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Assay Detail

CHEMBL2149805

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

Binding
Inhibition of human DPP9 using GLY-Pro-MCA as substrate after 30 mins by cell-based fluorescence assay
5
Total Activities
5
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 9 (CHEMBL4793)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Yoshida T, Akahoshi F, Sakashita H, Kitajima H, Nakamura M, Sonda S, Takeuchi M, Tanaka Y, Ueda N, Sekiguchi S, Ishige T, Shima K, Nabeno M, Abe Y, Anabuki J, Soejima A, Yoshida K, Takashina Y, Ishii S, Kiuchi S, Fukuda S, Tsutsumiuchi R, Kosaka K, Murozono T, Nakamaru Y, Utsumi H, Masutomi N, Kishida H, Miyaguchi I, Hayashi Y.
Bioorg Med Chem (2012) 20 : 5705 -5719
PubMed 22959556 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.69 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL391466 1 7.52
CHEMBL241253 1 6.96
CHEMBL2147712 1 6.48
CHEMBL2147777 TENELIGLIPTIN 4.0 1 6.27
CHEMBL2147771 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL391466 IC50 = 30.0 nM 7.52
CHEMBL241253 IC50 = 110.0 nM 6.96
CHEMBL2147712 IC50 = 330.0 nM 6.48
CHEMBL2147777 TENELIGLIPTIN IC50 = 540.0 nM 6.27
CHEMBL2147771 IC50 = 610.0 nM 6.21