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Assay Detail

CHEMBL4026941

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Potentiation of CFTR G551D mutant in primary HBE cells assessed as increase in channel conductivity measured every 2 mins for 20 mins by TECC assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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 N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent.
Van der Plas SE, Kelgtermans H, De Munck T, Martina SLX, Dropsit S, Quinton E, De Blieck A, Joannesse C, Tomaskovic L, Jans M, Christophe T, van der Aar E, Borgonovi M, Nelles L, Gees M, Stouten P, Van Der Schueren J, Mammoliti O, Conrath K, Andrews M.
J Med Chem (2018) 61 : 1425 -1435
PubMed 29148763 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 6.74 6.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4075348 1 6.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4075348 EC50 = 181.0 nM 6.74