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 GROUP) [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] |
| NLRP3/NACHT, LRR and PYD domains-containing protein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3779755] [GtoPdb: 1770] [UniProtKB: Q8R4B8] | ||||||||
| ChEMBL | Inhibition of NLRP3 inflammasome activation in LPS-primed mouse J774.A1 cells assessed as reduction in IL-1beta secretion preincubated for 1 hr followed by nigericin stimulation and measured after 1 hr by ELISA | B | 6.7 | pIC50 | 199.53 | nM | IC50 | J Med Chem (2022) 65: 11985-12001 [PMID:36063115] |
| nuclear factor kappa B subunit 1/nuclear factor kappa B subunit 2/RELA proto-oncogene, NF-kB subunit/Nuclear factor NF-kappa-B complex in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094258] [GtoPdb: 3281, 3282, 3280] [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 beta 1 proteasome (unknown origin) | B | 7.51 | pIC50 | 31 | nM | IC50 | J Med Chem (2021) 64: 2851-2877 [PMID:33656892] |
| 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 beta2 proteasome (unknown origin) | B | 5.46 | pIC50 | 3500 | nM | IC50 | J Med Chem (2021) 64: 2851-2877 [PMID:33656892] |
| 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 beta5 proteasome (unknown origin) | B | 8.47 | pIC50 | 3.4 | nM | IC50 | J Med Chem (2021) 64: 2851-2877 [PMID:33656892] |
| 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 | Inhibition of 20S proteasome beta5 subunit (unknown origin) using Suc-LLVY-AMC as flurogenic substrate measured after 1 hr by fluorescence based analysis | B | 8.54 | pIC50 | 2.88 | nM | IC50 | J Med Chem (2022) 65: 11985-12001 [PMID:36063115] |
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]
