cenicriviroc [Ligand Id: 801] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2110727 (Cenicriviroc, TAK-652, TBR-652) |
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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 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]
