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Assay Detail

CHEMBL774084

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

Functional
Tested for inhibition of Na+ -dependent [3H]taurocholate uptake into rabbit ileal brush border membrane vesicles
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 1 — Organism
Curated By Intermediate

Target

Oryctolagus cuniculus (CHEMBL374)
Type ORGANISM
Organism Oryctolagus cuniculus

Publication

Synthesis and biological activity of bile acid-derived HMG-CoA reductase inhibitors. The role of 21-methyl in recognition of HMG-CoA reductase and the ileal bile acid transport system.
Wess G, Kramer W, Han XB, Bock K, Enhsen A, Glombik H, Baringhaus KH, Böger G, Urmann M, Hoffmann A.
J Med Chem (1994) 37 : 3240 -3246
PubMed 7932551 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 4.19 4.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL185878 TAUROCHENODEOXYCHOLATE 1 4.55
CHEMBL205596 CHOLIC ACID 4.0 1 4.08
CHEMBL326894 1 4.07
CHEMBL322338 1 4.04
CHEMBL321906 1 -
CHEMBL503 LOVASTATIN 4.0 1 -
CHEMBL320943 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL185878 TAUROCHENODEOXYCHOLATE IC50 = 28000.0 nM 4.55
CHEMBL205596 CHOLIC ACID IC50 = 83000.0 nM 4.08
CHEMBL326894 IC50 = 85000.0 nM 4.07
CHEMBL322338 IC50 = 92000.0 nM 4.04
CHEMBL321906 IC50 = 186000.0 nM -
CHEMBL503 LOVASTATIN IC50 > 250000.0 nM -
CHEMBL320943 IC50 = 170000.0 nM -