bortezomib [Ligand Id: 6391] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL325041 (Bortezomib hydrate, Bortezomib, PS-341, Velcade, NSC-681239, LDP-341)
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  • carbonic anhydrase 1/Carbonic anhydrase I in Human [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
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  • carbonic anhydrase 2/Carbonic anhydrase II in Human [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
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  • carbonic anhydrase 4/Carbonic anhydrase IV in Human [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748]
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  • carbonic anhydrase 9/Carbonic anhydrase IX in Human [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790]
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  • carbonic anhydrase 5A/Carbonic anhydrase VA in Human [ChEMBL: CHEMBL4789] [GtoPdb: 3093] [UniProtKB: P35218]
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  • carbonic anhydrase 7/Carbonic anhydrase VII in Human [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166]
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  • carbonic anhydrase 12/Carbonic anhydrase XII in Human [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570]
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  • carbonic anhydrase 13/Carbonic anhydrase XIII in Human [ChEMBL: CHEMBL3912] [GtoPdb: 2748] [UniProtKB: Q8N1Q1]
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  • carbonic anhydrase 14/Carbonic anhydrase XIV in Human [ChEMBL: CHEMBL3510] [GtoPdb: 2598] [UniProtKB: Q9ULX7]
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  • elastase, neutrophil expressed/Leukocyte elastase in Human [ChEMBL: CHEMBL248] [GtoPdb: 2358] [UniProtKB: P08246]
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  • Cathepsin A/Lysosomal protective protein in Human [ChEMBL: CHEMBL6115] [GtoPdb: 1581] [UniProtKB: P10619]
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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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  • proteasome 20S subunit beta 8/Proteasome subunit beta type-8 in Human [ChEMBL: CHEMBL5620] [GtoPdb: 2408] [UniProtKB: P28062]
  • proteasome 20S subunit beta 8/Proteasome subunit beta type-8 in Mouse [ChEMBL: CHEMBL1944492] [GtoPdb: 2408] [UniProtKB: P28063]
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  • coagulation factor II, thrombin/Thrombin in Human [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
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  • Uncharacterized protein Rv1284/MT1322 in Mycobacterium tuberculosis [ChEMBL: CHEMBL5631] [UniProtKB: P9WPJ7]
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  • Plasmodium falciparum proteasome subunit beta type-5 in Plasmodium falciparum W2 [GtoPdb: 3088]
  • Plasmodium falciparum proteasome subunit beta type-5 in Plasmodium falciparum [GtoPdb: 3088]
  • Plasmodium falciparum proteasome subunit beta type-5 in Plasmodium falciparum 3D7 [GtoPdb: 3088] [UniProtKB: Q8IJT1]
  • Plasmodium falciparum proteasome subunit beta type-5 in Plasmodium falciparum Dd2 [GtoPdb: 3088]
  • Plasmodium falciparum proteasome subunit beta type-5 in Plasmodium falciparum HB3 [GtoPdb: 3088]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
proteasome 26S subunit, non-ATPase 14/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 2/26S proteasome in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2364701] [GtoPdb: 2410240424082409240724062405] [UniProtKB: A5LHX3O00231O00232O00487O14818O43242P17980P20618P25786P25787P25788P25789P28062P28065P28066P28070P28072P28074P35998P40306P43686P48556P49720P49721P51665P55036P60896P60900P62191P62195P62333Q13200Q15008Q16186Q8TAA3Q99436Q99460Q9UNM6]
ChEMBL Inhibition of trypsin-like activity of human 20S proteasome using Ac-RLR-AMC as substrate B 5.7 pIC50 2000 nM IC50 J. Med. Chem. (2014) 57: 2726-2735 [PMID:24524217]
ChEMBL Inhibition of caspase-like activity of human 20S proteasome using Ac-nLPnLD-AMC as substrate B 6.92 pIC50 120 nM IC50 J. Med. Chem. (2014) 57: 2726-2735 [PMID:24524217]
GtoPdb - - 7.7 pIC50 20 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 3220-4 [PMID:19428245]
ChEMBL Inhibition of chymotrypsin-like enzyme activity of purified human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate by fluorescence method B 8.15 pIC50 7.14 nM IC50 Bioorg. Med. Chem. (2014) 22: 2955-2965 [PMID:24767818]
ChEMBL Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-LLVY-AMC as substrate B 8.15 pIC50 7 nM IC50 J. Med. Chem. (2014) 57: 2726-2735 [PMID:24524217]
ChEMBL Inhibition of human 20S proteasome using Suc-LLVY-AMC as substrate preincubated for 30 mins followed by substrate addition measured after 90 mins by fluorescence assay B 8.59 pIC50 2.56 nM IC50 MedChemComm (2011) 2: 1083-1086
Alpha-chymotrypsin in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3314] [UniProtKB: P00766]
ChEMBL Inhibition of bovine pancreatic alpha-chymotrypsin using Suc-Leu-Leu-Val-Tyr-AMC as substrate by fluorescence assay B 5.62 pKi 2400 nM Ki Eur. J. Med. Chem. (2014) 83: 1-14 [PMID:24946214]
Beta-chymotrypsin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4796] [UniProtKB: P17538]
ChEMBL Inhibitory activity against human Chymotrypsinogen B 6.49 pKi 320 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 333-338 [PMID:9871680]
Carbonic anhydrase 15 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5973] [UniProtKB: Q99N23]
ChEMBL Inhibition of mouse CA15 by stopped-flow CO2 hydrase assay B 5.57 pKi 2680 nM Ki Bioorg Med Chem (2017) 25: 5064-5067 [PMID:28277280]
carbonic anhydrase 1/Carbonic anhydrase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
ChEMBL Inhibition of human carbonic anhydrase-1 preincubated for 15 mins by stopped-flow CO2 hydration assay B 5.89 pKi 1290 nM Ki Bioorg. Med. Chem. (2016) 24: 4406-4409 [PMID:27469982]
ChEMBL Inhibition of human CA1 by stopped-flow CO2 hydrase assay B 5.89 pKi 1290 nM Ki Bioorg Med Chem (2017) 25: 5064-5067 [PMID:28277280]
carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
ChEMBL Inhibition of human carbonic anhydrase-2 preincubated for 15 mins by stopped-flow CO2 hydration assay B 5.94 pKi 1160 nM Ki Bioorg. Med. Chem. (2016) 24: 4406-4409 [PMID:27469982]
ChEMBL Inhibition of human CA2 by stopped-flow CO2 hydrase assay B 5.94 pKi 1160 nM Ki Bioorg Med Chem (2017) 25: 5064-5067 [PMID:28277280]
Carbonic anhydrase III in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2885] [UniProtKB: P07451]
ChEMBL Inhibition of human CA3 by stopped-flow CO2 hydrase assay B 5.34 pKi 4570 nM Ki Bioorg Med Chem (2017) 25: 5064-5067 [PMID:28277280]
carbonic anhydrase 4/Carbonic anhydrase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748]
ChEMBL Inhibition of human CA4 by stopped-flow CO2 hydrase assay B 5.19 pKi 6510 nM Ki Bioorg Med Chem (2017) 25: 5064-5067 [PMID:28277280]
carbonic anhydrase 9/Carbonic anhydrase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790]
ChEMBL Inhibition of human CA9 by stopped-flow CO2 hydrase assay B 5.47 pKi 3380 nM Ki Bioorg Med Chem (2017) 25: 5064-5067 [PMID:28277280]
carbonic anhydrase 5A/Carbonic anhydrase VA in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4789] [GtoPdb: 3093] [UniProtKB: P35218]
ChEMBL Inhibition of human CA5A by stopped-flow CO2 hydrase assay B 5.16 pKi 6920 nM Ki Bioorg Med Chem (2017) 25: 5064-5067 [PMID:28277280]
Carbonic anhydrase VB in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3969] [UniProtKB: Q9Y2D0]
ChEMBL Inhibition of human CA5B by stopped-flow CO2 hydrase assay B 5.17 pKi 6830 nM Ki Bioorg Med Chem (2017) 25: 5064-5067 [PMID:28277280]
Carbonic anhydrase VI in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3025] [UniProtKB: P23280]
ChEMBL Inhibition of human CA6 by stopped-flow CO2 hydrase assay B 5.36 pKi 4380 nM Ki Bioorg Med Chem (2017) 25: 5064-5067 [PMID:28277280]
carbonic anhydrase 7/Carbonic anhydrase VII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166]
ChEMBL Inhibition of human CA7 by stopped-flow CO2 hydrase assay B 5.16 pKi 6940 nM Ki Bioorg Med Chem (2017) 25: 5064-5067 [PMID:28277280]
carbonic anhydrase 12/Carbonic anhydrase XII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570]
ChEMBL Inhibition of human CA12 by stopped-flow CO2 hydrase assay B 5.23 pKi 5870 nM Ki Bioorg Med Chem (2017) 25: 5064-5067 [PMID:28277280]
carbonic anhydrase 13/Carbonic anhydrase XIII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3912] [GtoPdb: 2748] [UniProtKB: Q8N1Q1]
ChEMBL Inhibition of human CA13 by stopped-flow CO2 hydrase assay B 5.07 pKi 8450 nM Ki Bioorg Med Chem (2017) 25: 5064-5067 [PMID:28277280]
carbonic anhydrase 14/Carbonic anhydrase XIV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3510] [GtoPdb: 2598] [UniProtKB: Q9ULX7]
ChEMBL Inhibition of human CA14 by stopped-flow CO2 hydrase assay B 5.48 pKi 3280 nM Ki Bioorg Med Chem (2017) 25: 5064-5067 [PMID:28277280]
cathepsin B/Cathepsin B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4072] [GtoPdb: 2343] [UniProtKB: P07858]
ChEMBL Inhibition of recombinant cathepsin B (unknown origin) using Z-Leu-Arg-AMC as substrate by spectrofluorometer analysis B 4.52 pIC50 >30000 nM IC50 J. Med. Chem. (2014) 57: 2726-2735 [PMID:24524217]
cathepsin G/Cathepsin G in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4071] [GtoPdb: 2348] [UniProtKB: P08311]
ChEMBL Inhibitory activity against human cathepsin G B 6.2 pKi 630 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 333-338 [PMID:9871680]
ChEMBL Inhibition of recombinant cathepsin G (unknown origin) using Suc-Ala-Ala-Pro-Phe-AMC as substrate by spectrofluorometer analysis B 5.51 pIC50 3100 nM IC50 J. Med. Chem. (2014) 57: 2726-2735 [PMID:24524217]
ChEMBL Inhibition of human cathepsin G B 6.28 pIC50 520 nM IC50 J. Med. Chem. (2008) 51: 1068-1072 [PMID:18247547]
chymase 1/Chymase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4068] [GtoPdb: 2340] [UniProtKB: P23946]
ChEMBL Inhibition of human chymase B 5.92 pIC50 1190 nM IC50 J. Med. Chem. (2008) 51: 1068-1072 [PMID:18247547]
elastase, neutrophil expressed/Leukocyte elastase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL248] [GtoPdb: 2358] [UniProtKB: P08246]
ChEMBL Inhibitory activity against human leukocyte elastase B 5.64 pKi 2300 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 333-338 [PMID:9871680]
Cathepsin A/Lysosomal protective protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6115] [GtoPdb: 1581] [UniProtKB: P10619]
ChEMBL Inhibition of recombinant cathepsin A (unknown origin) using Mca-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys(Dnp)-OH as substrate incubated with enzyme for 5 mins prior to substrate challenge for 2 hrs by spectrofluorometer analysis B 5.04 pIC50 9200 nM IC50 J. Med. Chem. (2014) 57: 2726-2735 [PMID:24524217]
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 8.01 pIC50 9.7 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 Inhibition of PGPH activity of human 20S proteasome using Z-LLE-MCA as substrate measured for 1 hr by fluorescence assay B 6.15 pIC50 700 nM IC50 Eur J Med Chem (2018) 146: 636-650 [PMID:29407987]
ChEMBL Inhibition of caspase-like activity of human 20S proteasome beta 1 subunit using Ac-nLPnLD-AMC as substrate after 60 mins by fluorescence assay B 6.89 pIC50 130 nM IC50 J. Med. Chem. (2013) 56: 3689-3700 [PMID:23547757]
ChEMBL Inhibition of caspase-like activity of human 20S proteasome B 7.02 pIC50 96.5 nM IC50 Bioorg Med Chem (2018) 26: 3975-3981 [PMID:29934218]
ChEMBL Reversible inhibition of human erythrocyte derived 20S proteasome subunit beta1 after 30 mins by fluorogenic assay B 7.28 pIC50 53 nM IC50 J. Med. Chem. (2012) 55: 10317-10327 [PMID:22978849]
ChEMBL Inhibition of caspase-like activity of 20S proteasome in human HL60 cells using Z-nLPnLDaminoluciferin as substrate after 2 hrs by fluorescence analysis B 7.52 pIC50 30 nM IC50 Eur J Med Chem (2017) 125: 925-939 [PMID:27769033]
ChEMBL Inhibition of PGPH activity of human 26S proteasome using Z-LLE-MCA as substrate measured for 1 hr by fluorescence assay B 7.72 pIC50 19 nM IC50 Eur J Med Chem (2018) 146: 636-650 [PMID:29407987]
proteasome 20S subunit beta 2/Proteasome Macropain subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3492] [GtoPdb: 2405] [UniProtKB: P49721]
ChEMBL Inhibition of trypsin-like activity of human 26S proteasome using Boc-LRR-MCA as substrate measured for 1 hr by fluorescence assay B 4.4 pIC50 >40000 nM IC50 Eur J Med Chem (2018) 146: 636-650 [PMID:29407987]
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 Inhibition of trypsin-like activity of human 20S proteasome B 5.4 pIC50 3998 nM IC50 Bioorg Med Chem (2018) 26: 3975-3981 [PMID:29934218]
ChEMBL Inhibition of trypsin-like activity of human 20S proteasome using Boc-LRR-MCA as substrate measured for 1 hr by fluorescence assay B 5.71 pIC50 1930 nM IC50 Eur J Med Chem (2018) 146: 636-650 [PMID:29407987]
ChEMBL Inhibition of trypsin-like activity of human 20S proteasome beta 2 subunit using Ac-RLR-AMC as substrate after 60 mins by fluorescence assay B 5.73 pIC50 1880 nM IC50 J. Med. Chem. (2013) 56: 3689-3700 [PMID:23547757]
ChEMBL Reversible inhibition of human erythrocyte derived 20S proteasome subunit beta2 after 30 mins by fluorogenic assay B 6.23 pIC50 590 nM IC50 J. Med. Chem. (2012) 55: 10317-10327 [PMID:22978849]
ChEMBL Inhibition of trypsin-like activity of 20S proteasome in human HL60 cells using Z-LRRaminoluciferin as substrate after 2 hrs by fluorescence analysis B 6.36 pIC50 440 nM IC50 Eur J Med Chem (2017) 125: 925-939 [PMID:27769033]
proteasome 20S subunit beta 5/Proteasome Macropain subunit MB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4662] [GtoPdb: 2406] [UniProtKB: P28074]
ChEMBL Inhibition of chymotrypsin-like activity of human 20S proteasome beta 5 subunit assessed as Suc-Leu-Leu-Val-Tyr-AMC substrate hydrolysis after 10 mins by fluorometric analysis B 8.01 pKi 9.8 nM Ki Eur. J. Med. Chem. (2014) 76: 1-9 [PMID:24561716]
ChEMBL Inhibition of chymotrypsin-like activity of 20S proteasome in human erythrocytes using Suc-Leu-Leu-Val-Tyr-AMC as substrate by fluorescence assay B 8.01 pKi 9.8 nM Ki Eur. J. Med. Chem. (2014) 83: 1-14 [PMID:24946214]
ChEMBL Inhibition of human 20S proteasome chymotrypsin like activity using Suc-Leu-Leu-Val-Tyr-AMC as substrate measured over 10 mins by fluorescence assay B 9.22 pKi 0.6 nM Ki Eur. J. Med. Chem. (2013) 64: 23-34 [PMID:23639651]
ChEMBL Inhibition of 20S proteasome beta5 subunit (unknown origin) assessed as formation of reversible adduct with N-terminal threonine B 9.26 pKi 0.55 nM Ki MedChemComm (2012) 3: 710-719
ChEMBL Inhibition of chymotrypsin-like activity of human 26S proteasome using Suc-LLVY-MCA as substrate measured for 1 hr by fluorescence assay B 5.68 pIC50 2100 nM IC50 Eur J Med Chem (2018) 146: 636-650 [PMID:29407987]
ChEMBL Inhibition of beta5 subunit of immunoproteasome (unknown origin) by active-site ELISA B 6.85 pIC50 140 nM IC50 J. Med. Chem. (2014) 57: 2726-2735 [PMID:24524217]
ChEMBL Inhibition of chymotrypsin-like activity of 20S proteasome in imatinib-resistant human SUP-B15 cells using Suc-LLVY aminoluciferin as substrate after 2 hrs by proteasome-Glo assay B 7.55 pIC50 28.09 nM IC50 J Med Chem (2018) 61: 10299-10309 [PMID:30365892]
GtoPdb - - 7.7 pIC50 20 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 3220-4 [PMID:19428245]
ChEMBL Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate after 1 hr by fluorescence analysis B 8.08 pIC50 8.3 nM IC50 Bioorg Med Chem Lett (2018) 28: 2148-2152 [PMID:29773504]
ChEMBL Reversible inhibition of human erythrocyte derived 20S proteasome subunit beta5 after 30 mins by fluorogenic assay B 8.1 pIC50 7.9 nM IC50 J. Med. Chem. (2012) 55: 10317-10327 [PMID:22978849]
ChEMBL Inhibition of chymotrypsin like activity of human erythrocyte-derived 20S proteasome preincubated for 10 mins using Suc-LLVY-AMC as substrate after 60 mins by fluorescence assay B 8.15 pIC50 7.09 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 1958-1962 [PMID:26965867]
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 8.15 pIC50 7.04 nM IC50 Bioorg Med Chem (2018) 26: 3975-3981 [PMID:29934218]
ChEMBL Inhibition of chymotrypsin-like activity of 20S proteasome in human HL60 cells using Suc-LLVY aminoluciferin as substrate after 2 hrs by proteasome-Glo assay B 8.18 pIC50 6.67 nM IC50 J Med Chem (2018) 61: 10299-10309 [PMID:30365892]
ChEMBL Inhibition of human 20S proteasome chymotryptic-like activity using Suc-LLVY-AMC as substrate measured for 30 mins by fluorescence assay B 8.21 pIC50 6.2 nM IC50 Bioorg. Med. Chem. (2016) 24: 2441-2450 [PMID:27112450]
ChEMBL Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate by fluorescence assay B 8.33 pIC50 4.68 nM IC50 Eur J Med Chem (2017) 128: 180-191 [PMID:28182990]
ChEMBL Inhibition of chymotrypsin-like activity of human 20S proteasome beta 5 subunit using Suc-LLVY-AMC as substrate after 60 mins by fluorescence assay B 8.35 pIC50 4.5 nM IC50 J. Med. Chem. (2013) 56: 3689-3700 [PMID:23547757]
ChEMBL Inhibition of chymotrypsin-like activity of 20S proteasome in human SEM cells using Suc-LLVY aminoluciferin as substrate after 2 hrs by proteasome-Glo assay B 8.35 pIC50 4.43 nM IC50 J Med Chem (2018) 61: 10299-10309 [PMID:30365892]
ChEMBL Inhibition of chymotrypsin-like activity of 26S proteasome beta 5 subunit in human U266 cells using Suc-LLVY-aminoluciferin as substrate after 1 hr by Proteosome-Glo luminescence assay B 8.4 pIC50 4 nM IC50 Eur J Med Chem (2017) 135: 142-158 [PMID:28441582]
ChEMBL Inhibition of chymotrypsin-like activity of 20S proteasome in human HL60 cells using Suc-LLVYaminoluciferin as substrate pretreated for 2 hrs followed by substrate addition by fluorescence assay B 8.4 pIC50 4 nM IC50 Bioorg Med Chem (2017) 25: 4031-4044 [PMID:28634039]
ChEMBL Inhibition of chymotrypsin-like activity of 20S proteasome in human HL60 cells using Suc-LLVYaminoluciferin as substrate after 2 hrs by fluorescence analysis B 8.4 pIC50 4 nM IC50 Eur J Med Chem (2017) 125: 925-939 [PMID:27769033]
ChEMBL Inhibition of 26S proteasome beta5 subunit in human Calu6 cells using Suc-LLVY-aminoluciferin as substrate after 1hr by luminescence assay B 8.41 pIC50 3.9 nM IC50 MedChemComm (2012) 3: 710-719
ChEMBL Inhibition of 20S proteasome beta5 subunit in human erythrocytes using Ac-WLA-AMC as substrate by fluorescence assay B 8.7 pIC50 2 nM IC50 MedChemComm (2012) 3: 710-719
ChEMBL Inhibition of chymotrypsin like activity of human 20S proteasome using ZGlyGlyLeuAMC/SucLeuLeuValTyrAMC as substrate measured every minute for 25 mins by fluorescence assay B 8.72 pIC50 1.9 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 1958-1962 [PMID:26965867]
ChEMBL Inhibition of chymotrypsin like activity of human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by spectrofluorimetric analysis B 8.72 pIC50 1.9 nM IC50 Bioorg. Med. Chem. (2016) 24: 2576-2588 [PMID:27117691]
ChEMBL Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-LLVY-MCA as substrate measured for 1 hr by fluorescence assay B 9.3 pIC50 0.5 nM IC50 Eur J Med Chem (2018) 146: 636-650 [PMID:29407987]
proteasome 20S subunit beta 8/Proteasome subunit beta type-8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5620] [GtoPdb: 2408] [UniProtKB: P28062]
ChEMBL Inhibition of beta5i subunit of immunoproteasome (unknown origin) by active-site ELISA B 7.11 pIC50 78 nM IC50 J. Med. Chem. (2014) 57: 2726-2735 [PMID:24524217]
ChEMBL Inhibition of chymotrypsin-like activity of LMP7 immunoproteasome by proteasome active site ELISA B 8.09 pIC50 8.1 nM IC50 J. Med. Chem. (2009) 52: 3028-3038 [PMID:19348473]
proteasome 20S subunit beta 8/Proteasome subunit beta type-8 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944492] [GtoPdb: 2408] [UniProtKB: P28063]
ChEMBL Inhibition of chymotrypsin like activity of mouse spleen 20S proteasome beta5i subunit using Suc-Leu-Leu-Val-Tyr-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 2 hrs by fluorescence-based assay B 7.77 pIC50 16.8 nM IC50 ACS Med Chem Lett (2016) 7: 1039-1043 [PMID:27994734]
coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
ChEMBL Inhibitory activity against thrombin B