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Assay Detail

CHEMBL832902

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Binding
Inhibitory concentration against 3-hydroxy-3-methylglutaryl-CoA reductase
35
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

3-hydroxy-3-methylglutaryl-coenzyme A reductase (CHEMBL402)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Three-dimensional quantitative structure (3-D QSAR) activity relationship studies on imidazolyl and N-pyrrolyl heptenoates as 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) inhibitors by comparative molecular similarity indices analysis (CoMSIA).
Thilagavathi R, Kumar R, Aparna V, Sobhia ME, Gopalakrishnan B, Chakraborti AK.
Bioorg Med Chem Lett (2005) 15 : 1027 -1032
PubMed 15686906 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 8.07 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1496 ROSUVASTATIN 4.0 1 8.30
CHEMBL1161663 1 8.24
CHEMBL1487 ATORVASTATIN 4.0 1 8.22
CHEMBL1161659 1 8.21
CHEMBL1161644 2 8.16
CHEMBL1161653 1 8.15
CHEMBL1161651 1 8.15
CHEMBL1161640 1 8.14
CHEMBL1161655 1 8.14
CHEMBL1161646 1 8.12
CHEMBL1161664 1 8.12
CHEMBL1161650 1 8.12
CHEMBL1161652 1 8.10
CHEMBL1161639 1 8.10
CHEMBL1161648 1 8.09
CHEMBL1161660 1 8.09
CHEMBL1161661 1 8.08
CHEMBL1161645 1 8.08
CHEMBL1161647 1 8.07
CHEMBL1161654 1 8.06
CHEMBL1161657 1 8.06
CHEMBL1161641 1 8.06
CHEMBL1161665 1 8.06
CHEMBL1161649 1 8.06
CHEMBL1161662 1 8.05
CHEMBL333760 1 8.05
CHEMBL1161656 1 8.05
CHEMBL1161658 1 8.03
CHEMBL1161642 1 8.02
CHEMBL1477 CERIVASTATIN 4.0 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1496 ROSUVASTATIN IC50 = 5.0 nM 8.30
CHEMBL1161663 IC50 = 5.7 nM 8.24
CHEMBL1487 ATORVASTATIN IC50 = 6.0 nM 8.22
CHEMBL1161659 IC50 = 6.15 nM 8.21
CHEMBL1161644 IC50 = 6.98 nM 8.16
CHEMBL1161653 IC50 = 7.0 nM 8.15
CHEMBL1161651 IC50 = 7.15 nM 8.15
CHEMBL1161640 IC50 = 7.25 nM 8.14
CHEMBL1161655 IC50 = 7.16 nM 8.14
CHEMBL1161646 IC50 = 7.6 nM 8.12
CHEMBL1161664 IC50 = 7.66 nM 8.12
CHEMBL1161650 IC50 = 7.52 nM 8.12
CHEMBL1161652 IC50 = 8.04 nM 8.10
CHEMBL1161639 IC50 = 7.89 nM 8.10
CHEMBL1161660 IC50 = 8.1 nM 8.09
CHEMBL1161648 IC50 = 8.15 nM 8.09
CHEMBL1161645 IC50 = 8.4 nM 8.08
CHEMBL1161661 IC50 = 8.3 nM 8.08
CHEMBL1161647 IC50 = 8.52 nM 8.07
CHEMBL1161654 IC50 = 8.7 nM 8.06
CHEMBL1161657 IC50 = 8.7 nM 8.06
CHEMBL1161641 IC50 = 8.7 nM 8.06
CHEMBL1161644 IC50 = 8.7 nM 8.06
CHEMBL1161665 IC50 = 8.7 nM 8.06
CHEMBL1161649 IC50 = 8.7 nM 8.06
CHEMBL333760 IC50 = 9.0 nM 8.05
CHEMBL1161656 IC50 = 9.0 nM 8.05
CHEMBL1161662 IC50 = 9.0 nM 8.05
CHEMBL1161658 IC50 = 9.3 nM 8.03
CHEMBL1161642 IC50 = 9.52 nM 8.02
CHEMBL1477 CERIVASTATIN IC50 = 10.0 nM 8.00
CHEMBL1064 SIMVASTATIN IC50 = 11.0 nM 7.96
CHEMBL54440 MEVASTATIN IC50 = 23.0 nM 7.64
CHEMBL2220442 FLUVASTATIN IC50 = 28.0 nM 7.55
CHEMBL1161643 IC50 < 7.0 nM -