MG-132 [Ligand Id: 8616] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL64925 (MG-132) |
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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 | Inhibition of the chymotrypsin-like activity of proteasome macropain. | - | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (2006) 49: 2953-68 [PMID:16686537] |
| ChEMBL | Inhibitory concentration to inhibit trypsin-like activity of 20S proteasome from human leukemia HL-60 cells was determined | F | 5.35 | pIC50 | 4500 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1867-1871 [PMID:15780623] |
| ChEMBL | Inhibitory concentration to inhibit the PGPH activity of 20S proteasome prepared from human leukemia HL-60 cells was determined | F | 5.85 | pIC50 | 1400 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1867-1871 [PMID:15780623] |
| ChEMBL | Inhibitory concentration to inhibit chymotrypsin-like activity of 20S proteasome prepared from human leukemia HL-60 cells was determined | F | 7.17 | pIC50 | 68 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1867-1871 [PMID:15780623] |
| calpain 2/Calpain 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2382] [GtoPdb: 2337] [UniProtKB: P17655] | ||||||||
| ChEMBL | Inhibition of m-calpain (unknown origin) using Suc-LY-AMC as substrate by fluorometric assay | B | 6.19 | pKi | 653 | nM | Ki | ACS Med Chem Lett (2016) 7: 250-255 [PMID:26985310] |
| Calpain-9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523126] [UniProtKB: O14815] | ||||||||
| ChEMBL | Inhibition of human recombinant mini-CAPN9 pre-incubated for 10 mins before calpain FRET peptide 5-FAM /QXL520 substrate addition by FLIPR assay | B | 5.01 | pIC50 | 9880 | nM | IC50 | US-20180318405-A1. Targeting capn9/capns2 activity as a therapeutic strategy for the treatment of myofibroblast differentiation and associated pathologies (null) |
| cathepsin B/Cathepsin B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4072] [GtoPdb: 2343] [UniProtKB: P07858] | ||||||||
| ChEMBL | Inhibition of human liver cathepsin B using Cbz-RR-AMC as substrate by fluorometric assay | B | 6.64 | pKi | 230 | nM | Ki | ACS Med Chem Lett (2016) 7: 250-255 [PMID:26985310] |
| ChEMBL | Inhibition of cathepsin B | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2006) 49: 2953-2968 [PMID:16686537] |
| cathepsin K/Cathepsin K in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL268] [GtoPdb: 2350] [UniProtKB: P43235] | ||||||||
| ChEMBL | The apparent binding affinity against cathepsin K. | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2000) 43: 305-341 [PMID:10669559] |
| NF-kappaB inhibitor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2898] [UniProtKB: P25963] | ||||||||
| ChEMBL | Induction of human IkappaBalpha stabilization in OCI-Ly3 cells assessed as ratio of green light emiting IkappaBalpha-fused luciferase expression to red light emiting native luciferase expression | B | 5.28 | pEC50 | 5200 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 329-335 [PMID:18024113] |
| ChEMBL | Induction of human IkappaBalpha stabilization in OCI-Ly3 cells by green light emiting IkappaBalpha-fused luciferase reporter gene assay | B | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 329-335 [PMID:18024113] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 cultured in human O+ erythrocytes after 50 to 60 hrs by ethidium bromide staining-based flow cytometric analysis | F | 7.46 | pIC50 | 35 | nM | IC50 | Bioorg Med Chem (2019) 27: 436-441 [PMID:30581047] |
| proteasome 20S subunit beta 1/Proteasome component C5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4208] [GtoPdb: 2404] [UniProtKB: P20618] | ||||||||
| ChEMBL | Inhibition of 20s constitutive proteasome beta1 caspase-like activity in human erythrocytes using Z-Leu-Leu-Glu-AMC as substrate after 10 mins by fluorescence assay | B | 4.66 | pKi | 22100 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 278-283 [PMID:29292224] |
| ChEMBL | Competitive inhibition of post-glutamyl peptide hydrolyzing activity of human 20S proteasome using Cbz-Leu-Leu-Glu-AMC as substrate measured for 10 mins by fluorescence assay | B | 5.26 | pKi | 5520 | nM | Ki | Eur J Med Chem (2016) 121: 578-591 [PMID:27318981] |
| ChEMBL | Inhibition of post glutamyl peptide hydrolase-like proteasome activity of human 20S proteasome | B | 6.33 | pKi | 470 | nM | Ki | J Med Chem (2006) 49: 2953-2968 [PMID:16686537] |
| ChEMBL | Inhibition of 20s immunoproteasome beta1 caspase-like activity in human spleen using Ac-Pro-Ala-Leu-AMC as substrate after 10 mins by fluorescence assay | B | 6.89 | pKi | 130 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 278-283 [PMID:29292224] |
| ChEMBL | Inhibition of 20S proteosome beta 1 purified from human HCT116 cells using Z-LLE-AMC as substrate incubated for 30 to 120 mins by fluorimetry | B | 5.84 | pIC50 | 1450 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1086-1092 [PMID:31312413] |
| ChEMBL | Inhibition of postacid activity of 20s proteasome beta-1 subunit in HEK293 cells using Z-nLPnLD-Glo as substrate incubated for 2 hrs prior to substrate addition measured after 10 mins by cell-based proteasome-Glo beta1 assay | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (2013) 56: 3367-3378 [PMID:23540790] |
| ChEMBL | Inhibition of caspase-like activity of beta1 subunit of 20S proteasome in human erythrocytes using Z-LLE-MCA as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured after 3 hrs by fluorescence spectrophotometeric analysis | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem (2019) 27: 115161-115161 [PMID:31732281] |
| ChEMBL | Inhibition of PGPH-like activity of human 20S proteasome beta 1 subunit assessed as hydrolysis of Z-LLE-AMC fluorogenic substrate measured for 1 hr by fluorometric analysis | B | 6.92 | pIC50 | 120 | nM | IC50 | Eur J Med Chem (2014) 71: 290-305 [PMID:24321833] |
| ChEMBL | Inhibition of caspase-like activity of 20S human proteasome assessed as Z-nLPnLD-AMC hydrolysis at using Promega proteasome-Glo-3 substrate incubated for 15 mins by luminescence assay | B | 7.36 | pIC50 | 44 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 2801-2805 [PMID:27158142] |
| proteasome 20S subunit beta 2/Proteasome Macropain subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3492] [GtoPdb: 2405] [UniProtKB: P49721] | ||||||||
| ChEMBL | Competitive inhibition of trypsin-like activity of human 20S proteasome using Boc-Leu-Arg-Arg-AMC as substrate measured for 10 mins by fluorescence assay | B | 4.66 | pKi | 22100 | nM | Ki | Eur J Med Chem (2016) 121: 578-591 [PMID:27318981] |
| ChEMBL | Inhibition of 20s constitutive proteasome beta2 trypsin-like activity in human erythrocytes using Boc-Leu-Arg-Arg-AMC as substrate after 10 mins by fluorescence assay | B | 5.26 | pKi | 5520 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 278-283 [PMID:29292224] |
| ChEMBL | Inhibition of trypsin-like proteasome activity of human 20S proteasome | B | 6.48 | pKi | 330 | nM | Ki | J Med Chem (2006) 49: 2953-2968 [PMID:16686537] |
| ChEMBL | Inhibition of 20s immunoproteasome beta2 trypsin-like activity in human spleen using Boc-Leu-Arg-Arg-AMC as substrate after 10 mins by fluorescence assay | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 278-283 [PMID:29292224] |
| ChEMBL | Inhibition of 20S proteosome beta 2 purified from human HCT116 cells using Boc-LRR-AMC as substrate incubated for 30 to 120 mins by fluorimetry | B | 5.34 | pIC50 | 4590 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1086-1092 [PMID:31312413] |
| ChEMBL | Inhibition of trypsin-like activity of human 20S proteasome beta 2 subunit assessed as hydrolysis of Boc-LRR-AMC fluorogenic substrate measured for 1 hr by fluorometric analysis | B | 5.68 | pIC50 | 2100 | nM | IC50 | Eur J Med Chem (2014) 71: 290-305 [PMID:24321833] |
| ChEMBL | Inhibition of trypsin-like activity of beta2 subunit of 20S proteasome in human erythrocytes using Boc-LRR-MCA as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured after 3 hrs by fluorescence spectrophotometric analysis | B | 5.8 | pIC50 | 1600 | nM | IC50 | Bioorg Med Chem (2019) 27: 115161-115161 [PMID:31732281] |
| ChEMBL | Inhibition of trypsin-like activity of 20S human proteasome assessed as Z-LRR-AMC hydrolysis at using Promega proteasome-Glo-3 substrate incubated for 15 mins by luminescence assay | B | 7.28 | pIC50 | 52 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 2801-2805 [PMID:27158142] |
| proteasome 20S subunit beta 5/Proteasome Macropain subunit MB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4662] [GtoPdb: 2406] [UniProtKB: P28074] | ||||||||
| ChEMBL | Inhibition of 20s immunoproteasome beta5 chymotrypsin-like activity in human spleen using Suc-Leu-Leu-Val-Tyr-AMC as substrate after 10 mins by fluorescence assay | B | 7.15 | pKi | 70 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 278-283 [PMID:29292224] |
| ChEMBL | Inhibition of 20s constitutive proteasome beta5 chymotrypsin-like activity in human erythrocytes using Suc-Leu-Leu-Val-Tyr-AMC as substrate after 10 mins by fluorescence assay | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 278-283 [PMID:29292224] |
| GtoPdb | Inhibition of the chymotrypsin-like activity of proteasome macropain. | - | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (2006) 49: 2953-68 [PMID:16686537] |
| ChEMBL | Inhibition of chymotrypsin-like proteasome activity of human 20S proteasome | B | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (2006) 49: 2953-2968 [PMID:16686537] |
| ChEMBL | Competitive inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate measured for 10 mins by fluorescence assay | B | 8.85 | pKi | 1.4 | nM | Ki | Eur J Med Chem (2016) 121: 578-591 [PMID:27318981] |
| ChEMBL | Inhibition of chymotrypsin-like activity of 20S human proteasome assessed as Suc-LLVY-AMC hydrolysis at using Promega proteasome-Glo-3 substrate incubated for 15 mins by luminescence assay | B | 7.43 | pIC50 | 37 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 2801-2805 [PMID:27158142] |
| ChEMBL | Inhibition of chymotrypsin-like activity of beta5 subunit of 20S proteasome in human erythrocytes using Suc-LLVY-MCA as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured after 3 hrs by fluorescence spectrophotometric analysis | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem (2019) 27: 115161-115161 [PMID:31732281] |
| ChEMBL | Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-LLVY-AMC as substrate by fluorometric method | B | 7.6 | pIC50 | 25 | nM | IC50 | Eur J Med Chem (2017) 126: 259-269 [PMID:27889629] |
| ChEMBL | Inhibition of chymotrypsin-like activity of human 20S proteasome beta 5 subunit assessed as hydrolysis of succinyl-LLVY-AMC fluorogenic substrate measured for 1 hr by fluorometric analysis | B | 7.96 | pIC50 | 11 | nM | IC50 | Eur J Med Chem (2014) 71: 290-305 [PMID:24321833] |
| ChEMBL | Inhibition of chymotrypsin-like activity of proteasome beta-5 subunit in HEK293 cells using Suc-LLVY-Glo as substrate incubated for 2 hrs prior to substrate addition measured after 10 mins by cell-based proteasome-Glo beta5 assay | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2013) 56: 3367-3378 [PMID:23540790] |
| ChEMBL | Inhibition of 20S proteosome beta 5 purified from human HCT116 cells using Suc-LLVY-AMC as substrate incubated for 30 to 120 mins by fluorimetry | B | 8.15 | pIC50 | 7 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1086-1092 [PMID:31312413] |
| ChEMBL | Inhibition of chymotrypsin like activity of 26S proteasome beta 5 subunit (unknown origin) by fluorescence assay | B | 8.92 | pIC50 | 1.2 | nM | IC50 | Bioorg Med Chem (2019) 27: 436-441 [PMID:30581047] |
| CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523582] [GtoPdb: 3125, 3139, 3206, 3261] [UniProtKB: P0DTD1] | ||||||||
| ChEMBL | Inhibition of SARS-CoV-2 3CLpro preincubated for 30 mins followed by addition of (Dabcyl)KTSAVLQSGFRKM(Glu) peptide substrate and measured after 1.5 hrs by FRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2021) 48: 128263-128263 [PMID:34271072] |
| ChEMBL | Inhibition of SARS-CoV-2 Main protease expressed in Escherichia coli BL21 (DE3) preincubated for 30 mins followed by addition of Dabcyl-KTSAVLQ/SGFRKME(Edans) substrate and measured after 1 hr by FRET assay | B | 5.41 | pIC50 | 3900 | nM | IC50 | Bioorg Med Chem Lett (2021) 48: 128263-128263 [PMID:34271072] |
| CoV 3C-like (main) protease in SARS-CoV-2 [GtoPdb: 3111] | ||||||||
| GtoPdb | - | - | 5.41 | pIC50 | 3900 | nM | IC50 | Cell Res (2020) 30: 678-692 [PMID:32541865] |
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]
