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Assay Detail

CHEMBL877465

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Binding
Inhibitory concentration against Dipeptidylpeptidase IV
27
Total Activities
27
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

Substituted piperazines as novel dipeptidyl peptidase IV inhibitors.
Brockunier LL, He J, Colwell LF, Habulihaz B, He H, Leiting B, Lyons KA, Marsilio F, Patel RA, Teffera Y, Wu JK, Thornberry NA, Weber AE, Parmee ER.
Bioorg Med Chem Lett (2004) 14 : 4763 -4766
PubMed 15324904 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.37 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183207 1 7.85
CHEMBL184636 1 7.72
CHEMBL360425 1 7.52
CHEMBL187293 1 7.47
CHEMBL263946 1 7.36
CHEMBL369738 1 7.29
CHEMBL186610 1 6.97
CHEMBL185067 1 6.94
CHEMBL184040 1 6.87
CHEMBL175872 1 6.86
CHEMBL185482 1 6.84
CHEMBL184808 1 6.81
CHEMBL184902 1 6.78
CHEMBL184071 1 6.65
CHEMBL184380 1 6.39
CHEMBL182861 1 6.21
CHEMBL364385 1 6.16
CHEMBL360488 1 6.04
CHEMBL186611 1 5.98
CHEMBL360167 1 5.96
CHEMBL264551 1 5.80
CHEMBL184262 1 5.52
CHEMBL184624 1 5.43
CHEMBL186032 1 4.96
CHEMBL362538 1 4.72
CHEMBL365414 1 4.46
CHEMBL184672 1 4.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183207 IC50 = 14.0 nM 7.85
CHEMBL184636 IC50 = 19.0 nM 7.72
CHEMBL360425 IC50 = 30.0 nM 7.52
CHEMBL187293 IC50 = 34.0 nM 7.47
CHEMBL263946 IC50 = 44.0 nM 7.36
CHEMBL369738 IC50 = 51.0 nM 7.29
CHEMBL186610 IC50 = 108.0 nM 6.97
CHEMBL185067 IC50 = 114.0 nM 6.94
CHEMBL184040 IC50 = 134.0 nM 6.87
CHEMBL175872 IC50 = 139.0 nM 6.86
CHEMBL185482 IC50 = 143.0 nM 6.84
CHEMBL184808 IC50 = 155.0 nM 6.81
CHEMBL184902 IC50 = 166.0 nM 6.78
CHEMBL184071 IC50 = 225.0 nM 6.65
CHEMBL184380 IC50 = 405.0 nM 6.39
CHEMBL182861 IC50 = 610.0 nM 6.21
CHEMBL364385 IC50 = 690.0 nM 6.16
CHEMBL360488 IC50 = 922.0 nM 6.04
CHEMBL186611 IC50 = 1040.0 nM 5.98
CHEMBL360167 IC50 = 1100.0 nM 5.96
CHEMBL264551 IC50 = 1600.0 nM 5.80
CHEMBL184262 IC50 = 3000.0 nM 5.52
CHEMBL184624 IC50 = 3700.0 nM 5.43
CHEMBL186032 IC50 = 11000.0 nM 4.96
CHEMBL362538 IC50 = 19000.0 nM 4.72
CHEMBL365414 IC50 = 35000.0 nM 4.46
CHEMBL184672 IC50 = 36000.0 nM 4.44