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Assay Detail

CHEMBL924005

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

Binding
Inhibition of Holtzman-Sprague-Dawley rat liver HMG CoA reductase after 30 mins
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Synthesis and HMG CoA reductase inhibition of 4-thiophenyl quinolines as potential hypocholesterolemic agents.
Cai Z, Zhou W, Sun L.
Bioorg Med Chem (2007) 15 : 7809 -7829
PubMed 17851082 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 4.88 5.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL239664 1 5.49
CHEMBL239881 1 5.44
CHEMBL239241 1 5.36
CHEMBL239665 1 5.36
CHEMBL391280 1 5.10
CHEMBL1744447 ROSUVASTATIN CALCIUM 4.0 1 5.04
CHEMBL239448 1 5.03
CHEMBL1237061 PITAVASTATIN CALCIUM 4.0 1 4.98
CHEMBL428560 1 4.97
CHEMBL239450 1 4.97
CHEMBL394156 1 4.92
CHEMBL239242 1 4.90
CHEMBL393220 ATORVASTATIN CALCIUM 4.0 1 4.88
CHEMBL269299 1 4.85
CHEMBL239240 1 4.81
CHEMBL391080 1 4.80
CHEMBL394172 1 4.73
CHEMBL2218894 FLUVASTATIN SODIUM 4.0 1 4.67
CHEMBL239449 1 4.66
CHEMBL239239 1 4.49
CHEMBL239666 1 4.41
CHEMBL392336 1 4.30
CHEMBL269527 1 4.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL239664 IC50 = 3210.0 nM 5.49
CHEMBL239881 IC50 = 3640.0 nM 5.44
CHEMBL239241 IC50 = 4350.0 nM 5.36
CHEMBL239665 IC50 = 4410.0 nM 5.36
CHEMBL391280 IC50 = 7930.0 nM 5.10
CHEMBL1744447 ROSUVASTATIN CALCIUM IC50 = 9030.0 nM 5.04
CHEMBL239448 IC50 = 9240.0 nM 5.03
CHEMBL1237061 PITAVASTATIN CALCIUM IC50 = 10550.0 nM 4.98
CHEMBL428560 IC50 = 10600.0 nM 4.97
CHEMBL239450 IC50 = 10670.0 nM 4.97
CHEMBL394156 IC50 = 11940.0 nM 4.92
CHEMBL239242 IC50 = 12650.0 nM 4.90
CHEMBL393220 ATORVASTATIN CALCIUM IC50 = 13220.0 nM 4.88
CHEMBL269299 IC50 = 14150.0 nM 4.85
CHEMBL239240 IC50 = 15370.0 nM 4.81
CHEMBL391080 IC50 = 15750.0 nM 4.80
CHEMBL394172 IC50 = 18560.0 nM 4.73
CHEMBL2218894 FLUVASTATIN SODIUM IC50 = 21210.0 nM 4.67
CHEMBL239449 IC50 = 22050.0 nM 4.66
CHEMBL239239 IC50 = 32550.0 nM 4.49
CHEMBL239666 IC50 = 38930.0 nM 4.41
CHEMBL392336 IC50 = 49670.0 nM 4.30
CHEMBL269527 IC50 = 74550.0 nM 4.13