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Assay Detail

CHEMBL681652

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

Functional
EC50 is measured as inhibition of ras processing in a whole cell assay for farnesyltransferase (FTase)
20
Total Activities
20
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

Potent and orally bioavailable noncysteine-containing inhibitors of protein farnesyltransferase.
Augeri DJ, Janowick D, Kalvin D, Sullivan G, Larsen J, Dickman D, Ding H, Cohen J, Lee J, Warner R, Kovar P, Cherian S, Saeed B, Zhang H, Tahir S, Ng SC, Sham H, Rosenberg SH.
Bioorg Med Chem Lett (1999) 9 : 1069 -1074
PubMed 10328287 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 8.82 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10877 1 10.00
CHEMBL10902 1 9.52
CHEMBL276602 1 9.11
CHEMBL11210 1 9.05
CHEMBL428001 1 8.92
CHEMBL273697 1 8.82
CHEMBL10990 1 8.74
CHEMBL11195 1 8.00
CHEMBL11003 1 8.00
CHEMBL430096 1 8.00
CHEMBL10762 1 -
CHEMBL10970 1 -
CHEMBL10687 1 -
CHEMBL417606 1 -
CHEMBL430307 1 -
CHEMBL273265 1 -
CHEMBL10812 1 -
CHEMBL10955 1 -
CHEMBL273721 1 -
CHEMBL10912 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10877 EC50 = 0.1 nM 10.00
CHEMBL10902 EC50 = 0.3 nM 9.52
CHEMBL276602 EC50 = 0.78 nM 9.11
CHEMBL11210 EC50 = 0.9 nM 9.05
CHEMBL428001 EC50 = 1.2 nM 8.92
CHEMBL273697 EC50 = 1.5 nM 8.82
CHEMBL10990 EC50 = 1.8 nM 8.74
CHEMBL11195 EC50 = 10.0 nM 8.00
CHEMBL11003 EC50 = 10.0 nM 8.00
CHEMBL430096 EC50 = 10.0 nM 8.00
CHEMBL10762 EC50 > 0.3 nM -
CHEMBL10970 EC50 > 1.0 nM -
CHEMBL10687 EC50 > 1.0 nM -
CHEMBL417606 EC50 > 1.0 nM -
CHEMBL430307 EC50 > 1.0 nM -
CHEMBL273265 EC50 > 1.0 nM -
CHEMBL10812 EC50 = - nM -
CHEMBL10955 EC50 > 1.0 nM -
CHEMBL273721 EC50 > 1.0 nM -
CHEMBL10912 EC50 > 0.3 nM -