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 to CCR2 (unknown origin) assessed as inhibition constant	B	6.5	pKi	316.23	nM	Ki	J Med Chem (2017) 60: 4735-4779 [PMID:28165741]
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	Inhibition of wild type CCR2 mutant (unknown origin)	B	4	pIC50	100000	nM	IC50	J Med Chem (2017) 60: 4735-4779 [PMID:28165741]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]