ChEMBL ligand: CHEMBL134074
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	5.2	pKi	6309.57	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	5.6	pKi	2511.89	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	6.07	pKi	851.14	nM	Ki	J Med Chem (2003) 46: 4070-4086 [PMID:12954060]
ChEMBL	Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells	B	6.28	pKi	524.81	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	6.35	pKi	446.68	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	6.66	pKi	218.78	nM	Ki	J Med Chem (2003) 46: 4070-4086 [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	6.68	pKi	208.93	nM	Ki	J Med Chem (2003) 46: 4070-4086 [PMID:12954060]
ChEMBL	Binding affinity to CCR2 (unknown origin) assessed as inhibition constant	B	6.7	pKi	199.53	nM	Ki	J Med Chem (2017) 60: 4735-4779 [PMID:28165741]
GtoPdb	-	-	6.7	pKi	-	-	-	J Med Chem (2003) 46: 4070-86 [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	6.76	pKi	173.78	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	7.23	pKi	58.88	nM	Ki	J Med Chem (2003) 46: 4070-4086 [PMID:12954060]
ChEMBL	Inhibition of wild type CCR2 mutant (unknown origin)	B	7	pIC50	100	nM	IC50	J Med Chem (2017) 60: 4735-4779 [PMID:28165741]
ChEMBL	Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)	F	7.05	pIC50	89	nM	IC50	J Med Chem (2003) 46: 4070-4086 [PMID:12954060]

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]