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Assay Detail

CHEMBL615201

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

Binding
In vitro inhibition of human 2,3-oxidosqualene cyclase.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Lanosterol synthase (CHEMBL3593)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity studies of novel orally active non-terpenoic 2,3-oxidosqualene cyclase inhibitors.
Dehmlow H, Aebi JD, Jolidon S, Ji YH, von der Mark EM, Himber J, Morand OH.
J Med Chem (2003) 46 : 3354 -3370
PubMed 12852766 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 8.08 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112210 1 8.54
CHEMBL543877 1 8.46
CHEMBL115085 1 8.39
CHEMBL116705 1 8.39
CHEMBL115020 1 8.34
CHEMBL114259 1 8.27
CHEMBL116000 1 8.25
CHEMBL115923 1 8.21
CHEMBL115375 1 8.20
CHEMBL324162 1 8.19
CHEMBL554209 1 8.17
CHEMBL324034 1 8.11
CHEMBL112693 1 8.10
CHEMBL114266 1 8.06
CHEMBL115884 1 7.94
CHEMBL419402 1 7.91
CHEMBL114910 1 7.80
CHEMBL115497 1 7.71
CHEMBL553281 1 7.65
CHEMBL114747 1 7.50
CHEMBL544345 1 7.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112210 IC50 = 2.9 nM 8.54
CHEMBL543877 IC50 = 3.5 nM 8.46
CHEMBL115085 IC50 = 4.1 nM 8.39
CHEMBL116705 IC50 = 4.1 nM 8.39
CHEMBL115020 IC50 = 4.6 nM 8.34
CHEMBL114259 IC50 = 5.4 nM 8.27
CHEMBL116000 IC50 = 5.6 nM 8.25
CHEMBL115923 IC50 = 6.2 nM 8.21
CHEMBL115375 IC50 = 6.3 nM 8.20
CHEMBL324162 IC50 = 6.5 nM 8.19
CHEMBL554209 IC50 = 6.7 nM 8.17
CHEMBL324034 IC50 = 7.8 nM 8.11
CHEMBL112693 IC50 = 7.9 nM 8.10
CHEMBL114266 IC50 = 8.7 nM 8.06
CHEMBL115884 IC50 = 11.4 nM 7.94
CHEMBL419402 IC50 = 12.3 nM 7.91
CHEMBL114910 IC50 = 15.7 nM 7.80
CHEMBL115497 IC50 = 19.6 nM 7.71
CHEMBL553281 IC50 = 22.5 nM 7.65
CHEMBL114747 IC50 = 31.8 nM 7.50
CHEMBL544345 IC50 = 35.3 nM 7.45