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Assay Detail

CHEMBL1022016

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

Binding
Inhibition of human recombinant DPP4
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 Autocuration

Target

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

Publication

(3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor.
Ammirati MJ, Andrews KM, Boyer DD, Brodeur AM, Danley DE, Doran SD, Hulin B, Liu S, McPherson RK, Orena SJ, Parker JC, Polivkova J, Qiu X, Soglia CB, Treadway JL, VanVolkenburg MA, Wilder DC, Piotrowski DW.
Bioorg Med Chem Lett (2009) 19 : 1991 -1995
PubMed 19275964 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.64 8.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL514011 1 8.32
CHEMBL474410 1 8.28
CHEMBL475586 1 8.28
CHEMBL474409 1 8.25
CHEMBL475574 1 8.24
CHEMBL475573 1 8.13
CHEMBL515597 1 8.09
CHEMBL475246 1 8.06
CHEMBL474421 1 7.89
CHEMBL515387 GOSOGLIPTIN 4.0 1 7.89
CHEMBL515869 1 7.60
CHEMBL473418 1 7.51
CHEMBL514623 1 7.51
CHEMBL473188 1 7.39
CHEMBL473419 1 7.29
CHEMBL514935 1 6.87
CHEMBL472993 1 6.51
CHEMBL472992 1 6.51
CHEMBL472995 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL514011 IC50 = 4.8 nM 8.32
CHEMBL474410 IC50 = 5.2 nM 8.28
CHEMBL475586 IC50 = 5.2 nM 8.28
CHEMBL474409 IC50 = 5.6 nM 8.25
CHEMBL475574 IC50 = 5.8 nM 8.24
CHEMBL475573 IC50 = 7.4 nM 8.13
CHEMBL515597 IC50 = 8.2 nM 8.09
CHEMBL475246 IC50 = 8.7 nM 8.06
CHEMBL474421 IC50 = 13.0 nM 7.89
CHEMBL515387 GOSOGLIPTIN IC50 = 12.9 nM 7.89
CHEMBL515869 IC50 = 25.0 nM 7.60
CHEMBL473418 IC50 = 31.0 nM 7.51
CHEMBL514623 IC50 = 31.0 nM 7.51
CHEMBL473188 IC50 = 41.0 nM 7.39
CHEMBL473419 IC50 = 51.0 nM 7.29
CHEMBL514935 IC50 = 134.0 nM 6.87
CHEMBL472993 IC50 = 309.0 nM 6.51
CHEMBL472992 IC50 = 309.0 nM 6.51
CHEMBL472995 IC50 = 338.0 nM 6.47