tezacaftor [Ligand Id: 10199] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3544914 (Tezacaftor, VX-661)
  • CFTR/Cystic fibrosis transmembrane conductance regulator in Human [ChEMBL: CHEMBL4051] [GtoPdb: 707] [UniProtKB: P13569]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CFTR/Cystic fibrosis transmembrane conductance regulator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4051] [GtoPdb: 707] [UniProtKB: P13569]
ChEMBL Correction activity at CFTR F508 deletion mutant (unknown origin) expressed in mouse NIH/3T3 cells assessed as increase in cAMP/genistein-dependent current amplitude incubated for 10 mins at 37 degC by patch clamp method B 6.57 pEC50 272 nM EC50 US-20090131492-A1. Indole derivatives as CFTR modulators (2009)
GtoPdb Measuring the increase in cAMP/genistein-dependent current amplitude via the ΔF508-CFTR mutant expressed in NIH/3T3 cells by patch-clamp recording, in response to tezacaftor exposure. - 6.57 pEC50 272 nM EC50 US20090131492A1. Indole derivatives as CFTR modulators. (2009)

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]