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Assay Detail

CHEMBL681468

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Binding
Inhibition of [3H]farnesyl pyrophosphate binding to human farnesyltransferase
7
Total Activities
7
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

A novel metal-chelating inhibitor of protein farnesyltransferase.
Hamasaki A, Naka H, Tamanoi F, Umezawa K, Otsuka M.
Bioorg Med Chem Lett (2003) 13 : 1523 -1526
PubMed 12699746 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.41 5.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39572 1 5.72
CHEMBL289404 1 5.60
CHEMBL285848 MANUMYCIN A 1 4.92
CHEMBL39879 DIPYRIDYL 1 -
CHEMBL816 ETHYLENEDIAMINE 3.0 1 -
CHEMBL36582 1 -
CHEMBL415879 PHENANTHROLINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39572 IC50 = 1900.0 nM 5.72
CHEMBL289404 IC50 = 2500.0 nM 5.60
CHEMBL285848 MANUMYCIN A IC50 = 11900.0 nM 4.92
CHEMBL39879 DIPYRIDYL IC50 = 100000000.0 nM -
CHEMBL816 ETHYLENEDIAMINE IC50 = 15500000.0 nM -
CHEMBL36582 IC50 = 620000.0 nM -
CHEMBL415879 PHENANTHROLINE IC50 = 4000000.0 nM -