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Assay Detail

CHEMBL1022131

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

Binding
Inhibition of rat recombinant protein farnesyltransferase expressed in Sf9 cells by [3H]-scintillation proximity assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type Sf9
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Rational modification of a candidate cancer drug for use against Chagas disease.
Kraus JM, Verlinde CL, Karimi M, Lepesheva GI, Gelb MH, Buckner FS.
J Med Chem (2009) 52 : 1639 -1647
PubMed 19239254 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.51 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL289228 TIPIFARNIB 3.0 1 9.15
CHEMBL514400 1 8.40
CHEMBL471607 1 7.89
CHEMBL510213 1 7.77
CHEMBL456001 1 6.53
CHEMBL456002 1 6.52
CHEMBL470996 1 6.31
CHEMBL471195 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL289228 TIPIFARNIB IC50 = 0.7 nM 9.15
CHEMBL514400 IC50 = 4.0 nM 8.40
CHEMBL471607 IC50 = 13.0 nM 7.89
CHEMBL510213 IC50 = 17.0 nM 7.77
CHEMBL456001 IC50 = 294.0 nM 6.53
CHEMBL456002 IC50 = 300.0 nM 6.52
CHEMBL470996 IC50 = 485.0 nM 6.31
CHEMBL471195 IC50 > 5000.0 nM -