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Assay Detail

CHEMBL829182

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Functional
Reduced farnesylation of H-ras transformed NIH3T3 cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type NIH3T3
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2096912)
Type PROTEIN COMPLEX
Organism Mus musculus

Publication

Synthesis of 1H-pyridin-2-one derivatives as potent and selective farnesyltransferase inhibitors.
Wang L, Lin NH, Li Q, Henry RF, Zhang H, Cohen J, Gu WZ, Marsh KC, Bauch JL, Rosenberg SH, Sham HL.
Bioorg Med Chem Lett (2004) 14 : 4603 -4606
PubMed 15324873 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 8.17 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL128309 1 9.30
CHEMBL158553 1 8.28
CHEMBL365269 1 8.05
CHEMBL363518 1 8.00
CHEMBL185492 1 7.94
CHEMBL365718 1 7.82
CHEMBL183265 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL128309 EC50 = 0.5 nM 9.30
CHEMBL158553 EC50 = 5.2 nM 8.28
CHEMBL365269 EC50 = 9.0 nM 8.05
CHEMBL363518 EC50 = 10.0 nM 8.00
CHEMBL185492 EC50 = 11.4 nM 7.94
CHEMBL365718 EC50 = 15.0 nM 7.82
CHEMBL183265 EC50 = 15.0 nM 7.82