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Assay Detail

CHEMBL4232373

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

Binding
Inhibition of DPP4 (unknown origin) using Gly-Pro-AMC as substrate preincubated for 4 secs followed by substrate addition and measured after 30 mins by luminescence assay
17
Total Activities
17
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

Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus.
Li N, Wang LJ, Jiang B, Li XQ, Guo CL, Guo SJ, Shi DY.
Eur J Med Chem (2018) 151 : 145 -157
PubMed 29609120 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.20 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL165 RESVERATROL 3.0 1 9.22
CHEMBL151 LUTEOLIN 2.0 1 6.92
CHEMBL28 APIGENIN 1 6.85
CHEMBL275638 FLAVONE 2.0 1 6.77
CHEMBL9352 NARINGENIN 1 6.62
CHEMBL399121 HESPERETIN 0.5 1 6.55
CHEMBL257839 KUROMANIN 1 6.38
CHEMBL44 GENISTEIN 2.0 1 6.32
CHEMBL150 KAEMPFEROL 1.0 1 6.31
CHEMBL592005 MALVIDIN CHLORIDE 1 5.85
CHEMBL511367 CYANIDIN CHLORIDE 1 5.85
CHEMBL50 QUERCETIN 3.0 1 5.54
CHEMBL145 CAFFEIC ACID 3.0 1 5.47
CHEMBL214381 DIPROTIN A 1 5.38
CHEMBL288114 GALLIC ACID 2.0 1 5.33
CHEMBL2165586 ERIOCITRIN 1 4.99
CHEMBL297453 EPIGALOCATECHIN GALLATE 3.0 1 4.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL165 RESVERATROL IC50 = 0.6 nM 9.22
CHEMBL151 LUTEOLIN IC50 = 120.0 nM 6.92
CHEMBL28 APIGENIN IC50 = 140.0 nM 6.85
CHEMBL275638 FLAVONE IC50 = 170.0 nM 6.77
CHEMBL9352 NARINGENIN IC50 = 240.0 nM 6.62
CHEMBL399121 HESPERETIN IC50 = 280.0 nM 6.55
CHEMBL257839 KUROMANIN IC50 = 420.0 nM 6.38
CHEMBL44 GENISTEIN IC50 = 480.0 nM 6.32
CHEMBL150 KAEMPFEROL IC50 = 490.0 nM 6.31
CHEMBL592005 MALVIDIN CHLORIDE IC50 = 1410.0 nM 5.85
CHEMBL511367 CYANIDIN CHLORIDE IC50 = 1410.0 nM 5.85
CHEMBL50 QUERCETIN IC50 = 2920.0 nM 5.54
CHEMBL145 CAFFEIC ACID IC50 = 3370.0 nM 5.47
CHEMBL214381 DIPROTIN A IC50 = 4210.0 nM 5.38
CHEMBL288114 GALLIC ACID IC50 = 4650.0 nM 5.33
CHEMBL2165586 ERIOCITRIN IC50 = 10360.0 nM 4.99
CHEMBL297453 EPIGALOCATECHIN GALLATE IC50 = 10210.0 nM 4.99