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Assay Detail

CHEMBL5584747

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

Binding
Inhibition of DPP4 (unknown origin)
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

Synthesis and clinical application of representative small-molecule dipeptidyl Peptidase-4 (DPP-4) inhibitors for the treatment of type 2 diabetes mellitus (T2DM).
Shao DW, Zhao LJ, Sun JF.
Eur J Med Chem (2024) 272 : 116464 -116464
PubMed 38704940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.49 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL237500 LINAGLIPTIN 4.0 1 9.00
CHEMBL5597715 1 8.64
CHEMBL2105754 TRELAGLIPTIN SUCCINATE 4.0 1 8.40
CHEMBL4646510 COFROGLIPTIN 2.0 1 8.38
CHEMBL1201174 SITAGLIPTIN PHOSPHATE 4.0 1 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL237500 LINAGLIPTIN IC50 = 1.0 nM 9.00
CHEMBL5597715 IC50 = 2.27 nM 8.64
CHEMBL2105754 TRELAGLIPTIN SUCCINATE IC50 = 4.0 nM 8.40
CHEMBL4646510 COFROGLIPTIN IC50 = 4.18 nM 8.38
CHEMBL1201174 SITAGLIPTIN PHOSPHATE IC50 = 9.0 nM 8.05