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Assay Detail

CHEMBL3737789

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

Binding
Inhibition of recombinant human DPP4 expressed in Sf9 cells using Gly-Pro-AMC substrate after 30 mins by plate reader analysis
27
Total Activities
27
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

Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin.
Chen P, Feng D, Qian X, Apgar J, Wilkening R, Kuethe JT, Gao YD, Scapin G, Cox J, Doss G, Eiermann G, He H, Li X, Lyons KA, Metzger J, Petrov A, Wu JK, Xu S, Weber AE, Yan Y, Roy RS, Biftu T.
Bioorg Med Chem Lett (2015) 25 : 5767 -5771
PubMed 26546218 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 8.75 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3736137 1 9.52
CHEMBL3735843 1 9.40
CHEMBL3735865 1 9.15
CHEMBL3734828 1 8.96
CHEMBL3735461 1 8.89
CHEMBL3736135 1 8.85
CHEMBL2425070 1 8.85
CHEMBL3736085 1 8.80
CHEMBL3735329 1 8.80
CHEMBL3736190 1 8.80
CHEMBL3734964 1 8.80
CHEMBL3735694 1 8.77
CHEMBL3735917 1 8.77
CHEMBL3735433 1 8.74
CHEMBL3734999 1 8.74
CHEMBL3735281 1 8.74
CHEMBL3736423 1 8.72
CHEMBL3736067 1 8.72
CHEMBL3736188 1 8.64
CHEMBL3736511 1 8.64
CHEMBL2105762 OMARIGLIPTIN 4.0 1 8.59
CHEMBL3645492 1 8.59
CHEMBL3734769 1 8.49
CHEMBL3735925 1 8.43
CHEMBL3735129 1 8.37
CHEMBL3735852 1 8.31
CHEMBL3734912 1 8.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3736137 IC50 = 0.3 nM 9.52
CHEMBL3735843 IC50 = 0.4 nM 9.40
CHEMBL3735865 IC50 = 0.7 nM 9.15
CHEMBL3734828 IC50 = 1.1 nM 8.96
CHEMBL3735461 IC50 = 1.3 nM 8.89
CHEMBL3736135 IC50 = 1.4 nM 8.85
CHEMBL2425070 IC50 = 1.4 nM 8.85
CHEMBL3736085 IC50 = 1.6 nM 8.80
CHEMBL3735329 IC50 = 1.6 nM 8.80
CHEMBL3736190 IC50 = 1.6 nM 8.80
CHEMBL3734964 IC50 = 1.6 nM 8.80
CHEMBL3735694 IC50 = 1.7 nM 8.77
CHEMBL3735917 IC50 = 1.7 nM 8.77
CHEMBL3735433 IC50 = 1.8 nM 8.74
CHEMBL3734999 IC50 = 1.8 nM 8.74
CHEMBL3735281 IC50 = 1.8 nM 8.74
CHEMBL3736423 IC50 = 1.9 nM 8.72
CHEMBL3736067 IC50 = 1.9 nM 8.72
CHEMBL3736188 IC50 = 2.3 nM 8.64
CHEMBL3736511 IC50 = 2.3 nM 8.64
CHEMBL2105762 OMARIGLIPTIN IC50 = 2.6 nM 8.59
CHEMBL3645492 IC50 = 2.6 nM 8.59
CHEMBL3734769 IC50 = 3.2 nM 8.49
CHEMBL3735925 IC50 = 3.7 nM 8.43
CHEMBL3735129 IC50 = 4.3 nM 8.37
CHEMBL3735852 IC50 = 4.9 nM 8.31
CHEMBL3734912 IC50 = 5.7 nM 8.24