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Assay Detail

CHEMBL691796

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Binding
In vitro inhibition of rat liver HMG-CoA reductase
30
Total Activities
30
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

Synthesis and biological activity of new HMG-CoA reductase inhibitors. 1. Lactones of pyridine- and pyrimidine-substituted 3,5-dihydroxy-6-heptenoic (-heptanoic) acids.
Beck G, Kesseler K, Baader E, Bartmann W, Bergmann A, Granzer E, Jendralla H, von Kerekjarto B, Krause R, Paulus E.
J Med Chem (1990) 33 : 52 -60
PubMed 2296036 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 7.85 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2368185 1 9.00
CHEMBL2368197 1 9.00
CHEMBL2368189 1 9.00
CHEMBL2368202 1 8.70
CHEMBL350895 1 8.52
CHEMBL2368199 GLENVASTATIN 2.0 1 8.52
CHEMBL2368187 1 8.52
CHEMBL2368190 1 8.52
CHEMBL2368188 1 8.52
CHEMBL2368191 1 8.40
CHEMBL2368200 1 8.40
CHEMBL2368205 1 8.30
CHEMBL503 LOVASTATIN 4.0 1 8.10
CHEMBL2368204 1 8.10
CHEMBL2368198 1 8.05
CHEMBL2368194 1 7.89
CHEMBL2368192 1 7.75
CHEMBL156695 1 7.72
CHEMBL2368201 1 7.52
CHEMBL2368193 1 7.44
CHEMBL2111268 1 7.42
CHEMBL2368195 1 7.40
CHEMBL2368196 1 7.03
CHEMBL2111238 1 7.00
CHEMBL2111271 1 6.58
CHEMBL2368203 1 6.30
CHEMBL2111270 1 6.22
CHEMBL158323 1 6.00
CHEMBL2111237 1 -
CHEMBL2111239 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2368185 IC50 = 1.0 nM 9.00
CHEMBL2368197 IC50 = 1.0 nM 9.00
CHEMBL2368189 IC50 = 1.0 nM 9.00
CHEMBL2368202 IC50 = 2.0 nM 8.70
CHEMBL350895 IC50 = 3.0 nM 8.52
CHEMBL2368199 GLENVASTATIN IC50 = 3.0 nM 8.52
CHEMBL2368187 IC50 = 3.0 nM 8.52
CHEMBL2368190 IC50 = 3.0 nM 8.52
CHEMBL2368188 IC50 = 3.0 nM 8.52
CHEMBL2368191 IC50 = 4.0 nM 8.40
CHEMBL2368200 IC50 = 4.0 nM 8.40
CHEMBL2368205 IC50 = 5.0 nM 8.30
CHEMBL503 LOVASTATIN IC50 = 8.0 nM 8.10
CHEMBL2368204 IC50 = 8.0 nM 8.10
CHEMBL2368198 IC50 = 9.0 nM 8.05
CHEMBL2368194 IC50 = 13.0 nM 7.89
CHEMBL2368192 IC50 = 18.0 nM 7.75
CHEMBL156695 IC50 = 19.0 nM 7.72
CHEMBL2368201 IC50 = 30.0 nM 7.52
CHEMBL2368193 IC50 = 36.0 nM 7.44
CHEMBL2111268 IC50 = 38.0 nM 7.42
CHEMBL2368195 IC50 = 40.0 nM 7.40
CHEMBL2368196 IC50 = 94.0 nM 7.03
CHEMBL2111238 IC50 = 100.0 nM 7.00
CHEMBL2111271 IC50 = 260.0 nM 6.58
CHEMBL2368203 IC50 = 500.0 nM 6.30
CHEMBL2111270 IC50 = 600.0 nM 6.22
CHEMBL158323 IC50 = 1000.0 nM 6.00
CHEMBL2111237 IC50 > 1000.0 nM -
CHEMBL2111239 IC50 > 1000.0 nM -