Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4417041

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

Binding
Inhibition of 5-[(S)-3-(3-Chloro-5-fluoro-benzylcarbamoyl)-3-hydroxy-2-oxopyrrolidin-1-yl]-1H-indole-2-carboxylic Acid (3-Amino-propyl)-amide-Dy647 binding to recombinant full length N-terminal GFP-fused MetAP2 (unknown origin) expressed in HEK293 cells by Cheng-Prusoff equation analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Identification of Methionine Aminopeptidase-2 (MetAP-2) Inhibitor M8891: A Clinical Compound for the Treatment of Cancer.
Heinrich T, Seenisamy J, Becker F, Blume B, Bomke J, Dietz M, Eckert U, Friese-Hamim M, Gunera J, Hansen K, Leuthner B, Musil D, Pfalzgraf J, Rohdich F, Siegl C, Spuck D, Wegener A, Zenke FT.
J Med Chem (2019) 62 : 11119 -11134
PubMed 31725285 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.92 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4475680 1 9.80
CHEMBL4451402 1 9.05
CHEMBL4448724 1 8.47
CHEMBL4464946 1 8.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4475680 Ki = 0.16 nM 9.80
CHEMBL4451402 Ki = 0.9 nM 9.05
CHEMBL4448724 Ki = 3.36 nM 8.47
CHEMBL4464946 Ki = 4.33 nM 8.36