ixazomib [Ligand Id: 8450] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2141296 (Ixazomib, MLN-2238, MLN2238, MLN-9708 FREE BASE, Ninlaro) |
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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: 2404, 2408, 2409, 2407, 2406, 2405] [UniProtKB: A5LHX3, O14818, P20618, P25786, P25787, P25788, P25789, P28062, P28065, P28066, P28070, P28072, P28074, P40306, P49720, P49721, P60900, Q8TAA3, Q99436] | ||||||||
| 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: P19838, Q00653, Q04206] | ||||||||
| 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 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]
