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Assay Detail

CHEMBL5112289

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

Binding
Inhibition of human recombinant DPP4 using H-Gly-Pro-AMC as substrate incubated for 30 mins by fluorescence based microplate reader assay
17
Total Activities
17
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

Discovery of a Potent and Highly Selective Dipeptidyl Peptidase IV and Carbonic Anhydrase Inhibitor as "Antidiabesity" Agents Based on Repurposing and Morphing of WB-4101.
Artasensi A, Angeli A, Lammi C, Bollati C, Gervasoni S, Baron G, Matucci R, Supuran CT, Vistoli G, Fumagalli L.
J Med Chem (2022) 65 : 13946 -13966
PubMed 36201615 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.93 8.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1422 SITAGLIPTIN 4.0 1 8.06
CHEMBL5205289 1 7.55
CHEMBL5198237 1 7.48
CHEMBL5177166 1 7.31
CHEMBL5193531 1 4.24
CHEMBL5201114 1 -
CHEMBL5191609 1 -
CHEMBL5193118 1 -
CHEMBL5184240 1 -
CHEMBL5194237 1 -
CHEMBL5203377 1 -
CHEMBL5176469 1 -
CHEMBL5171860 1 -
CHEMBL5206696 1 -
CHEMBL25554 1 -
CHEMBL20 ACETAZOLAMIDE 4.0 1 -
CHEMBL5191973 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1422 SITAGLIPTIN IC50 = 8.8 nM 8.06
CHEMBL5205289 IC50 = 28.3 nM 7.55
CHEMBL5198237 IC50 = 33.2 nM 7.48
CHEMBL5177166 IC50 = 49.0 nM 7.31
CHEMBL5193531 IC50 = 57440.0 nM 4.24
CHEMBL5201114 IC50 > 700000.0 nM -
CHEMBL5191609 IC50 > 700000.0 nM -
CHEMBL5193118 IC50 > 700000.0 nM -
CHEMBL5184240 IC50 > 700000.0 nM -
CHEMBL5194237 IC50 = 300200.0 nM -
CHEMBL5203377 IC50 > 700000.0 nM -
CHEMBL5176469 IC50 = 326600.0 nM -
CHEMBL5171860 IC50 > 700000.0 nM -
CHEMBL5206696 IC50 = 326600.0 nM -
CHEMBL25554 IC50 > 700000.0 nM -
CHEMBL20 ACETAZOLAMIDE IC50 - -
CHEMBL5191973 IC50 = 669300.0 nM -