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Assay Detail

CHEMBL680528

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Binding
In vitro inhibitory activity against Farnesyltransferase (FTase)
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2095197)
Type PROTEIN COMPLEX
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
IC50 27 9.11 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL358363 1 9.85
CHEMBL344771 1 9.80
CHEMBL175628 1 9.77
CHEMBL367324 1 9.77
CHEMBL144175 1 9.70
CHEMBL344100 1 9.70
CHEMBL178483 1 9.66
CHEMBL367008 1 9.60
CHEMBL367456 1 9.55
CHEMBL145317 1 9.39
CHEMBL342315 1 9.38
CHEMBL177452 1 9.34
CHEMBL144536 1 9.22
CHEMBL368038 1 9.18
CHEMBL175682 1 9.15
CHEMBL369548 1 9.15
CHEMBL362186 1 9.06
CHEMBL144745 1 9.00
CHEMBL177340 1 8.96
CHEMBL145699 1 8.92
CHEMBL177445 1 8.54
CHEMBL178430 1 8.46
CHEMBL424119 1 8.40
CHEMBL343435 1 8.34
CHEMBL145417 1 8.10
CHEMBL144183 1 8.00
CHEMBL145950 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL358363 IC50 = 0.14 nM 9.85
CHEMBL344771 IC50 = 0.16 nM 9.80
CHEMBL175628 IC50 = 0.17 nM 9.77
CHEMBL367324 IC50 = 0.17 nM 9.77
CHEMBL144175 IC50 = 0.2 nM 9.70
CHEMBL344100 IC50 = 0.2 nM 9.70
CHEMBL178483 IC50 = 0.22 nM 9.66
CHEMBL367008 IC50 = 0.25 nM 9.60
CHEMBL367456 IC50 = 0.28 nM 9.55
CHEMBL145317 IC50 = 0.41 nM 9.39
CHEMBL342315 IC50 = 0.42 nM 9.38
CHEMBL177452 IC50 = 0.46 nM 9.34
CHEMBL144536 IC50 = 0.6 nM 9.22
CHEMBL368038 IC50 = 0.66 nM 9.18
CHEMBL175682 IC50 = 0.7 nM 9.15
CHEMBL369548 IC50 = 0.7 nM 9.15
CHEMBL362186 IC50 = 0.87 nM 9.06
CHEMBL144745 IC50 = 1.0 nM 9.00
CHEMBL177340 IC50 = 1.1 nM 8.96
CHEMBL145699 IC50 = 1.2 nM 8.92
CHEMBL177445 IC50 = 2.9 nM 8.54
CHEMBL178430 IC50 = 3.5 nM 8.46
CHEMBL424119 IC50 = 4.0 nM 8.40
CHEMBL343435 IC50 = 4.6 nM 8.34
CHEMBL145417 IC50 = 8.0 nM 8.10
CHEMBL144183 IC50 = 10.0 nM 8.00
CHEMBL145950 IC50 = 12.0 nM 7.92