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Assay Detail

CHEMBL5366935

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

Binding
Inhibition of mouse DPP-4 using Gly-Pro-AMC as substrate measured after 5 mins by CF assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dipeptidyl peptidase 4 (CHEMBL3883)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Development of Long-Acting Dipeptidyl Peptidase-4 Inhibitors: Structural Evolution and Long-Acting Determinants.
Li Q, Deng X, Xu YJ, Dong L.
J Med Chem (2023) 66 : 11593 -11631
PubMed 37647598 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.40 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL237500 LINAGLIPTIN 4.0 1 9.92
CHEMBL385517 SAXAGLIPTIN ANHYDROUS 4.0 1 8.72
CHEMBL376359 ALOGLIPTIN 4.0 1 8.07
CHEMBL1422 SITAGLIPTIN 4.0 1 7.70
CHEMBL142703 VILDAGLIPTIN 4.0 1 7.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL237500 LINAGLIPTIN IC50 = 0.12 nM 9.92
CHEMBL385517 SAXAGLIPTIN ANHYDROUS IC50 = 1.9 nM 8.72
CHEMBL376359 ALOGLIPTIN IC50 = 8.6 nM 8.07
CHEMBL1422 SITAGLIPTIN IC50 = 20.0 nM 7.70
CHEMBL142703 VILDAGLIPTIN IC50 = 26.0 nM 7.58