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Assay Detail

CHEMBL4432069

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Binding
Binding affinity to human recombinant DPP4 (39 to 766 residues) by surface plasmon resonance analysis
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 Autocuration

Target

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

Publication

Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure.
Schnapp G, Klein T, Hoevels Y, Bakker RA, Nar H.
J Med Chem (2016) 59 : 7466 -7477
PubMed 27438064 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 8.47 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL385517 SAXAGLIPTIN ANHYDROUS 4.0 1 9.52
CHEMBL2147777 TENELIGLIPTIN 4.0 1 9.39
CHEMBL237067 1 9.38
CHEMBL142703 VILDAGLIPTIN 4.0 1 8.62
CHEMBL376359 ALOGLIPTIN 4.0 1 8.62
CHEMBL1422 SITAGLIPTIN 4.0 1 8.28
CHEMBL399216 1 7.88
CHEMBL4456228 1 6.09
CHEMBL237500 LINAGLIPTIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL385517 SAXAGLIPTIN ANHYDROUS Kd = 0.3 nM 9.52
CHEMBL2147777 TENELIGLIPTIN Kd = 0.41 nM 9.39
CHEMBL237067 Kd = 0.42 nM 9.38
CHEMBL142703 VILDAGLIPTIN Kd = 2.4 nM 8.62
CHEMBL376359 ALOGLIPTIN Kd = 2.4 nM 8.62
CHEMBL1422 SITAGLIPTIN Kd = 5.3 nM 8.28
CHEMBL399216 Kd = 13.2 nM 7.88
CHEMBL4456228 Kd = 806.0 nM 6.09
CHEMBL237500 LINAGLIPTIN Kd = 0.0066 nM -