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Assay Detail

CHEMBL1061470

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

Binding
Inhibition of human recombinant DPP4 by fluorescence assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Bicyclic cyanothiazolidines as novel dipeptidyl peptidase 4 inhibitors.
Betancort JM, Winn DT, Liu R, Xu Q, Liu J, Liao W, Chen SH, Carney D, Hanway D, Schmeits J, Li X, Gordon E, Campbell DA.
Bioorg Med Chem Lett (2009) 19 : 4437 -4440
PubMed 19482472 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.32 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL142703 VILDAGLIPTIN 4.0 1 8.52
CHEMBL385517 SAXAGLIPTIN ANHYDROUS 4.0 1 8.52
CHEMBL564670 1 7.58
CHEMBL564854 1 7.48
CHEMBL563772 1 7.28
CHEMBL560583 1 7.25
CHEMBL560985 1 7.23
CHEMBL561263 1 7.20
CHEMBL558956 1 7.05
CHEMBL539691 1 6.98
CHEMBL561462 1 6.96
CHEMBL556219 1 6.93
CHEMBL552403 1 6.82
CHEMBL558313 1 6.69
CHEMBL558509 1 -
CHEMBL556220 1 -
CHEMBL552404 1 -
CHEMBL551323 1 -
CHEMBL87265 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL142703 VILDAGLIPTIN IC50 = 3.0 nM 8.52
CHEMBL385517 SAXAGLIPTIN ANHYDROUS IC50 = 3.0 nM 8.52
CHEMBL564670 IC50 = 26.0 nM 7.58
CHEMBL564854 IC50 = 33.0 nM 7.48
CHEMBL563772 IC50 = 53.0 nM 7.28
CHEMBL560583 IC50 = 56.0 nM 7.25
CHEMBL560985 IC50 = 59.0 nM 7.23
CHEMBL561263 IC50 = 63.0 nM 7.20
CHEMBL558956 IC50 = 89.0 nM 7.05
CHEMBL539691 IC50 = 105.0 nM 6.98
CHEMBL561462 IC50 = 109.0 nM 6.96
CHEMBL556219 IC50 = 118.0 nM 6.93
CHEMBL552403 IC50 = 152.0 nM 6.82
CHEMBL558313 IC50 = 205.0 nM 6.69
CHEMBL558509 IC50 > 1600.0 nM -
CHEMBL556220 IC50 > 16000.0 nM -
CHEMBL552404 IC50 > 16000.0 nM -
CHEMBL551323 IC50 > 1600.0 nM -
CHEMBL87265 IC50 > 1600.0 nM -