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Assay Detail

CHEMBL1816904

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

Binding
Inhibition of human seminal plasma DPP2 assessed as pNA release from Lys-Ala-p-nitroanilide substrate pre-incubated with enzyme for 15 min prior to substrate addition by fluorescence technique
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal?
Van Goethem S, Matheeussen V, Joossens J, Lambeir AM, Chen X, De Meester I, Haemers A, Augustyns K, Van der Veken P.
J Med Chem (2011) 54 : 5737 -5746
PubMed 21711053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 5.62 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1814759 1 7.48
CHEMBL1814757 1 6.77
CHEMBL3216065 1 6.54
CHEMBL1814758 1 6.19
CHEMBL1814751 1 5.72
CHEMBL1814755 1 5.68
CHEMBL1814745 1 5.48
CHEMBL1814760 1 5.44
CHEMBL1814737 1 4.85
CHEMBL1814632 1 4.82
CHEMBL1814752 1 4.76
CHEMBL1814634 1 4.71
CHEMBL1814754 1 4.64
CHEMBL1814633 1 -
CHEMBL1814738 1 -
CHEMBL1814739 1 -
CHEMBL1814740 1 -
CHEMBL1814741 1 -
CHEMBL3216066 1 -
CHEMBL1814743 1 -
CHEMBL1814744 1 -
CHEMBL3215830 1 -
CHEMBL1814747 1 -
CHEMBL1814748 1 -
CHEMBL1814749 1 -
CHEMBL3216276 1 -
CHEMBL1814753 1 -
CHEMBL1811949 1 -
CHEMBL1814756 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1814759 IC50 = 33.0 nM 7.48
CHEMBL1814757 IC50 = 170.0 nM 6.77
CHEMBL3216065 IC50 = 290.0 nM 6.54
CHEMBL1814758 IC50 = 650.0 nM 6.19
CHEMBL1814751 IC50 = 1900.0 nM 5.72
CHEMBL1814755 IC50 = 2100.0 nM 5.68
CHEMBL1814745 IC50 = 3300.0 nM 5.48
CHEMBL1814760 IC50 = 3600.0 nM 5.44
CHEMBL1814737 IC50 = 14000.0 nM 4.85
CHEMBL1814632 IC50 = 15200.0 nM 4.82
CHEMBL1814752 IC50 = 17300.0 nM 4.76
CHEMBL1814634 IC50 = 19300.0 nM 4.71
CHEMBL1814754 IC50 = 23000.0 nM 4.64
CHEMBL1814633 IC50 > 50000.0 nM -
CHEMBL1814738 IC50 > 100000.0 nM -
CHEMBL1814739 IC50 > 50000.0 nM -
CHEMBL1814740 IC50 > 25000.0 nM -
CHEMBL1814741 IC50 > 50000.0 nM -
CHEMBL3216066 IC50 > 50000.0 nM -
CHEMBL1814743 IC50 > 25000.0 nM -
CHEMBL1814744 IC50 > 100000.0 nM -
CHEMBL3215830 IC50 > 25000.0 nM -
CHEMBL1814747 IC50 > 25000.0 nM -
CHEMBL1814748 IC50 > 50000.0 nM -
CHEMBL1814749 IC50 > 25000.0 nM -
CHEMBL3216276 IC50 > 50000.0 nM -
CHEMBL1814753 IC50 > 25000.0 nM -
CHEMBL1811949 IC50 > 25000.0 nM -
CHEMBL1814756 IC50 > 100000.0 nM -