Assay Detail

CHEMBL5037015

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Binding

Potentiation of CFTR G551D mutant (unknown origin) expressed in FRT cells assessed as chloride transport by measuring membrane potential in presence of forskolin

ChEMBL ↗

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Target

Cystic fibrosis transmembrane conductance regulator (CHEMBL4051) ↗

Open DB target context

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Cystic fibrosis transmembrane conductance regulator (CHEMBL4051) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Cystic fibrosis transmembrane conductance regulator

CHEMBL4051

Anchored from Assay target.

Protein identity Cystic fibrosis transmembrane conductance regulator

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Cell Type	FRT
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Cystic fibrosis transmembrane conductance regulator (CHEMBL4051) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease.

Grand DL, Gosling M, Baettig U, Bahra P, Bala K, Brocklehurst C, Budd E, Butler R, Cheung AK, Choudhury H, Collingwood SP, Cox B, Danahay H, Edwards L, Everatt B, Glaenzel U, Glotin AL, Groot-Kormelink P, Hall E, Hatto J, Howsham C, Hughes G, King A, Koehler J, Kulkarni S, Lightfoot M, Nicholls I, Page C, Pergl-Wilson G, Popa MO, Robinson R, Rowlands D, Sharp T, Spendiff M, Stanley E, Steward O, Taylor RJ, Tranter P, Wagner T, Watson H, Williams G, Wright P, Young A, Sandham DA.
J Med Chem (2021) 64 : 7241 -7260
PubMed 34028270 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	3	6.67	6.88

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2010601	IVACAFTOR	4.0	1	6.88
CHEMBL5084140	—	—	1	6.82
CHEMBL4650318	ICENTICAFTOR	2.0	1	6.30

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2010601	IVACAFTOR	EC50	=	131.0	nM	6.88
CHEMBL5084140	—	EC50	=	150.0	nM	6.82
CHEMBL4650318	ICENTICAFTOR	EC50	=	497.0	nM	6.30