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 GROUP) [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 PGPH-like activity using Cbz-LLE-AMC as a fluorogenic substrate measured every 20 seconds for 10 mins by fluorescence based assay | B | 5.98 | pIC50 | 1050 | nM | IC50 | ACS Med Chem Lett (2024) 15: 533-539 [PMID:38628795] |
| 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 human 20S proteasome chymotrypsin-like activity using Suc-LLVY-AMC as a fluorogenic substrate measured every 20 seconds for 10 mins by fluorescence based assay | B | 7.77 | pIC50 | 17 | nM | IC50 | ACS Med Chem Lett (2024) 15: 533-539 [PMID:38628795] |
| 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 beta 1 proteasome (unknown origin) | B | 5.62 | pIC50 | 2400 | nM | IC50 | J Med Chem (2021) 64: 2851-2877 [PMID:33656892] |
| 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 beta2 proteasome (unknown origin) | B | 5.44 | pIC50 | 3600 | nM | IC50 | J Med Chem (2021) 64: 2851-2877 [PMID:33656892] |
| 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 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 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 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 beta5 proteasome (unknown origin) | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2021) 64: 2851-2877 [PMID:33656892] |
| 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] |
| ChEMBL | Inhibition of human 20S proteasome beta5 subunit using Suc-LLVY-AMC as substrate preincubated for 2 hrs followed by substrate addition and measured after 1 hr by fluorescence intensity assay | B | 8.68 | pIC50 | 2.1 | nM | IC50 | J Med Chem (2021) 64: 10230-10245 [PMID:34228444] |
| 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] |
| ChEMBL | Inhibition of human 20S immunoproteasome beta-2i subunit using Ac-RLR-AMC as substrate preincubated for 2 hrs followed by substrate addition and measured after 1 hr by fluorescence intensity assay | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2021) 64: 10230-10245 [PMID:34228444] |
| 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 6/Proteasome subunit beta type-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944496] [GtoPdb: 2407] [UniProtKB: P28072] | ||||||||
| ChEMBL | Inhibition of human 20S immunoproteasome beta1 subunit using Ac-nLPnLD-AMC as substrate preincubated for 2 hrs followed by substrate addition and measured after 1 hr by fluorescence intensity assay | B | 6.05 | pIC50 | 890 | nM | IC50 | J Med Chem (2021) 64: 10230-10245 [PMID:34228444] |
| Proteasome subunit beta type-7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3347256] [UniProtKB: Q99436] | ||||||||
| ChEMBL | Inhibition of human 20S proteasome beta2 subunit using Ac-RLR-AMC as substrate preincubated for 2 hrs followed by substrate addition and measured after 1 hr by fluorescence intensity assay | B | 7.37 | pIC50 | 43 | nM | IC50 | J Med Chem (2021) 64: 10230-10245 [PMID:34228444] |
| 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] |
| ChEMBL | Inhibition of human 20S immunoproteasome beta-5i subunit using Suc-LLVY-AMC as substrate preincubated for 2 hrs followed by substrate addition and measured after 1 hr by fluorescence intensity assay | B | 8.49 | pIC50 | 3.2 | nM | IC50 | J Med Chem (2021) 64: 10230-10245 [PMID:34228444] |
| 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 | Inhibition of human 20S immunoproteasome beta-1i subunit using (Ac-PAL)2R110 as substrate preincubated for 2 hrs followed by substrate addition and measured after 1 hr by fluorescence intensity assay | B | 7.16 | pIC50 | 69 | nM | IC50 | J Med Chem (2021) 64: 10230-10245 [PMID:34228444] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
