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Assay Detail

CHEMBL833108

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

Functional
Effective concentration against H-ras processing in transformed NIH3T3 cells
28
Total Activities
27
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

Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase.
Wang GT, Wang X, Wang W, Hasvold LA, Sullivan G, Hutchins CW, O'Conner S, Gentiles R, Sowin T, Cohen J, Gu WZ, Zhang H, Rosenberg SH, Sham HL.
Bioorg Med Chem Lett (2005) 15 : 153 -158
PubMed 15582430 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 7.03 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183356 1 7.96
CHEMBL183832 1 7.89
CHEMBL182180 2 7.80
CHEMBL183719 1 7.52
CHEMBL359959 1 7.28
CHEMBL360525 1 7.07
CHEMBL179902 1 7.05
CHEMBL181318 1 7.05
CHEMBL361357 1 7.00
CHEMBL182330 1 6.96
CHEMBL41748 1 6.96
CHEMBL183902 1 6.92
CHEMBL183224 1 6.89
CHEMBL368904 1 6.77
CHEMBL360694 1 6.70
CHEMBL183523 1 6.68
CHEMBL183276 1 6.62
CHEMBL183372 1 6.54
CHEMBL361353 1 6.48
CHEMBL182978 1 6.38
CHEMBL182812 1 -
CHEMBL179857 1 -
CHEMBL182679 1 -
CHEMBL183246 1 -
CHEMBL183548 1 -
CHEMBL183725 1 -
CHEMBL359950 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183356 EC50 = 11.0 nM 7.96
CHEMBL183832 EC50 = 13.0 nM 7.89
CHEMBL182180 EC50 = 16.0 nM 7.80
CHEMBL183719 EC50 = 30.0 nM 7.52
CHEMBL359959 EC50 = 53.0 nM 7.28
CHEMBL360525 EC50 = 85.0 nM 7.07
CHEMBL181318 EC50 = 90.0 nM 7.05
CHEMBL179902 EC50 = 89.0 nM 7.05
CHEMBL361357 EC50 = 100.0 nM 7.00
CHEMBL182330 EC50 = 110.0 nM 6.96
CHEMBL41748 EC50 = 110.0 nM 6.96
CHEMBL183902 EC50 = 120.0 nM 6.92
CHEMBL183224 EC50 = 130.0 nM 6.89
CHEMBL368904 EC50 = 170.0 nM 6.77
CHEMBL360694 EC50 = 201.0 nM 6.70
CHEMBL183523 EC50 = 210.0 nM 6.68
CHEMBL183276 EC50 = 240.0 nM 6.62
CHEMBL183372 EC50 = 285.0 nM 6.54
CHEMBL361353 EC50 = 330.0 nM 6.48
CHEMBL182978 EC50 = 420.0 nM 6.38
CHEMBL182812 EC50 > 1000.0 nM -
CHEMBL182679 EC50 > 1000.0 nM -
CHEMBL179857 EC50 = 83.0 % -
CHEMBL183246 EC50 > 1000.0 nM -
CHEMBL183548 EC50 > 1000.0 nM -
CHEMBL183725 EC50 = 89.0 % -
CHEMBL182180 EC50 > 1000.0 nM -
CHEMBL359950 EC50 > 1000.0 nM -