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Assay Detail

CHEMBL923807

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

Binding
Inhibition of QPP
17
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dipeptidyl peptidase 2 (CHEMBL3976)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors.
Kowalchick JE, Leiting B, Pryor KD, Marsilio F, Wu JK, He H, Lyons KA, Eiermann GJ, Petrov A, Scapin G, Patel RA, Thornberry NA, Weber AE, Kim D.
Bioorg Med Chem Lett (2007) 17 : 5934 -5939
PubMed 17827003 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 4.73 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL401057 1 5.40
CHEMBL249945 2 5.39
CHEMBL400752 1 5.13
CHEMBL250351 1 5.02
CHEMBL250999 1 4.82
CHEMBL404210 1 4.75
CHEMBL400068 1 4.66
CHEMBL250787 1 4.60
CHEMBL250147 1 4.58
CHEMBL400722 1 4.48
CHEMBL250353 1 4.31
CHEMBL399499 1 4.27
CHEMBL401304 1 4.22
CHEMBL251376 1 4.14
CHEMBL248936 1 -
CHEMBL248743 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL401057 IC50 = 4000.0 nM 5.40
CHEMBL249945 IC50 = 4100.0 nM 5.39
CHEMBL249945 IC50 = 5767.0 nM 5.24
CHEMBL400752 IC50 = 7400.0 nM 5.13
CHEMBL250351 IC50 = 9600.0 nM 5.02
CHEMBL250999 IC50 = 15000.0 nM 4.82
CHEMBL404210 IC50 = 18000.0 nM 4.75
CHEMBL400068 IC50 = 22000.0 nM 4.66
CHEMBL250787 IC50 = 25000.0 nM 4.60
CHEMBL250147 IC50 = 26000.0 nM 4.58
CHEMBL400722 IC50 = 33000.0 nM 4.48
CHEMBL250353 IC50 = 49000.0 nM 4.31
CHEMBL399499 IC50 = 54000.0 nM 4.27
CHEMBL401304 IC50 = 60000.0 nM 4.22
CHEMBL251376 IC50 = 72000.0 nM 4.14
CHEMBL248743 IC50 > 100000.0 nM -
CHEMBL248936 IC50 > 100000.0 nM -