cenicriviroc [Ligand Id: 801] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2110727 (Cenicriviroc, TAK-652, TBR-652)
  • CCR2/C-C chemokine receptor type 2 in Human [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
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  • CCR5/C-C chemokine receptor type 5 in Human [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681]
  • CCR5/C-C chemokine receptor type 5 in Mouse [ChEMBL: CHEMBL3676] [GtoPdb: 62] [UniProtKB: P51682]
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  • CCR7/C-C chemokine receptor type 7 in Human [ChEMBL: CHEMBL4594] [GtoPdb: 64] [UniProtKB: P32248]
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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 assessed as inhibition of CCL2 binding B 8.23 pIC50 5.9 nM IC50 J. Med. Chem. (2012) 55: 9363-9392 [PMID:22931505]
ChEMBL Inhibition of CCR2 (unknown origin) B 8.23 pIC50 5.9 nM IC50 J Med Chem (2020) 63: 5031-5073 [PMID:31930920]
CCR5/C-C chemokine receptor type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681]
ChEMBL Antagonist activity at CCR5 assessed as inhibition of CCL3 binding B 8.52 pIC50 3 nM IC50 J. Med. Chem. (2012) 55: 9363-9392 [PMID:22931505]
GtoPdb - - 8.6 pIC50 - - - Antimicrob Agents Chemother (2005) 49: 4584-4591 [PMID:16251299]
CCR5/C-C chemokine receptor type 5 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3676] [GtoPdb: 62] [UniProtKB: P51682]
ChEMBL Displacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hr B 9.6 pIC50 0.25 nM IC50 Eur J Med Chem (2018) 147: 115-129 [PMID:29425816]
CCR7/C-C chemokine receptor type 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4594] [GtoPdb: 64] [UniProtKB: P32248]
ChEMBL Inhibition of CCR7 (unknown origin) B 8.51 pIC50 3.1 nM IC50 J Med Chem (2020) 63: 5031-5073 [PMID:31930920]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]