ChEMBL ligand: CHEMBL337246
CCR2/C-C chemokine receptor type 2 in Human [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
CCR2/C-C chemokine receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
ChEMBL	Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells	B	5.11	pKi	7762.47	nM	Ki	J Med Chem (2003) 46: 4070-4086 [PMID:12954060]
ChEMBL	Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells	B	5.59	pKi	2570.4	nM	Ki	J Med Chem (2003) 46: 4070-4086 [PMID:12954060]
ChEMBL	Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells	B	5.74	pKi	1819.7	nM	Ki	J Med Chem (2003) 46: 4070-4086 [PMID:12954060]
ChEMBL	Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells	B	6.14	pKi	724.44	nM	Ki	J Med Chem (2003) 46: 4070-4086 [PMID:12954060]
ChEMBL	Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells	B	6.18	pKi	660.69	nM	Ki	J Med Chem (2003) 46: 4070-4086 [PMID:12954060]
ChEMBL	Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells	B	6.47	pKi	338.84	nM	Ki	J Med Chem (2003) 46: 4070-4086 [PMID:12954060]
ChEMBL	Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells	B	6.5	pKi	316.23	nM	Ki	J Med Chem (2003) 46: 4070-4086 [PMID:12954060]
ChEMBL	Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells	B	6.5	pKi	316.23	nM	Ki	J Med Chem (2003) 46: 4070-4086 [PMID:12954060]
GtoPdb	-	-	6.5	pKi	-	-	-	J Med Chem (2003) 46: 4070-86 [PMID:12954060]
ChEMBL	Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)	B	6.54	pKi	288.4	nM	Ki	J Med Chem (2003) 46: 4070-4086 [PMID:12954060]
ChEMBL	Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells	B	6.21	pIC50	610	nM	IC50	Bioorg Med Chem Lett (2010) 20: 2099-2102 [PMID:20223662]
ChEMBL	Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level	F	6.52	pIC50	300	nM	IC50	Bioorg Med Chem Lett (2010) 20: 2099-2102 [PMID:20223662]
ChEMBL	Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining	F	7.15	pIC50	70	nM	IC50	Bioorg Med Chem Lett (2010) 20: 2099-2102 [PMID:20223662]
ChEMBL	Displacement of [125I]MCP1 from human CCR2b in THP1 cells	B	7.27	pIC50	54	nM	IC50	Bioorg Med Chem Lett (2008) 18: 1869-1873 [PMID:18313297]
ChEMBL	Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)	F	7.27	pIC50	54	nM	IC50	J Med Chem (2003) 46: 4070-4086 [PMID:12954060]
ChEMBL	Displacement of [125]MCP1 from CCR2 in human PBMCs	B	7.77	pIC50	17	nM	IC50	Bioorg Med Chem Lett (2007) 17: 5455-5461 [PMID:17720492]
ChEMBL	Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis	F	7.8	pIC50	16	nM	IC50	Bioorg Med Chem Lett (2008) 18: 1869-1873 [PMID:18313297]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]