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Assay Detail

CHEMBL4125284

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

Binding
Binding affinity to Aspergillus fumigatus CYP51 by spectral titration method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Aspergillus fumigatus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Lanosterol 14-alpha demethylase (CHEMBL3390824)
Type SINGLE PROTEIN
Organism Aspergillus

Publication

Sterol 14α-Demethylase Structure-Based Design of VNI (( R)- N-(1-(2,4-Dichlorophenyl)-2-(1 H-imidazol-1-yl)ethyl)-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide)) Derivatives To Target Fungal Infections: Synthesis, Biological Evaluation, and Crystallographic Analysis.
Friggeri L, Hargrove TY, Wawrzak Z, Blobaum AL, Rachakonda G, Lindsley CW, Villalta F, Nes WD, Botta M, Guengerich FP, Lepesheva GI.
J Med Chem (2018) 61 : 5679 -5691
PubMed 29894182 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 7.14 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4128885 1 7.70
CHEMBL4127493 1 7.26
CHEMBL638 VORICONAZOLE 4.0 1 7.25
CHEMBL4129161 1 7.24
CHEMBL4128615 1 7.21
CHEMBL4126063 1 6.88
CHEMBL1397 POSACONAZOLE 4.0 1 6.88
CHEMBL1236677 1 6.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4128885 Kd = 20.0 nM 7.70
CHEMBL4127493 Kd = 55.0 nM 7.26
CHEMBL638 VORICONAZOLE Kd = 56.0 nM 7.25
CHEMBL4129161 Kd = 57.0 nM 7.24
CHEMBL4128615 Kd = 61.0 nM 7.21
CHEMBL4126063 Kd = 132.0 nM 6.88
CHEMBL1397 POSACONAZOLE Kd = 131.0 nM 6.88
CHEMBL1236677 Kd = 203.0 nM 6.69