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Assay Detail

CHEMBL4009811

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

Binding
Antagonist activity at GAL4-DBD fused human FXR LBD expressed in HEK293T cells assessed as inhibition of CDCA-induced receptor activation after 24 hrs by luciferase reporter gene assay
ChEMBL ↗
29
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and biological evaluations of chalcones, flavones and chromenes as farnesoid x receptor (FXR) antagonists.
Zhang G, Liu S, Tan W, Verma R, Chen Y, Sun D, Huan Y, Jiang Q, Wang X, Wang N, Xu Y, Wong C, Shen Z, Deng R, Liu J, Zhang Y, Fang W.
Eur J Med Chem (2017) 129 : 303 -309
PubMed 28235703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.00 5.45
Inhibition 11 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4089646 — — 2 5.45
CHEMBL4067798 — — 2 5.41
CHEMBL4094011 — — 2 5.40
CHEMBL575499 — — 2 5.37
CHEMBL4105380 — — 2 5.09
CHEMBL573523 — — 2 4.82
CHEMBL4070048 — — 2 4.82
CHEMBL4083985 — — 2 4.79
CHEMBL4067328 — — 2 4.76
CHEMBL4104940 — — 2 4.74
CHEMBL4087479 — — 1 4.70
CHEMBL4067658 — — 1 4.70
CHEMBL3329258 — — 1 -
CHEMBL4099654 — — 1 -
CHEMBL4081652 — — 1 -
CHEMBL1528842 — — 1 -
CHEMBL182653 — — 1 -
CHEMBL4087168 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4089646 — IC50 = 3580.0 nM 5.45
CHEMBL4067798 — IC50 = 3870.0 nM 5.41
CHEMBL4094011 — IC50 = 3980.0 nM 5.40
CHEMBL575499 — IC50 = 4290.0 nM 5.37
CHEMBL4105380 — IC50 = 8110.0 nM 5.09
CHEMBL573523 — IC50 = 15100.0 nM 4.82
CHEMBL4070048 — IC50 = 15300.0 nM 4.82
CHEMBL4083985 — IC50 = 16200.0 nM 4.79
CHEMBL4067328 — IC50 = 17300.0 nM 4.76
CHEMBL4104940 — IC50 = 18200.0 nM 4.74
CHEMBL4067658 — IC50 = 20000.0 nM 4.70
CHEMBL4087479 — IC50 = 20000.0 nM 4.70
CHEMBL1528842 — IC50 - — -
CHEMBL4081652 — IC50 - — -
CHEMBL4099654 — IC50 - — -
CHEMBL3329258 — IC50 - — -
CHEMBL182653 — IC50 - — -
CHEMBL4087168 — IC50 - — -
CHEMBL4067328 — Inhibition - % -
CHEMBL4087168 — Inhibition - % -
CHEMBL575499 — Inhibition - % -
CHEMBL573523 — Inhibition - % -
CHEMBL4070048 — Inhibition - % -
CHEMBL4104940 — Inhibition - % -
CHEMBL4105380 — Inhibition - % -
CHEMBL4089646 — Inhibition - % -
CHEMBL4067798 — Inhibition - % -
CHEMBL4094011 — Inhibition - % -
CHEMBL4083985 — Inhibition - % -