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Assay Detail

CHEMBL4432067

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Binding
Inhibition of human recombinant DPP4 (39 to 766 residues) using Ala-Pro-AFC as substrate incubated for 1 hr by fluorescence assay
7
Total Activities
7
Compounds Tested
2
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
IC50 6 7.50 9.00
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL237500 LINAGLIPTIN 4.0 1 9.00
CHEMBL237067 1 8.30
CHEMBL376359 ALOGLIPTIN 4.0 1 8.15
CHEMBL399216 1 7.09
CHEMBL142703 VILDAGLIPTIN 4.0 1 7.02
CHEMBL4456228 1 5.41
CHEMBL2147777 TENELIGLIPTIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL237500 LINAGLIPTIN IC50 = 1.0 nM 9.00
CHEMBL237067 IC50 = 5.0 nM 8.30
CHEMBL376359 ALOGLIPTIN IC50 = 7.0 nM 8.15
CHEMBL399216 IC50 = 82.0 nM 7.09
CHEMBL142703 VILDAGLIPTIN IC50 = 95.0 nM 7.02
CHEMBL4456228 IC50 = 3900.0 nM 5.41
CHEMBL2147777 TENELIGLIPTIN Inhibition - % -