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Assay Detail

CHEMBL4336749

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Binding
Inhibition of FAP (unknown origin)
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prolyl endopeptidase FAP (CHEMBL4683)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Integrated Synthetic, Biophysical, and Computational Investigations of Covalent Inhibitors of Prolyl Oligopeptidase and Fibroblast Activation Protein α.
Plescia J, De Cesco S, Patrascu MB, Kurian J, Di Trani J, Dufresne C, Wahba AS, Janmamode N, Mittermaier AK, Moitessier N.
J Med Chem (2019) 62 : 7874 -7884
PubMed 31393718 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.44 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1243126 1 7.70
CHEMBL67279 TALABOSTAT 3.0 1 7.18
CHEMBL2333026 1 -
CHEMBL4464623 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1243126 IC50 = 20.0 nM 7.70
CHEMBL67279 TALABOSTAT IC50 = 66.0 nM 7.18
CHEMBL2333026 IC50 > 36.0 nM -
CHEMBL4464623 IC50 > 100000.0 nM -