compound 3b [PMID: 24946214] [Ligand Id: 8618] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3287940
  • proteasome 20S subunit beta 1/Proteasome component C5 in Human [ChEMBL: CHEMBL4208] [GtoPdb: 2404] [UniProtKB: P20618]
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  • proteasome 20S subunit beta 5/Proteasome Macropain subunit MB1 in Human [ChEMBL: CHEMBL4662] [GtoPdb: 2406] [UniProtKB: P28074]
  • proteasome 20S subunit beta 5 in Bovine [GtoPdb: 2406]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
proteasome 20S subunit beta 1/Proteasome component C5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4208] [GtoPdb: 2404] [UniProtKB: P20618]
ChEMBL Inhibition of PGPH-like activity of 20S proteasome in human erythrocytes using Z-Leu-Leu-Glu-AMC as substrate by fluorescence assay B 6.62 pKi 240 nM Ki Eur J Med Chem (2014) 83: 1-14 [PMID:24946214]
GtoPdb - - 6.62 pKi 240 nM Ki Eur J Med Chem (2014) 83: 1-14 [PMID:24946214]
proteasome 20S subunit beta 5/Proteasome Macropain subunit MB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4662] [GtoPdb: 2406] [UniProtKB: P28074]
ChEMBL Inhibition of chymotrypsin-like activity of 20S proteasome in human erythrocytes using Suc-Leu-Leu-Val-Tyr-AMC as substrate by fluorescence assay B 7.29 pKi 51 nM Ki Eur J Med Chem (2014) 83: 1-14 [PMID:24946214]
proteasome 20S subunit beta 5 in Bovine [GtoPdb: 2406]
GtoPdb Inhibition of chymotrypsin-like activity. - 8.29 pKi 5.1 nM Ki Eur J Med Chem (2014) 83: 1-14 [PMID:24946214]

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]