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Assay Detail

CHEMBL908233

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Binding
Inhibitory constant against POP
17
Total Activities
17
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

Prolyl endopeptidase (CHEMBL3202)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP.
Tran T, Quan C, Edosada CY, Mayeda M, Wiesmann C, Sutherlin D, Wolf BB.
Bioorg Med Chem Lett (2007) 17 : 1438 -1442
PubMed 17174090 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.59 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL217802 1 8.77
CHEMBL386890 1 8.66
CHEMBL217244 1 8.64
CHEMBL387444 1 8.57
CHEMBL387050 1 8.55
CHEMBL443836 1 8.36
CHEMBL216410 1 8.35
CHEMBL385419 1 8.13
CHEMBL216376 1 7.89
CHEMBL217753 1 7.60
CHEMBL217754 1 7.28
CHEMBL217056 1 7.00
CHEMBL216411 1 6.72
CHEMBL217561 1 6.68
CHEMBL383855 1 6.45
CHEMBL217065 1 5.87
CHEMBL387462 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL217802 Ki = 1.7 nM 8.77
CHEMBL386890 Ki = 2.2 nM 8.66
CHEMBL217244 Ki = 2.3 nM 8.64
CHEMBL387444 Ki = 2.7 nM 8.57
CHEMBL387050 Ki = 2.8 nM 8.55
CHEMBL443836 Ki = 4.4 nM 8.36
CHEMBL216410 Ki = 4.5 nM 8.35
CHEMBL385419 Ki = 7.4 nM 8.13
CHEMBL216376 Ki = 13.0 nM 7.89
CHEMBL217753 Ki = 25.0 nM 7.60
CHEMBL217754 Ki = 53.0 nM 7.28
CHEMBL217056 Ki = 101.0 nM 7.00
CHEMBL216411 Ki = 191.0 nM 6.72
CHEMBL217561 Ki = 211.0 nM 6.68
CHEMBL383855 Ki = 353.0 nM 6.45
CHEMBL217065 Ki = 1359.0 nM 5.87
CHEMBL387462 Ki = 2705.0 nM 5.57