Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL682935

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

Binding
In vitro inhibitory activity against farnesyl transferase
10
Total Activities
10
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

Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.
Gwaltney SL, O'Connor SJ, Nelson LT, Sullivan GM, Imade H, Wang W, Hasvold L, Li Q, Cohen J, Gu WZ, Tahir SK, Bauch J, Marsh K, Ng SC, Frost DJ, Zhang H, Muchmore S, Jakob CG, Stoll V, Hutchins C, Rosenberg SH, Sham HL.
Bioorg Med Chem Lett (2003) 13 : 1359 -1362
PubMed 12657282 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.78 9.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL417481 1 9.25
CHEMBL29356 1 9.15
CHEMBL29980 1 9.04
CHEMBL280976 1 8.92
CHEMBL282793 1 8.60
CHEMBL29946 1 6.89
CHEMBL29748 1 6.62
CHEMBL25968 1 6.55
CHEMBL282964 1 6.51
CHEMBL29466 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL417481 IC50 = 0.56 nM 9.25
CHEMBL29356 IC50 = 0.71 nM 9.15
CHEMBL29980 IC50 = 0.92 nM 9.04
CHEMBL280976 IC50 = 1.2 nM 8.92
CHEMBL282793 IC50 = 2.5 nM 8.60
CHEMBL29946 IC50 = 130.0 nM 6.89
CHEMBL29748 IC50 = 240.0 nM 6.62
CHEMBL25968 IC50 = 280.0 nM 6.55
CHEMBL282964 IC50 = 310.0 nM 6.51
CHEMBL29466 IC50 = 560.0 nM 6.25