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Assay Detail

CHEMBL1120109

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

Binding
Inhibition of DPP4
11
Total Activities
11
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

Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.
Cho TP, Long YF, Gang LZ, Yang W, Jun LH, Yuan SG, Hong FJ, Lin W, Liang GD, Lei Z, Jing LJ, Shen GA, Hong SG, Dan W, Ying F, Ke YP, Ying L, Jun F, Tai MX.
Bioorg Med Chem Lett (2010) 20 : 3565 -3568
PubMed 20488702 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.57 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL142703 VILDAGLIPTIN 4.0 1 8.05
CHEMBL1085269 1 8.05
CHEMBL1083287 1 7.89
CHEMBL1083588 1 7.89
CHEMBL1083032 1 7.85
CHEMBL1083031 1 7.62
CHEMBL1082707 1 7.41
CHEMBL1082716 1 7.30
CHEMBL1082708 1 7.16
CHEMBL1086466 1 7.08
CHEMBL1085522 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL142703 VILDAGLIPTIN IC50 = 9.0 nM 8.05
CHEMBL1085269 IC50 = 9.0 nM 8.05
CHEMBL1083287 IC50 = 13.0 nM 7.89
CHEMBL1083588 IC50 = 13.0 nM 7.89
CHEMBL1083032 IC50 = 14.0 nM 7.85
CHEMBL1083031 IC50 = 24.0 nM 7.62
CHEMBL1082707 IC50 = 39.0 nM 7.41
CHEMBL1082716 IC50 = 50.0 nM 7.30
CHEMBL1082708 IC50 = 69.0 nM 7.16
CHEMBL1086466 IC50 = 83.0 nM 7.08
CHEMBL1085522 IC50 = 120.0 nM 6.92