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Assay Detail

CHEMBL1663348

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

Binding
Inhibition of DPP4 after 20 mins by fluorescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes.
Deng J, Peng L, Zhang G, Lan X, Li C, Chen F, Zhou Y, Lin Z, Chen L, Dai R, Xu H, Yang L, Zhang X, Hu W.
Eur J Med Chem (2011) 46 : 71 -76
PubMed 21106276 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.62 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1651766 1 9.48
CHEMBL1651763 1 9.06
CHEMBL1651764 1 8.88
CHEMBL1651767 1 8.76
CHEMBL376359 ALOGLIPTIN 4.0 1 8.47
CHEMBL1651765 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1651766 IC50 = 0.33 nM 9.48
CHEMBL1651763 IC50 = 0.87 nM 9.06
CHEMBL1651764 IC50 = 1.32 nM 8.88
CHEMBL1651767 IC50 = 1.72 nM 8.76
CHEMBL376359 ALOGLIPTIN IC50 = 3.4 nM 8.47
CHEMBL1651765 IC50 = 88.82 nM 7.05