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Assay Detail

CHEMBL943880

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Functional
Antagonist activity at human FXR expressed in monkey CV1 cells after 24 hrs by ecdysone receptor response element-driven luciferase reporter assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Scalarane sesterterpenes from a marine sponge of the genus Spongia and their FXR antagonistic activity.
Nam SJ, Ko H, Ju MK, Hwang H, Chin J, Ham J, Lee B, Lee J, Won DH, Choi H, Ko J, Shin K, Oh T, Kim S, Rho JR, Kang H.
J Nat Prod (2007) 70 : 1691 -1695
PubMed 17988093 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 4.75 5.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL251695 1 5.62
CHEMBL402063 E-GUGGULSTERONE 1 5.39
CHEMBL251696 1 4.62
CHEMBL250263 1 4.50
CHEMBL269105 1 4.22
CHEMBL399743 1 4.12
CHEMBL438521 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL251695 IC50 = 2400.0 nM 5.62
CHEMBL402063 E-GUGGULSTERONE IC50 = 4100.0 nM 5.39
CHEMBL251696 IC50 = 24000.0 nM 4.62
CHEMBL250263 IC50 = 31600.0 nM 4.50
CHEMBL269105 IC50 = 60400.0 nM 4.22
CHEMBL399743 IC50 = 75000.0 nM 4.12
CHEMBL438521 IC50 > 100000.0 nM -