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Assay Detail

CHEMBL3887953

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Binding
DPP-IV Activity InhibitoryAssay: Gly-Pro-7-amido-4-methylcoumarin can be hydrolyzed by dipeptidyl peptidase IV (DPP-IV) at room temperature, to generate 7-amido-4-methyl coumarin, which can emit fluorescence with wavelength of 460 nm at excitation wavelength of 355 nm. The variation of the product amount can be determined by the variation of fluorescence intensity, so as to reflect the activity level of the enzyme. The dipeptidyl peptidase IV (DPP-IV), DPP-IV buffer and test samples were used to construct the reaction system of 200 uL, while the blank control (without enzyme and samples) and negative control (without samples) having the same volume were set up. The reaction system and the controls were reacted at room temperature for 10 min, and then dipeptidyl peptidase IV substrate was added thereto respectively, then reacted at room temperature for 30 min. The fluorescence intensity F (excitation wavelength of 355 nm, emission wavelength of 460 nm) was determined.
6
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Xanthine derivative
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 9.82 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4113723 2 10.30
CHEMBL4111229 2 10.00
CHEMBL4109453 1 9.70
CHEMBL237500 LINAGLIPTIN 4.0 1 9.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4113723 IC50 = 0.05 nM 10.30
CHEMBL4113723 IC50 = 0.08 nM 10.10
CHEMBL4111229 IC50 = 0.1 nM 10.00
CHEMBL4111229 IC50 = 0.15 nM 9.82
CHEMBL4109453 IC50 = 0.2 nM 9.70
CHEMBL237500 LINAGLIPTIN IC50 = 1.0 nM 9.00