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Assay Detail

CHEMBL3880922

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

Binding
Correction activity at CFTR F508 deletion mutant (unknown origin) expressed in mouse NIH/3T3 cells assessed as increase in cAMP/genistein-dependent current amplitude incubated for 10 mins at 37 degC by patch clamp method
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NIH/3T3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cystic fibrosis transmembrane conductance regulator (CHEMBL4051)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Indole derivatives as CFTR modulators
(2009)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 6.44 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3897147 1 7.42
CHEMBL3948182 1 7.41
CHEMBL3923765 1 7.18
CHEMBL3908746 1 7.09
CHEMBL3898560 1 6.74
CHEMBL3936630 1 6.64
CHEMBL3544914 TEZACAFTOR 4.0 1 6.57
CHEMBL3986594 1 6.55
CHEMBL3933231 1 6.54
CHEMBL3956217 1 6.01
CHEMBL3979390 1 5.74
CHEMBL3894447 1 5.51
CHEMBL3897640 1 5.37
CHEMBL3910383 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3897147 EC50 = 38.1 nM 7.42
CHEMBL3948182 EC50 = 39.05 nM 7.41
CHEMBL3923765 EC50 = 65.95 nM 7.18
CHEMBL3908746 EC50 = 81.75 nM 7.09
CHEMBL3898560 EC50 = 181.0 nM 6.74
CHEMBL3936630 EC50 = 228.5 nM 6.64
CHEMBL3544914 TEZACAFTOR EC50 = 272.0 nM 6.57
CHEMBL3986594 EC50 = 283.5 nM 6.55
CHEMBL3933231 EC50 = 285.0 nM 6.54
CHEMBL3956217 EC50 = 981.0 nM 6.01
CHEMBL3979390 EC50 = 1810.0 nM 5.74
CHEMBL3894447 EC50 = 3095.0 nM 5.51
CHEMBL3897640 EC50 = 4315.0 nM 5.37
CHEMBL3910383 EC50 = 4525.0 nM 5.34