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Assay Detail

CHEMBL692514

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

Binding
Inhibition of rat microsomal HMG-CoA reductase activity by 50%
28
Total Activities
28
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

Phosphorus-containing inhibitors of HMG-CoA reductase. 1. 4-[(2-arylethyl)hydroxyphosphinyl]-3-hydroxy-butanoic acids: a new class of cell-selective inhibitors of cholesterol biosynthesis.
Karanewsky DS, Badia MC, Ciosek CP, Robl JA, Sofia MJ, Simpkins LM, DeLange B, Harrity TW, Biller SA, Gordon EM.
J Med Chem (1990) 33 : 2952 -2956
PubMed 2231594 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.24 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL319318 1 8.92
CHEMBL102145 1 8.72
CHEMBL329989 1 8.68
CHEMBL101621 1 8.66
CHEMBL318784 1 8.55
CHEMBL101826 1 8.52
CHEMBL101436 1 8.42
CHEMBL175236 1 8.40
CHEMBL99700 1 8.22
CHEMBL100820 1 8.17
CHEMBL101438 1 8.07
CHEMBL100947 1 7.89
CHEMBL98469 1 7.82
CHEMBL321279 1 7.62
CHEMBL330182 1 7.58
CHEMBL690 PRAVASTATIN SODIUM 4.0 1 7.58
CHEMBL419344 1 7.16
CHEMBL101764 1 7.06
CHEMBL321712 1 6.92
CHEMBL101721 1 6.79
CHEMBL319834 1 6.53
CHEMBL101668 1 5.52
CHEMBL99954 1 5.35
CHEMBL101493 1 5.34
CHEMBL100742 1 4.67
CHEMBL100807 1 4.15
CHEMBL99898 1 4.05
CHEMBL100504 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL319318 IC50 = 1.2 nM 8.92
CHEMBL102145 IC50 = 1.9 nM 8.72
CHEMBL329989 IC50 = 2.1 nM 8.68
CHEMBL101621 IC50 = 2.2 nM 8.66
CHEMBL318784 IC50 = 2.8 nM 8.55
CHEMBL101826 IC50 = 3.0 nM 8.52
CHEMBL101436 IC50 = 3.8 nM 8.42
CHEMBL175236 IC50 = 4.0 nM 8.40
CHEMBL99700 IC50 = 6.0 nM 8.22
CHEMBL100820 IC50 = 6.7 nM 8.17
CHEMBL101438 IC50 = 8.5 nM 8.07
CHEMBL100947 IC50 = 13.0 nM 7.89
CHEMBL98469 IC50 = 15.0 nM 7.82
CHEMBL321279 IC50 = 24.0 nM 7.62
CHEMBL330182 IC50 = 26.0 nM 7.58
CHEMBL690 PRAVASTATIN SODIUM IC50 = 26.0 nM 7.58
CHEMBL419344 IC50 = 70.0 nM 7.16
CHEMBL101764 IC50 = 87.5 nM 7.06
CHEMBL321712 IC50 = 120.0 nM 6.92
CHEMBL101721 IC50 = 162.0 nM 6.79
CHEMBL319834 IC50 = 297.0 nM 6.53
CHEMBL101668 IC50 = 3000.0 nM 5.52
CHEMBL99954 IC50 = 4500.0 nM 5.35
CHEMBL101493 IC50 = 4600.0 nM 5.34
CHEMBL100742 IC50 = 21600.0 nM 4.67
CHEMBL100807 IC50 = 70500.0 nM 4.15
CHEMBL99898 IC50 = 89300.0 nM 4.05
CHEMBL100504 IC50 = 150000.0 nM -