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Assay Detail

CHEMBL828003

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Binding
Inhibition of bovine farnesyl transferase
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity.
Li Q, Li T, Woods KW, Gu WZ, Cohen J, Stoll VS, Galicia T, Hutchins C, Frost D, Rosenberg SH, Sham HL.
Bioorg Med Chem Lett (2005) 15 : 2918 -2922
PubMed 15911281 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.70 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL372208 1 9.30
CHEMBL382288 1 8.85
CHEMBL383579 1 8.29
CHEMBL197255 1 8.28
CHEMBL383797 1 8.18
CHEMBL435915 1 8.17
CHEMBL363823 1 8.10
CHEMBL372514 1 7.80
CHEMBL426274 1 7.68
CHEMBL197555 1 7.62
CHEMBL372904 1 7.44
CHEMBL373093 1 7.15
CHEMBL364506 1 6.82
CHEMBL372000 1 6.82
CHEMBL273987 1 6.70
CHEMBL2096825 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL372208 IC50 = 0.5 nM 9.30
CHEMBL382288 IC50 = 1.4 nM 8.85
CHEMBL383579 IC50 = 5.1 nM 8.29
CHEMBL197255 IC50 = 5.2 nM 8.28
CHEMBL383797 IC50 = 6.6 nM 8.18
CHEMBL435915 IC50 = 6.7 nM 8.17
CHEMBL363823 IC50 = 8.0 nM 8.10
CHEMBL372514 IC50 = 16.0 nM 7.80
CHEMBL426274 IC50 = 21.0 nM 7.68
CHEMBL197555 IC50 = 24.0 nM 7.62
CHEMBL372904 IC50 = 36.0 nM 7.44
CHEMBL373093 IC50 = 71.0 nM 7.15
CHEMBL364506 IC50 = 150.0 nM 6.82
CHEMBL372000 IC50 = 150.0 nM 6.82
CHEMBL273987 IC50 = 200.0 nM 6.70
CHEMBL2096825 IC50 = 1100.0 nM 5.96