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Assay Detail

CHEMBL1119686

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

Binding
Inhibition of DPP4 in presence of 50% human serum
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
Yeh TK, Tsai TY, Hsu T, Cheng JH, Chen X, Song JS, Shy HS, Chiou MC, Chien CH, Tseng YJ, Huang CY, Yeh KC, Huang YL, Huang CH, Huang YW, Wang MH, Tang HK, Chao YS, Chen CT, Jiaang WT.
Bioorg Med Chem Lett (2010) 20 : 3596 -3600
PubMed 20483603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.66 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1082462 DBPR-108 3.0 1 8.30
CHEMBL1085333 1 7.89
CHEMBL1085074 1 7.85
CHEMBL1085595 1 7.82
CHEMBL142703 VILDAGLIPTIN 4.0 1 7.77
CHEMBL1422 SITAGLIPTIN 4.0 1 7.75
CHEMBL1085552 1 7.75
CHEMBL1085306 1 7.72
CHEMBL1082463 1 7.68
CHEMBL1082996 1 6.07
CHEMBL1085579 1 -
CHEMBL1085580 1 -
CHEMBL1085075 1 -
CHEMBL1084972 1 -
CHEMBL1085305 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1082462 DBPR-108 IC50 = 5.0 nM 8.30
CHEMBL1085333 IC50 = 13.0 nM 7.89
CHEMBL1085074 IC50 = 14.0 nM 7.85
CHEMBL1085595 IC50 = 15.0 nM 7.82
CHEMBL142703 VILDAGLIPTIN IC50 = 17.0 nM 7.77
CHEMBL1422 SITAGLIPTIN IC50 = 18.0 nM 7.75
CHEMBL1085552 IC50 = 18.0 nM 7.75
CHEMBL1085306 IC50 = 19.0 nM 7.72
CHEMBL1082463 IC50 = 21.0 nM 7.68
CHEMBL1082996 IC50 = 847.0 nM 6.07
CHEMBL1085579 IC50 - -
CHEMBL1085580 IC50 - -
CHEMBL1085075 IC50 - -
CHEMBL1084972 IC50 - -
CHEMBL1085305 IC50 - -