nM Bind
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 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.).
541 6 4 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(C(F)(F)F)cc2)CC1
CHEMBL3681900 ccr2_human Human No 6.9 IC50 = 130 nM Bind
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 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.).
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
CHEMBL2313777 ccr2_human Human No 6.9 IC50 = 130 nM Bind
Binding affinity to human CCR2Binding affinity to human CCR2
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
CHEMBL1944773 ccr2_human Human No 6.9 IC50 = 130 nM Bind
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
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
CHEMBL1684689 ccr2_human Human No 6.9 IC50 = 130 nM Bind
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
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
CHEMBL246221 ccr2_human Human No 6.9 IC50 = 130 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL427705 ccr2_human Human No 6.9 IC50 = 130 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL249608 ccr2_human Human No 6.9 IC50 = 130 nM Bind
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
472 7 1 3 5.3 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1
CHEMBL226066 ccr2_mouse Mouse No 6.9 IC50 = 130 nM Bind
Displacement of [125]hMCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125]hMCP1 from mouse CCR2 receptor expressed in CHO cells
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
CHEMBL1829615 ccr2_human Human No 5.9 IC50 = 1300 nM Funct
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
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
CHEMBL1922805 ccr2_human Human No 5.9 IC50 = 1300 nM Funct
Antagonist activity at human CCR2Antagonist activity at human CCR2
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
CHEMBL1922808 ccr2_human Human No 5.9 IC50 = 1300 nM Funct
Antagonist activity at human CCR2Antagonist activity at human CCR2
498 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)C2CC2c2ccccc2)CC1
CHEMBL520228 ccr2_human Human No 5.9 IC50 = 1300 nM Funct
Antagonist activity at human CCR2Antagonist activity at human CCR2
482 5 1 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ncccc34)CC2)CC1
CHEMBL3115270 ccr2_human Human No 5.9 IC50 = 1300 nM Bind
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
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
CHEMBL246412 ccr2_human Human No 5.9 IC50 = 1300 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL184053 ccr2_human Human No 4.9 IC50 = 13000 nM Bind
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
462 8 0 4 4.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1
CHEMBL2088386 ccr2_human Human No 6.9 IC50 = 131.5 nM Bind
Binding affinity to CCR2Binding affinity to CCR2
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
CHEMBL1088874 ccr2_human Human No 5.9 IC50 = 1310 nM Bind
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
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
CHEMBL130937 ccr2_human Human No 5.9 IC50 = 1310 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
364 4 1 4 4.6 O=C(O)c1cc2c([N+](=O)[O-])cccc2n1Cc1ccc(Cl)c(Cl)c1
CHEMBL1922794 ccr2_human Human No 6.9 IC50 = 132 nM Bind
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 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.).
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
CHEMBL377432 ccr2_human Human No 4.9 IC50 = 13400 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
402 5 1 3 5.5 CN(CCN1CCCCC1)c1ccc(-c2nc3cc(Cl)c(Cl)cc3[nH]2)cc1
CHEMBL231142 ccr2_human Human No 6.9 IC50 = 135 nM Bind
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
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
CHEMBL1782375 ccr2_human Human No 6.9 IC50 = 135 nM Bind
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
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
CHEMBL480036 ccr2_human Human No 6.9 IC50 = 135.7 nM Bind
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
550 9 4 5 4.0 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1
CHEMBL1922818 ccr2_human Human No 6.9 IC50 = 136 nM Bind
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 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.).
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
CHEMBL2088382 ccr2_human Human No 6.9 IC50 = 136.5 nM Bind
Binding affinity to CCR2Binding affinity to CCR2
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
CHEMBL272542 ccr2_human Human No 5.9 IC50 = 1360 nM Bind
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
435 7 2 4 2.8 COc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1
CHEMBL132725 ccr2_human Human Yes 5.9 IC50 = 1360 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
285 3 1 2 4.0 O=C(O)c1cc2ccccc2n1Cc1ccc(Cl)cc1
CHEMBL3650369 ccr2_human Human No 5.9 IC50 = 1390 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL2018400 ccr2_human Human No 7.9 IC50 = 14 nM Funct
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
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
CHEMBL1829624 ccr2_human Human No 7.9 IC50 = 14 nM Funct
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
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
CHEMBL455682 ccr2_human Human No 7.9 IC50 = 14 nM Funct
Antagonist activity at human CCR2Antagonist activity at human CCR2
515 5 3 4 5.4 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1
CHEMBL3263268 ccr2_human Human No 7.9 IC50 = 14 nM Bind
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
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
CHEMBL255209 ccr2_human Human Yes 7.9 IC50 = 14 nM Funct
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
466 7 4 6 2.1 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O
CHEMBL1834781 ccr2_human Human No 7.9 IC50 = 14 nM Funct
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
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
CHEMBL1834793 ccr2_human Human No 7.9 IC50 = 14 nM Funct
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
492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc21
CHEMBL252412 ccr2_human Human No 7.9 IC50 = 14 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL1290636 ccr2_mouse Mouse No 7.9 IC50 = 14 nM Funct
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
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
CHEMBL3681870 ccr2_human Human No 7.9 IC50 = 14 nM Bind
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 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.).
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
CHEMBL3671259 ccr2_human Human No 7.9 IC50 = 14 nM Bind
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.
545 5 1 6 4.1 COC1COCCC1NC1CC2OC(c3ccccc3)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1
CHEMBL441856 ccr2_human Human No 7.9 IC50 = 14 nM Bind
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
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
CHEMBL1951773 ccr2_human Human No 7.9 IC50 = 14 nM Bind
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
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
CHEMBL231149 ccr2_human Human No 7.9 IC50 = 14 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
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
CHEMBL408908 ccr2_human Human No 7.9 IC50 = 14 nM Bind
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
451 6 5 6 1.7 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O
CHEMBL3263259 ccr2_human Human No 7.9 IC50 = 14 nM Bind
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
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
CHEMBL252412 ccr2_human Human No 7.9 IC50 = 14.1 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL397750 ccr2_human Human No 7.8 IC50 = 14.3 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL397750 ccr2_human Human No 7.8 IC50 = 14.3 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
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
CHEMBL492564 ccr2_human Human No 7.8 IC50 = 14.3 nM Bind
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
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
CHEMBL397750 ccr2_human Human No 7.8 IC50 = 14.5 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL438514 ccr2_human Human No 7.8 IC50 = 14.5 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
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
CHEMBL1684696 ccr2_human Human No 7.8 IC50 = 14.6 nM Bind
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
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
CHEMBL1684709 ccr2_human Human No 7.8 IC50 = 14.7 nM Bind
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
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
CHEMBL1922818 ccr2_human Human No 6.9 IC50 = 140 nM Funct
Antagonist activity at human CCR2Antagonist activity at human CCR2
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
CHEMBL1834851 ccr2_human Human No 6.9 IC50 = 140 nM Funct
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
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
CHEMBL4070869 ccr2_human Human No 6.9 IC50 = 140 nM Funct
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
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
CHEMBL1834647 ccr2_human Human No 6.9 IC50 = 140 nM Bind
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
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
CHEMBL400483 ccr2_human Human No 6.9 IC50 = 140 nM Bind
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
486 7 1 3 6.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4ccc(Cl)c(Cl)c4)C3)CC2)cc1
CHEMBL211092 ccr2_human Human No 6.9 IC50 = 140 nM Bind
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
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
CHEMBL3650350 ccr2_human Human No 6.9 IC50 = 140 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL392493 ccr2_human Human No 5.9 IC50 = 1400 nM Funct
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
542 10 1 4 7.5 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1
CHEMBL1688888 ccr2_mouse Mouse No 5.9 IC50 = 1400 nM Funct
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
395 2 2 5 3.4 Cc1nn(C)c2ncc(C(=O)NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc12
CHEMBL1922803 ccr2_human Human No 5.9 IC50 = 1400 nM Funct
Antagonist activity at human CCR2Antagonist activity at human CCR2
457 6 2 3 3.0 NC(=O)C(NC1Cc2ccccc2C1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1
CHEMBL1834850 ccr2_human Human No 5.9 IC50 = 1400 nM Bind
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
489 6 2 7 3.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccn4C)CC3)C2)c2cc(C(F)(F)F)ccc21
CHEMBL249010 ccr2_human Human No 5.9 IC50 = 1400 nM Bind
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
490 5 0 2 6.5 O=C(/C=C/c1cccc(C(F)(F)F)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1
CHEMBL186878 ccr2_human Human No 4.9 IC50 = 14000 nM Bind
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
399 7 2 3 3.2 Cc1cccc(C(=O)NCC(=O)NCC2CCCN2Cc2ccc(Cl)cc2)c1
CHEMBL223815 ccr2_human Human Yes 4.9 IC50 = 14000 nM Funct
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
337 4 1 3 4.6 Clc1cccc(CN2CCC(Nc3cccc4cnccc34)C2)c1
CHEMBL388285 ccr2_human Human Yes 4.9 IC50 = 14000 nM Funct
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
318 4 2 4 3.5 Nc1ccccc1CN1CCC(Nc2cccc3cnccc23)C1
CHEMBL522688 ccr2_human Human No 6.9 IC50 = 141 nM Bind
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
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
CHEMBL1092921 ccr2_human Human No 5.9 IC50 = 1410 nM Bind
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
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
CHEMBL3650400 ccr2_human Human No 5.9 IC50 = 1410 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL402010 ccr2_human Human No 6.8 IC50 = 144 nM Bind
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
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
CHEMBL3650353 ccr2_human Human No 4.8 IC50 = 14430 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL2036765 ccr2_human Human No 5.8 IC50 = 1458 nM Bind
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
372 5 1 4 2.7 COc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1
CHEMBL1782574 ccr2_human Human No 6.8 IC50 = 147 nM Funct
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
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
CHEMBL231142 ccr2_mouse Mouse No 6.8 IC50 = 147 nM Bind
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
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
CHEMBL3650356 ccr2_human Human No 5.8 IC50 = 1470 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL378658 ccr2_human Human No 5.8 IC50 = 1477 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
447 8 2 3 4.2 CN(C)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1
CHEMBL3650374 ccr2_human Human No 6.8 IC50 = 148 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL339842 ccr2_human Human No 5.8 IC50 = 1480 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
319 3 1 2 4.7 O=C(O)c1cc2cc(Cl)ccc2n1Cc1ccccc1Cl
CHEMBL3681877 ccr2_human Human No 6.8 IC50 = 149 nM Bind
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 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.).
526 7 3 4 4.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCO3)CC1
CHEMBL2315920 ccr2_human Human No 7.8 IC50 = 15 nM Bind
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
483 6 2 5 4.6 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1
CHEMBL2315921 ccr2_human Human No 7.8 IC50 = 15 nM Bind
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
499 6 3 6 3.7 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C1
CHEMBL3752627 ccr2_human Human No 7.8 IC50 = 15 nM Funct
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
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
CHEMBL1829605 ccr2_human Human No 7.8 IC50 = 15 nM Funct
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
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
CHEMBL2029417 ccr2_human Human No 7.8 IC50 = 15 nM Funct
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
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
CHEMBL1834719 ccr2_human Human No 7.8 IC50 = 15 nM Funct
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
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
CHEMBL1834790 ccr2_human Human No 7.8 IC50 = 15 nM Funct
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
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
CHEMBL1829631 ccr2_human Human No 7.8 IC50 = 15 nM Bind
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
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
CHEMBL1834721 ccr2_human Human No 7.8 IC50 = 15 nM Bind
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
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
CHEMBL385540 ccr2_human Human No 7.8 IC50 = 15 nM Bind
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
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
CHEMBL4742683 ccr2_human Human No 7.8 IC50 = 15 nM Bind
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
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
CHEMBL4760566 ccr2_human Human No 7.8 IC50 = 15 nM Bind
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
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
CHEMBL1683068 ccr2_human Human No 7.8 IC50 = 15 nM Bind
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
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
CHEMBL230721 ccr2_mouse Mouse No 7.8 IC50 = 15 nM Bind
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
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
CHEMBL436796 ccr2_mouse Mouse No 7.8 IC50 = 15 nM Bind
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
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
CHEMBL247455 ccr2_human Human No 7.8 IC50 = 15 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL3577929 ccr2_human Human No 7.8 IC50 = 15 nM Bind
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
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
CHEMBL236722 ccr2_human Human No 7.8 IC50 = 15 nM Bind
Inhibition of human CCR2Inhibition of human CCR2
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
CHEMBL392097 ccr2_human Human No 7.8 IC50 = 15 nM Bind
Inhibition of human CCR2Inhibition of human CCR2
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
CHEMBL1684714 ccr2_human Human No 7.8 IC50 = 15.2 nM Bind
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
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
CHEMBL1782580 ccr2_human Human No 7.8 IC50 = 15.4 nM Bind
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
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
CHEMBL230831 ccr2_human Human No 7.8 IC50 = 15.5 nM Bind
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
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
CHEMBL1782577 ccr2_human Human No 7.8 IC50 = 15.5 nM Bind
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
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
CHEMBL1782566 ccr2_human Human No 7.8 IC50 = 15.6 nM Bind
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
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
CHEMBL1782568 ccr2_human Human No 7.8 IC50 = 15.8 nM Bind
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
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
CHEMBL4760108 ccr2_human Human No 7.8 IC50 = 15.9 nM Bind
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
471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1
CHEMBL387587 ccr2_human Human No 7.8 IC50 = 15.9 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL246804 ccr2_human Human No 6.8 IC50 = 150 nM Funct
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
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
CHEMBL3681878 ccr2_human Human No 6.8 IC50 = 150 nM Bind
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 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.).
541 6 4 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cccc(C(F)(F)F)c2)CC1
CHEMBL2313771 ccr2_human Human No 6.8 IC50 = 150 nM Bind
Binding affinity to human CCR2Binding affinity to human CCR2
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
CHEMBL3752690 ccr2_human Human No 6.8 IC50 = 150 nM Bind
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
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
CHEMBL246417 ccr2_human Human No 6.8 IC50 = 150 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL247208 ccr2_human Human No 6.8 IC50 = 150 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL400793 ccr2_human Human No 6.8 IC50 = 150 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL209899 ccr2_human Human No 6.8 IC50 = 150 nM Bind
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
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
CHEMBL339099 ccr2_human Human No 6.8 IC50 = 150 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
353 3 1 2 5.3 O=C(O)c1cc2c(Cl)cccc2n1Cc1ccc(Cl)c(Cl)c1
CHEMBL1688879 ccr2_human Human No 5.8 IC50 = 1500 nM Funct
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
352 2 2 4 3.7 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1ccc(Cl)c(Cl)c1
CHEMBL1688880 ccr2_human Human No 5.8 IC50 = 1500 nM Funct
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
352 2 2 4 3.4 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1cccc(C(F)(F)F)c1
CHEMBL2313785 ccr2_human Human No 5.8 IC50 = 1500 nM Bind
Binding affinity to human CCR2Binding affinity to human CCR2
444 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc([N+](=O)[O-])cc3C2)C1
CHEMBL184256 ccr2_human Human No 5.8 IC50 = 1500 nM Bind
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
495 8 3 6 2.9 NS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1
CHEMBL185517 ccr2_human Human No 5.8 IC50 = 1500 nM Bind
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
512 8 2 6 3.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(F)cc3)c3cccc(O)c3)CC2)cc1
CHEMBL186689 ccr2_human Human No 5.8 IC50 = 1500 nM Bind
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
528 8 2 6 4.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(Cl)cc3)c3cccc(O)c3)CC2)cc1
CHEMBL185180 ccr2_human Human No 5.8 IC50 = 1500 nM Bind
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
510 8 3 7 3.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(O)c3)CC2)cc1
CHEMBL247405 ccr2_human Human No 5.8 IC50 = 1500 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
465 9 3 5 2.5 COC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1
CHEMBL249183 ccr2_human Human No 5.8 IC50 = 1500 nM Bind
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
474 10 1 3 6.2 COc1ccc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)cc1
CHEMBL209423 ccr2_human Human No 5.8 IC50 = 1500 nM Bind
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
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
CHEMBL246218 ccr2_human Human No 4.8 IC50 = 15000 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
465 9 3 5 2.5 COC(=O)[C@@H](CNC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)NCc1ccc(C)cc1C
CHEMBL223907 ccr2_human Human Yes 4.8 IC50 = 15000 nM Funct
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
318 4 2 4 3.5 Nc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1
CHEMBL1092940 ccr2_human Human No 6.8 IC50 = 151 nM Bind
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
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
CHEMBL3115269 ccr2_human Human No 6.8 IC50 = 152 nM Bind
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
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
CHEMBL3650388 ccr2_human Human No 5.8 IC50 = 1520 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL2314057 ccr2_human Human No 5.8 IC50 = 1529 nM Bind
Binding affinity to human CCR2Binding affinity to human CCR2
435 3 1 3 4.9 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCCC1)C2
CHEMBL502248 ccr2_human Human No 6.8 IC50 = 153 nM Bind
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
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
CHEMBL272331 ccr2_human Human No 6.8 IC50 = 153 nM Bind
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
451 7 3 5 2.5 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)ccc1O
CHEMBL3650367 ccr2_human Human No 6.8 IC50 = 153 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL239143 ccr2_human Human No 6.8 IC50 = 154 nM Funct
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
594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1
CHEMBL482387 ccr2_human Human No 6.8 IC50 = 155 nM Bind
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
508 7 4 5 3.6 CSc1ccc(C(=O)NC2CCCCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1
CHEMBL523857 ccr2_human Human No 6.8 IC50 = 156.0 nM Bind
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
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
CHEMBL257511 ccr2_human Human No 5.8 IC50 = 1550 nM Bind
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
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
CHEMBL1951766 ccr2_mouse Mouse No 6.8 IC50 = 156 nM Funct
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
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
CHEMBL523857 ccr2_human Human No 6.8 IC50 = 156 nM Bind
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
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
CHEMBL4127096 ccr2_human Human No 5.8 IC50 = 1566 nM Funct
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
476 7 1 5 5.0 COC1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1
CHEMBL1290637 ccr2_mouse Mouse No 6.8 IC50 = 158 nM Funct
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
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
CHEMBL2018533 ccr2_human Human No 6.8 IC50 = 158 nM Bind
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
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
CHEMBL1922800 ccr2_human Human No 4.8 IC50 = 15800 nM Funct
Antagonist activity at human CCR2Antagonist activity at human CCR2
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
CHEMBL3577939 ccr2_human Human No 7.8 IC50 = 16 nM Bind
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
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
CHEMBL450231 ccr2_human Human No 7.8 IC50 = 16 nM Funct
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
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
CHEMBL4463626 ccr2_human Human No 7.8 IC50 = 16 nM Funct
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
300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12
CHEMBL4517518 ccr2_human Human No 7.8 IC50 = 16 nM Funct
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
315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1
CHEMBL1922789 ccr2_human Human No 7.8 IC50 = 16 nM Funct
Antagonist activity at human CCR2Antagonist activity at human CCR2
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
CHEMBL4760108 ccr2_human Human No 7.8 IC50 = 16 nM Bind
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
471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1
CHEMBL337246 ccr2_human Human No 7.8 IC50 = 16 nM Funct
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
433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F
CHEMBL387587 ccr2_human Human No 7.8 IC50 = 16 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL2029422 ccr2_mouse Mouse No 7.8 IC50 = 16 nM Funct
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
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
CHEMBL3671251 ccr2_human Human No 7.8 IC50 = 16 nM Bind
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.
469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1
CHEMBL3671255 ccr2_human Human No 7.8 IC50 = 16 nM Bind
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.
509 5 1 6 3.1 COC1COCCC1NC1CC2OC(C3CC3)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1
CHEMBL2313768 ccr2_human Human No 7.8 IC50 = 16 nM Bind
Binding affinity to human CCR2Binding affinity to human CCR2
482 5 1 5 3.8 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(OC(F)(F)F)cc3C2)C1
CHEMBL2036758 ccr2_human Human No 7.8 IC50 = 16 nM Bind
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
412 4 1 3 4.3 CC(C)N1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1
CHEMBL2204262 ccr2_human Human No 7.8 IC50 = 16 nM Bind
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
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
CHEMBL1834792 ccr2_human Human No 7.8 IC50 = 16 nM Bind
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
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
CHEMBL2092884 ccr2_human Human No 7.8 IC50 = 16 nM Bind
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
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
CHEMBL479642 ccr2_human Human No 7.8 IC50 = 16 nM Bind
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
510 8 3 4 3.8 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)cc2)C1
CHEMBL387587 ccr2_human Human No 7.8 IC50 = 16 nM Bind
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
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
CHEMBL230165 ccr2_human Human No 7.8 IC50 = 16 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
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
CHEMBL398134 ccr2_human Human No 7.8 IC50 = 16 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL3263255 ccr2_human Human No 7.8 IC50 = 16 nM Bind
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
469 4 1 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1
CHEMBL3263258 ccr2_human Human No 7.8 IC50 = 16 nM Bind
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
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
CHEMBL499467 ccr2_human Human No 7.8 IC50 = 16.5 nM Funct
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
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
CHEMBL518772 ccr2_human Human No 7.8 IC50 = 16.5 nM Bind
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
518 9 3 4 4.3 CC(C)c1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1
CHEMBL3650408 ccr2_human Human No 7.8 IC50 = 16.5 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL399617 ccr2_human Human No 7.8 IC50 = 16.7 nM Bind
Inhibition of human CCR2Inhibition of human CCR2
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
CHEMBL1829637 ccr2_human Human No 6.8 IC50 = 160 nM Funct
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
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
CHEMBL411726 ccr2_human Human No 6.8 IC50 = 160 nM Funct
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
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
CHEMBL1092656 ccr2_human Human No 6.8 IC50 = 160 nM Funct
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
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
CHEMBL2018377 ccr2_human Human No 6.8 IC50 = 160 nM Bind
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
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
CHEMBL214747 ccr2_human Human No 6.8 IC50 = 160 nM Bind
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
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
CHEMBL246405 ccr2_human Human No 6.8 IC50 = 160 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL249413 ccr2_human Human No 6.8 IC50 = 160 nM Bind
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
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
CHEMBL249415 ccr2_human Human No 6.8 IC50 = 160 nM Bind
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
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
CHEMBL215515 ccr2_human Human No 6.8 IC50 = 160 nM Bind
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
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
CHEMBL3589949 ccr2_human Human No 5.8 IC50 = 1600 nM Funct
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
572 7 1 3 6.7 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1
CHEMBL1688878 ccr2_human Human No 5.8 IC50 = 1600 nM Funct
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
318 2 2 4 3.0 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1cccc(Cl)c1
CHEMBL3753478 ccr2_human Human No 5.8 IC50 = 1600 nM Bind
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
284 2 1 1 4.2 C[C@@]1(c2cccc(C(F)(F)F)c2)CCCC=C1C(=O)O
CHEMBL3650355 ccr2_human Human No 5.8 IC50 = 1600 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL3650382 ccr2_human Human No 5.8 IC50 = 1600 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL3650383 ccr2_human Human No 5.8 IC50 = 1600 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL3650389 ccr2_human Human No 5.8 IC50 = 1600 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL183001 ccr2_human Human No 4.8 IC50 = 16000 nM Bind
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
492 8 1 5 4.2 Cc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1
CHEMBL504065 ccr2_human Human No 5.8 IC50 = 1605 nM Bind
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
642 10 4 6 4.9 CSc1ccc(C(=O)NC2CCC(NC(=O)OCc3ccccc3)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1
CHEMBL2036754 ccr2_human Human No 6.8 IC50 = 161 nM Funct
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
424 5 1 3 4.3 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CC3CC3)C2)CC1
CHEMBL3263266 ccr2_human Human No 4.8 IC50 = 16100 nM Bind
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
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
CHEMBL4128487 ccr2_human Human No 5.8 IC50 = 1614 nM Funct
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
566 6 1 5 7.1 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC2(CC1)SCc1ccccc12
CHEMBL2036764 ccr2_human Human No 6.8 IC50 = 162 nM Funct
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
420 4 1 3 3.5 O=C(Nc1ccc(Br)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1
CHEMBL3588870 ccr2_human Human No 6.8 IC50 = 163 nM Funct
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
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
CHEMBL134230 ccr2_human Human No 5.8 IC50 = 1640 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
364 4 1 4 4.6 O=C(O)c1cc2ccc([N+](=O)[O-])cc2n1Cc1ccc(Cl)c(Cl)c1
CHEMBL257159 ccr2_human Human No 6.8 IC50 = 165 nM Bind
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
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
CHEMBL438128 ccr2_mouse Mouse No 6.8 IC50 = 165 nM Bind
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
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
CHEMBL257316 ccr2_human Human No 6.8 IC50 = 166 nM Bind
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
483 6 2 3 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1
CHEMBL480035 ccr2_human Human No 6.8 IC50 = 167.5 nM Bind
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
523 7 5 6 2.5 CSc1ccc(C(=O)NC2CCC(N)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1
CHEMBL238937 ccr2_human Human No 6.8 IC50 = 167.9 nM Bind
Inhibition of CCR2Inhibition of CCR2
530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(Cl)c2)nn1-c1ccc2ccccc2c1
CHEMBL238937 ccr2_human Human No 6.8 IC50 = 168 nM Bind
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
530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(Cl)c2)nn1-c1ccc2ccccc2c1
CHEMBL3753563 ccr2_human Human No 5.8 IC50 = 1685 nM Bind
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
248 2 1 1 3.5 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(F)cc2)C1
CHEMBL2204252 ccr2_human Human No 7.8 IC50 = 17 nM Funct
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
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
CHEMBL2315933 ccr2_human Human No 7.8 IC50 = 17 nM Bind
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
499 6 3 7 3.6 Nc1cccnc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1
CHEMBL3589952 ccr2_human Human No 7.8 IC50 = 17 nM Funct
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
554 7 1 3 6.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)C1CC1
CHEMBL2018384 ccr2_human Human No 7.8 IC50 = 17 nM Funct
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
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
CHEMBL487070 ccr2_human Human No 7.8 IC50 = 17 nM Funct
Antagonist activity at human CCR2Antagonist activity at human CCR2
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
CHEMBL1834794 ccr2_human Human No 7.8 IC50 = 17 nM Funct
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
492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21
CHEMBL2029422 ccr2_mouse Mouse No 7.8 IC50 = 17 nM Bind
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
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
CHEMBL2036760 ccr2_human Human No 7.8 IC50 = 17 nM Bind
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
444 4 1 3 4.4 O=C(Nc1ccc(C(F)(F)F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1
CHEMBL2036775 ccr2_human Human No 7.8 IC50 = 17 nM Bind
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
414 4 1 4 3.3 CC(C)N1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1
CHEMBL1683075 ccr2_human Human No 7.8 IC50 = 17 nM Bind
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
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
CHEMBL1683189 ccr2_human Human No 7.8 IC50 = 17 nM Bind
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
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
CHEMBL2018378 ccr2_human Human No 7.8 IC50 = 17 nM Bind
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
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
CHEMBL1288324 ccr2_human Human No 7.8 IC50 = 17 nM Bind
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
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
CHEMBL388869 ccr2_human Human No 7.8 IC50 = 17 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
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
CHEMBL1684697 ccr2_human Human No 7.8 IC50 = 17 nM Bind
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
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
CHEMBL231038 ccr2_mouse Mouse No 7.8 IC50 = 17 nM Bind
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
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
CHEMBL231246 ccr2_mouse Mouse No 7.8 IC50 = 17 nM Bind
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
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
CHEMBL337246 ccr2_human Human No 7.8 IC50 = 17 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F
CHEMBL1684708 ccr2_human Human No 7.8 IC50 = 17.3 nM Bind
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
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
CHEMBL480621 ccr2_human Human No 7.8 IC50 = 17.4 nM Funct
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
533 9 4 5 3.2 CC(=O)Nc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1
CHEMBL526859 ccr2_human Human No 7.8 IC50 = 17.5 nM Funct
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1
CHEMBL1684710 ccr2_human Human No 7.8 IC50 = 17.5 nM Bind
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
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
CHEMBL388007 ccr2_mouse Mouse No 7.8 IC50 = 17.5 nM Bind
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
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
CHEMBL3650391 ccr2_human Human No 7.8 IC50 = 17.6 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL1782570 ccr2_human Human No 7.8 IC50 = 17.8 nM Bind
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
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
CHEMBL3650407 ccr2_human Human No 7.8 IC50 = 17.9 nM Bind
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
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
CHEMBL1829621 ccr2_human Human No 6.8 IC50 = 170 nM Funct
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
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
CHEMBL1829636 ccr2_human Human No 6.8 IC50 = 170 nM Funct
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
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
CHEMBL1834636 ccr2_human Human No 6.8 IC50 = 170 nM Funct
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
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
CHEMBL1092343 ccr2_human Human No 6.8 IC50 = 170 nM Funct
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
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
CHEMBL3671251 ccr2_human Human No 6.8 IC50 = 170 nM Bind
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.
469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1
CHEMBL2313784 ccr2_human Human No 6.8 IC50 = 170 nM Bind
Binding affinity to human CCR2Binding affinity to human CCR2
467 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1
CHEMBL2036748 ccr2_human Human Yes 6.8 IC50 = 170 nM Bind
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
384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1
CHEMBL2204242 ccr2_human Human No 6.8 IC50 = 170 nM Bind
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
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
CHEMBL1834783 ccr2_human Human No 6.8 IC50 = 170 nM Bind
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
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
CHEMBL246933 ccr2_human Human No 6.8 IC50 = 170 nM Bind
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
407 5 1 3 4.2 Cc1ccc2c(c1)OCC(C(=O)Nc1ccc(C[N+](C)(C)C3CCOCC3)cc1)=C2
CHEMBL401009 ccr2_human Human No 6.8 IC50 = 170 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL339851 ccr2_human Human No 6.8 IC50 = 170 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
387 3 1 2 5.7 O=C(O)c1cc2cc(C(F)(F)F)ccc2n1Cc1ccc(Cl)c(Cl)c1
CHEMBL4519152 ccr2_human Human Yes 6.8 IC50 = 170 nM Bind
Negative allosteric modulation of CCR2 (unknown origin)Negative allosteric modulation of CCR2 (unknown origin)
351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C
CHEMBL2018537 ccr2_human Human No 5.8 IC50 = 1700 nM Bind
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
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
CHEMBL247214 ccr2_human Human No 5.8 IC50 = 1700 nM Bind
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
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
CHEMBL336399 ccr2_human Human Yes 5.8 IC50 = 1700 nM Bind
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
251 3 1 2 3.4 O=C(O)c1cc2ccccc2n1Cc1ccccc1
CHEMBL185518 ccr2_human Human No 4.8 IC50 = 17000 nM Bind
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
476 9 3 5 3.7 Cc1csc(C(=O)NNC(=O)CN2CCC(NCCC(c3ccccc3)c3ccccc3)C2)c1
CHEMBL362780 ccr2_human Human No 4.8 IC50 = 17000 nM Bind
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
399 6 2 3 3.2 Cc1cccc(C(=O)NCC(=O)NC2CCCN(Cc3ccc(Cl)cc3)C2)c1
CHEMBL389926 ccr2_human Human Yes 4.8 IC50 = 17000 nM Funct
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
337 4 1 3 4.6 Clc1ccccc1CN1CCC(Nc2cccc3cnccc23)C1
CHEMBL2036763 ccr2_human Human No 6.8 IC50 = 171 nM Bind
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
376 4 1 3 3.4 O=C(Nc1cccc(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1
CHEMBL496632 ccr2_human Human No 6.8 IC50 = 172 nM Bind
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
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
CHEMBL3589847 ccr2_human Human No 6.8 IC50 = 173 nM Funct
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
558 7 1 3 6.3 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1
CHEMBL409162 ccr2_human Human No 6.8 IC50 = 173 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL409162 ccr2_human Human No 6.8 IC50 = 173 nM Bind
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
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
CHEMBL210606 ccr2_human Human No 6.8 IC50 = 173.8 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL1092294 ccr2_human Human No 5.8 IC50 = 1730 nM Bind
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
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
CHEMBL4126779 ccr2_human Human No 5.8 IC50 = 1731 nM Funct
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
537 8 1 6 3.8 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(F)c3)C2=O)CC1)S(C)(=O)=O
CHEMBL2036751 ccr2_human Human No 6.8 IC50 = 174 nM Funct
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
398 4 1 3 3.9 CCN1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1
CHEMBL494399 ccr2_human Human No 6.8 IC50 = 175.0 nM Bind
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
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
CHEMBL1092293 ccr2_human Human No 5.8 IC50 = 1740 nM Bind
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
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
CHEMBL210606 ccr2_human Human No 6.8 IC50 = 175 nM Funct
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
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
CHEMBL1683062 ccr2_human Human No 6.8 IC50 = 175 nM Bind
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
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
CHEMBL210606 ccr2_human Human No 6.8 IC50 = 175 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
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
CHEMBL494399 ccr2_human Human No 6.8 IC50 = 175 nM Bind
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
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
CHEMBL3681879 ccr2_human Human No 6.8 IC50 = 177 nM Bind
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 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.).
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
CHEMBL396621 ccr2_human Human No 6.8 IC50 = 178 nM Funct
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
608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1
CHEMBL273083 ccr2_human Human Yes 7.8 IC50 = 18 nM Funct
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
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
CHEMBL2029571 ccr2_human Human No 7.8 IC50 = 18 nM Funct
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
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
CHEMBL3115109 ccr2_human Human No 7.8 IC50 = 18 nM Bind
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
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
CHEMBL273083 ccr2_human Human Yes 7.8 IC50 = 18 nM Funct
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
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
CHEMBL408908 ccr2_human Human No 7.8 IC50 = 18 nM Funct
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
451 6 5 6 1.7 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O
CHEMBL1093469 ccr2_human Human No 7.8 IC50 = 18 nM Funct
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
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
CHEMBL2204249 ccr2_human Human No 7.8 IC50 = 18 nM Bind
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
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
CHEMBL2204261 ccr2_human Human No 7.8 IC50 = 18 nM Bind
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
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
CHEMBL1834798 ccr2_human Human No 7.8 IC50 = 18 nM Bind
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
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
CHEMBL1683055 ccr2_human Human No 7.8 IC50 = 18 nM Bind
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
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
CHEMBL396101 ccr2_human Human No 7.8 IC50 = 18 nM Bind
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
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
CHEMBL2029414 ccr2_human Human No 7.8 IC50 = 18 nM Bind
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
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
CHEMBL1951766 ccr2_mouse Mouse No 7.8 IC50 = 18 nM Bind
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
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
CHEMBL1683075 ccr2_human Human No 7.7 IC50 = 18.2 nM Funct
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
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
CHEMBL1782567 ccr2_human Human No 7.7 IC50 = 18.3 nM Funct
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
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
CHEMBL1782573 ccr2_human Human No 7.7 IC50 = 18.3 nM Funct
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
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
CHEMBL1683188 ccr2_human Human No 7.7 IC50 = 18.5 nM Bind
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
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
CHEMBL1782567 ccr2_human Human No 7.7 IC50 = 18.7 nM Bind
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
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
CHEMBL1683073 ccr2_human Human No 7.7 IC50 = 18.8 nM Funct
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
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
CHEMBL3589842 ccr2_human Human No 6.8 IC50 = 180 nM Funct
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
464 6 1 3 4.8 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(F)cc(C(F)(F)F)c1
CHEMBL3115116 ccr2_human Human No 6.8 IC50 = 180 nM Bind
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
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