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Assay Detail

CHEMBL769088

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

Binding
Inhibition of Trypanosoma brucei protein farnesyltransferase
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Trypanosoma brucei brucei
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2094108)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Design and synthesis of peptidomimetic protein farnesyltransferase inhibitors as anti-Trypanosoma brucei agents.
Ohkanda J, Buckner FS, Lockman JW, Yokoyama K, Carrico D, Eastman R, de Luca-Fradley K, Davies W, Croft SL, Van Voorhis WC, Gelb MH, Sebti SM, Hamilton AD.
J Med Chem (2004) 47 : 432 -445
PubMed 14711313 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.26 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54044 1 8.77
CHEMBL431828 1 8.74
CHEMBL336915 1 8.23
CHEMBL138192 1 8.18
CHEMBL135561 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54044 IC50 = 1.7 nM 8.77
CHEMBL431828 IC50 = 1.8 nM 8.74
CHEMBL336915 IC50 = 5.9 nM 8.23
CHEMBL138192 IC50 = 6.6 nM 8.18
CHEMBL135561 IC50 = 40.0 nM 7.40