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Assay Detail

CHEMBL5247212

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

Binding
Inhibition of human DPP-4 expressed in human Caco-2 cells using H-Gly-Pro-AMC as substrate measured for 30 mins by microplate reader analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Caco-2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dipeptidyl peptidase 4 (CHEMBL284)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A review upon medicinal perspective and designing rationale of DPP-4 inhibitors.
Kumar S, Mittal A, Mittal A.
Bioorg Med Chem (2021) 46 : 116354 -116354
PubMed 34428715 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 9.05 9.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5274129 1 9.06
CHEMBL5276657 1 9.06
CHEMBL5265910 1 9.06
CHEMBL5269746 1 9.06
CHEMBL5277828 1 9.06
CHEMBL5269884 1 9.06
CHEMBL5273793 1 9.06
CHEMBL5276298 1 9.06
CHEMBL5289339 1 9.06
CHEMBL5279474 1 9.06
CHEMBL1422 SITAGLIPTIN 4.0 1 9.06
CHEMBL5272644 1 8.97
CHEMBL5275046 1 8.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5274129 IC50 = 0.87 nM 9.06
CHEMBL5276657 IC50 = 0.87 nM 9.06
CHEMBL5265910 IC50 = 0.87 nM 9.06
CHEMBL5269746 IC50 = 0.87 nM 9.06
CHEMBL5277828 IC50 = 0.87 nM 9.06
CHEMBL5269884 IC50 = 0.87 nM 9.06
CHEMBL5273793 IC50 = 0.87 nM 9.06
CHEMBL5276298 IC50 = 0.87 nM 9.06
CHEMBL5289339 IC50 = 0.87 nM 9.06
CHEMBL5279474 IC50 = 0.87 nM 9.06
CHEMBL1422 SITAGLIPTIN IC50 = 0.87 nM 9.06
CHEMBL5272644 IC50 = 1.06 nM 8.97
CHEMBL5275046 IC50 = 1.1 nM 8.96