Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4323745

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

Binding
Inhibition of recombinant full length human CYP51 expressed in Escherichia coli incubated for 1 hr using [3H] lanosterol as substrate by HPLC analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Lanosterol 14-alpha demethylase (CHEMBL3849)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Validation of Human Sterol 14α-Demethylase (CYP51) Druggability: Structure-Guided Design, Synthesis, and Evaluation of Stoichiometric, Functionally Irreversible Inhibitors.
Friggeri L, Hargrove TY, Wawrzak Z, Guengerich FP, Lepesheva GI.
J Med Chem (2019) 62 : 10391 -10401
PubMed 31663733 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.03 5.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4439225 1 5.44
CHEMBL4461447 1 5.36
CHEMBL4277680 1 5.23
CHEMBL4444489 1 4.82
CHEMBL4466288 1 4.72
CHEMBL3629567 1 4.61
CHEMBL4458275 1 -
CHEMBL4593688 1 -
CHEMBL4452294 1 -
CHEMBL4472919 1 -
CHEMBL4435160 1 -
CHEMBL4522116 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4439225 IC50 = 3600.0 nM 5.44
CHEMBL4461447 IC50 = 4400.0 nM 5.36
CHEMBL4277680 IC50 = 5900.0 nM 5.23
CHEMBL4444489 IC50 = 15000.0 nM 4.82
CHEMBL4466288 IC50 = 19000.0 nM 4.72
CHEMBL3629567 IC50 = 24400.0 nM 4.61
CHEMBL4458275 IC50 > 25000.0 nM -
CHEMBL4593688 IC50 > 25000.0 nM -
CHEMBL4452294 IC50 > 25000.0 nM -
CHEMBL4472919 IC50 > 25000.0 nM -
CHEMBL4435160 IC50 < 1000.0 nM -
CHEMBL4522116 IC50 < 1000.0 nM -