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Assay Detail

CHEMBL3802985

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

Binding
Inhibition of DPP2 in human seminal plasma using Lys-Ala-p-nitroanilide as substrate preincubated for 15 mins followed by substrate addition measured for 10 mins by spectrofluorimetry
21
Total Activities
21
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

Probing for improved selectivity with dipeptide-derived inhibitors of dipeptidyl peptidases 8 and 9: the impact of P1-variation
Heirbaut L, van Goethem S, Jansen K, de Winter H, Lamoen N, Joossens J, Cheng J, Chen X, Lambeir A, de Meester I, Augustyns K, van der Veken P
Medchemcomm (2016) 7 : 433 -438
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.05 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3797842 1 7.60
CHEMBL3798441 1 5.96
CHEMBL3800380 1 5.03
CHEMBL3798691 1 4.96
CHEMBL3798777 1 4.89
CHEMBL3797398 1 4.83
CHEMBL3797299 1 4.66
CHEMBL3799388 1 4.64
CHEMBL471547 1 4.62
CHEMBL397070 1 4.54
CHEMBL3798277 1 4.51
CHEMBL3797358 1 4.40
CHEMBL3799074 1 -
CHEMBL3797536 1 -
CHEMBL3797355 1 -
CHEMBL3800132 1 -
CHEMBL3800436 1 -
CHEMBL3798975 1 -
CHEMBL3800113 1 -
CHEMBL3797441 1 -
CHEMBL1814633 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3797842 IC50 = 25.0 nM 7.60
CHEMBL3798441 IC50 = 1100.0 nM 5.96
CHEMBL3800380 IC50 = 9400.0 nM 5.03
CHEMBL3798691 IC50 = 10900.0 nM 4.96
CHEMBL3798777 IC50 = 12900.0 nM 4.89
CHEMBL3797398 IC50 = 14800.0 nM 4.83
CHEMBL3797299 IC50 = 22000.0 nM 4.66
CHEMBL3799388 IC50 = 23000.0 nM 4.64
CHEMBL471547 IC50 = 24000.0 nM 4.62
CHEMBL397070 IC50 = 29000.0 nM 4.54
CHEMBL3798277 IC50 = 31000.0 nM 4.51
CHEMBL3797358 IC50 = 40000.0 nM 4.40
CHEMBL3799074 IC50 > 100000.0 nM -
CHEMBL3797536 IC50 > 100000.0 nM -
CHEMBL3797355 IC50 > 100000.0 nM -
CHEMBL3800132 IC50 > 100000.0 nM -
CHEMBL3800436 IC50 > 100000.0 nM -
CHEMBL3798975 IC50 > 100000.0 nM -
CHEMBL3800113 IC50 > 100000.0 nM -
CHEMBL3797441 IC50 > 25000.0 nM -
CHEMBL1814633 IC50 > 50000.0 nM -