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Assay Detail

CHEMBL3806574

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

Binding
Inhibition of porcine kidney leucine aminopeptidase M17 using Leu-AMC as substrate preincubated for 30 to 60 mins followed by substrate addition measured for 15 mins by spectrofluorimetric analysis
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytosol aminopeptidase (CHEMBL5624)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

A structural insight into the P1S1 binding mode of diaminoethylphosphonic and phosphinic acids, selective inhibitors of alanine aminopeptidases.
Węglarz-Tomczak E, Berlicki Ł, Pawełczak M, Nocek B, Joachimiak A, Mucha A.
Eur J Med Chem (2016) 117 : 187 -196
PubMed 27100031 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 4.63 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1673064 1 6.68
CHEMBL3805288 1 5.15
CHEMBL3805028 1 4.82
CHEMBL3806197 1 4.71
CHEMBL3805573 1 4.68
CHEMBL3805495 1 4.68
CHEMBL3806187 1 4.68
CHEMBL3805118 1 4.62
CHEMBL3805817 1 4.58
CHEMBL3804956 1 4.58
CHEMBL3804856 1 4.55
CHEMBL3806230 1 4.25
CHEMBL3805472 1 4.19
CHEMBL3805338 1 4.17
CHEMBL3805487 1 4.16
CHEMBL3805193 1 4.15
CHEMBL3805964 1 4.14
CHEMBL3806247 1 -
CHEMBL3805544 1 -
CHEMBL3805251 1 -
CHEMBL3806100 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1673064 Ki = 210.0 nM 6.68
CHEMBL3805288 Ki = 7020.0 nM 5.15
CHEMBL3805028 Ki = 15200.0 nM 4.82
CHEMBL3806197 Ki = 19500.0 nM 4.71
CHEMBL3805573 Ki = 20800.0 nM 4.68
CHEMBL3805495 Ki = 21100.0 nM 4.68
CHEMBL3806187 Ki = 21000.0 nM 4.68
CHEMBL3805118 Ki = 23800.0 nM 4.62
CHEMBL3805817 Ki = 26200.0 nM 4.58
CHEMBL3804956 Ki = 26500.0 nM 4.58
CHEMBL3804856 Ki = 28300.0 nM 4.55
CHEMBL3806230 Ki = 55800.0 nM 4.25
CHEMBL3805472 Ki = 64400.0 nM 4.19
CHEMBL3805338 Ki = 68400.0 nM 4.17
CHEMBL3805487 Ki = 69100.0 nM 4.16
CHEMBL3805193 Ki = 71100.0 nM 4.15
CHEMBL3805964 Ki = 72600.0 nM 4.14
CHEMBL3806247 Ki = 119000.0 nM -
CHEMBL3805544 Ki = 108000.0 nM -
CHEMBL3805251 Ki = 240000.0 nM -
CHEMBL3806100 Ki = 289000.0 nM -