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Assay Detail

CHEMBL4397082

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

Binding
Inhibition of recombinant human N-terminal His-tagged MetAP2 expressed in baculovirus infected BTI-TN-5B1-4 insect cells using Met-Pro-pNA as substrate preincubated for 20 mins followed by substrate addition and measured after 30 mins
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BTI-TN-5B1-4
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery and Structure-Based Optimization of Next-Generation Reversible Methionine Aminopeptidase-2 (MetAP-2) Inhibitors.
Heinrich T, Seenisamy J, Blume B, Bomke J, Calderini M, Eckert U, Friese-Hamim M, Kohl R, Lehmann M, Leuthner B, Musil D, Rohdich F, Zenke FT.
J Med Chem (2019) 62 : 5025 -5039
PubMed 30939017 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.26 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1454910 NITROXOLINE 4.0 1 7.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1454910 NITROXOLINE IC50 = 55.0 nM 7.26