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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 |
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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] |
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 |