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Assay Detail

CHEMBL1041790

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

Functional
Agonist activity at human FXR expressed in COS1 cells by luciferase reporter gene assay
ChEMBL ↗
56
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-activity relationship study of betulinic acid, a novel and selective TGR5 agonist, and its synthetic derivatives: potential impact in diabetes.
Genet C, Strehle A, Schmidt C, Boudjelal G, Lobstein A, Schoonjans K, Souchet M, Auwerx J, Saladin R, Wagner A.
J Med Chem (2010) 53 : 178 -190
PubMed 19911773 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 56 5.17 5.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1478 LITHOCHOLIC ACID — 1 5.17
CHEMBL585494 — — 1 -
CHEMBL571293 — — 1 -
CHEMBL571649 — — 1 -
CHEMBL576714 — — 1 -
CHEMBL576521 — — 1 -
CHEMBL571736 — — 1 -
CHEMBL576520 — — 1 -
CHEMBL566478 — — 1 -
CHEMBL295602 METHYL BETULINATE — 1 -
CHEMBL429204 — — 1 -
CHEMBL576716 — — 1 -
CHEMBL576715 — — 1 -
CHEMBL567749 — — 1 -
CHEMBL571516 — — 1 -
CHEMBL571415 — — 1 -
CHEMBL571497 — — 1 -
CHEMBL583224 — — 1 -
CHEMBL583640 — — 1 -
CHEMBL566930 — — 1 -
CHEMBL576519 — — 1 -
CHEMBL571642 — — 1 -
CHEMBL576518 — — 1 -
CHEMBL80460 PLATANIC ACID — 1 -
CHEMBL583203 — — 1 -
CHEMBL567578 — — 1 -
CHEMBL108505 DIHYDROBETULINIC ACID — 1 -
CHEMBL571592 — — 1 -
CHEMBL571735 — — 1 -
CHEMBL571348 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1478 LITHOCHOLIC ACID EC50 = 6700.0 nM 5.17
CHEMBL455357 — EC50 = - nM -
CHEMBL576521 — EC50 = - nM -
CHEMBL576714 — EC50 = - nM -
CHEMBL571649 — EC50 = - nM -
CHEMBL571293 — EC50 = - nM -
CHEMBL269277 BETULINIC ACID EC50 = - nM -
CHEMBL168 OLEANOLIC_ACID EC50 = - nM -
CHEMBL169 URSOLIC ACID EC50 = - nM -
CHEMBL486393 LUPENONE EC50 = - nM -
CHEMBL485998 FRIEDELINE EC50 = - nM -
CHEMBL23236 BETULIN EC50 = - nM -
CHEMBL399873 UVAOL EC50 = - nM -
CHEMBL571736 — EC50 = - nM -
CHEMBL464466 ARJUNOLIC ACID EC50 = - nM -
CHEMBL404313 ASIATIC ACID EC50 = - nM -
CHEMBL579272 — EC50 = - nM -
CHEMBL566929 BETA-ELEMONIC ACID EC50 = - nM -
CHEMBL446317 — EC50 = - nM -
CHEMBL568584 — EC50 = - nM -
CHEMBL571294 — EC50 = - nM -
CHEMBL431525 BETUNOLIC ACID EC50 = - nM -
CHEMBL568374 — EC50 = - nM -
CHEMBL296302 — EC50 = - nM -
CHEMBL569634 — EC50 = - nM -
CHEMBL571478 — EC50 = - nM -
CHEMBL583640 — EC50 = - nM -
CHEMBL571348 — EC50 = - nM -
CHEMBL571735 — EC50 = - nM -
CHEMBL571592 — EC50 = - nM -
CHEMBL108505 DIHYDROBETULINIC ACID EC50 = - nM -
CHEMBL567578 — EC50 = - nM -
CHEMBL583203 — EC50 = - nM -
CHEMBL80460 PLATANIC ACID EC50 = - nM -
CHEMBL576518 — EC50 = - nM -
CHEMBL571642 — EC50 = - nM -
CHEMBL576519 — EC50 = - nM -
CHEMBL566930 — EC50 = - nM -
CHEMBL576520 — EC50 = - nM -
CHEMBL583224 — EC50 = - nM -
CHEMBL571497 — EC50 = - nM -
CHEMBL585494 — EC50 = - nM -
CHEMBL571415 — EC50 = - nM -
CHEMBL571516 — EC50 = - nM -
CHEMBL567749 — EC50 = - nM -
CHEMBL576715 — EC50 = - nM -
CHEMBL576716 — EC50 = - nM -
CHEMBL429204 — EC50 = - nM -
CHEMBL295602 METHYL BETULINATE EC50 = - nM -
CHEMBL566478 — EC50 = - nM -