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Assay Detail

CHEMBL691935

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

Binding
Inhibition of solubilized, partially purified rat liver HMG-CoA reductase
ChEMBL ↗
57
Total Activities
54
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

3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 2. Structural modification of 7-(substituted aryl)-3,5-dihydroxy-6-heptenoic acids and their lactone derivatives.
Hoffman WF, Alberts AW, Cragoe EJ, Deana AA, Evans BE, Gilfillan JL, Gould NP, Huff JW, Novello FC, Prugh JD.
J Med Chem (1986) 29 : 159 -169
PubMed 3950901 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 57 5.79 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2114971 — — 2 7.30
CHEMBL2115421 — — 3 7.17
CHEMBL295300 — — 1 6.82
CHEMBL2115420 — — 1 6.77
CHEMBL2368926 — — 1 6.70
CHEMBL2368891 — — 1 6.70
CHEMBL47378 — — 1 6.68
CHEMBL47537 — — 1 6.48
CHEMBL2114972 — — 1 6.41
CHEMBL2368903 — — 1 6.37
CHEMBL2368894 — — 1 6.35
CHEMBL2368919 — — 1 6.32
CHEMBL2368910 — — 1 6.29
CHEMBL2368889 — — 1 6.24
CHEMBL2368890 — — 1 6.22
CHEMBL2368887 — — 1 6.22
CHEMBL2368905 — — 1 6.21
CHEMBL2368915 — — 1 6.17
CHEMBL2368923 — — 1 6.16
CHEMBL2368913 — — 1 6.12
CHEMBL296915 — — 1 6.12
CHEMBL2368895 — — 1 6.12
CHEMBL2368921 — — 1 6.00
CHEMBL2368918 — — 1 6.00
CHEMBL2368906 — — 1 5.96
CHEMBL2368939 — — 1 5.92
CHEMBL2368922 — — 1 5.84
CHEMBL2368886 — — 1 5.72
CHEMBL2368875 — — 1 5.70
CHEMBL2368876 — — 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2114971 — IC50 = 50.0 nM 7.30
CHEMBL2115421 — IC50 = 68.0 nM 7.17
CHEMBL2114971 — IC50 = 76.0 nM 7.12
CHEMBL295300 — IC50 = 150.0 nM 6.82
CHEMBL2115420 — IC50 = 170.0 nM 6.77
CHEMBL2368926 — IC50 = 200.0 nM 6.70
CHEMBL2368891 — IC50 = 200.0 nM 6.70
CHEMBL2115421 — IC50 = 200.0 nM 6.70
CHEMBL47378 — IC50 = 210.0 nM 6.68
CHEMBL47537 — IC50 = 330.0 nM 6.48
CHEMBL2114972 — IC50 = 390.0 nM 6.41
CHEMBL2368903 — IC50 = 430.0 nM 6.37
CHEMBL2368894 — IC50 = 450.0 nM 6.35
CHEMBL2368919 — IC50 = 480.0 nM 6.32
CHEMBL2368910 — IC50 = 510.0 nM 6.29
CHEMBL2368889 — IC50 = 580.0 nM 6.24
CHEMBL2368887 — IC50 = 600.0 nM 6.22
CHEMBL2368890 — IC50 = 600.0 nM 6.22
CHEMBL2368905 — IC50 = 620.0 nM 6.21
CHEMBL2368915 — IC50 = 670.0 nM 6.17
CHEMBL2368923 — IC50 = 700.0 nM 6.16
CHEMBL2368913 — IC50 = 760.0 nM 6.12
CHEMBL296915 — IC50 = 750.0 nM 6.12
CHEMBL2368895 — IC50 = 760.0 nM 6.12
CHEMBL2368918 — IC50 = 1000.0 nM 6.00
CHEMBL2368921 — IC50 = 1000.0 nM 6.00
CHEMBL2368906 — IC50 = 1100.0 nM 5.96
CHEMBL2368939 — IC50 = 1200.0 nM 5.92
CHEMBL2368922 — IC50 = 1450.0 nM 5.84
CHEMBL2368886 — IC50 = 1900.0 nM 5.72
CHEMBL2368875 — IC50 = 2000.0 nM 5.70
CHEMBL2368876 — IC50 = 2500.0 nM 5.60
CHEMBL2368908 — IC50 = 2600.0 nM 5.58
CHEMBL2368907 — IC50 = 3000.0 nM 5.52
CHEMBL2368911 — IC50 = 3000.0 nM 5.52
CHEMBL2368932 — IC50 = 3400.0 nM 5.47
CHEMBL2368938 — IC50 = 3700.0 nM 5.43
CHEMBL2368917 — IC50 = 4400.0 nM 5.36
CHEMBL2368920 — IC50 = 4900.0 nM 5.31
CHEMBL2115421 — IC50 = 5200.0 nM 5.28
CHEMBL2368888 — IC50 = 6300.0 nM 5.20
CHEMBL2368900 — IC50 = 7400.0 nM 5.13
CHEMBL2368896 — IC50 = 7900.0 nM 5.10
CHEMBL46049 — IC50 = 7900.0 nM 5.10
CHEMBL2368901 — IC50 = 11000.0 nM 4.96
CHEMBL2368914 — IC50 = 13000.0 nM 4.89
CHEMBL298223 — IC50 = 13000.0 nM 4.89
CHEMBL2368916 — IC50 = 17000.0 nM 4.77
CHEMBL2368928 — IC50 = 22000.0 nM 4.66
CHEMBL2368897 — IC50 = 29900.0 nM 4.52