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Assay Detail

CHEMBL5112502

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

Binding
Inhibition of Cryptococcus neoformans farnesyltransferase assessed as inhibition of farnesylation of dansyl-GCVVM peptide using fluorescent peptide dansyl-GCVVM and 1uM farnesyl diphosphate as substrate by fluorescence assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cryptococcus neoformans
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structure-Guided Discovery of Potent Antifungals that Prevent Ras Signaling by Inhibiting Protein Farnesyltransferase.
Wang Y, Xu F, Nichols CB, Shi Y, Hellinga HW, Alspaugh JA, Distefano MD, Beese LS.
J Med Chem (2022) 65 : 13753 -13770
PubMed 36218371 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.30 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5189765 1 7.40
CHEMBL125162 1 7.00
CHEMBL5196678 1 6.92
CHEMBL5204302 1 6.82
CHEMBL5174289 1 6.80
CHEMBL5195805 1 6.75
CHEMBL5182445 1 6.72
CHEMBL5180405 1 6.68
CHEMBL5171383 1 6.58
CHEMBL5202247 1 6.55
CHEMBL5176914 1 6.50
CHEMBL5209874 1 6.47
CHEMBL5179982 1 6.26
CHEMBL5171138 1 6.15
CHEMBL5206115 1 6.13
CHEMBL5195372 1 6.04
CHEMBL5182735 1 5.96
CHEMBL5197720 1 5.96
CHEMBL5199791 1 5.80
CHEMBL5198833 1 5.72
CHEMBL125648 1 5.66
CHEMBL5199356 1 5.58
CHEMBL5205812 1 5.57
CHEMBL279433 L-778123 FREE BASE 1.0 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5189765 IC50 = 40.0 nM 7.40
CHEMBL125162 IC50 = 100.0 nM 7.00
CHEMBL5196678 IC50 = 120.0 nM 6.92
CHEMBL5204302 IC50 = 150.0 nM 6.82
CHEMBL5174289 IC50 = 160.0 nM 6.80
CHEMBL5195805 IC50 = 180.0 nM 6.75
CHEMBL5182445 IC50 = 190.0 nM 6.72
CHEMBL5180405 IC50 = 210.0 nM 6.68
CHEMBL5171383 IC50 = 260.0 nM 6.58
CHEMBL5202247 IC50 = 280.0 nM 6.55
CHEMBL5176914 IC50 = 320.0 nM 6.50
CHEMBL5209874 IC50 = 340.0 nM 6.47
CHEMBL5179982 IC50 = 550.0 nM 6.26
CHEMBL5171138 IC50 = 710.0 nM 6.15
CHEMBL5206115 IC50 = 740.0 nM 6.13
CHEMBL5195372 IC50 = 920.0 nM 6.04
CHEMBL5182735 IC50 = 1100.0 nM 5.96
CHEMBL5197720 IC50 = 1100.0 nM 5.96
CHEMBL5199791 IC50 = 1600.0 nM 5.80
CHEMBL5198833 IC50 = 1900.0 nM 5.72
CHEMBL125648 IC50 = 2200.0 nM 5.66
CHEMBL5199356 IC50 = 2600.0 nM 5.58
CHEMBL5205812 IC50 = 2700.0 nM 5.57
CHEMBL279433 L-778123 FREE BASE IC50 = 5800.0 nM 5.24