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Assay Detail

CHEMBL3385491

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

Binding
Inhibition of human ERG channel by patch-clamp assay
9
Total Activities
8
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

Publication

Decreasing the rate of metabolic ketone reduction in the discovery of a clinical acetyl-CoA carboxylase inhibitor for the treatment of diabetes.
Griffith DA, Kung DW, Esler WP, Amor PA, Bagley SW, Beysen C, Carvajal-Gonzalez S, Doran SD, Limberakis C, Mathiowetz AM, McPherson K, Price DA, Ravussin E, Sonnenberg GE, Southers JA, Sweet LJ, Turner SM, Vajdos FF.
J Med Chem (2014) 57 : 10512 -10526
PubMed 25423286 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.58 4.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3359261 1 4.68
CHEMBL3359262 1 4.64
CHEMBL3359264 1 4.54
CHEMBL2419601 1 4.47
CHEMBL3359265 PF-05175157 2.0 1 -
CHEMBL3359263 1 -
CHEMBL3359260 1 -
CHEMBL3359259 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3359261 IC50 = 21000.0 nM 4.68
CHEMBL3359262 IC50 = 23000.0 nM 4.64
CHEMBL3359264 IC50 = 29000.0 nM 4.54
CHEMBL2419601 IC50 = 34000.0 nM 4.47
CHEMBL3359265 PF-05175157 IC50 = 141000.0 nM -
CHEMBL3359263 IC50 - -
CHEMBL3359260 IC50 - -
CHEMBL3359259 IC50 - -
CHEMBL3359259 IC50 - -