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Assay Detail

CHEMBL978964

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Binding
Binding affinity to Mycobacterium tuberculosis His4-tagged recombinant CYP51 inhibitor binding site expressed in Escherichia coli HMS174(DE3) by UV-visible spectral titration method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mycobacterium tuberculosis
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sterol 14alpha-demethylase (CHEMBL5090)
Type SINGLE PROTEIN
Organism Mycobacterium tuberculosis

Publication

Small-molecule scaffolds for CYP51 inhibitors identified by high-throughput screening and defined by X-ray crystallography.
Podust LM, von Kries JP, Eddine AN, Kim Y, Yermalitskaya LV, Kuehne R, Ouellet H, Warrier T, Alteköster M, Lee JS, Rademann J, Oschkinat H, Kaufmann SH, Waterman MR.
Antimicrob Agents Chemother (2007) 51 : 3915 -3923
PubMed 17846131 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 5.20 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL507264 1 5.30
CHEMBL489925 1 5.30
CHEMBL490941 1 5.30
CHEMBL521787 1 5.30
CHEMBL491289 1 5.30
CHEMBL455684 1 5.30
CHEMBL183282 1 5.30
CHEMBL106 FLUCONAZOLE 4.0 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL507264 Kd = 5000.0 nM 5.30
CHEMBL489925 Kd = 5000.0 nM 5.30
CHEMBL490941 Kd = 5000.0 nM 5.30
CHEMBL521787 Kd = 5000.0 nM 5.30
CHEMBL491289 Kd = 5000.0 nM 5.30
CHEMBL455684 Kd = 5000.0 nM 5.30
CHEMBL183282 Kd = 5000.0 nM 5.30
CHEMBL106 FLUCONAZOLE Kd = 30000.0 nM 4.52