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Assay Detail

CHEMBL1030770

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

Binding
Inhibition of DPP4
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors.
Tsai TY, Hsu T, Chen CT, Cheng JH, Chiou MC, Huang CH, Tseng YJ, Yeh TK, Huang CY, Yeh KC, Huang YW, Wu SH, Wang MH, Chen X, Chao YS, Jiaang WT.
Bioorg Med Chem Lett (2009) 19 : 1908 -1912
PubMed 19269819 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 7.80 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL493543 1 8.70
CHEMBL2364733 1 8.70
CHEMBL492733 1 8.30
CHEMBL494146 1 8.30
CHEMBL474048 1 8.22
CHEMBL494340 1 8.22
CHEMBL475465 1 8.15
CHEMBL474049 1 8.15
CHEMBL492536 1 8.15
CHEMBL474808 1 8.10
CHEMBL475662 1 8.10
CHEMBL474047 1 8.05
CHEMBL474211 1 8.00
CHEMBL493544 1 8.00
CHEMBL474983 1 7.96
CHEMBL475863 1 7.92
CHEMBL474003 1 7.92
CHEMBL514317 1 7.89
CHEMBL475870 1 7.85
CHEMBL474800 1 7.82
CHEMBL474025 1 7.80
CHEMBL475634 1 7.77
CHEMBL474982 1 7.72
CHEMBL474394 1 7.66
CHEMBL514006 1 7.60
CHEMBL1422 SITAGLIPTIN 4.0 1 7.52
CHEMBL516080 1 7.51
CHEMBL475169 1 7.51
CHEMBL474002 1 7.51
CHEMBL494147 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL493543 IC50 = 2.0 nM 8.70
CHEMBL2364733 IC50 = 2.0 nM 8.70
CHEMBL492733 IC50 = 5.0 nM 8.30
CHEMBL494146 IC50 = 5.0 nM 8.30
CHEMBL474048 IC50 = 6.0 nM 8.22
CHEMBL494340 IC50 = 6.0 nM 8.22
CHEMBL475465 IC50 = 7.0 nM 8.15
CHEMBL474049 IC50 = 7.0 nM 8.15
CHEMBL492536 IC50 = 7.0 nM 8.15
CHEMBL474808 IC50 = 8.0 nM 8.10
CHEMBL475662 IC50 = 8.0 nM 8.10
CHEMBL474047 IC50 = 9.0 nM 8.05
CHEMBL474211 IC50 = 10.0 nM 8.00
CHEMBL493544 IC50 = 10.0 nM 8.00
CHEMBL474983 IC50 = 11.0 nM 7.96
CHEMBL475863 IC50 = 12.0 nM 7.92
CHEMBL474003 IC50 = 12.0 nM 7.92
CHEMBL514317 IC50 = 13.0 nM 7.89
CHEMBL475870 IC50 = 14.0 nM 7.85
CHEMBL474800 IC50 = 15.0 nM 7.82
CHEMBL474025 IC50 = 16.0 nM 7.80
CHEMBL475634 IC50 = 17.0 nM 7.77
CHEMBL474982 IC50 = 19.0 nM 7.72
CHEMBL474394 IC50 = 22.0 nM 7.66
CHEMBL514006 IC50 = 25.0 nM 7.60
CHEMBL1422 SITAGLIPTIN IC50 = 30.0 nM 7.52
CHEMBL516080 IC50 = 31.0 nM 7.51
CHEMBL474002 IC50 = 31.0 nM 7.51
CHEMBL475169 IC50 = 31.0 nM 7.51
CHEMBL494147 IC50 = 35.0 nM 7.46
CHEMBL515435 IC50 = 37.0 nM 7.43
CHEMBL494339 IC50 = 40.0 nM 7.40
CHEMBL142703 VILDAGLIPTIN IC50 = 56.0 nM 7.25
CHEMBL522002 IC50 = 298.0 nM 6.53
CHEMBL493760 IC50 = 1600.0 nM 5.80