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Assay Detail

CHEMBL1246392

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

Binding
Inhibition of human recombinant His-tagged DPP2 expressed in insect cells
33
Total Activities
33
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 2 (CHEMBL3976)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein.
Tsai TY, Yeh TK, Chen X, Hsu T, Jao YC, Huang CH, Song JS, Huang YC, Chien CH, Chiu JH, Yen SC, Tang HK, Chao YS, Jiaang WT.
J Med Chem (2010) 53 : 6572 -6583
PubMed 20718420 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.76 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98762 1 8.30
CHEMBL1243184 1 6.40
CHEMBL1243372 1 5.58
CHEMBL387050 1 -
CHEMBL1243373 1 -
CHEMBL1243374 1 -
CHEMBL1243402 1 -
CHEMBL1243403 1 -
CHEMBL1242939 1 -
CHEMBL1242940 1 -
CHEMBL1242966 1 -
CHEMBL1242967 1 -
CHEMBL1242993 1 -
CHEMBL1422 SITAGLIPTIN 4.0 1 -
CHEMBL1243027 1 -
CHEMBL1243248 1 -
CHEMBL1243216 1 -
CHEMBL1243215 1 -
CHEMBL1243183 1 -
CHEMBL1243154 1 -
CHEMBL1242994 1 -
CHEMBL1243127 1 -
CHEMBL1243126 1 -
CHEMBL1243093 1 -
CHEMBL1243092 1 -
CHEMBL1243091 1 -
CHEMBL1243061 1 -
CHEMBL1243060 1 -
CHEMBL1243028 1 -
CHEMBL1243153 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98762 IC50 = 5.0 nM 8.30
CHEMBL1243184 IC50 = 400.0 nM 6.40
CHEMBL1243372 IC50 = 2600.0 nM 5.58
CHEMBL1243027 IC50 > 100000.0 nM -
CHEMBL142703 VILDAGLIPTIN IC50 > 50000.0 nM -
CHEMBL1422 SITAGLIPTIN IC50 > 100000.0 nM -
CHEMBL1242993 IC50 > 100000.0 nM -
CHEMBL1242967 IC50 > 100000.0 nM -
CHEMBL1242966 IC50 > 100000.0 nM -
CHEMBL1242940 IC50 > 100000.0 nM -
CHEMBL1242939 IC50 > 100000.0 nM -
CHEMBL1243403 IC50 > 100000.0 nM -
CHEMBL1243402 IC50 > 100000.0 nM -
CHEMBL1243374 IC50 > 100000.0 nM -
CHEMBL1243373 IC50 > 100000.0 nM -
CHEMBL387050 IC50 > 100000.0 nM -
CHEMBL362018 IC50 > 100000.0 nM -
CHEMBL397070 IC50 > 100000.0 nM -
CHEMBL1243248 IC50 > 100000.0 nM -
CHEMBL1243216 IC50 > 100000.0 nM -
CHEMBL1243215 IC50 > 100000.0 nM -
CHEMBL1243183 IC50 > 100000.0 nM -
CHEMBL1243154 IC50 > 100000.0 nM -
CHEMBL1242994 IC50 > 100000.0 nM -
CHEMBL1243127 IC50 > 100000.0 nM -
CHEMBL1243126 IC50 > 100000.0 nM -
CHEMBL1243093 IC50 > 100000.0 nM -
CHEMBL1243092 IC50 > 100000.0 nM -
CHEMBL1243091 IC50 > 100000.0 nM -
CHEMBL1243061 IC50 > 100000.0 nM -
CHEMBL1243060 IC50 > 100000.0 nM -
CHEMBL1243028 IC50 > 100000.0 nM -
CHEMBL1243153 IC50 > 100000.0 nM -