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Assay Detail

CHEMBL5217466

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

Binding
Inhibition of human DPP4 using Gly-Pro-AMC as substrate incubated for 30 mins by continuous fluorescent assay
5
Total Activities
5
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

Proline based rationally designed peptide esters against dipeptidyl peptidase-4: Highly potent anti-diabetic agents.
Vivesh, Kaur B, Jaglan S, Rani S, Batra Y, Singh P.
Bioorg Med Chem Lett (2022) 76 : 129018 -129018
PubMed 36209967 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.31 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL237500 LINAGLIPTIN 4.0 1 9.40
CHEMBL385517 SAXAGLIPTIN ANHYDROUS 4.0 1 8.82
CHEMBL376359 ALOGLIPTIN 4.0 1 8.12
CHEMBL3185489 1 7.75
CHEMBL142703 VILDAGLIPTIN 4.0 1 7.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL237500 LINAGLIPTIN IC50 = 0.4 nM 9.40
CHEMBL385517 SAXAGLIPTIN ANHYDROUS IC50 = 1.5 nM 8.82
CHEMBL376359 ALOGLIPTIN IC50 = 7.5 nM 8.12
CHEMBL3185489 IC50 = 18.0 nM 7.75
CHEMBL142703 VILDAGLIPTIN IC50 = 34.0 nM 7.47