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 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]
