M8891 [Ligand Id: 12714] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4464946
  • Methionyl aminopeptidase 2/Methionine aminopeptidase 2 in Human [ChEMBL: CHEMBL3922] [GtoPdb: 1573] [UniProtKB: P50579]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Methionyl aminopeptidase 2/Methionine aminopeptidase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3922] [GtoPdb: 1573] [UniProtKB: P50579]
ChEMBL 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 FCCS analysis B 8.68 pKd 2.1 nM Kd J Med Chem (2019) 62: 11119-11134 [PMID:31725285]
ChEMBL 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 B 8.36 pKi 4.33 nM Ki J Med Chem (2019) 62: 11119-11134 [PMID:31725285]
ChEMBL Inhibition of recombinant human N-terminal His-tagged MetAP2 (2 to 478 residues) using Met-Ala-Ser as substrate and MnCl2 as co-facor preincubated for 15 mins followed by substrate addition and measured after 45 mins by AAO/horse radish peroxidase enzyme coupled assay B 7.27 pIC50 54 nM IC50 J Med Chem (2019) 62: 11119-11134 [PMID:31725285]
GtoPdb Inhibition of recombinant human N-terminal His-tagged MetAP2 - 7.27 pIC50 54 nM IC50 J Med Chem (2019) 62: 11119-11134 [PMID:31725285]
ChEMBL Inhibition of MetAP2 in HUVEC assessed as reduction in viability incubated for 3 days by CyQUANT Direct Cell proliferation assay B 7.7 pIC50 20 nM IC50 J Med Chem (2019) 62: 11119-11134 [PMID:31725285]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]