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Assay Detail

CHEMBL1816907

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

Binding
Inhibition of bovine testes DPP9 assessed as pNA release from Ala-Pro- 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 Bos taurus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 6.02 7.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1814739 1 7.59
CHEMBL1814740 1 7.57
CHEMBL1814741 1 7.30
CHEMBL1814753 1 7.19
CHEMBL1814633 1 7.08
CHEMBL3216066 1 6.65
CHEMBL1814747 1 6.62
CHEMBL1814745 1 6.58
CHEMBL1814748 1 6.58
CHEMBL1814743 1 6.28
CHEMBL1814749 1 6.27
CHEMBL1811949 1 6.27
CHEMBL1814751 1 6.20
CHEMBL1814752 1 6.17
CHEMBL3215830 1 5.95
CHEMBL1814756 1 5.85
CHEMBL1814755 1 5.77
CHEMBL1814760 1 5.68
CHEMBL3216276 1 5.58
CHEMBL1814634 1 5.40
CHEMBL1814737 1 5.30
CHEMBL1814759 1 4.79
CHEMBL1814754 1 4.65
CHEMBL1814757 1 4.54
CHEMBL1814758 1 4.46
CHEMBL1814744 1 4.27
CHEMBL1814738 1 -
CHEMBL1814632 1 -
CHEMBL3216065 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1814739 IC50 = 25.4 nM 7.59
CHEMBL1814740 IC50 = 26.9 nM 7.57
CHEMBL1814741 IC50 = 50.0 nM 7.30
CHEMBL1814753 IC50 = 65.0 nM 7.19
CHEMBL1814633 IC50 = 84.0 nM 7.08
CHEMBL3216066 IC50 = 224.0 nM 6.65
CHEMBL1814747 IC50 = 240.0 nM 6.62
CHEMBL1814745 IC50 = 260.0 nM 6.58
CHEMBL1814748 IC50 = 260.0 nM 6.58
CHEMBL1814743 IC50 = 530.0 nM 6.28
CHEMBL1814749 IC50 = 540.0 nM 6.27
CHEMBL1811949 IC50 = 540.0 nM 6.27
CHEMBL1814751 IC50 = 630.0 nM 6.20
CHEMBL1814752 IC50 = 680.0 nM 6.17
CHEMBL3215830 IC50 = 1130.0 nM 5.95
CHEMBL1814756 IC50 = 1400.0 nM 5.85
CHEMBL1814755 IC50 = 1700.0 nM 5.77
CHEMBL1814760 IC50 = 2100.0 nM 5.68
CHEMBL3216276 IC50 = 2600.0 nM 5.58
CHEMBL1814634 IC50 = 4000.0 nM 5.40
CHEMBL1814737 IC50 = 5000.0 nM 5.30
CHEMBL1814759 IC50 = 16400.0 nM 4.79
CHEMBL1814754 IC50 = 22600.0 nM 4.65
CHEMBL1814757 IC50 = 29100.0 nM 4.54
CHEMBL1814758 IC50 = 35000.0 nM 4.46
CHEMBL1814744 IC50 = 54000.0 nM 4.27
CHEMBL1814738 IC50 > 10000.0 nM -
CHEMBL1814632 IC50 > 10000.0 nM -
CHEMBL3216065 IC50 > 50000.0 nM -