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Assay Detail

CHEMBL4374468

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Binding
Agonist activity at GST-tagged FXR-LBD (unknown origin) assessed as biotinylated SRC-1 recruitment after 30 mins by Alpha Screen assay
2
Total Activities
2
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

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

Publication

Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool.
Passeri D, Carotti A, Pittol JMR, Ciaccioli G, Pellicciari R, van Mil SWC, Gioiello A.
Medchemcomm (2019) 10 : 1412 -1419
PubMed 31673308 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 5.10 5.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL240597 CHENODIOL 4.0 1 5.10
CHEMBL402063 E-GUGGULSTERONE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL240597 CHENODIOL EC50 = 8000.0 nM 5.10
CHEMBL402063 E-GUGGULSTERONE EC50 > 100000.0 nM -