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Assay Detail

CHEMBL4021437

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Binding
Inhibition of DPP8 (unknown origin)
5
Total Activities
5
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 8 (CHEMBL4657)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome.
Sattigeri JA, Sethi S, Davis JA, Ahmed S, Rayasam GV, Jadhav BG, Chilla SM, Datta D, Gadhave A, Tulasi VK, Jain T, Voleti S, Benjamin B, Udupa S, Jain G, Singh Y, Srinivas K, Bansal VS, Ray A, Bhatnagar PK, Cliffe IA.
Bioorg Med Chem Lett (2017) 27 : 2313 -2318
PubMed 28442252 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.32 4.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4067185 1 4.57
CHEMBL4078112 1 4.24
CHEMBL4086264 1 4.16
CHEMBL1422 SITAGLIPTIN 4.0 1 -
CHEMBL4090635 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4067185 IC50 = 27000.0 nM 4.57
CHEMBL4078112 IC50 = 57000.0 nM 4.24
CHEMBL4086264 IC50 = 69000.0 nM 4.16
CHEMBL1422 SITAGLIPTIN IC50 > 100000.0 nM -
CHEMBL4090635 IC50 > 100000.0 nM -