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Assay Detail

CHEMBL706596

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Binding
Inhibitory activity against Leucine aminopeptidase
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Streptomyces olivoreticuli
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cytosol aminopeptidase (CHEMBL3965)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of sulfur-containing analogues of bestatin. Inhibition of aminopeptidases by alpha-thiolbestatin analogues.
Ocain TD, Rich DH.
J Med Chem (1988) 31 : 2193 -2199
PubMed 3184126 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 5.89 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL29292 UBENIMEX 2.0 1 7.70
CHEMBL68979 1 6.48
CHEMBL309130 1 6.29
CHEMBL305198 1 6.26
CHEMBL1204264 1 6.00
CHEMBL67868 1 5.36
CHEMBL69238 1 4.58
CHEMBL68686 1 4.48
CHEMBL69239 1 -
CHEMBL69814 1 -
CHEMBL68092 1 -
CHEMBL68511 1 -
CHEMBL71171 1 -
CHEMBL68509 1 -
CHEMBL69349 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL29292 UBENIMEX Ki = 20.0 nM 7.70
CHEMBL68979 Ki = 330.0 nM 6.48
CHEMBL309130 Ki = 510.0 nM 6.29
CHEMBL305198 Ki = 550.0 nM 6.26
CHEMBL1204264 Ki = 1000.0 nM 6.00
CHEMBL67868 Ki = 4400.0 nM 5.36
CHEMBL69238 Ki = 26000.0 nM 4.58
CHEMBL68686 Ki = 33000.0 nM 4.48
CHEMBL69239 Ki = 167000.0 nM -
CHEMBL69814 Ki > 500000.0 nM -
CHEMBL68092 Ki = 300000.0 nM -
CHEMBL68511 Ki = 507000.0 nM -
CHEMBL71171 Ki > 1000000.0 nM -
CHEMBL68509 Ki > 1000000.0 nM -
CHEMBL69349 Ki = 450000.0 nM -