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Assay Detail

CHEMBL750319

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

Functional
Inhibition of farnesylation in NIH-3T3H-ras cell line
19
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2094108)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 4-[3-biphenyl-2-yl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl]-1-yl-benzonitrile as novel farnesyltransferase inhibitor.
Lin NH, Wang L, Cohen J, Gu WZ, Frost D, Zhang H, Rosenberg S, Sham H.
Bioorg Med Chem Lett (2003) 13 : 1293 -1296
PubMed 12657267 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 8.15 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL24043 1 10.00
CHEMBL22703 1 8.91
CHEMBL25620 1 8.85
CHEMBL22702 2 8.56
CHEMBL24048 1 8.42
CHEMBL23578 1 8.41
CHEMBL26068 1 8.40
CHEMBL24733 1 8.10
CHEMBL283051 1 8.02
CHEMBL282349 1 8.01
CHEMBL23753 1 7.31
CHEMBL277646 1 7.00
CHEMBL23370 1 6.89
CHEMBL24271 1 6.77
CHEMBL24159 1 -
CHEMBL26511 1 -
CHEMBL25621 1 -
CHEMBL24554 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL24043 EC50 = 0.1 nM 10.00
CHEMBL22703 EC50 = 1.24 nM 8.91
CHEMBL25620 EC50 = 1.4 nM 8.85
CHEMBL22702 EC50 = 2.74 nM 8.56
CHEMBL22702 EC50 = 2.74 nM 8.56
CHEMBL24048 EC50 = 3.8 nM 8.42
CHEMBL23578 EC50 = 3.86 nM 8.41
CHEMBL26068 EC50 = 4.0 nM 8.40
CHEMBL24733 EC50 = 7.9 nM 8.10
CHEMBL283051 EC50 = 9.5 nM 8.02
CHEMBL282349 EC50 = 9.8 nM 8.01
CHEMBL23753 EC50 = 49.0 nM 7.31
CHEMBL277646 EC50 = 100.0 nM 7.00
CHEMBL23370 EC50 = 130.0 nM 6.89
CHEMBL24271 EC50 = 170.0 nM 6.77
CHEMBL25621 EC50 < 1.0 nM -
CHEMBL26511 EC50 < 0.1 nM -
CHEMBL24554 EC50 < 1.0 nM -
CHEMBL24159 EC50 < 1.0 nM -