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Assay Detail

CHEMBL906990

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

Functional
Antagonist activity against FXR assessed as transactivation of luciferase reporter gene in CV1 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CV-1
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Farnesoid X-activated receptor antagonists from a marine sponge Spongia sp.
Nam SJ, Ko H, Shin M, Ham J, Chin J, Kim Y, Kim H, Shin K, Choi H, Kang H.
Bioorg Med Chem Lett (2006) 16 : 5398 -5402
PubMed 16905319 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.60 5.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL373765 1 5.09
CHEMBL410683 GUGGULSTERONE 1 5.00
CHEMBL218308 1 4.61
CHEMBL216782 1 4.60
CHEMBL219377 1 4.19
CHEMBL413656 1 4.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL373765 IC50 = 8100.0 nM 5.09
CHEMBL410683 GUGGULSTERONE IC50 = 10000.0 nM 5.00
CHEMBL218308 IC50 = 24800.0 nM 4.61
CHEMBL216782 IC50 = 25300.0 nM 4.60
CHEMBL219377 IC50 = 64500.0 nM 4.19
CHEMBL413656 IC50 = 81100.0 nM 4.09