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Assay Detail

CHEMBL4259980

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Binding
Transactivation of full-length FXR (unknown origin) expressed in HEK293 cells after 18 hrs by dual-glo luciferase reporter gene assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of new FXR agonists based on 6-ECDCA binding properties by virtual screening and molecular docking.
Giancristofaro A, Barbosa AJM, Ammazzalorso A, Amoia P, De Filippis B, Fantacuzzi M, Giampietro L, Maccallini C, Amoroso R.
Medchemcomm (2018) 9 : 1630 -1638
PubMed 30393515 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.14 5.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4281889 1 5.36
CHEMBL4279753 1 5.22
CHEMBL240597 CHENODIOL 4.0 1 5.15
CHEMBL4289098 1 4.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4281889 EC50 = 4330.0 nM 5.36
CHEMBL4279753 EC50 = 5990.0 nM 5.22
CHEMBL240597 CHENODIOL EC50 = 7010.0 nM 5.15
CHEMBL4289098 EC50 = 14400.0 nM 4.84