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Assay Detail

CHEMBL779510

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Functional
Inhibitory activity against whole cell Ras prenylation
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Discovery of a series of cyclohexylethylamine-containing protein farnesyltransferase inhibitors exhibiting potent cellular activity.
Henry KJ, Wasicak J, Tasker AS, Cohen J, Ewing P, Mitten M, Larsen JJ, Kalvin DM, Swenson R, Ng SC, Saeed B, Cherian S, Sham H, Rosenberg SH.
J Med Chem (1999) 42 : 4844 -4852
PubMed 10579847 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 7.62 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL144536 1 8.55
CHEMBL177452 1 8.37
CHEMBL344100 1 8.36
CHEMBL362186 1 7.92
CHEMBL144175 1 7.92
CHEMBL367456 1 7.28
CHEMBL367324 1 6.80
CHEMBL344771 1 6.72
CHEMBL175628 1 6.70
CHEMBL369548 1 -
CHEMBL177445 1 -
CHEMBL178430 1 -
CHEMBL175682 1 -
CHEMBL177340 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL144536 EC50 = 2.8 nM 8.55
CHEMBL177452 EC50 = 4.3 nM 8.37
CHEMBL344100 EC50 = 4.4 nM 8.36
CHEMBL362186 EC50 = 12.0 nM 7.92
CHEMBL144175 EC50 = 12.0 nM 7.92
CHEMBL367456 EC50 = 52.0 nM 7.28
CHEMBL367324 EC50 = 160.0 nM 6.80
CHEMBL344771 EC50 = 190.0 nM 6.72
CHEMBL175628 EC50 = 200.0 nM 6.70
CHEMBL369548 EC50 > 1000.0 nM -
CHEMBL177445 EC50 > 1000.0 nM -
CHEMBL178430 EC50 > 1000.0 nM -
CHEMBL175682 EC50 > 1000.0 nM -
CHEMBL177340 EC50 > 1000.0 nM -