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Assay Detail

CHEMBL3859650

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

Binding
Inhibition of rat DPP1 using Gly-Arg-AMC as substrate preincubated for 30 mins followed by substrate addition by fluorometric assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dipeptidyl peptidase 1 (CHEMBL3308944)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).
Doyle K, Lönn H, Käck H, Van de Poël A, Swallow S, Gardiner P, Connolly S, Root J, Wikell C, Dahl G, Stenvall K, Johannesson P.
J Med Chem (2016) 59 : 9457 -9472
PubMed 27690432 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.70 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3900409 BRENSOCATIB 3.0 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3900409 BRENSOCATIB IC50 = 19.95 nM 7.70