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Assay Detail

CHEMBL2060148

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

Binding
Inhibition of human recombinant DPP8 using Gly-Pro-MCA as substrate after 30 mins by fluorometry
2
Total Activities
2
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 8 (CHEMBL4657)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fused bicyclic heteroarylpiperazine-substituted L-prolylthiazolidines as highly potent DPP-4 inhibitors lacking the electrophilic nitrile group.
Yoshida T, Akahoshi F, Sakashita H, Sonda S, Takeuchi M, Tanaka Y, Nabeno M, Kishida H, Miyaguchi I, Hayashi Y.
Bioorg Med Chem (2012) 20 : 5033 -5041
PubMed 22824762 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.53 7.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL391466 1 7.91
CHEMBL2058971 1 7.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL391466 IC50 = 12.2 nM 7.91
CHEMBL2058971 IC50 = 72.4 nM 7.14