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Assay Detail

CHEMBL5366936

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

Binding
Binding affinity to human DPP-4 using gly-pro-pNA as substrate assessed as inhibition constant
4
Total Activities
4
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

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
Ki 4 8.28 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL385517 SAXAGLIPTIN ANHYDROUS 4.0 1 8.89
CHEMBL3350936 1 8.59
CHEMBL142703 VILDAGLIPTIN 4.0 1 7.89
CHEMBL1422 SITAGLIPTIN 4.0 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL385517 SAXAGLIPTIN ANHYDROUS Ki = 1.3 nM 8.89
CHEMBL3350936 Ki = 2.6 nM 8.59
CHEMBL142703 VILDAGLIPTIN Ki = 13.0 nM 7.89
CHEMBL1422 SITAGLIPTIN Ki = 18.0 nM 7.75