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ChEMBL ligand: CHEMBL2010601 (Ivacaftor, Kalydeco, VX-770) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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CFTR/Cystic fibrosis transmembrane conductance regulator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4051] [GtoPdb: 707] [UniProtKB: P13569] | ||||||||
ChEMBL | Potentiation of CFTR G551D mutant (unknown origin) expressed in HEK293 cells incubated for 10 mins in presence of forskolin measured for 2 mins by YFP halide assay | B | 5.89 | pEC50 | 1300 | nM | EC50 | J Med Chem (2018) 61: 1425-1435 [PMID:29148763] |
ChEMBL | Corrector activity at human bronchial epithelium CFTR F508del and G551D mutant assessed as increase in channel gating | B | 6.63 | pEC50 | 236 | nM | EC50 | J Med Chem (2014) 57: 9774-9775 [PMID:25384240] |
ChEMBL | Potentiation of human CFTR F508del mutant in human bronchial epithelial cells by Ussing chambers recording technique | B | 6.63 | pEC50 | 236 | nM | EC50 | J Med Chem (2014) 57: 9776-9795 [PMID:25441013] |
ChEMBL | Potentiation of CFTR G551D mutant (unknown origin) expressed in FRT cells assessed as chloride transport by measuring membrane potential in presence of forskolin | B | 6.88 | pEC50 | 131 | nM | EC50 | J Med Chem (2021) 64: 7241-7260 [PMID:34028270] |
ChEMBL | Potentiation of wild-type CFTR (unknown origin) expressed in FRT cells assessed as chloride transport by measuring membrane potential in presence of forskolin | B | 7.15 | pEC50 | 70 | nM | EC50 | J Med Chem (2021) 64: 7241-7260 [PMID:34028270] |
ChEMBL | Potentiation of CFTR F508 deletion mutant (unknown origin) expressed in HBE cells assessed as change in short circuit current in presence of forskolin and amiloride | B | 7.17 | pEC50 | 68 | nM | EC50 | J Med Chem (2021) 64: 7241-7260 [PMID:34028270] |
ChEMBL | Potentiation of CFTR F508del mutant (unknown origin) expressed in FRT cells assessed as chloride transport by measuring membrane potential in presence of forskolin | B | 7.31 | pEC50 | 49 | nM | EC50 | J Med Chem (2021) 64: 7241-7260 [PMID:34028270] |
ChEMBL | Potentiation of wild type CFTR (unknown origin) expressed in HBE cells assessed as change in short circuit current in presence of forskolin and amiloride | B | 7.47 | pEC50 | 34 | nM | EC50 | J Med Chem (2021) 64: 7241-7260 [PMID:34028270] |
ChEMBL | Potentiation of human CFTR F508del/G551D mutant in human bronchial epithelial cells by Ussing chambers recording technique | B | 7.66 | pEC50 | 22 | nM | EC50 | J Med Chem (2014) 57: 9776-9795 [PMID:25441013] |
ChEMBL | Potentiator activity at CFTR F508del mutant (unknown origin) expressed in CFBE41o cells assessed as increase in forskolin induced transepithelial short circuit current by Ussing chamber assay | B | 7.93 | pEC50 | 11.7 | nM | EC50 | Eur J Med Chem (2020) 190: 112116-112116 [PMID:32078860] |
ChEMBL | Corrector activity at CFTR mutant (unknown origin) by phenotypic screening assay | B | 8.52 | pEC50 | 3 | nM | EC50 | J Med Chem (2014) 57: 9774-9775 [PMID:25384240] |
ChEMBL | Potentiation of human CFTR F508del mutant expressed in mouse NIH-3T3 cells after 30 mins by fluorescent voltage sensing optical assay | B | 8.52 | pEC50 | 3 | nM | EC50 | J Med Chem (2014) 57: 9776-9795 [PMID:25441013] |
CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635] | ||||||||
ChEMBL | Inhibition of human ERG | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2014) 57: 9776-9795 [PMID:25441013] |
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]