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Potentiator Assay from US Patent US20240058315: "Pyridine and Pyrazine derivative for the Treatment of CF, COPD, and Bronchiectasis"
Assay data:13 Active, 13 Activity ≤ 1 µM, 13 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Induction of stabilisation of human CFTR F508 deletion mutant bound with FAP expressed in human HEK293 cells assessed as trafficking of CFTR to plasma membrane in presence of VX-809 measured by western blotting assay
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Induction of stabilisation of human CFTR F508 deletion mutant fused with FAP expressed in human HEK293 cells assessed as trafficking of CFTR to plasma membrane measured by western blotting assay
Assay data:1 Active, 2 Tested
Induction of stabilisation of human CFTR F508 deletion mutant expressed in human CFBE41o- cells assessed as VX-809-dependent maturation by measuring banc C at 10 uM measured after 24 hrs by western blotting assay relative to VX-809
Induction of stabilisation of human CFTR F508 deletion mutant expressed in human HEK293 cells assessed as VX-809-dependent maturation by measuring banc C at 10 uM measured after 24 hrs by Western blotting assay
Assay data:2 Active, 2 Tested
Induction of stabilisation of human CFTR F508 deletion mutant expressed in human HEK293 cells assessed as transport from endoplasmic reticulum to golgi complex by measuring band C at 10 uM measured after 24 hrs by Western blotting assay
Inhibition of human CFTR ubiquitination in human HEK293 cells assessed as inhibition of binding of 25I-ubiquitin in presence of ATP at 300 uM measured by radiography method relative to PYR-41
Inhibition of human CFTR F508 deletion mutant ubiquitination expressed in human HEK293 cells assessed as inhibition of binding of 25I-ubiquitin in presence of ATP at 300 uM measured by radiography method relative to PYR-41
Invivo activation of human CTFR-G542X mutant xenografted in mouse model assessed as induction of CTFR channel expression at 34 mg/kg administered daily
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Potentiation of CD4-HRP tagged CFTR F508del mutant NBD1 (unknown origin) expressed in MDCK cells assessed as increase in chloride current by measuring fold increase in luminescence signal incubated for 24 hrs relative to control
Assay data:3 Tested
Potentiation of CFTR F508del mutant (unknown origin) expressed in rat FRT cells assessed as increase in chloride current by measuring maximal effect at 30 uM in presence of forskolin relative to control
Potentiation of CFTR F508del mutant (unknown origin) expressed in rat FRT cells assessed as increase in iodide influx by measuring Vmax in presence of forskolin incubated for 24 hrs
Assay data:5 Tested
Potentiation of CFTR F508del mutant (unknown origin) expressed in rat FRT cells assessed as increase in iodide influx in presence of forskolin incubated for 24 hrs
Assay data:1 Active, 5 Tested
Corrector activity at CFTR F508del mutant (unknown origin) expressed in rat FRT cells assessed as increase in iodide influx by measuring Vmax in presence of forskolin incubated for 24 hrs
Corrector activity at CFTR F508del mutant (unknown origin) expressed in rat FRT cells assessed as increase in iodide influx in presence of forskolin incubated for 24 hrs
Assay data:5 Active, 5 Tested
Potentiation of CFTR F508del mutant activity (unknown origin)
Assay data:3 Active, 1 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Potency index, ratio of genistein EC50 to test compound EC50 for potentiation of CFTR F508del mutant in rat FRT cells assessed as increase in iodide influx in presence of forskolin
Potentiation of CFTR F508del mutant in rat FRT cells assessed as increase in iodide influx in presence of forskolin
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Bioactivity Assay from US Patent US11866450: "Modulators of Cystic Fibrosis Transmembrane Conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulators"
Assay data:192 Active, 183 Activity ≤ 1 µM, 210 Tested
Selectivity interaction (CSE-HRP surface expression (cell surface expression-horseradish peroxidase assay)) EUB0000544a CFTR
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