Assay Detail

CHEMBL5037007

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Binding

Potentiation of CFTR F508del mutant (unknown origin) expressed in CHO cells assessed as chloride transport by measuring membrane potential preincubated for 5 mins followed by forskolin addition by FLIPR assay

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	CHO
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	5.85	6.41

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1949980	—	—	1	6.41
CHEMBL5080252	—	—	1	6.04
CHEMBL44	GENISTEIN	2.0	1	5.09

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1949980	—	EC50	=	390.0	nM	6.41
CHEMBL5080252	—	EC50	=	920.0	nM	6.04
CHEMBL44	GENISTEIN	EC50	=	8200.0	nM	5.09