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Assay Detail

CHEMBL681887

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

Binding
The concentration required to displace 50% of a highly potent radiolabeled FPTase inhibitor
17
Total Activities
16
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 (CHEMBL2094108)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases.
Tucker TJ, Abrams MT, Buser CA, Davide JP, Ellis-Hutchings M, Fernandes C, Gibbs JB, Graham SL, Hartman GD, Huber HE, Liu D, Lobell RB, Lumma WC, Robinson RG, Sisko JT, Smith AM.
Bioorg Med Chem Lett (2002) 12 : 2027 -2030
PubMed 12113834 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 8.07 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59963 1 9.07
CHEMBL293623 1 8.95
CHEMBL64183 1 8.66
CHEMBL303326 2 8.40
CHEMBL63107 1 8.35
CHEMBL291580 1 8.10
CHEMBL418513 1 8.06
CHEMBL63106 1 8.04
CHEMBL305138 1 7.96
CHEMBL63270 1 7.92
CHEMBL304703 1 7.89
CHEMBL304449 1 7.20
CHEMBL293924 1 6.78
CHEMBL293015 1 -
CHEMBL302429 1 -
CHEMBL64168 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59963 IC50 = 0.85 nM 9.07
CHEMBL293623 IC50 = 1.13 nM 8.95
CHEMBL64183 IC50 = 2.2 nM 8.66
CHEMBL303326 IC50 = 4.0 nM 8.40
CHEMBL63107 IC50 = 4.52 nM 8.35
CHEMBL291580 IC50 = 7.95 nM 8.10
CHEMBL418513 IC50 = 8.67 nM 8.06
CHEMBL63106 IC50 = 9.1 nM 8.04
CHEMBL305138 IC50 = 10.9 nM 7.96
CHEMBL63270 IC50 = 12.1 nM 7.92
CHEMBL304703 IC50 = 13.0 nM 7.89
CHEMBL303326 IC50 = 27.0 nM 7.57
CHEMBL304449 IC50 = 62.9 nM 7.20
CHEMBL293924 IC50 = 166.0 nM 6.78
CHEMBL302429 IC50 - nM -
CHEMBL64168 IC50 - nM -
CHEMBL293015 IC50 - nM -