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Assay Detail

CHEMBL908251

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Binding
Inhibition of DPP-IV
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Dipeptidyl peptidase 4 (CHEMBL284)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of non-covalent dipeptidyl peptidase IV inhibitors which induce a conformational change in the active site.
Sheehan SM, Mest HJ, Watson BM, Klimkowski VJ, Timm DE, Cauvin A, Parsons SH, Shi Q, Canada EJ, Wiley MR, Ruehter G, Evers B, Petersen S, Blaszczak LC, Pulley SR, Margolis BJ, Wishart GN, Renson B, Hankotius D, Mohr M, Zechel JC, Michael Kalbfleisch J, Dingess-Hammond EA, Boelke A, Weichert AG.
Bioorg Med Chem Lett (2007) 17 : 1765 -1768
PubMed 17239592 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.55 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL541664 1 8.30
CHEMBL217017 1 7.41
CHEMBL218289 1 7.08
CHEMBL554090 1 6.96
CHEMBL217388 1 6.55
CHEMBL553006 1 6.47
CHEMBL217801 1 6.09
CHEMBL217532 1 5.42
CHEMBL386895 1 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL541664 IC50 = 5.0 nM 8.30
CHEMBL217017 IC50 = 39.0 nM 7.41
CHEMBL218289 IC50 = 84.0 nM 7.08
CHEMBL554090 IC50 = 110.0 nM 6.96
CHEMBL217388 IC50 = 280.0 nM 6.55
CHEMBL553006 IC50 = 340.0 nM 6.47
CHEMBL217801 IC50 = 820.0 nM 6.09
CHEMBL217532 IC50 = 3800.0 nM 5.42
CHEMBL386895 IC50 = 21000.0 nM 4.68