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Assay Detail

CHEMBL4185520

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

Binding
Inhibition of FTase isolated from human Burkitt's lymphoma cells assessed as decrease in transfer of [3H]farnesyl from [3H]farnesyl PPi to H-Ras-CVLS
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Intermediate

Target

Protein farnesyltransferase (CHEMBL2094108)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins.
Buuh ZY, Lyu Z, Wang RE.
J Med Chem (2018) 61 : 3239 -3252
PubMed 28505447 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.54 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54044 1 9.30
CHEMBL135561 1 9.30
CHEMBL4218727 1 8.85
CHEMBL27449 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54044 IC50 = 0.5 nM 9.30
CHEMBL135561 IC50 = 0.5 nM 9.30
CHEMBL4218727 IC50 = 1.4 nM 8.85
CHEMBL27449 IC50 = 200.0 nM 6.70