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

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ChEMBL ligand: CHEMBL325041 (Bortezomib, Bortezomib accord, Bortezomib hydrate, LDP-341, NSC-681239, PS-341, Velcade)
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  • ATP-dependent Clp protease proteolytic subunit in Staphylococcus aureus (strain NCTC 8325) [ChEMBL: CHEMBL1932910] [UniProtKB: Q2G036]
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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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  • histone deacetylase 1/Histone deacetylase 1 in Human [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
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  • histone deacetylase 2/Histone deacetylase 2 in Human [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
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  • histone deacetylase 3/Histone deacetylase 3 in Human [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379]
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  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
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  • histone deacetylase 8/Histone deacetylase 8 in Human [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
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  • elastase, neutrophil expressed/Leukocyte elastase in Human [ChEMBL: CHEMBL248] [GtoPdb: 2358] [UniProtKB: P08246]
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  • lon peptidase 1, mitochondrial/Lon protease homolog, mitochondrial in Human [ChEMBL: CHEMBL4879436] [GtoPdb: 3180] [UniProtKB: P36776]
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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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  • proteasome 20S subunit beta 9/Proteasome subunit beta type-9 in Human [ChEMBL: CHEMBL1944495] [GtoPdb: 2409] [UniProtKB: P28065]
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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 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: 240424082409240724062405] [UniProtKB: A5LHX3O14818P20618P25786P25787P25788P25789P28062P28065P28066P28070P28072P28074P40306P49720P49721P60900Q8TAA3Q99436]
ChEMBL Inhibition of human erythrocytes 20S proteasome using QXL520-YRGITCSGRQK(5-FAM)-NH2 fluorogenic peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by HTRF assay B 7.01 pIC50 97 nM IC50 J Med Chem (2021) 64: 4857-4869 [PMID:33821636]
GtoPdb - - 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2009) 19: 3220-4 [PMID:19428245]
ChEMBL Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate addition B 7.97 pIC50 10.8 nM IC50 Eur J Med Chem (2019) 164: 602-614 [PMID:30639896]
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]
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 4.63 pEC50 23500 nM EC50 J Med Chem (2020) 63: 3104-3119 [PMID:32031798]
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]
histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
ChEMBL Inhibition of HDAC1 in human RPMI-8226 cells incubated for 2 hrs by ELISA B 6.21 pIC50 620