M8891 [Ligand Id: 12714] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4464946 |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
