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Assay Detail

CHEMBL2346132

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

Binding
Inhibition of human DPP4 using H-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay
7
Total Activities
7
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

Dipeptidyl peptidase 4 (CHEMBL284)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase.
Poplawski SE, Lai JH, Li Y, Jin Z, Liu Y, Wu W, Wu Y, Zhou Y, Sudmeier JL, Sanford DG, Bachovchin WW.
J Med Chem (2013) 56 : 3467 -3477
PubMed 23594271 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.06 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL67279 TALABOSTAT 3.0 1 9.05
CHEMBL67089 1 7.89
CHEMBL2333023 1 5.75
CHEMBL2333025 1 5.55
CHEMBL2333024 1 -
CHEMBL2333026 1 -
CHEMBL1243373 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL67279 TALABOSTAT IC50 = 0.9 nM 9.05
CHEMBL67089 IC50 = 13.0 nM 7.89
CHEMBL2333023 IC50 = 1800.0 nM 5.75
CHEMBL2333025 IC50 = 2800.0 nM 5.55
CHEMBL2333024 IC50 > 100000.0 nM -
CHEMBL2333026 IC50 > 100000.0 nM -
CHEMBL1243373 IC50 > 100000.0 nM -