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Assay Detail

CHEMBL666613

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Binding
Inhibitory activity of compound against Dipeptidylpeptidase II (DPP II)
ChEMBL ↗
63
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases.
Senten K, Van der Veken P, De Meester I, Lambeir AM, Scharpé S, Haemers A, Augustyns K.
J Med Chem (2003) 46 : 5005 -5014
PubMed 14584950 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 63 5.30 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL147923 — — 3 6.89
CHEMBL356207 — — 1 6.85
CHEMBL356055 — — 1 6.70
CHEMBL148461 — — 1 6.66
CHEMBL97180 — — 1 6.48
CHEMBL329171 — — 1 6.35
CHEMBL146509 — — 1 6.31
CHEMBL343616 — — 1 6.29
CHEMBL145862 — — 1 6.20
CHEMBL148954 — — 1 6.12
CHEMBL461912 — — 1 6.00
CHEMBL317944 — — 1 5.92
CHEMBL145813 — — 1 5.82
CHEMBL461506 — — 2 5.80
CHEMBL147583 — — 1 5.74
CHEMBL148955 — — 2 5.52
CHEMBL344507 — — 1 5.42
CHEMBL144226 — — 1 5.31
CHEMBL148025 — — 1 5.00
CHEMBL328694 — — 1 5.00
CHEMBL359211 — — 1 4.96
CHEMBL357606 — — 1 4.55
CHEMBL148392 — — 1 4.53
CHEMBL147314 — — 1 4.49
CHEMBL278393 — — 1 4.38
CHEMBL358358 — — 1 4.37
CHEMBL144027 — — 1 4.32
CHEMBL149498 — — 1 4.29
CHEMBL444537 — — 1 4.28
CHEMBL146190 — — 1 4.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL147923 — IC50 = 130.0 nM 6.89
CHEMBL356207 — IC50 = 140.0 nM 6.85
CHEMBL356055 — IC50 = 200.0 nM 6.70
CHEMBL148461 — IC50 = 220.0 nM 6.66
CHEMBL97180 — IC50 = 330.0 nM 6.48
CHEMBL329171 — IC50 = 450.0 nM 6.35
CHEMBL146509 — IC50 = 490.0 nM 6.31
CHEMBL343616 — IC50 = 510.0 nM 6.29
CHEMBL145862 — IC50 = 630.0 nM 6.20
CHEMBL148954 — IC50 = 750.0 nM 6.12
CHEMBL461912 — IC50 = 1000.0 nM 6.00
CHEMBL147923 — IC50 = 1150.0 nM 5.94
CHEMBL317944 — IC50 = 1200.0 nM 5.92
CHEMBL145813 — IC50 = 1500.0 nM 5.82
CHEMBL461506 — IC50 = 1600.0 nM 5.80
CHEMBL147583 — IC50 = 1840.0 nM 5.74
CHEMBL461506 — IC50 = 2100.0 nM 5.68
CHEMBL148955 — IC50 = 3000.0 nM 5.52
CHEMBL148955 — IC50 = 3000.0 nM 5.52
CHEMBL344507 — IC50 = 3800.0 nM 5.42
CHEMBL144226 — IC50 = 4900.0 nM 5.31
CHEMBL328694 — IC50 = 9900.0 nM 5.00
CHEMBL148025 — IC50 = 9900.0 nM 5.00
CHEMBL359211 — IC50 = 10900.0 nM 4.96
CHEMBL357606 — IC50 = 28000.0 nM 4.55
CHEMBL148392 — IC50 = 29300.0 nM 4.53
CHEMBL147314 — IC50 = 32400.0 nM 4.49
CHEMBL278393 — IC50 = 42000.0 nM 4.38
CHEMBL358358 — IC50 = 43000.0 nM 4.37
CHEMBL144027 — IC50 = 48000.0 nM 4.32
CHEMBL149498 — IC50 = 51900.0 nM 4.29
CHEMBL444537 — IC50 = 52000.0 nM 4.28
CHEMBL146190 — IC50 = 57100.0 nM 4.24
CHEMBL93507 — IC50 = 59000.0 nM 4.23
CHEMBL146995 — IC50 = 62000.0 nM 4.21
CHEMBL97064 — IC50 = 65000.0 nM 4.19
CHEMBL145855 — IC50 = 78100.0 nM 4.11
CHEMBL93931 — IC50 = 79000.0 nM 4.10
CHEMBL148285 — IC50 = 88700.0 nM 4.05
CHEMBL147691 — IC50 = 299000.0 nM -
CHEMBL348246 — IC50 = 159000.0 nM -
CHEMBL148569 — IC50 = 288000.0 nM -
CHEMBL146450 — IC50 = 130000.0 nM -
CHEMBL343907 — IC50 > 500000.0 nM -
CHEMBL328795 — IC50 = 152000.0 nM -
CHEMBL319514 — IC50 = 110000.0 nM -
CHEMBL148261 — IC50 = 111000.0 nM -
CHEMBL443622 — IC50 = 179000.0 nM -
CHEMBL146437 — IC50 > 500000.0 nM -
CHEMBL148142 — IC50 = 500000.0 nM -