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Assay Detail

CHEMBL681644

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

Binding
Inhibition of farnesyl transferase (FTase) of rat brain
14
Total Activities
12
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

Constrained analogs of KCVFM with improved inhibitory properties against farnesyl transferase
Clerc F, Guitton J, Fromage N, Lelievre Y, Duchesne M, Tocque B, James-Surcouf E, Commercon A, Becquart J
Bioorg Med Chem Lett (1995) 5 : 1779 -1784
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.63 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL299956 1 8.30
CHEMBL2115457 1 7.70
CHEMBL48182 1 7.40
CHEMBL50624 1 6.00
CHEMBL51436 1 6.00
CHEMBL433279 1 6.00
CHEMBL297242 1 6.00
CHEMBL2115458 1 5.70
CHEMBL2115025 2 4.82
CHEMBL289302 1 4.60
CHEMBL3350314 2 4.30
CHEMBL3350692 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL299956 IC50 = 5.0 nM 8.30
CHEMBL2115457 IC50 = 20.0 nM 7.70
CHEMBL48182 IC50 = 40.0 nM 7.40
CHEMBL50624 IC50 = 1000.0 nM 6.00
CHEMBL51436 IC50 = 1000.0 nM 6.00
CHEMBL433279 IC50 = 1000.0 nM 6.00
CHEMBL297242 IC50 = 1000.0 nM 6.00
CHEMBL2115458 IC50 = 2000.0 nM 5.70
CHEMBL2115025 IC50 = 15000.0 nM 4.82
CHEMBL289302 IC50 = 25000.0 nM 4.60
CHEMBL3350314 IC50 = 50000.0 nM 4.30
CHEMBL3350314 IC50 = 100000.0 nM 4.00
CHEMBL3350692 IC50 = 100000.0 nM 4.00
CHEMBL2115025 IC50 = 100000.0 nM 4.00