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 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 | 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 (2018) |
| 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] |
| cathepsin L/Cathepsin L in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3837] [GtoPdb: 2351] [UniProtKB: P07711] | ||||||||
| ChEMBL | Inhibition of Cathepsin L (unknown origin) preincubated for 30 mins followed by fluorogenic substrate addition and measured for 15 mins by fluorescence microplate reader analysis | B | 9.82 | pIC50 | 0.15 | nM | IC50 | J Med Chem (2022) 65: 12500-12534 [PMID:36169610] |
| 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] |
| 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 TNF-alpha induced NFkappaB activation in HEK293T cells transfected with kappaB-luciferase/pTK-renilla reporters pretreated for 6 hrs followed by stimulation of TNFalpha and measured after 2 hrs by Dual Luciferase Reporter Assay | B | 5.44 | pIC50 | 3600 | nM | IC50 | J Nat Prod (2023) 86: 1449-1462 [PMID:37243616] |
| 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 | Inhibition of 20S constitutive proteosome beta1c subunit (unknown origin) assessed as substrate hydrolysis using Z-Leu-Leu-Leu-al as substrate | B | 4.66 | pKi | 22100 | nM | Ki | Bioorg Med Chem Lett (2022) 55: 128478-128478 [PMID:34838650] |
| 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 immuno proteosome beta1i subunit (unknown origin) assessed as substrate hydrolysis using Z-Leu-Leu-Leu-al as substrate | B | 6.89 | pKi | 130 | nM | Ki | Bioorg Med Chem Lett (2022) 55: 128478-128478 [PMID:34838650] |
| 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 beta 1 proteasome (unknown origin) | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2021) 64: 2851-2877 [PMID:33656892] |
| 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 20S constitutive proteosome beta2c subunit (unknown origin) assessed as substrate hydrolysis using Z-Leu-Leu-Leu-al as substrate | B | 5.26 | pKi | 5520 | nM | Ki | Bioorg Med Chem Lett (2022) 55: 128478-128478 [PMID:34838650] |
| 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 immuno proteosome beta2i subunit (unknown origin) assessed as substrate hydrolysis using Z-Leu-Leu-Leu-al as substrate | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2022) 55: 128478-128478 [PMID:34838650] |
| 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 beta2 proteasome (unknown origin) | B | 5.97 | pIC50 | 1080 | nM | IC50 | J Med Chem (2021) 64: 2851-2877 [PMID:33656892] |
| 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 20S constitutive proteosome beta5c subunit (unknown origin) assessed as substrate hydrolysis using Z-Leu-Leu-Leu-al as substrate | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2022) 55: 128478-128478 [PMID:34838650] |
| 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 beta5 proteasome (unknown origin) | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2021) 64: 2851-2877 [PMID:33656892] |
| 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) using DABCYL-KTSAVLQSGFRKM-EDANS as substrate preincubated for 1 hr followed by substrate addition and measured after 15 mins by FRET assay | B | 5.13 | pIC50 | 7400 | nM | IC50 | J Med Chem (2022) 65: 12500-12534 [PMID:36169610] |
| 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] |
| ChEMBL | Inhibition of SARS-CoV-2 MPro | B | 5.41 | pIC50 | 3900 | nM | IC50 | Bioorg Med Chem (2021) 29: 115860-115860 [PMID:33191083] |
| ChEMBL | Inhibition of SARS-CoV-2 Main protease | B | 5.41 | pIC50 | 3900 | nM | IC50 | Eur J Med Chem (2023) 257: 115491-115491 [PMID:37244162] |
| ChEMBL | Inhibition of SARS-CoV-2 MPro | B | 5.41 | pIC50 | 3899.42 | nM | IC50 | Bioorg Med Chem (2021) 29: 115860-115860 [PMID:33191083] |
| 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 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]
