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Assay Detail

CHEMBL4307489

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

Binding
Inhibition of recombinant human DPPI using H-Gly-Arg-AFC as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence plate reader analysis
6
Total Activities
6
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 1 (CHEMBL2252)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

DPP1 Inhibitors: Exploring the Role of Water in the S2 Pocket of DPP1 with Substituted Pyrrolidines.
Käck H, Doyle K, Hughes SJ, Bodnarchuk MS, Lönn H, Van De Poël A, Palmer N.
ACS Med Chem Lett (2019) 10 : 1222 -1227
PubMed 31413809 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.83 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4561264 1 9.40
CHEMBL4579467 1 8.80
CHEMBL4513306 1 8.20
CHEMBL4570759 1 7.30
CHEMBL4451898 1 7.10
CHEMBL4461966 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4561264 IC50 = 0.3981 nM 9.40
CHEMBL4579467 IC50 = 1.585 nM 8.80
CHEMBL4513306 IC50 = 6.31 nM 8.20
CHEMBL4570759 IC50 = 50.12 nM 7.30
CHEMBL4451898 IC50 = 79.43 nM 7.10
CHEMBL4461966 IC50 = 630.96 nM 6.20