carfilzomib [Ligand Id: 7420] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL451887 (Carfilzomib, Kyprolis, NSC-758252, PR-171) |
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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 20S proteasome chymotrypsin-like activity in human RPMI-8226 cells overexpressing ABCB1 using Suc-LLVY-AMC as fluorogenic substrate incubated for 3 hrs by fluorescence assay | B | 6.57 | pIC50 | 269.8 | nM | IC50 | J Med Chem (2021) 64: 10934-10950 [PMID:34309393] |
| ChEMBL | Inhibition of 20S proteasome activity in human ANBL-6 cells | B | 8 | pIC50 | <10 | nM | IC50 | J Med Chem (2018) 61: 7448-7470 [PMID:29652143] |
| ChEMBL | Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate addition | B | 8.07 | pIC50 | 8.6 | nM | IC50 | Eur J Med Chem (2019) 164: 602-614 [PMID:30639896] |
| ChEMBL | Inhibition of human 20S proteasome chymotrypsin-like activity in human RPMI-8226 cells using Suc-LLVY-AMC as fluorogenic substrate incubated for 3 hrs by fluorescence assay | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2021) 64: 10934-10950 [PMID:34309393] |
| GtoPdb | - | - | 8.24 | pIC50 | 5.7 | nM | IC50 | J Med Chem (2009) 52: 3028-38 [PMID:19348473] |
| 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 chymotrypsin-like enzyme activity of purified human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate by fluorescence method | B | 8.07 | pIC50 | 8.6 | nM | IC50 | Bioorg Med Chem (2014) 22: 2955-2965 [PMID:24767818] |
| GtoPdb | - | - | 8.24 | pIC50 | 5.7 | nM | IC50 | J Med Chem (2009) 52: 3028-38 [PMID:19348473] |
| 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 | 4.96 | pIC50 | 11000 | 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 | Inhibition of recombinant cathepsin G (unknown origin) using Suc-Ala-Ala-Pro-Phe-AMC as substrate by spectrofluorometer analysis | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2014) 57: 2726-2735 [PMID:24524217] |
| glutathione S-transferase omega 1/Glutathione transferase omega 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3174] [GtoPdb: 3110] [UniProtKB: P78417] | ||||||||
| ChEMBL | Inhibition of GSTO1-1 (unknown origin) pre-incubated for 1 hr before GSH addition by CDNB-GSH conjugation assay | B | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2018) 61: 7448-7470 [PMID:29652143] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG in HEK293 cells assessed as effect on QT interval | B | 4.04 | pIC50 | 92100 | nM | IC50 | Bioorg Med Chem (2019) 27: 4151-4162 [PMID:31383629] |
| 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 | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2014) 57: 2726-2735 [PMID:24524217] |
| 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 beta 1c (unknown origin) after 1 hr by fluorescence based assay | B | 5.62 | pIC50 | 2400 | nM | IC50 | Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028] |
| ChEMBL | Inhibition of human caspase-like activity of 20S constitutive proteasome preincubated for 15 mins followed by substrate addition by fluorescence assay | B | 5.84 | pIC50 | 1452 | nM | IC50 | Eur J Med Chem (2019) 161: 543-558 [PMID:30391816] |
| proteasome 20S subunit beta 2/Proteasome Macropain subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3492] [GtoPdb: 2405] [UniProtKB: P49721] | ||||||||
| ChEMBL | Inhibition of 20S proteasome beta 2c (unknown origin) after 1 hr by fluorescence based assay | B | 5.44 | pIC50 | 3600 | nM | IC50 | Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028] |
| 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 | 5.74 | pIC50 | 1812 | nM | IC50 | Eur J Med Chem (2019) 164: 602-614 [PMID:30639896] |
| ChEMBL | Inhibition of human trypsin-like activity of 20S constitutive proteasome using Z-VLR-AMC as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay | B | 6.08 | pIC50 | 825 | nM | IC50 | Eur J Med Chem (2019) 161: 543-558 [PMID:30391816] |
| ChEMBL | Inhibition of 20S proteasome beta2 subunit in human Jurkat cell lysate using Suc-RLR-AMC as substrate pretreated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence assay | B | 6.69 | pIC50 | 203 | nM | IC50 | Eur J Med Chem (2018) 157: 962-977 [PMID:30165344] |
| proteasome 20S subunit beta 5/Proteasome Macropain subunit MB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4662] [GtoPdb: 2406] [UniProtKB: P28074] | ||||||||
| ChEMBL | Inhibition of human chymotrypsin-like activity of 20S proteasome using Suc-LLVY-AMC as substrate pre-incubated for 10 mins followed by substrate addition and measured after 1 hr by spectrofluorimetry | B | 7.63 | pIC50 | 23.6 | nM | IC50 | Bioorg Med Chem (2019) 27: 4151-4162 [PMID:31383629] |
| ChEMBL | Inhibition of 20S proteasome beta5 subunit in human Jurkat cell lysate using Suc-LLVY-AMC as substrate pretreated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence assay | B | 8.02 | pIC50 | 9.6 | nM | IC50 | Eur J Med Chem (2018) 157: 962-977 [PMID:30165344] |
| 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 | 8.07 | pIC50 | 8.6 | 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 preincubated for 15 mins followed by substrate addition by fluorescence assay | B | 8.08 | pIC50 | 8.4 | nM | IC50 | Bioorg Med Chem (2021) 29: 115867-115867 [PMID:33223460] |
| ChEMBL | Inhibition of chymotrypsin-like activity of human 20S proteasome pretreated for 15 mins followed by Suc-Leu-Leu-Val-Tyr-AMC substrate addition by fluorescence assay | B | 8.08 | pIC50 | 8.4 | nM | IC50 | Eur J Med Chem (2017) 126: 1056-1070 [PMID:28027531] |
| ChEMBL | Inhibition of chymotrypsin-like activity of human 20S proteasome preincubated for 15 mins followed by addition of Suc-Leu-Leu-Val-Tyr-AMC as substrate by fluorescence analysis | B | 8.08 | pIC50 | 8.4 | nM | IC50 | Bioorg Med Chem (2016) 24: 6206-6214 [PMID:27765408] |
| 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 | 8.15 | pIC50 | 7 | nM | IC50 | Eur J Med Chem (2019) 164: 423-439 [PMID:30611983] |
| ChEMBL | Inhibition of 20S proteasome beta 5c (unknown origin) after 1 hr by fluorescence based assay | B | 8.22 | pIC50 | 6 | nM | IC50 | Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028] |
| GtoPdb | - | - | 8.24 | pIC50 | 5.7 | nM | IC50 | J Med Chem (2009) 52: 3028-38 [PMID:19348473] |
| ChEMBL | Inhibition of human chymotrypsin-like activity of 20S constitutive proteasome using Suc-LLVY-AMC as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay | B | 8.3 | pIC50 | 5 | nM | IC50 | Eur J Med Chem (2019) 161: 543-558 [PMID:30391816] |
| ChEMBL | Inhibition of 20S proteasome beta5 subunit in human RPMI8226 cell lysate using Suc-LLVY-AMC as substrate pretreated for 1 hr followed by substrate addition and measured at 1 min interval by fluorescence assay | B | 8.57 | pIC50 | 2.7 | nM | IC50 | J Med Chem (2019) 62: 4444-4455 [PMID:30964987] |
| Proteasome subunit beta type-1 in Saccharomyces cerevisiae (strain ATCC 204508 / S288c) (Baker's yeast) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295578] [UniProtKB: P38624] | ||||||||
| ChEMBL | Inhibition of yeast 20S proteasome beta1 subunit using fluorescent substrate pretreated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2018) 157: 962-977 [PMID:30165344] |
| 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 | 6.21 | pIC50 | 620 | nM | IC50 | Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028] |
| Proteasome subunit beta type-2 in Saccharomyces cerevisiae (strain ATCC 204508 / S288c) (Baker's yeast) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295577] [UniProtKB: P25043] | ||||||||
| ChEMBL | Inhibition of yeast 20S proteasome beta2 subunit using SUC-RLR-AMC as substrate pretreated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2018) 157: 962-977 [PMID:30165344] |
| 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 human 20s immunoproteasome beta5i activity using Suc-LLVY-AMC as substrate preincubated for 15 mins followed by substrate addition | B | 7.47 | pIC50 | 34 | nM | IC50 | Eur J Med Chem (2019) 164: 602-614 [PMID:30639896] |
| ChEMBL | Inhibition of 20S proteasome beta 5i (unknown origin) after 1 hr by fluorescence based assay | B | 7.48 | pIC50 | 33 | nM | IC50 | Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028] |
| ChEMBL | Inhibition of human immunoproteasome beta5 subunit using Suc-RLR-AMC as substrate pretreated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence assay | B | 7.49 | pIC50 | 32.6 | nM | IC50 | Eur J Med Chem (2018) 157: 962-977 [PMID:30165344] |
| ChEMBL | Inhibition of 20S immunoproteasome LMP7 (unknown origin) using Ac-ANW-AMC as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay | B | 7.57 | pIC50 | 27 | nM | IC50 | Eur J Med Chem (2019) 161: 543-558 [PMID:30391816] |
| ChEMBL | Inhibition of chymotrypsin-like activity of LMP7 immunoproteasome by proteasome active site ELISA | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2009) 52: 3028-3038 [PMID:19348473] |
| 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 purified human 20S immunoproteasome beta1 subunit using Ac-Pro-Ala-Leu-AMC as substrate pretreated for 1 hr followed by substrate addition and measured at 1 min interval by fluorescence assay | B | 5.53 | pIC50 | 2940 | nM | IC50 | J Med Chem (2019) 62: 4444-4455 [PMID:30964987] |
| ChEMBL | Inhibition of 20S proteasome beta 1i (unknown origin) after 1 hr by fluorescence based assay | B | 5.62 | pIC50 | 2420 | nM | IC50 | Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028] |
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]
