zetomipzomib [Ligand Id: 10409] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4297468 (Zetomipzomib, KZR-616, Kzr-616) |
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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 component C5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4208] [GtoPdb: 2404] [UniProtKB: P20618] | ||||||||
| ChEMBL | Inhibition of 20S proteosome beta 1 in human MOLT4 cells by ELISA | B | 4.97 | pIC50 | >10600 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| ChEMBL | Inhibition of 20S proteasome beta 1c (unknown origin) after 1 hr by fluorescence based assay | B | 6.37 | pIC50 | 430 | nM | IC50 | Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028] |
| proteasome 20S subunit beta 2/Proteasome Macropain subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3492] [GtoPdb: 2405] [UniProtKB: P49721] | ||||||||
| ChEMBL | Inhibition of 20S proteosome beta 2 in human MOLT4 cells by ELISA | B | 6.22 | pIC50 | 604 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| GtoPdb | Inhibition of proteolytic activity measured in MOLT-4 (human T cell leukemia) cell lysate using the ProCISE ELISA. | - | 6.22 | pIC50 | 604 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| ChEMBL | Inhibition of 20S proteasome beta 2c (unknown origin) after 1 hr by fluorescence based assay | B | 7.55 | pIC50 | 28 | nM | IC50 | Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028] |
| 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 20S proteosome beta5c subunit using Ac-WLA-AMC as substrate preincubated with compound for 30 mins followed by substrate addition and measured after 1 hr by fluorescence based analysis | B | 6.14 | pIC50 | 720 | nM | IC50 | Bioorg Med Chem (2024) 109: 117790-117790 [PMID:38906067] |
| GtoPdb | Inhibition of proteolytic activity measured in MOLT-4 (human T cell leukemia) cell lysate using the ProCISE ELISA. | - | 6.16 | pIC50 | 688 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| ChEMBL | Inhibition of 20S proteosome beta 5 in human MOLT4 cells by ELISA | B | 6.16 | pIC50 | 688 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| ChEMBL | Inhibition of 20S proteasome beta 5c (unknown origin) after 1 hr by fluorescence based assay | B | 9.16 | pIC50 | 0.69 | nM | IC50 | Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028] |
| proteasome 20S subunit beta 1/Proteasome subunit beta type-1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523121] [GtoPdb: 2404] [UniProtKB: O09061] | ||||||||
| ChEMBL | Inhibition of 20S proteosome beta 1 in mouse A20 cells by ELISA | B | 4.6 | pIC50 | >25000 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| Proteasome subunit beta type-10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3317334] [UniProtKB: P40306] | ||||||||
| ChEMBL | Inhibition of MECL1 in human MOLT4 cells by ELISA | B | 6.21 | pIC50 | 623 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| ChEMBL | Inhibition of 20S proteasome beta 2i (unknown origin) after 1 hr by fluorescence based assay | B | 9.88 | pIC50 | 0.13 | nM | IC50 | Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028] |
| Proteasome subunit beta type-10 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523133] [UniProtKB: O35955] | ||||||||
| ChEMBL | Inhibition of MECL1 in mouse A20 cells by ELISA | B | 6.28 | pIC50 | 522 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| proteasome 20S subunit beta 2 in Human [GtoPdb: 2405] [UniProtKB: P49721] | ||||||||
| GtoPdb | Inhibition of proteolytic activity measured in MOLT-4 (human T cell leukemia) cell lysate using the ProCISE ELISA. | - | 6.22 | pIC50 | 604 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| proteasome 20S subunit beta 2/Proteasome subunit beta type-2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3112378] [GtoPdb: 2405] [UniProtKB: Q9R1P3] | ||||||||
| ChEMBL | Inhibition of 20S proteosome beta 2 in mouse A20 cells by ELISA | B | 6.07 | pIC50 | 857 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| proteasome 20S subunit beta 5 in Human [GtoPdb: 2406] [UniProtKB: P28074] | ||||||||
| GtoPdb | Inhibition of proteolytic activity measured in MOLT-4 (human T cell leukemia) cell lysate using the ProCISE ELISA. | - | 6.16 | pIC50 | 688 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| proteasome 20S subunit beta 5/Proteasome subunit beta type-5 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944494] [GtoPdb: 2406] [UniProtKB: O55234] | ||||||||
| ChEMBL | Inhibition of 20S proteosome beta 5 in mouse A20 cells by ELISA | B | 6.32 | pIC50 | 483 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| 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 LMP7 beta -5i subunit using Ac-ANW-AMC as substrate preincubated with compound for 30 mins followed by substrate addition and measured after 1 hr by fluorescence based analysis | B | 7.12 | pIC50 | 75 | nM | IC50 | Bioorg Med Chem (2024) 109: 117790-117790 [PMID:38906067] |
| ChEMBL | Inhibition of LMP7 in human MOLT4 cells by ELISA | B | 7.41 | pIC50 | 39 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| GtoPdb | Inhibition of proteolytic activity measured in MOLT-4 (human T cell leukemia) cells using the ProCISE ELISA. | - | 7.41 | pIC50 | 39 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| ChEMBL | Inhibition of 20S proteasome beta 5i (unknown origin) after 1 hr by fluorescence based assay | B | 10.41 | pIC50 | 0.04 | nM | IC50 | Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028] |
| proteasome 20S subunit beta 8/Proteasome subunit beta type-8 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944492] [GtoPdb: 2408] [UniProtKB: P28063] | ||||||||
| GtoPdb | Inhibition of proteolytic activity measured in A20 (mouse B-cell lymphoma) cell lysate using the ProCISE ELISA. | - | 7.24 | pIC50 | 57 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| ChEMBL | Inhibition of LMP7 in mouse A20 cells by ELISA | B | 7.24 | pIC50 | 57 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| 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 human LMP2 beta-1i subunit using Ac-PAL-AMC as substrate preincubated with compound for 30 mins followed by substrate addition and measured after 1 hr by fluorescence based analysis | B | 6.25 | pIC50 | 557 | nM | IC50 | Bioorg Med Chem (2024) 109: 117790-117790 [PMID:38906067] |
| GtoPdb | Inhibition of proteolytic activity measured in MOLT-4 (human T cell leukemia) cell lysate using the ProCISE ELISA. | - | 6.88 | pIC50 | 131 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| ChEMBL | Inhibition of LMP2 in human MOLT4 cells by ELISA | B | 6.88 | pIC50 | 131 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| ChEMBL | Inhibition of 20S proteasome beta 1i (unknown origin) after 1 hr by fluorescence based assay | B | 9.21 | pIC50 | 0.62 | nM | IC50 | Eur J Med Chem (2019) 182: 111646-111646 [PMID:31521028] |
| proteasome 20S subunit beta 9/Proteasome subunit beta type-9 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944491] [GtoPdb: 2409] [UniProtKB: P28076] | ||||||||
| ChEMBL | Inhibition of LMP2 in mouse A20 cells by ELISA | B | 6.75 | pIC50 | 179 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
| GtoPdb | Inhibition of proteolytic activity measured in A20 (mouse B-cell lymphoma) cell lysate using the ProCISE ELISA. | - | 6.75 | pIC50 | 179 | nM | IC50 | J Med Chem (2018) 61: 11127-11143 [PMID:30380863] |
ChEMBL data shown on this page come from version 37:
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]
