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Assay Detail

CHEMBL691939

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

Binding
Ability to inhibit microsomal preparation of HMG-CoA reductase in rat liver.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

3-hydroxy-3-methylglutaryl-coenzyme A reductase (CHEMBL3247)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Relationship between tissue selectivity and lipophilicity for inhibitors of HMG-CoA reductase.
Roth BD, Bocan TM, Blankley CJ, Chucholowski AW, Creger PL, Creswell MW, Ferguson E, Newton RS, O'Brien P, Picard JA.
J Med Chem (1991) 34 : 463 -466
PubMed 1992149 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.71 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2368094 1 8.70
CHEMBL2367472 1 8.18
CHEMBL2367478 1 8.14
CHEMBL3349878 1 8.12
CHEMBL2368089 1 8.11
CHEMBL2368088 1 8.03
CHEMBL2367477 1 8.00
CHEMBL11804 1 7.89
CHEMBL3349881 1 7.89
CHEMBL3349880 1 7.58
CHEMBL2218894 FLUVASTATIN SODIUM 4.0 1 7.50
CHEMBL690 PRAVASTATIN SODIUM 4.0 1 7.40
CHEMBL3349882 1 7.00
CHEMBL3349879 1 6.85
CHEMBL2368093 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2368094 IC50 = 2.0 nM 8.70
CHEMBL2367472 IC50 = 6.6 nM 8.18
CHEMBL2367478 IC50 = 7.2 nM 8.14
CHEMBL3349878 IC50 = 7.5 nM 8.12
CHEMBL2368089 IC50 = 7.7 nM 8.11
CHEMBL2368088 IC50 = 9.4 nM 8.03
CHEMBL2367477 IC50 = 10.0 nM 8.00
CHEMBL11804 IC50 = 13.0 nM 7.89
CHEMBL3349881 IC50 = 13.0 nM 7.89
CHEMBL3349880 IC50 = 26.0 nM 7.58
CHEMBL2218894 FLUVASTATIN SODIUM IC50 = 32.0 nM 7.50
CHEMBL690 PRAVASTATIN SODIUM IC50 = 40.0 nM 7.40
CHEMBL3349882 IC50 = 100.0 nM 7.00
CHEMBL3349879 IC50 = 141.0 nM 6.85
CHEMBL2368093 IC50 = 480.0 nM 6.32