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Assay Detail

CHEMBL680082

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

Binding
Inhibition of Farnesyltransferase in PSN-1 cells at 10 pM
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PSN-1
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2094108)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.
Bell IM, Gallicchio SN, Abrams M, Beese LS, Beshore DC, Bhimnathwala H, Bogusky MJ, Buser CA, Culberson JC, Davide J, Ellis-Hutchings M, Fernandes C, Gibbs JB, Graham SL, Hamilton KA, Hartman GD, Heimbrook DC, Homnick CF, Huber HE, Huff JR, Kassahun K, Koblan KS, Kohl NE, Lobell RB, Lynch JJ, Robinson R, Rodrigues AD, Taylor JS, Walsh ES, Williams TM, Zartman CB.
J Med Chem (2002) 45 : 2388 -2409
PubMed 12036349 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 10.22 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL310586 1 10.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL310586 IC50 = 0.06 nM 10.22