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Assay Detail

CHEMBL4315807

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of DPP4 in human serum assessed as decrease in p-nitroaniline formation using Gly-Pro-p-nitroanilide as substrate preincubated for 5 mins followed by incubation with substrate for 15 mins by microplate reader analysis
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Serum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Nitrothiadiazolo[3,2-a]pyrimidines as promising antiglycating agents.
Savateev K, Fedotov V, Butorin I, Eltsov O, Slepukhin P, Ulomsky E, Rusinov V, Litvinov R, Babkov D, Khokhlacheva E, Radaev P, Vassiliev P, Spasov A.
Eur J Med Chem (2020) 185 : 111808 -111808
PubMed 31683103 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.09 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL142703 VILDAGLIPTIN 4.0 1 7.82
CHEMBL4571225 1 4.25
CHEMBL4554062 1 4.16
CHEMBL4535561 1 4.12
CHEMBL4540237 1 -
CHEMBL4582763 1 -
CHEMBL4557028 1 -
CHEMBL4471409 1 -
CHEMBL4448038 1 -
CHEMBL4525051 1 -
CHEMBL4435578 1 -
CHEMBL4567960 1 -
CHEMBL4463269 1 -
CHEMBL4466627 1 -
CHEMBL4563602 1 -
CHEMBL225304 PIMAGEDINE 2.0 1 -
CHEMBL595 PIOGLITAZONE 4.0 1 -
CHEMBL4555157 1 -
CHEMBL134342 THIOCTIC ACID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL142703 VILDAGLIPTIN IC50 = 15.0 nM 7.82
CHEMBL4571225 IC50 = 55870.0 nM 4.25
CHEMBL4554062 IC50 = 68510.0 nM 4.16
CHEMBL4535561 IC50 = 76170.0 nM 4.12
CHEMBL4540237 IC50 > 100000.0 nM -
CHEMBL4582763 IC50 > 100000.0 nM -
CHEMBL4557028 IC50 > 100000.0 nM -
CHEMBL4471409 IC50 > 100000.0 nM -
CHEMBL4448038 IC50 > 100000.0 nM -
CHEMBL4525051 IC50 = 121300.0 nM -
CHEMBL4435578 IC50 > 100000.0 nM -
CHEMBL4567960 IC50 > 100000.0 nM -
CHEMBL4463269 IC50 > 100000.0 nM -
CHEMBL4466627 IC50 > 100000.0 nM -
CHEMBL4563602 IC50 > 100000.0 nM -
CHEMBL225304 PIMAGEDINE IC50 - -
CHEMBL595 PIOGLITAZONE IC50 - -
CHEMBL4555157 IC50 > 100000.0 nM -
CHEMBL134342 THIOCTIC ACID IC50 - -