Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3101628

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

Binding
Agonist activity at wild type TGR5 (unknown origin)
6
Total Activities
6
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

G-protein coupled bile acid receptor 1 (CHEMBL5409)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Probing the Binding Site of Bile Acids in TGR5.
Macchiarulo A, Gioiello A, Thomas C, Pols TW, Nuti R, Ferrari C, Giacchè N, De Franco F, Pruzanski M, Auwerx J, Schoonjans K, Pellicciari R.
ACS Med Chem Lett (2013) 4 : 1158 -1162
PubMed 24900622 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 5.91 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL566315 OBETICHOLIC ACID 4.0 1 7.00
CHEMBL567640 1 6.75
CHEMBL1478 LITHOCHOLIC ACID 1 6.14
CHEMBL3098607 1 5.88
CHEMBL240597 CHENODIOL 4.0 1 4.99
CHEMBL205596 CHOLIC ACID 4.0 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL566315 OBETICHOLIC ACID EC50 = 100.0 nM 7.00
CHEMBL567640 EC50 = 180.0 nM 6.75
CHEMBL1478 LITHOCHOLIC ACID EC50 = 730.0 nM 6.14
CHEMBL3098607 EC50 = 1320.0 nM 5.88
CHEMBL240597 CHENODIOL EC50 = 10290.0 nM 4.99
CHEMBL205596 CHOLIC ACID EC50 = 19830.0 nM 4.70