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Assay Detail

CHEMBL749434

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

Functional
Effective concentration required for inhibition of farnesylation of Ras protein in NIH3T3 cells
ChEMBL ↗
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type NIH3T3
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2094108) ↗
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors.
Wang L, Wang GT, Wang X, Tong Y, Sullivan G, Park D, Leonard NM, Li Q, Cohen J, Gu WZ, Zhang H, Bauch JL, Jakob CG, Hutchins CW, Stoll VS, Marsh K, Rosenberg SH, Sham HL, Lin NH.
J Med Chem (2004) 47 : 612 -626
PubMed 14736242 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 44 7.92 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL399482 — — 1 9.85
CHEMBL435247 — — 1 9.72
CHEMBL43455 — — 1 9.12
CHEMBL345895 — — 1 9.09
CHEMBL160563 — — 1 9.00
CHEMBL156387 — — 1 8.48
CHEMBL155310 — — 1 8.46
CHEMBL157077 — — 1 8.34
CHEMBL157782 — — 1 8.29
CHEMBL158553 — — 1 8.28
CHEMBL160562 — — 1 8.15
CHEMBL43631 — — 1 8.10
CHEMBL156523 — — 1 8.04
CHEMBL346290 — — 1 8.01
CHEMBL352237 — — 1 7.92
CHEMBL347435 — — 1 7.89
CHEMBL155876 — — 1 7.89
CHEMBL160670 — — 1 7.85
CHEMBL348861 — — 1 7.82
CHEMBL347172 — — 1 7.75
CHEMBL160619 — — 1 7.44
CHEMBL156530 — — 1 7.02
CHEMBL157794 — — 1 7.00
CHEMBL156862 — — 1 6.89
CHEMBL127296 — — 1 6.85
CHEMBL156629 — — 1 6.82
CHEMBL157581 — — 1 6.81
CHEMBL157094 — — 1 6.41
CHEMBL158262 — — 1 6.28
CHEMBL346696 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL399482 — EC50 = 0.14 nM 9.85
CHEMBL435247 — EC50 = 0.19 nM 9.72
CHEMBL43455 — EC50 = 0.75 nM 9.12
CHEMBL345895 — EC50 = 0.81 nM 9.09
CHEMBL160563 — EC50 = 1.0 nM 9.00
CHEMBL156387 — EC50 = 3.3 nM 8.48
CHEMBL155310 — EC50 = 3.5 nM 8.46
CHEMBL157077 — EC50 = 4.6 nM 8.34
CHEMBL157782 — EC50 = 5.1 nM 8.29
CHEMBL158553 — EC50 = 5.2 nM 8.28
CHEMBL160562 — EC50 = 7.0 nM 8.15
CHEMBL43631 — EC50 = 8.0 nM 8.10
CHEMBL156523 — EC50 = 9.1 nM 8.04
CHEMBL346290 — EC50 = 9.8 nM 8.01
CHEMBL352237 — EC50 = 12.0 nM 7.92
CHEMBL347435 — EC50 = 13.0 nM 7.89
CHEMBL155876 — EC50 = 13.0 nM 7.89
CHEMBL160670 — EC50 = 14.0 nM 7.85
CHEMBL348861 — EC50 = 15.0 nM 7.82
CHEMBL347172 — EC50 = 17.7 nM 7.75
CHEMBL160619 — EC50 = 36.0 nM 7.44
CHEMBL156530 — EC50 = 96.0 nM 7.02
CHEMBL157794 — EC50 = 100.0 nM 7.00
CHEMBL156862 — EC50 = 130.0 nM 6.89
CHEMBL127296 — EC50 = 140.0 nM 6.85
CHEMBL156629 — EC50 = 150.0 nM 6.82
CHEMBL157581 — EC50 = 154.0 nM 6.81
CHEMBL157094 — EC50 = 390.0 nM 6.41
CHEMBL158262 — EC50 = 525.0 nM 6.28
CHEMBL155939 — EC50 > 100.0 nM -
CHEMBL347942 — EC50 - nM -
CHEMBL351548 — EC50 > 1000.0 nM -
CHEMBL158333 — EC50 > 100.0 nM -
CHEMBL156061 — EC50 > 100.0 nM -
CHEMBL347174 — EC50 > 100.0 nM -
CHEMBL347482 — EC50 - nM -
CHEMBL345130 — EC50 > 100.0 nM -
CHEMBL157692 — EC50 > 100.0 nM -
CHEMBL158139 — EC50 < 1.0 nM -
CHEMBL2114434 — EC50 > 100.0 nM -
CHEMBL155785 — EC50 > 100.0 nM -
CHEMBL156107 — EC50 > 100.0 nM -
CHEMBL156026 — EC50 > 100.0 nM -
CHEMBL346696 — EC50 > 100.0 nM -