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Assay Detail

CHEMBL5678936

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

Binding
Inhibition of recombinant bovine FTase incubated for 30 mins in presence of [3H]FPP by SPA based Topcount scintillation plate reader analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
2
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

A highly potent and selective farnesyltransferase inhibitor ABT-100 in preclinical studies.
Gu WZ, Joseph I, Wang YC, Frost D, Sullivan GM, Wang L, Lin NH, Cohen J, Stoll VS, Jakob CG, Muchmore SW, Harlan JE, Holzman T, Walten KA, Ladror US, Anderson MG, Kroeger P, Rodriguez LE, Jarvis KP, Ferguson D, Marsh K, Ng S, Rosenberg SH, Sham HL, Zhang H.
Anticancer Drugs (2005) 16 : 1059 -1069
PubMed 16222147 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.60 9.89

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - MONDO:0004992
EFO_TERM EFO_TERM - cancer

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4586794 ABT-100 1 9.89
CHEMBL351706 BMS-214662 1.0 1 9.17
CHEMBL298734 LONAFARNIB 4.0 1 8.11
CHEMBL289228 TIPIFARNIB 3.0 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4586794 ABT-100 IC50 = 0.13 nM 9.89
CHEMBL351706 BMS-214662 IC50 = 0.67 nM 9.17
CHEMBL298734 LONAFARNIB IC50 = 7.8 nM 8.11
CHEMBL289228 TIPIFARNIB IC50 = 57.0 nM 7.24