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Assay Detail

CHEMBL5730502

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

Binding
Glycocholic acid Uptake Radiometric Assay: ISBT Hu HEK Uptake SPA 13203 IBAT HUM Ileal Bile Acid Transporter Human HEK Glycocholic acid Uptake Radiometric¿SPA Inhibitor IC50 Mean IC50 (nM) was determined.
36
Total Activities
12
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Bile acid receptor (CHEMBL2047)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

IBAT inhibitors for the treatment of liver disease
(2017)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 9.58 9.96
kon 12 - -
k_off 12 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5778792 3 9.96
CHEMBL5980362 3 9.89
CHEMBL5890939 3 9.82
CHEMBL4297588 ODEVIXIBAT 4.0 3 9.80
CHEMBL5868054 3 9.74
CHEMBL5776872 3 9.70
CHEMBL5808613 3 9.52
CHEMBL6016158 3 9.46
CHEMBL6045294 3 9.44
CHEMBL6002118 3 9.41
CHEMBL5906168 3 9.35
CHEMBL3039515 ELOBIXIBAT 3.0 3 8.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5778792 IC50 = 0.11 nM 9.96
CHEMBL5980362 IC50 = 0.13 nM 9.89
CHEMBL5890939 IC50 = 0.15 nM 9.82
CHEMBL4297588 ODEVIXIBAT IC50 = 0.16 nM 9.80
CHEMBL5868054 IC50 = 0.18 nM 9.74
CHEMBL5776872 IC50 = 0.2 nM 9.70
CHEMBL5808613 IC50 = 0.3 nM 9.52
CHEMBL6016158 IC50 = 0.35 nM 9.46
CHEMBL6045294 IC50 = 0.36 nM 9.44
CHEMBL6002118 IC50 = 0.39 nM 9.41
CHEMBL5906168 IC50 = 0.45 nM 9.35
CHEMBL3039515 ELOBIXIBAT IC50 = 1.2 nM 8.92
CHEMBL6045294 k_off = - s-1 -
CHEMBL6045294 kon = - -
CHEMBL4297588 ODEVIXIBAT k_off = - s-1 -
CHEMBL4297588 ODEVIXIBAT kon = - -
CHEMBL6016158 k_off = - s-1 -
CHEMBL6016158 kon = - -
CHEMBL5868054 k_off = - s-1 -
CHEMBL5868054 kon = - -
CHEMBL6002118 k_off = - s-1 -
CHEMBL6002118 kon = - -
CHEMBL5906168 k_off = - s-1 -
CHEMBL5906168 kon = - -
CHEMBL5778792 kon = - -
CHEMBL5778792 k_off = - s-1 -
CHEMBL3039515 ELOBIXIBAT k_off = - s-1 -
CHEMBL5776872 kon = - -
CHEMBL5776872 k_off = - s-1 -
CHEMBL3039515 ELOBIXIBAT kon = - -
CHEMBL5890939 kon = - -
CHEMBL5980362 k_off = - s-1 -
CHEMBL5890939 k_off = - s-1 -
CHEMBL5980362 kon = - -
CHEMBL5808613 k_off = - s-1 -
CHEMBL5808613 kon = - -