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Assay Detail

CHEMBL4413686

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

Binding
Inhibition of recombinant human DPP4 expressed in baculovirus infected Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Identification of novel uracil derivatives incorporating benzoic acid moieties as highly potent Dipeptidyl Peptidase-IV inhibitors.
Huang J, Deng X, Zhou S, Wang N, Qin Y, Meng L, Li G, Xiong Y, Fan Y, Guo L, Lan D, Xing J, Jiang W, Li Q.
Bioorg Med Chem (2019) 27 : 644 -654
PubMed 30642693 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.92 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4446618 1 8.77
CHEMBL4558007 1 8.60
CHEMBL376359 ALOGLIPTIN 4.0 1 8.57
CHEMBL4516959 1 8.46
CHEMBL4562685 1 8.41
CHEMBL4581959 1 8.40
CHEMBL4527363 1 8.34
CHEMBL1422 SITAGLIPTIN 4.0 1 8.16
CHEMBL4538597 1 8.12
CHEMBL4438210 1 8.12
CHEMBL4530011 1 7.25
CHEMBL4436620 1 7.13
CHEMBL4468423 1 7.05
CHEMBL4453917 1 7.03
CHEMBL4445783 1 6.40
CHEMBL4537845 1 -
CHEMBL4585574 1 -
CHEMBL4559809 1 -
CHEMBL4571572 1 -
CHEMBL4437931 1 -
CHEMBL4540469 1 -
CHEMBL4440121 1 -
CHEMBL4581624 1 -
CHEMBL142703 VILDAGLIPTIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4446618 IC50 = 1.7 nM 8.77
CHEMBL4558007 IC50 = 2.5 nM 8.60
CHEMBL376359 ALOGLIPTIN IC50 = 2.7 nM 8.57
CHEMBL4516959 IC50 = 3.5 nM 8.46
CHEMBL4562685 IC50 = 3.9 nM 8.41
CHEMBL4581959 IC50 = 4.0 nM 8.40
CHEMBL4527363 IC50 = 4.6 nM 8.34
CHEMBL1422 SITAGLIPTIN IC50 = 6.9 nM 8.16
CHEMBL4538597 IC50 = 7.5 nM 8.12
CHEMBL4438210 IC50 = 7.6 nM 8.12
CHEMBL4530011 IC50 = 56.6 nM 7.25
CHEMBL4436620 IC50 = 74.6 nM 7.13
CHEMBL4468423 IC50 = 89.8 nM 7.05
CHEMBL4453917 IC50 = 93.2 nM 7.03
CHEMBL4445783 IC50 = 395.0 nM 6.40
CHEMBL4537845 IC50 - -
CHEMBL4585574 IC50 - -
CHEMBL4559809 IC50 - -
CHEMBL4571572 IC50 - -
CHEMBL4437931 IC50 - -
CHEMBL4540469 IC50 - -
CHEMBL4440121 IC50 - -
CHEMBL4581624 IC50 - -
CHEMBL142703 VILDAGLIPTIN IC50 - -