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Assay Detail

CHEMBL4724677

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

Binding
Inhibition of rat recombinant FTase expressed in Escherichia coli using 3H-FPP and biotinylated-DESGPGCMSCKCVLS peptide as substrates incubated for 30 mins in presence of 5 mM thiosulfate by scintillation proximity assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen.
Bukhtiyarova M,Cook EM,Hancock PJ,Hruza AW,Shaw AW,Adam GC,Barnard RJO,McKenna PM,Holloway MK,Bell IM,Carroll S,Cornella-Taracido I,Cox CD,Kutchukian PS,Powell DA,Strickland C,Trotter BW,Tudor M,Wolkenberg S,Li J,Tellers DM
ACS Med Chem Lett (2021) 12 : 99 -106
PubMed 33488970 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.49 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279433 L-778123 FREE BASE 1.0 1 7.30
CHEMBL4758112 1 5.68
CHEMBL4759194 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279433 L-778123 FREE BASE IC50 = 50.0 nM 7.30
CHEMBL4758112 IC50 = 2100.0 nM 5.68
CHEMBL4759194 IC50 > 40000.0 nM -