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Assay Detail

CHEMBL938687

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Binding
Inhibition of DPP2
63
Total Activities
62
Compounds Tested
2
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

Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads.
Van der Veken P, De Meester I, Dubois V, Soroka A, Van Goethem S, Maes MB, Brandt I, Lambeir AM, Chen X, Haemers A, Scharpé S, Augustyns K.
Bioorg Med Chem Lett (2008) 18 : 4154 -4158
PubMed 18556199 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 62 5.29 7.60
Ki 1 10.09 10.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98869 2 10.09
CHEMBL518144 1 7.60
CHEMBL472128 1 7.47
CHEMBL481466 1 7.17
CHEMBL510594 1 7.07
CHEMBL471731 1 6.51
CHEMBL471747 1 6.46
CHEMBL461912 1 6.24
CHEMBL471544 1 6.08
CHEMBL461290 1 6.07
CHEMBL461092 1 5.99
CHEMBL501521 1 5.92
CHEMBL461913 1 5.82
CHEMBL461506 1 5.80
CHEMBL488226 1 5.75
CHEMBL488227 1 5.60
CHEMBL455298 1 5.54
CHEMBL461289 1 5.51
CHEMBL460065 1 5.43
CHEMBL456298 1 5.31
CHEMBL459642 1 5.24
CHEMBL459643 1 5.01
CHEMBL501126 1 5.00
CHEMBL511346 1 4.80
CHEMBL459159 1 4.72
CHEMBL471547 1 4.62
CHEMBL98408 1 4.55
CHEMBL397070 1 4.54
CHEMBL460887 1 4.52
CHEMBL471546 1 4.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98869 Ki = 0.082 nM 10.09
CHEMBL518144 IC50 = 25.0 nM 7.60
CHEMBL472128 IC50 = 34.0 nM 7.47
CHEMBL481466 IC50 = 68.0 nM 7.17
CHEMBL510594 IC50 = 86.0 nM 7.07
CHEMBL471731 IC50 = 310.0 nM 6.51
CHEMBL471747 IC50 = 350.0 nM 6.46
CHEMBL461912 IC50 = 577.0 nM 6.24
CHEMBL471544 IC50 = 840.0 nM 6.08
CHEMBL461290 IC50 = 860.0 nM 6.07
CHEMBL461092 IC50 = 1020.0 nM 5.99
CHEMBL501521 IC50 = 1200.0 nM 5.92
CHEMBL461913 IC50 = 1500.0 nM 5.82
CHEMBL461506 IC50 = 1600.0 nM 5.80
CHEMBL488226 IC50 = 1780.0 nM 5.75
CHEMBL488227 IC50 = 2500.0 nM 5.60
CHEMBL455298 IC50 = 2900.0 nM 5.54
CHEMBL461289 IC50 = 3100.0 nM 5.51
CHEMBL460065 IC50 = 3700.0 nM 5.43
CHEMBL456298 IC50 = 4900.0 nM 5.31
CHEMBL459642 IC50 = 5700.0 nM 5.24
CHEMBL459643 IC50 = 9800.0 nM 5.01
CHEMBL501126 IC50 = 9900.0 nM 5.00
CHEMBL511346 IC50 = 15700.0 nM 4.80
CHEMBL459159 IC50 = 19000.0 nM 4.72
CHEMBL471547 IC50 = 24000.0 nM 4.62
CHEMBL98408 IC50 = 28000.0 nM 4.55
CHEMBL397070 IC50 = 29000.0 nM 4.54
CHEMBL460887 IC50 = 30000.0 nM 4.52
CHEMBL471546 IC50 = 38000.0 nM 4.42
CHEMBL98008 IC50 = 42000.0 nM 4.38
CHEMBL469890 IC50 = 43000.0 nM 4.37
CHEMBL460885 IC50 = 43000.0 nM 4.37
CHEMBL461911 IC50 = 48000.0 nM 4.32
CHEMBL452029 IC50 = 49000.0 nM 4.31
CHEMBL452470 IC50 = 52000.0 nM 4.28
CHEMBL83418 IC50 = 59000.0 nM 4.23
CHEMBL442952 IC50 = 60000.0 nM 4.22
CHEMBL459641 IC50 = 65000.0 nM 4.19
CHEMBL453918 IC50 = 79000.0 nM 4.10
CHEMBL511659 IC50 = 90000.0 nM 4.05
CHEMBL1422 SITAGLIPTIN IC50 > 100000.0 nM -
CHEMBL142703 VILDAGLIPTIN IC50 > 1000000.0 nM -
CHEMBL98869 IC50 < 0.5 nM -
CHEMBL443622 IC50 = 179000.0 nM -
CHEMBL403882 IC50 > 500000.0 nM -
CHEMBL503274 IC50 = 110000.0 nM -
CHEMBL453573 IC50 = 145000.0 nM -
CHEMBL97025 IC50 > 1000000.0 nM -
CHEMBL383705 IC50 = 153000.0 nM -