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Assay Detail

CHEMBL682420

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

Binding
Inhibition of [3H]FPP incorporation into recombinant [Leu68]-RAS1CVIM by Farnesyltransferase
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2094108)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Design and in vivo analysis of potent non-thiol inhibitors of farnesyl protein transferase.
Anthony NJ, Gomez RP, Schaber MD, Mosser SD, Hamilton KA, O'Neil TJ, Koblan KS, Graham SL, Hartman GD, Shah D, Rands E, Kohl NE, Gibbs JB, Oliff AI.
J Med Chem (1999) 42 : 3356 -3368
PubMed 10464022 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 8.76 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL252953 1 9.82
CHEMBL322355 1 9.82
CHEMBL324081 1 9.80
CHEMBL115502 1 9.39
CHEMBL326210 1 9.35
CHEMBL114739 1 9.26
CHEMBL325396 1 8.55
CHEMBL325840 1 8.55
CHEMBL114990 1 8.40
CHEMBL326745 1 8.00
CHEMBL320244 1 7.13
CHEMBL324008 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL252953 IC50 = 0.15 nM 9.82
CHEMBL322355 IC50 = 0.15 nM 9.82
CHEMBL324081 IC50 = 0.16 nM 9.80
CHEMBL115502 IC50 = 0.41 nM 9.39
CHEMBL326210 IC50 = 0.45 nM 9.35
CHEMBL114739 IC50 = 0.55 nM 9.26
CHEMBL325396 IC50 = 2.8 nM 8.55
CHEMBL325840 IC50 = 2.8 nM 8.55
CHEMBL114990 IC50 = 4.0 nM 8.40
CHEMBL326745 IC50 = 10.0 nM 8.00
CHEMBL320244 IC50 = 74.0 nM 7.13
CHEMBL324008 IC50 = 82.0 nM 7.09