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Assay Detail

CHEMBL681128

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

Binding
Inhibition of Farnesyltransferase in H-ras-transformed Rat cells by radiotracer assay (CRAFTI)
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2095197)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

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 4 7.56 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL312459 1 8.19
CHEMBL524909 1 7.89
CHEMBL310943 1 7.47
CHEMBL312034 1 6.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL312459 IC50 = 6.4 nM 8.19
CHEMBL524909 IC50 = 13.0 nM 7.89
CHEMBL310943 IC50 = 34.0 nM 7.47
CHEMBL312034 IC50 = 210.0 nM 6.68