ChEMBL ligand: CHEMBL4442783
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!
CCR5/C-C chemokine receptor type 5 in Human [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681] 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	Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins	B	8.96	pIC50	1.1	nM	IC50	ACS Med Chem Lett (2019) 10: 300-305 [PMID:30891130]
ChEMBL	Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis	B	8.96	pIC50	1.1	nM	IC50	ACS Med Chem Lett (2021) 12: 969-975 [PMID:34141082]
GtoPdb	Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.	-	8.96	pIC50	1.1	nM	IC50	ACS Med Chem Lett (2019) 10: 300-305 [PMID:30891130]
ChEMBL	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 assay	B	9.15	pIC50	0.7	nM	IC50	ACS Med Chem Lett (2021) 12: 969-975 [PMID:34141082]
ChEMBL	Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis	F	9.15	pIC50	0.7	nM	IC50	ACS Med Chem Lett (2021) 12: 1753-1758 [PMID:34795864]
ChEMBL	Inhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assay	B	9.17	pIC50	0.67	nM	IC50	ACS Med Chem Lett (2019) 10: 300-305 [PMID:30891130]
CCR5/C-C chemokine receptor type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681]
ChEMBL	Binding affinity to CCR5 in T-cell (unknown origin)	B	7.63	pKd	23.6	nM	Kd	ACS Med Chem Lett (2019) 10: 300-305 [PMID:30891130]
ChEMBL	Antagonist activity at CCR5 (unknown origin) expressed in human HT1080 cells assessed as blockade of MIP1beta-binding to receptor	B	6.11	pIC50	780	nM	IC50	ACS Med Chem Lett (2019) 10: 300-305 [PMID:30891130]
ChEMBL	Antagonist activity at CCR5 in human HT1080 cell membrane assessed as inhibition of [125I]MIP1beta-binding incubated for 4 to 6 hrs by topcount assay	B	6.11	pIC50	780	nM	IC50	ACS Med Chem Lett (2021) 12: 969-975 [PMID:34141082]
GtoPdb	Antagonism of MIP-1β binding to HT1080 cells stably expressing CCR5	-	6.11	pIC50	780	nM	IC50	ACS Med Chem Lett (2019) 10: 300-305 [PMID:30891130]

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]