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Assay Detail

CHEMBL4132759

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Binding
Inhibition of human DPP4
8
Total Activities
8
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

Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling.
Rea D, Van Elzen R, De Winter H, Van Goethem S, Landuyt B, Luyten W, Schoofs L, Van Der Veken P, Augustyns K, De Meester I, Fülöp V, Lambeir AM.
Eur J Med Chem (2017) 139 : 482 -491
PubMed 28826083 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.54 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL237500 LINAGLIPTIN 4.0 1 8.70
CHEMBL4176189 1 7.66
CHEMBL1422 SITAGLIPTIN 4.0 1 7.40
CHEMBL142703 VILDAGLIPTIN 4.0 1 6.92
CHEMBL98408 1 5.77
CHEMBL383705 1 5.27
CHEMBL397070 1 4.05
CHEMBL98869 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL237500 LINAGLIPTIN IC50 = 2.0 nM 8.70
CHEMBL4176189 IC50 = 22.0 nM 7.66
CHEMBL1422 SITAGLIPTIN IC50 = 40.0 nM 7.40
CHEMBL142703 VILDAGLIPTIN IC50 = 120.0 nM 6.92
CHEMBL98408 IC50 = 1700.0 nM 5.77
CHEMBL383705 IC50 = 5400.0 nM 5.27
CHEMBL397070 IC50 = 90000.0 nM 4.05
CHEMBL98869 IC50 = 165000.0 nM -