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Assay Detail

CHEMBL3879302

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Binding
Inhibition of recombinant full length human N-terminal GST/His6-tagged methionine aminopeptidase 2 expressed in baculovirus infected sf9 cells using methionylprolyl-p-nitroanilide as substrate preincubated for 20 mins followed by substrate addition measured for 20 mins in presence of MnCl2 by proline aminopeptidase coupled enzyme assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Methionine aminopeptidase 2 (CHEMBL3922)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Rickettsia prowazekii methionine aminopeptidase as a promising target for the development of antibacterial agents.
Helgren TR, Chen C, Wangtrakuldee P, Edwards TE, Staker BL, Abendroth J, Sankaran B, Housley NA, Myler PJ, Audia JP, Horn JR, Hagen TJ.
Bioorg Med Chem (2017) 25 : 813 -824
PubMed 28089350 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.28 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225164 CLOXYQUIN 2.0 1 7.26
CHEMBL310555 OXYQUINOLINE -1.0 1 5.90
CHEMBL316892 8-HYDROXY QUINALDINE 1 5.69
CHEMBL2407096 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225164 CLOXYQUIN IC50 = 55.0 nM 7.26
CHEMBL310555 OXYQUINOLINE IC50 = 1270.0 nM 5.90
CHEMBL316892 8-HYDROXY QUINALDINE IC50 = 2030.0 nM 5.69
CHEMBL2407096 IC50 > 15000.0 nM -