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Assay Detail

CHEMBL827215

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

Binding
Inhibition of [3H]FPP incorporation by Protein Farnesyltransferase
12
Total Activities
12
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

Design, synthesis, and evaluation of sugar amino acid based inhibitors of protein prenyl transferases PFT and PGGT-1.
El Oualid F, Burm BE, Leroy IM, Cohen LH, van Boom JH, van den Elst H, Overkleeft HS, van der Marel GA, Overhand M.
J Med Chem (2004) 47 : 3920 -3923
PubMed 15267228 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.22 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL363025 1 6.60
CHEMBL55423 1 6.38
CHEMBL185816 1 5.66
CHEMBL185908 1 4.38
CHEMBL189409 1 4.24
CHEMBL365616 1 4.04
CHEMBL360809 1 -
CHEMBL185863 1 -
CHEMBL187467 1 -
CHEMBL185629 1 -
CHEMBL363549 1 -
CHEMBL186327 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL363025 IC50 = 250.0 nM 6.60
CHEMBL55423 IC50 = 420.0 nM 6.38
CHEMBL185816 IC50 = 2200.0 nM 5.66
CHEMBL185908 IC50 = 42000.0 nM 4.38
CHEMBL189409 IC50 = 57000.0 nM 4.24
CHEMBL365616 IC50 = 91000.0 nM 4.04
CHEMBL360809 IC50 ~ 1000000.0 nM -
CHEMBL185863 IC50 ~ 1000000.0 nM -
CHEMBL187467 IC50 = 321000.0 nM -
CHEMBL185629 IC50 ~ 1000000.0 nM -
CHEMBL363549 IC50 > 1000000.0 nM -
CHEMBL186327 IC50 > 1000000.0 nM -