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Assay Detail

CHEMBL664534

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

Binding
Inhibitory activity against Dipeptidylpeptidase IV (DPP IV)
64
Total Activities
60
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 4 (CHEMBL284)
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 64 4.85 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL319514 1 6.70
CHEMBL461912 1 6.50
CHEMBL357606 1 5.77
CHEMBL148261 1 5.46
CHEMBL503274 1 5.40
CHEMBL383705 1 5.40
CHEMBL317126 1 4.85
CHEMBL403882 1 4.82
CHEMBL278393 1 4.77
CHEMBL145862 1 4.74
CHEMBL93931 1 4.68
CHEMBL317944 1 4.64
CHEMBL328694 1 4.41
CHEMBL443622 1 4.39
CHEMBL346877 1 4.30
CHEMBL145813 1 4.29
CHEMBL444537 1 4.28
CHEMBL93507 1 4.17
CHEMBL146995 1 4.17
CHEMBL148954 1 4.09
CHEMBL147691 1 4.03
CHEMBL148955 2 -
CHEMBL148002 1 -
CHEMBL344507 1 -
CHEMBL97025 1 -
CHEMBL343650 1 -
CHEMBL328795 1 -
CHEMBL343907 1 -
CHEMBL148569 1 -
CHEMBL148285 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL319514 IC50 = 200.0 nM 6.70
CHEMBL461912 IC50 = 320.0 nM 6.50
CHEMBL357606 IC50 = 1700.0 nM 5.77
CHEMBL148261 IC50 = 3500.0 nM 5.46
CHEMBL503274 IC50 = 4000.0 nM 5.40
CHEMBL383705 IC50 = 4000.0 nM 5.40
CHEMBL317126 IC50 = 14000.0 nM 4.85
CHEMBL403882 IC50 = 15000.0 nM 4.82
CHEMBL278393 IC50 = 17000.0 nM 4.77
CHEMBL145862 IC50 = 18100.0 nM 4.74
CHEMBL93931 IC50 = 21000.0 nM 4.68
CHEMBL317944 IC50 = 23100.0 nM 4.64
CHEMBL328694 IC50 = 39000.0 nM 4.41
CHEMBL443622 IC50 = 41000.0 nM 4.39
CHEMBL346877 IC50 = 50400.0 nM 4.30
CHEMBL145813 IC50 = 51000.0 nM 4.29
CHEMBL444537 IC50 = 52000.0 nM 4.28
CHEMBL93507 IC50 = 67000.0 nM 4.17
CHEMBL146995 IC50 = 67000.0 nM 4.17
CHEMBL148954 IC50 = 81000.0 nM 4.09
CHEMBL147691 IC50 = 93000.0 nM 4.03
CHEMBL145855 IC50 > 1000000.0 nM -
CHEMBL147314 IC50 = 250000.0 nM -
CHEMBL147923 IC50 > 1000000.0 nM -
CHEMBL148461 IC50 > 1000000.0 nM -
CHEMBL461506 IC50 = 134900.0 nM -
CHEMBL146450 IC50 >> 1000000.0 nM -
CHEMBL147583 IC50 > 1000000.0 nM -
CHEMBL147923 IC50 > 1000000.0 nM -
CHEMBL148955 IC50 = 318000.0 nM -
CHEMBL434886 IC50 = 167000.0 nM -
CHEMBL146509 IC50 > 1000000.0 nM -
CHEMBL148026 IC50 > 500000.0 nM -
CHEMBL499101 IC50 = 122000.0 nM -
CHEMBL359211 IC50 > 500000.0 nM -
CHEMBL149498 IC50 > 1000000.0 nM -
CHEMBL461506 IC50 = 247000.0 nM -
CHEMBL97064 IC50 = 190000.0 nM -
CHEMBL329171 IC50 > 500000.0 nM -
CHEMBL148002 IC50 = 360000.0 nM -
CHEMBL348246 IC50 = 500000.0 nM -
CHEMBL148285 IC50 = 250000.0 nM -
CHEMBL148569 IC50 - nM -
CHEMBL343907 IC50 > 500000.0 nM -
CHEMBL328795 IC50 = 188000.0 nM -
CHEMBL343650 IC50 = 377000.0 nM -
CHEMBL97025 IC50 > 1000000.0 nM -
CHEMBL344507 IC50 > 125000.0 nM -
CHEMBL148955 IC50 = 318000.0 nM -
CHEMBL144027 IC50 = 500000.0 nM -