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Assay Detail

CHEMBL908237

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

Binding
In vitro inhibition of DPP-4
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

3-[2-((2S)-2-cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-butyramide analogues as selective DPP-IV inhibitors for the treatment of type-II diabetes.
Coumar MS, Chang CN, Chen CT, Chen X, Chien CH, Tsai TY, Cheng JH, Wu HY, Han CH, Wu SH, Huang YW, Hsu T, Hsu LJ, Chao YS, Hsieh HP, Jiaang WT.
Bioorg Med Chem Lett (2007) 17 : 1274 -1279
PubMed 17194587 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.60 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL217245 1 7.38
CHEMBL217198 1 6.94
CHEMBL218026 1 6.93
CHEMBL201158 1 6.92
CHEMBL217059 1 6.90
CHEMBL274770 1 6.84
CHEMBL385394 1 6.76
CHEMBL218393 1 6.74
CHEMBL216453 1 6.72
CHEMBL385637 1 6.71
CHEMBL216383 1 6.68
CHEMBL386326 1 6.65
CHEMBL217290 1 6.63
CHEMBL274103 1 6.63
CHEMBL216377 1 6.62
CHEMBL384493 1 6.61
CHEMBL217339 1 6.60
CHEMBL384985 1 6.60
CHEMBL217060 1 6.57
CHEMBL371480 1 6.53
CHEMBL216878 1 6.50
CHEMBL216296 1 6.36
CHEMBL382907 1 6.34
CHEMBL201544 1 6.25
CHEMBL216203 1 6.04
CHEMBL202711 1 5.96
CHEMBL217212 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL217245 IC50 = 42.0 nM 7.38
CHEMBL217198 IC50 = 116.0 nM 6.94
CHEMBL218026 IC50 = 118.0 nM 6.93
CHEMBL201158 IC50 = 119.0 nM 6.92
CHEMBL217059 IC50 = 127.0 nM 6.90
CHEMBL274770 IC50 = 144.0 nM 6.84
CHEMBL385394 IC50 = 174.0 nM 6.76
CHEMBL218393 IC50 = 181.0 nM 6.74
CHEMBL216453 IC50 = 190.0 nM 6.72
CHEMBL385637 IC50 = 197.0 nM 6.71
CHEMBL216383 IC50 = 207.0 nM 6.68
CHEMBL386326 IC50 = 225.0 nM 6.65
CHEMBL217290 IC50 = 232.0 nM 6.63
CHEMBL274103 IC50 = 236.0 nM 6.63
CHEMBL216377 IC50 = 239.0 nM 6.62
CHEMBL384493 IC50 = 247.0 nM 6.61
CHEMBL217339 IC50 = 252.0 nM 6.60
CHEMBL384985 IC50 = 253.0 nM 6.60
CHEMBL217060 IC50 = 269.0 nM 6.57
CHEMBL371480 IC50 = 298.0 nM 6.53
CHEMBL216878 IC50 = 320.0 nM 6.50
CHEMBL216296 IC50 = 433.0 nM 6.36
CHEMBL382907 IC50 = 452.0 nM 6.34
CHEMBL201544 IC50 = 564.0 nM 6.25
CHEMBL216203 IC50 = 911.0 nM 6.04
CHEMBL202711 IC50 = 1108.0 nM 5.96
CHEMBL217212 IC50 = 1300.0 nM 5.89