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Assay Detail

CHEMBL691936

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
39
Total Activities
35
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. 3. 7-(3,5-Disubstituted [1,1'-biphenyl]-2-yl)-3,5-dihydroxy-6-heptenoic acids and their lactone derivatives.
Stokker GE, Alberts AW, Anderson PS, Cragoe EJ, Deana AA, Gilfillan JL, Hirshfield J, Holtz WJ, Hoffman WF, Huff JW.
J Med Chem (1986) 29 : 170 -181
PubMed 3950902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 7.11 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2368970 3 8.30
CHEMBL2368973 1 8.22
CHEMBL440891 3 8.15
CHEMBL2368988 1 8.10
CHEMBL2368968 1 8.00
CHEMBL2368985 1 7.89
CHEMBL2368984 1 7.89
CHEMBL2368971 1 7.89
CHEMBL2368974 1 7.89
CHEMBL2368982 1 7.82
CHEMBL2368964 1 7.80
CHEMBL50566 1 7.66
CHEMBL2368986 1 7.60
CHEMBL2368962 1 7.54
CHEMBL2368979 1 7.52
CHEMBL2368980 1 7.44
CHEMBL2368990 1 7.44
CHEMBL2368989 1 7.43
CHEMBL2368966 1 7.36
CHEMBL2368976 1 7.31
CHEMBL2368965 1 7.30
CHEMBL2368978 1 7.16
CHEMBL2368975 1 7.10
CHEMBL54240 1 7.00
CHEMBL2368983 1 6.97
CHEMBL2368963 1 6.72
CHEMBL2368969 1 6.43
CHEMBL2368967 1 6.37
CHEMBL2368972 1 6.33
CHEMBL300495 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2368970 IC50 = 5.0 nM 8.30
CHEMBL2368973 IC50 = 6.0 nM 8.22
CHEMBL440891 IC50 = 7.0 nM 8.15
CHEMBL440891 IC50 = 7.6 nM 8.12
CHEMBL2368988 IC50 = 8.0 nM 8.10
CHEMBL2368968 IC50 = 10.0 nM 8.00
CHEMBL2368974 IC50 = 13.0 nM 7.89
CHEMBL2368984 IC50 = 13.0 nM 7.89
CHEMBL2368985 IC50 = 13.0 nM 7.89
CHEMBL2368971 IC50 = 13.0 nM 7.89
CHEMBL2368982 IC50 = 15.0 nM 7.82
CHEMBL2368964 IC50 = 16.0 nM 7.80
CHEMBL50566 IC50 = 22.0 nM 7.66
CHEMBL2368970 IC50 = 24.0 nM 7.62
CHEMBL2368986 IC50 = 25.0 nM 7.60
CHEMBL2368962 IC50 = 29.0 nM 7.54
CHEMBL2368979 IC50 = 30.0 nM 7.52
CHEMBL2368990 IC50 = 36.0 nM 7.44
CHEMBL2368980 IC50 = 36.0 nM 7.44
CHEMBL2368989 IC50 = 37.0 nM 7.43
CHEMBL2368966 IC50 = 44.0 nM 7.36
CHEMBL2368976 IC50 = 49.0 nM 7.31
CHEMBL2368965 IC50 = 50.0 nM 7.30
CHEMBL2368978 IC50 = 70.0 nM 7.16
CHEMBL2368975 IC50 = 80.0 nM 7.10
CHEMBL54240 IC50 = 100.0 nM 7.00
CHEMBL2368983 IC50 = 106.0 nM 6.97
CHEMBL2368963 IC50 = 190.0 nM 6.72
CHEMBL2368970 IC50 = 260.0 nM 6.58
CHEMBL2368969 IC50 = 370.0 nM 6.43
CHEMBL2368967 IC50 = 430.0 nM 6.37
CHEMBL2368972 IC50 = 470.0 nM 6.33
CHEMBL300495 IC50 = 530.0 nM 6.28
CHEMBL2368981 IC50 = 630.0 nM 6.20
CHEMBL2368977 IC50 = 860.0 nM 6.07
CHEMBL2368911 IC50 = 3000.0 nM 5.52
CHEMBL440891 IC50 = 7300.0 nM 5.14
CHEMBL2368928 IC50 = 21900.0 nM 4.66
CHEMBL50348 IC50 = 44000.0 nM 4.36