Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3862758

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

Binding
Binding affinity to DPP4 (unknown origin) assessed as dissociation constant by SPR assay
4
Total Activities
4
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 and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes.
Li S, Xu H, Cui S, Wu F, Zhang Y, Su M, Gong Y, Qiu S, Jiao Q, Qin C, Shan J, Zhang M, Wang J, Yin Q, Xu M, Liu X, Wang R, Zhu L, Li J, Xu Y, Jiang H, Zhao Z, Li J, Li H.
J Med Chem (2016) 59 : 6772 -6790
PubMed 27396490 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 8.26 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3941804 1 8.62
CHEMBL2105762 OMARIGLIPTIN 4.0 1 8.56
CHEMBL3944427 1 7.96
CHEMBL1422 SITAGLIPTIN 4.0 1 7.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3941804 Kd = 2.38 nM 8.62
CHEMBL2105762 OMARIGLIPTIN Kd = 2.75 nM 8.56
CHEMBL3944427 Kd = 11.0 nM 7.96
CHEMBL1422 SITAGLIPTIN Kd = 12.7 nM 7.90