lumacaftor [Ligand Id: 7481] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2103870 (Lumacaftor, VRT 826809, VRT-826809, VRT826809, VX 809, VX-809, VX809) |
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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 | Binding affinity to His-tagged human CFTR-F508del mutant by surface plasmon resonance assay | B | 4.14 | pKd | 72800 | nM | Kd | Eur J Med Chem (2020) 208: 112833-112833 [PMID:32971410] |
| ChEMBL | Binding affinity to sensorchip-immobilized human His-tagged CFTR F508 deletion mutant by surface plasmon resonance analysis | B | 4.32 | pKd | 47800 | nM | Kd | Eur J Med Chem (2021) 213: 113186-113186 [PMID:33472120] |
| ChEMBL | Corrector activity at human CFTR F508 deletion mutant expressed in FRT cells incubated for 25 mins with forskolin by YFP-based fluorescence analysis relative to control | B | 5.59 | pEC50 | 2600 | nM | EC50 | J Med Chem (2015) 58: 9697-9711 [PMID:26561003] |
| ChEMBL | Corrector activity at CFTR F508-del mutant (unknown origin) | B | 5.59 | pEC50 | 2600 | nM | EC50 | Eur J Med Chem (2018) 144: 179-200 [PMID:29272749] |
| ChEMBL | Corrector activity at CFTR F508del mutant (unknown origin) | B | 5.59 | pEC50 | 2600 | nM | EC50 | Eur J Med Chem (2019) 180: 430-448 [PMID:31326599] |
| ChEMBL | Corrector activity at CFTR F508-del mutant (unknown origin) expressed in human CFBE41o cells harboring HS-YFP preincubated for 24 hrs followed by forskolin/genistein stimulation for 30 mins by fluorescence assay | B | 5.59 | pEC50 | 2570.4 | nM | EC50 | Eur J Med Chem (2018) 144: 179-200 [PMID:29272749] |
| GtoPdb | EC50 determined by measuring F508del-CFTR (expressed in FRT cells) activity (I– influx; wih co-expression of a fluorescent YFP halide sensor) in the presence of increasing doses of test compound. | - | 5.59 | pEC50 | 2600 | nM | EC50 | J Med Chem (2015) 58: 9697-711 [PMID:26561003] |
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]
