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Assay Detail

CHEMBL651598

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

Functional
Inhibition of Ras farnesylation in Human Ha-Ras oncogene-transformed BALB/c 3T3 cells (EJ3 cells)
11
Total Activities
11
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

Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency.
Gwaltney SL, O'Connor SJ, Nelson LT, Sullivan GM, Imade H, Wang W, Hasvold L, Li Q, Cohen J, Gu WZ, Tahir SK, Bauch J, Marsh K, Ng SC, Frost DJ, Zhang H, Muchmore S, Jakob CG, Stoll V, Hutchins C, Rosenberg SH, Sham HL.
Bioorg Med Chem Lett (2003) 13 : 1363 -1366
PubMed 12657283 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 8.03 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL280847 1 9.30
CHEMBL30059 1 8.41
CHEMBL282161 1 8.40
CHEMBL29633 1 7.55
CHEMBL30118 1 7.51
CHEMBL430073 1 7.01
CHEMBL27677 1 -
CHEMBL29619 1 -
CHEMBL29980 1 -
CHEMBL29503 1 -
CHEMBL282166 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL280847 EC50 = 0.5 nM 9.30
CHEMBL30059 EC50 = 3.9 nM 8.41
CHEMBL282161 EC50 = 4.0 nM 8.40
CHEMBL29633 EC50 = 28.0 nM 7.55
CHEMBL30118 EC50 = 31.0 nM 7.51
CHEMBL430073 EC50 = 97.0 nM 7.01
CHEMBL27677 EC50 > 100.0 nM -
CHEMBL29619 EC50 > 100.0 nM -
CHEMBL29980 EC50 > 100.0 nM -
CHEMBL29503 EC50 > 1.0 nM -
CHEMBL282166 EC50 > 100.0 nM -