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Assay Detail

CHEMBL3117844

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

Binding
Inhibition of FTase (unknown origin) assessed as transfer of [H3]farnesyl from [H3]farnesyl pyrophosphate to trichloroacetic acid-precipitable HaRas-CVLS
27
Total Activities
27
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

New class of azaheptapyridine FPT inhibitors as potential cancer therapy agents.
Zhu HY, Desai J, Cooper AB, Wang J, Rane DF, Kirschmeier P, Strickland C, Liu M, Nomeir AA, Girijavallabhan VM.
Bioorg Med Chem Lett (2014) 24 : 1228 -1231
PubMed 24462667 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 8.97 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3115255 1 10.00
CHEMBL3115256 1 10.00
CHEMBL3115258 1 9.70
CHEMBL601202 1 9.52
CHEMBL3115265 1 9.40
CHEMBL3115426 1 9.22
CHEMBL3115261 1 9.22
CHEMBL3115429 1 9.22
CHEMBL3115266 1 9.15
CHEMBL3115254 1 9.10
CHEMBL3115257 1 9.05
CHEMBL3115253 1 8.85
CHEMBL3115427 1 8.85
CHEMBL3115259 1 8.77
CHEMBL3115263 1 8.74
CHEMBL3115251 1 8.74
CHEMBL3115248 1 8.72
CHEMBL3115262 1 8.59
CHEMBL3115431 1 8.49
CHEMBL3115430 1 8.49
CHEMBL3115252 1 8.30
CHEMBL3115260 1 8.26
CHEMBL603067 1 7.92
CHEMBL3115264 1 -
CHEMBL3115249 1 -
CHEMBL3115250 1 -
CHEMBL3115428 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3115255 IC50 = 0.1 nM 10.00
CHEMBL3115256 IC50 = 0.1 nM 10.00
CHEMBL3115258 IC50 = 0.2 nM 9.70
CHEMBL601202 IC50 = 0.3 nM 9.52
CHEMBL3115265 IC50 = 0.4 nM 9.40
CHEMBL3115426 IC50 = 0.6 nM 9.22
CHEMBL3115261 IC50 = 0.6 nM 9.22
CHEMBL3115429 IC50 = 0.6 nM 9.22
CHEMBL3115266 IC50 = 0.7 nM 9.15
CHEMBL3115254 IC50 = 0.8 nM 9.10
CHEMBL3115257 IC50 = 0.9 nM 9.05
CHEMBL3115253 IC50 = 1.4 nM 8.85
CHEMBL3115427 IC50 = 1.4 nM 8.85
CHEMBL3115259 IC50 = 1.7 nM 8.77
CHEMBL3115263 IC50 = 1.8 nM 8.74
CHEMBL3115251 IC50 = 1.8 nM 8.74
CHEMBL3115248 IC50 = 1.9 nM 8.72
CHEMBL3115262 IC50 = 2.6 nM 8.59
CHEMBL3115431 IC50 = 3.2 nM 8.49
CHEMBL3115430 IC50 = 3.2 nM 8.49
CHEMBL3115252 IC50 = 5.0 nM 8.30
CHEMBL3115260 IC50 = 5.5 nM 8.26
CHEMBL603067 IC50 = 12.0 nM 7.92
CHEMBL3115264 IC50 > 20.0 nM -
CHEMBL3115249 IC50 > 18.0 nM -
CHEMBL3115250 IC50 > 18.0 nM -
CHEMBL3115428 IC50 - -