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Assay Detail

CHEMBL4397059

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

Binding
Inhibition of recombinant human N-terminal His-tagged MetAP2 (2 to 478 residues) using Met-Ala-Ser as substrate and cobalt as co-facor preincubated for 15 mins followed by substrate addition and measured after 45 mins by AAO/horse radish peroxidase enzyme coupled assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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 6.80 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4475680 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4475680 IC50 = 160.0 nM 6.80