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Assay Detail

CHEMBL2066845

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

Binding
Inhibition of human DPP9 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dipeptidyl peptidase 9 (CHEMBL4793)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-Substituted boro-proline dipeptides: synthesis, characterization, and dipeptidyl peptidase IV, 8, and 9 activities.
Wu W, Liu Y, Milo LJ, Shu Y, Zhao P, Li Y, Woznica I, Yu G, Sanford DG, Zhou Y, Poplawski SE, Connolly BA, Sudmeier JL, Bachovchin WW, Lai JH.
Bioorg Med Chem Lett (2012) 22 : 5536 -5540
PubMed 22853995 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.42 9.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2063040 1 9.51
CHEMBL2063033 1 8.68
CHEMBL63860 1 8.55
CHEMBL2063024 1 8.46
CHEMBL2063031 1 8.19
CHEMBL2063035 1 8.03
CHEMBL2063037 1 8.02
CHEMBL2063026 1 7.96
CHEMBL2063032 1 7.85
CHEMBL2063029 1 7.46
CHEMBL2063039 1 7.40
CHEMBL2063030 1 7.07
CHEMBL2063034 1 7.01
CHEMBL2063025 1 6.90
CHEMBL2063027 1 6.75
CHEMBL2063036 1 6.70
CHEMBL2063038 1 6.62
CHEMBL2063028 1 5.16
CHEMBL393336 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2063040 IC50 = 0.31 nM 9.51
CHEMBL2063033 IC50 = 2.1 nM 8.68
CHEMBL63860 IC50 = 2.8 nM 8.55
CHEMBL2063024 IC50 = 3.5 nM 8.46
CHEMBL2063031 IC50 = 6.4 nM 8.19
CHEMBL2063035 IC50 = 9.3 nM 8.03
CHEMBL2063037 IC50 = 9.5 nM 8.02
CHEMBL2063026 IC50 = 11.0 nM 7.96
CHEMBL2063032 IC50 = 14.0 nM 7.85
CHEMBL2063029 IC50 = 35.0 nM 7.46
CHEMBL2063039 IC50 = 40.0 nM 7.40
CHEMBL2063030 IC50 = 86.0 nM 7.07
CHEMBL2063034 IC50 = 98.0 nM 7.01
CHEMBL2063025 IC50 = 125.0 nM 6.90
CHEMBL2063027 IC50 = 180.0 nM 6.75
CHEMBL2063036 IC50 = 200.0 nM 6.70
CHEMBL2063038 IC50 = 240.0 nM 6.62
CHEMBL2063028 IC50 = 6900.0 nM 5.16
CHEMBL393336 IC50 = 20000.0 nM 4.70