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Assay Detail

CHEMBL677849

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Binding
Inhibition of [3H]FPP incorporation into recombinant human K-Ras by Farnesyltransferase
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2094108)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

N-arylpiperazinone inhibitors of farnesyltransferase: discovery and biological activity.
Williams TM, Bergman JM, Brashear K, Breslin MJ, Dinsmore CJ, Hutchinson JH, MacTough SC, Stump CA, Wei DD, Zartman CB, Bogusky MJ, Culberson JC, Buser-Doepner C, Davide J, Greenberg IB, Hamilton KA, Koblan KS, Kohl NE, Liu D, Lobell RB, Mosser SD, O'Neill TJ, Rands E, Schaber MD, Huff JR.
J Med Chem (1999) 42 : 3779 -3784
PubMed 10508426 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.65 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL125162 1 9.96
CHEMBL125558 1 9.74
CHEMBL125648 1 9.36
CHEMBL333317 1 8.05
CHEMBL331496 1 7.68
CHEMBL125129 1 7.10
CHEMBL124576 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL125162 IC50 = 0.11 nM 9.96
CHEMBL125558 IC50 = 0.18 nM 9.74
CHEMBL125648 IC50 = 0.44 nM 9.36
CHEMBL333317 IC50 = 9.0 nM 8.05
CHEMBL331496 IC50 = 21.0 nM 7.68
CHEMBL125129 IC50 = 80.0 nM 7.10
CHEMBL124576 IC50 > 0.15 nM -