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Assay Detail

CHEMBL892675

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Binding
Inhibition of FTase by SPA
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Impact on farnesyltransferase inhibition of 4-chlorophenyl moiety replacement in the Zarnestra series.
Angibaud P, Mevellec L, Meyer C, Bourdrez X, Lezouret P, Pilatte I, Poncelet V, Roux B, Merillon S, End DW, Van Dun J, Wouters W, Venet M.
Eur J Med Chem (2007) 42 : 702 -714
PubMed 17316920 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.49 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL243659 (S)-TIPIFARNIB 1 9.05
CHEMBL388241 1 9.00
CHEMBL395718 1 9.00
CHEMBL341586 1 8.46
CHEMBL337751 1 8.46
CHEMBL395964 1 8.40
CHEMBL244907 1 8.30
CHEMBL394371 1 7.96
CHEMBL242594 1 7.80
CHEMBL244724 1 -
CHEMBL243660 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL243659 (S)-TIPIFARNIB IC50 = 0.9 nM 9.05
CHEMBL388241 IC50 = 1.0 nM 9.00
CHEMBL395718 IC50 = 1.0 nM 9.00
CHEMBL341586 IC50 = 3.5 nM 8.46
CHEMBL337751 IC50 = 3.5 nM 8.46
CHEMBL395964 IC50 = 4.0 nM 8.40
CHEMBL244907 IC50 = 5.0 nM 8.30
CHEMBL394371 IC50 = 11.0 nM 7.96
CHEMBL242594 IC50 = 16.0 nM 7.80
CHEMBL244724 IC50 < 100.0 nM -
CHEMBL243660 IC50 > 100.0 nM -