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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| 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] | ||||||||
| 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: 2410, 2404, 2408, 2409, 2407, 2406, 2405] [UniProtKB: A5LHX3, O00231, O00232, O00487, O14818, O43242, P17980, P20618, P25786, P25787, P25788, P25789, P28062, P28065, P28066, P28070, P28072, P28074, P35998, P40306, P43686, P48556, P49720, P49721, P51665, P55036, P60896, P60900, P62191, P62195, P62333, Q13200, Q15008, Q16186, Q8TAA3, Q99436, Q99460, Q9UNM6] | ||||||||
| 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] |
| chymotrypsinogen B1/Beta-chymotrypsin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4796] [GtoPdb: 3272] [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 | nM | IC50 | Eur J Med Chem (2020) 189: 112062-112062 [PMID:31986406] |
| histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769] | ||||||||
| ChEMBL | Inhibition of HDAC2 in human RPMI-8226 cells incubated for 2 hrs by ELISA | B | 6.1 | pIC50 | 800 | nM | IC50 | Eur J Med Chem (2020) 189: 112062-112062 [PMID:31986406] |
| histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379] | ||||||||
| ChEMBL | Inhibition of HDAC3 in human RPMI-8226 cells incubated for 2 hrs by ELISA | B | 5.93 | pIC50 | 1180 | nM | IC50 | Eur J Med Chem (2020) 189: 112062-112062 [PMID:31986406] |
| histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
| ChEMBL | Inhibition of HDAC6 in human RPMI-8226 cells incubated for 2 hrs by ELISA | B | 4.16 | pIC50 | 69440 | nM | IC50 | Eur J Med Chem (2020) 189: 112062-112062 [PMID:31986406] |
| histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41] | ||||||||
| ChEMBL | Inhibition of HDAC8 in human RPMI-8226 cells incubated for 2 hrs by ELISA | B | 7.14 | pIC50 | 72 | nM | IC50 | Eur J Med Chem (2020) 189: 112062-112062 [PMID:31986406] |
| 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] |
| lon peptidase 1, mitochondrial/Lon protease homolog, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879436] [GtoPdb: 3180] [UniProtKB: P36776] | ||||||||
| ChEMBL | Inhibition of LONP1 (unknown origin) using QXL520-YRGITCSGRQK(5-FAM)-NH2 peptide as substrate incubated for 50 mins in presence of ATP by HTRF assay | B | 6.74 | pIC50 | 183 | nM | IC50 | J Med Chem (2021) 64: 4857-4869 [PMID:33821636] |
| 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: P19838, Q00653, Q04206] | ||||||||
| ChEMBL | Inhibition of TNFalpha-induced NFkappaB activation in HEK293 cells assessed as luciferase expression by luciferase reporter activity assay | B | 7.07 | pIC50 | 85 | nM | IC50 | Bioorg Med Chem Lett (2021) 42: 128042-128042 [PMID:33862226] |
| 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 |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antimalarial activity against erythrocytic stage of Plasmodium falciparum Dd2 harboring 20S beta5 proteasome A49S mutant measured after 72 hrs by SYBR green dye based fluorescence assay | F | 5.99 | pEC50 | 1024 | nM | EC50 | J Med Chem (2019) 62: 6137-6145 [PMID:31177777] |
| ChEMBL | Antimalarial activity against erythrocytic stage of Plasmodium falciparum Dd2 measured after 72 hrs by SYBR green dye based fluorescence assay | F | 6.38 | pEC50 | 419 | nM | EC50 | J Med Chem (2019) 62: 6137-6145 [PMID:31177777] |
| ChEMBL | Antimalarial activity against erythrocytic stage of Plasmodium falciparum Dd2 harboring 20S beta2 proteasome A117D mutant measured after 72 hrs by SYBR green dye based fluorescence assay | F | 6.97 | pEC50 | 106 | nM | EC50 | J Med Chem (2019) 62: 6137-6145 [PMID:31177777] |
| 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 human hepatic cell derived 20s constitutive proteasome beta1 caspase-like activity using Suc-LLE-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay | B | 6.98 | pIC50 | 104 | nM | IC50 | Eur J Med Chem (2019) 164: 423-439 [PMID:30611983] |
| 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 | Inhibition of human 20S constitutive proteasome beta 1 subunit caspase-like activity using fluorogenic peptide Ac-nLPnLD-AMC as substrate in presence of PA28alpha incubated for 1 to 2 hrs by fluorescence microplate reader assay | B | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2018) 61: 10053-10066 [PMID:30373366] |
| ChEMBL | Inhibition of 20S proteasome beta 1c (unknown origin) after 1 hr by fluorescence based assay | B | 7.15 | pIC50 | 70 | nM | IC50 | Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028] |
| 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 human hepatic cell derived 20s constitutive proteasome beta2 trypsin-like activity using Suc-LLE-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay | B | 5.67 | pIC50 | 2119 | nM | IC50 | Eur J Med Chem (2019) 164: 423-439 [PMID:30611983] |
| 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 | Inhibition of 20S proteasome beta 2c (unknown origin) after 1 hr by fluorescence based assay | B | 5.82 | pIC50 | 1500 | nM | IC50 | Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028] |
| ChEMBL | Inhibition of human 20S constitutive proteasome beta 2 subunit trypsin-like activity using fluorogenic peptide Ac-WLR-AMC as substrate in presence of PA28alpha incubated for 1 to 2 hrs by fluorescence microplate reader assay | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2018) 61: 10053-10066 [PMID:30373366] |
| 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] |
| ChEMBL | Inhibition of human 20s proteasome subunit beta2 caspase-like activity using Z-LLE-AMC as substrate preincubated for 15 mins followed by substrate addition | B | 6.89 | pIC50 | 128 | nM | IC50 | Eur J Med Chem (2019) 164: 602-614 [PMID:30639896] |
| 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 human hepatic cell derived 20s constitutive proteasome beta5 chymotrypsin-like activity using Suc-WLA-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay | B | 7.96 | pIC50 | 11 | nM | IC50 | Eur J Med Chem (2019) 164: 423-439 [PMID:30611983] |
| ChEMBL | Inhibition of human 20s constitutive proteasome beta5 chymotrypsin-like activity using Suc-LLVY-AMC as substrate 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] |
| 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 20S proteasome beta 5c (unknown origin) after 1 hr by fluorescence based assay | B | 8.15 | pIC50 | 7 | nM | IC50 | Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028] |
| 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 human 20S constitutive proteasome beta 5 subunit chymotrypsin-like activity using fluorogenic peptide Ac-WLA-AMC as substrate in presence of PA28alpha incubated for 1 to 2 hrs by fluorescence microplate reader assay | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2018) 61: 10053-10066 [PMID:30373366] |
| 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 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 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 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 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 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-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 subunit beta type-10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3317334] [UniProtKB: P40306] | ||||||||
| ChEMBL | Inhibition of 20S proteasome beta 2i (unknown origin) after 1 hr by fluorescence based assay | B | 6.03 | pIC50 | 940 | nM | IC50 | Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028] |
| ChEMBL | Inhibition of human 20S immunoproteasome beta 2 subunit trypsin-like activity using fluorogenic peptide Ac-WLR-AMC as substrate in presence of PA28alpha incubated for 1 to 2 hrs by fluorescence microplate reader assay | B | 6.27 | pIC50 | 540 | nM | IC50 | J Med Chem (2018) 61: 10053-10066 [PMID:30373366] |
| 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] |
| ChEMBL | Inhibition of human 20s immunoproteasome beta5i activity using Suc-LLVY-AMC as substrate preincubated for 15 mins followed by substrate addition | B | 8.1 | pIC50 | 8 | nM | IC50 | Eur J Med Chem (2019) 164: 602-614 [PMID:30639896] |
| ChEMBL | Inhibition of human peripheral blood derived 20s immunoproteasome beta5 chymotrypsin-like activity using Suc-PAL-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay | B | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Med Chem (2019) 164: 423-439 [PMID:30611983] |
| ChEMBL | Inhibition of 20S proteasome beta 5i (unknown origin) after 1 hr by fluorescence based assay | B | 8.48 | pIC50 | 3.3 | nM | IC50 | Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028] |
| ChEMBL | Inhibition of human 20S immunoproteasome beta 5 subunit chymotrypsin-like activity using fluorogenic peptide Ac-WLA-AMC as substrate in presence of PA28alpha incubated for 1 to 2 hrs by fluorescence microplate reader assay | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2018) 61: 10053-10066 [PMID:30373366] |
| 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] |
| proteasome 20S subunit beta 9/Proteasome subunit beta type-9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944495] [GtoPdb: 2409] [UniProtKB: P28065] | ||||||||
| ChEMBL | Inhibition of 20S proteasome beta 1i (unknown origin) after 1 hr by fluorescence based assay | B | 8.26 | pIC50 | 5.5 | nM | IC50 | Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028] |
| ChEMBL | Inhibition of human 20S immunoproteasome beta 1 subunit caspase-like activity using fluorogenic peptide Ac-nLPnLD-AMC as substrate in presence of PA28alpha incubated for 1 to 2 hrs by fluorescence microplate reader assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2018) 61: 10053-10066 [PMID:30373366] |
| ChEMBL | Inhibition of human peripheral blood derived 20s immunoproteasome beta1 caspase-like activity using Suc-PAL-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2019) 164: 423-439 [PMID:30611983] |
| coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734] | ||||||||
| ChEMBL | Inhibitory activity against thrombin | B | 4.89 | pKi | 13000 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 333-338 [PMID:9871680] |
| Uncharacterized protein Rv1284/MT1322 in Mycobacterium tuberculosis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5631] [UniProtKB: P9WPJ7] | ||||||||
| ChEMBL | Inhibition of Mycobacterium tuberculosis beta-carbonic anhydrase Rv1284 preincubated for 15 mins by stopped-flow CO2 hydration assay | B | 5.14 | pKi | 7300 | nM | Ki | Bioorg Med Chem (2016) 24: 4406-4409 [PMID:27469982] |
| Plasmodium falciparum proteasome subunit beta type-5 in Plasmodium falciparum W2 [GtoPdb: 3088] | ||||||||
| GtoPdb | Parasite growth inhibition assay | - | 7.37 | pIC50 | 43 | nM | IC50 | BMC Clin Pharmacol (2007) 7: 13 [PMID:17956613] |
| Plasmodium falciparum proteasome subunit beta type-5 in Plasmodium falciparum [GtoPdb: 3088] | ||||||||
| GtoPdb | - | - | 7.28 | pIC50 | 53 | nM | IC50 | J Med Chem (2018) 61: 10053-10066 [PMID:30373366] |
| Plasmodium falciparum proteasome subunit beta type-5 in Plasmodium falciparum 3D7 [GtoPdb: 3088] [UniProtKB: Q8IJT1] | ||||||||
| GtoPdb | Parasite growth inhibition assay | - | 7.51 | pIC50 | 31 | nM | IC50 | BMC Clin Pharmacol (2007) 7: 13 [PMID:17956613] |
| Plasmodium falciparum proteasome subunit beta type-5 in Plasmodium falciparum Dd2 [GtoPdb: 3088] | ||||||||
| GtoPdb | Parasite growth inhibition assay | - | 7.43 | pIC50 | 37 | nM | IC50 | BMC Clin Pharmacol (2007) 7: 13 [PMID:17956613] |
| Plasmodium falciparum proteasome subunit beta type-5 in Plasmodium falciparum HB3 [GtoPdb: 3088] | ||||||||
| GtoPdb | Parasite growth inhibition assay | - | 7.51 | pIC50 | 31 | nM | IC50 | BMC Clin Pharmacol (2007) 7: 13 [PMID:17956613] |
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]
