ixazomib [Ligand Id: 8450] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2141296 (Ixazomib, MLN2238, MLN-2238, MLN-9708 FREE BASE, Ninlaro)
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  • ATP-dependent Clp protease proteolytic subunit in Staphylococcus aureus (strain NCTC 8325) [ChEMBL: CHEMBL1932910] [UniProtKB: Q2G036]
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  • proteasome 20S subunit beta 1/Proteasome component C5 in Human [ChEMBL: CHEMBL4208] [GtoPdb: 2404] [UniProtKB: P20618]
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  • proteasome 20S subunit beta 2/Proteasome Macropain subunit in Human [ChEMBL: CHEMBL3492] [GtoPdb: 2405] [UniProtKB: P49721]
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  • proteasome 20S subunit beta 5/Proteasome Macropain subunit MB1 in Human [ChEMBL: CHEMBL4662] [GtoPdb: 2406] [UniProtKB: P28074]
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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 20S subunit beta 8/proteasome 20S subunit beta 9/proteasome 20S subunit beta 6/proteasome 20S subunit beta 5/proteasome 20S subunit beta 2/20S proteasome in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3831201] [GtoPdb: 240424082409240724062405] [UniProtKB: A5LHX3O14818P20618P25786P25787P25788P25789P28062P28065P28066P28070P28072P28074P40306P49720P49721P60900Q8TAA3Q99436]
GtoPdb - - 9.03 pKi 0.93 nM Ki Cancer Res (2010) 70: 1970-80 [PMID:20160034]
ChEMBL Inhibition of human 20S proteasome using Suc-LLVY-AMC as substrate measured every 5 mins for 120 mins by fluorescence based assay B 7.82 pIC50 15 nM IC50 J Med Chem (2020) 63: 334-348 [PMID:31801019]
ATP-dependent Clp protease proteolytic subunit in Staphylococcus aureus (strain NCTC 8325) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1932910] [UniProtKB: Q2G036]
ChEMBL Inhibition of N-terminal His6-sumo-tagged full length Staphylococcus aureus ClpP expressed in Escherichia coli BL2 (DE3) pre-incubated for 10 mins before Suc-LY-AMC addition and measured after 1 hr by fluorescence based assay B 5.28 pIC50 5300 nM IC50 J Med Chem (2020) 63: 3104-3119 [PMID:32031798]
ChEMBL Inhibition of ClpP in methicillin-resistant Staphylococcus aureus ATCC 33591 assessed as reduction in bacteria-induced hemolysis of sheep erythrocytes by measuring hemoglobin release incubated for 15 mins B 5.44 pEC50 3600 nM EC50 J Med Chem (2020) 63: 3104-3119 [PMID:32031798]
Nuclear factor NF-kappa-B complex in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094258] [UniProtKB: P19838Q00653Q04206]
ChEMBL Inhibition of NFkappaB in HEK293 cells incubated for 1 hr prior to TNF-alpha challenge measured after 3 hrs by luciferase reporter gene assay relative to control B 8.21 pIC50 6.2 nM IC50 MedChemComm (2012) 3: 710-719
proteasome 20S subunit beta 1/Proteasome component C5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4208] [GtoPdb: 2404] [UniProtKB: P20618]
ChEMBL Inhibition of 20S proteasome beta1 subunit in human erythrocytes using Z-LLE-AMC as substrate by fluorescence assay B 5 pIC50 >10000 nM IC50 MedChemComm (2012) 3: 710-719
ChEMBL Reversible inhibition of human erythrocyte derived 20S proteasome subunit beta1 after 30 mins by fluorogenic assay B 7.51 pIC50 31 nM IC50 J. Med. Chem. (2012) 55: 10317-10327 [PMID:22978849]
ChEMBL Inhibition of 20S proteasome beta 1c (unknown origin) after 1 hr by fluorescence based assay B 8.52 pIC50 3 nM IC50 Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028]
proteasome 20S subunit beta 2/Proteasome Macropain subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3492] [GtoPdb: 2405] [UniProtKB: P49721]
ChEMBL Inhibition of 20S proteasome beta2 subunit in human erythrocytes using Ac-KQL-AMC as substrate by fluorescence assay B 5 pIC50 >10000 nM IC50 MedChemComm (2012) 3: 710-719
ChEMBL Reversible inhibition of human erythrocyte derived 20S proteasome subunit beta2 after 30 mins by fluorogenic assay B 5.46 pIC50 3500 nM IC50 J. Med. Chem. (2012) 55: 10317-10327 [PMID:22978849]
ChEMBL Inhibition of 20S proteasome beta 2c (unknown origin) after 1 hr by fluorescence based assay B 7.52 pIC50 30 nM IC50 Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028]
proteasome 20S subunit beta 5/Proteasome Macropain subunit MB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4662] [GtoPdb: 2406] [UniProtKB: P28074]
GtoPdb - - 9.03 pKi 0.93 nM Ki Cancer Res (2010) 70: 1970-80 [PMID:20160034]
ChEMBL Inhibition of 26S proteasome beta5 subunit in human Calu6 cells using Suc-LLVY-aminoluciferin as substrate after 1hr by luminescence assay B 8.05 pIC50 9 nM IC50 MedChemComm (2012) 3: 710-719
ChEMBL Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate incubated for 10 mins followed by substrate addition measured after 1 hr by spectrofluorimetric method B 8.11 pIC50 7.73 nM IC50 Bioorg Med Chem (2018) 26: 3975-3981 [PMID:29934218]
ChEMBL Reversible inhibition of human erythrocyte derived 20S proteasome subunit beta5 after 30 mins by fluorogenic assay B 8.47 pIC50 3.4 nM IC50 J. Med. Chem. (2012) 55: 10317-10327 [PMID:22978849]
ChEMBL Inhibition of 20S proteasome beta 5c (unknown origin) after 1 hr by fluorescence based assay B 8.47 pIC50 3.4 nM IC50 Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028]
ChEMBL Inhibition of 20S proteasome beta5 subunit in human erythrocytes using Ac-WLA-AMC as substrate by fluorescence assay B 8.52 pIC50 3 nM IC50 MedChemComm (2012) 3: 710-719

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]