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	Antagonist activity at CCR2 (unknown origin)	B	8.85	pIC50	1.4	nM	IC50	Eur J Med Chem (2020) 208: 112736-112736 [PMID:32966895]
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 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]