ChEMBL ligand: CHEMBL2010601 (Ivacaftor, Kalydeco, VX-770)
CFTR/Cystic fibrosis transmembrane conductance regulator in Human [ChEMBL: CHEMBL4051] [GtoPdb: 707] [UniProtKB: P13569] There should be some charts here, you may need to enable JavaScript!
CYP2D6/Cytochrome P450 2D6 in Human [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635] There should be some charts here, you may need to enable JavaScript!

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	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 CFTR F508del mutant (unknown origin) expressed in human CFBE41o cells incubated for 10 mins in presence of forskolin measured for 7 secs by YFP halide assay	B	6.9	pEC50	126	nM	EC50	J Med Chem (2018) 61: 1425-1435 [PMID:29148763]
ChEMBL	Inhibition of CFTR G551D mutant (unknown origin)	B	7	pEC50	100	nM	EC50	Eur J Med Chem (2022) 243: 114742-114742 [PMID:36155354]
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	Inhibition of CFTR F508 deletion mutant (unknown origin)	B	7.6	pEC50	25	nM	EC50	Eur J Med Chem (2022) 243: 114742-114742 [PMID:36155354]
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	Corrector activity at CFTR F508del mutant in forskolin-stimulated human bronchial epithelial cells derived from primary CF assessed as increase in membrane expression by measuring change in Ieq preincubated for 24 hrs followed by measured for 20 mins for every 2 mins by transepithelial clamp circuit (TECC) assay	B	7.89	pEC50	13	nM	EC50	J Med Chem (2024) 67: 5216-5232 [PMID:38527911]
ChEMBL	Corrector activity at CFTR F508del mutant in forskolin-stimulated human bronchial epithelial cells derived from primary CF assessed as increase in membrane expression by measuring change in Ieq preincubated for 24 hrs followed by measured for 20 mins for every 2 mins by transepithelial clamp circuit (TECC) assay	B	7.9	pEC50	12.59	nM	EC50	J Med Chem (2024) 67: 5216-5232 [PMID:38527911]
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]
GtoPdb	Measuring ligand-induced changes in membrane potential due to CFTR-mediated, forskolin-stimulated chloride efflux	-	8.52	pEC50	3	nM	EC50	J Med Chem (2014) 57: 9776-95 [PMID:25441013]
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 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]