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IC50 Determination from US Patent US20240043470: "MACROCYCLIC COMPOUNDS AS PROTEASOME INHIBITORS"
Assay data:80 Active, 18 Activity ≤ 1 µM, 160 Tested
SummaryRelated BioAssays by Target
Inhibition of human 20S immuno proteosome beta5i subunit using Suc-LLVY-AMC as substrate measured after 10 mins by fluorescence based analysis
Assay data:2 Active, 4 Tested
Competitive inhibition of human 20S constitutive proteosome beta5c subunit using Suc-LLVY-AMC as substrate measured after 10 mins by fluorescence based analysis
Assay data:4 Active, 4 Tested
Inhibition of human 20S constitutive proteosome beta5c subunit using Suc-LLVY-AMC as substrate measured after 10 mins by fluorescence based analysis
Assay data:2 Active, 9 Tested
Inhibition of human 20S proteasome
Assay data:1 Active, 2 Tested
Inhibition of beta5 proteasome (unknown origin)
Assay data:8 Active, 8 Activity ≤ 1 µM, 8 Tested
Inhibition of beta2 proteasome (unknown origin)
Assay data:5 Active, 1 Activity ≤ 1 µM, 5 Tested
Inhibition of 20S proteasome (unknown origin)
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of beta 1 proteasome (unknown origin)
Assay data:5 Active, 4 Activity ≤ 1 µM, 5 Tested
Proteasome Inhibitory Activity from US Patent US11542283: "Synthesis of peptide borate ester compound and use thereof"
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Activation of human 20S proteosome at chymotrypsin like site assessed as maximum fold change in substrate degradation using Suc-LLVY-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by spectrometric analysis relative to control
Assay data:7 Tested
SummaryPubMed CitationRelated BioAssays by Target
Activation of human 20S proteosome at chymotrypsin like site assessed as substrate degradation using Suc-LLVY-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by spectrometric analysis
Assay data:7 Active, 1 Activity ≤ 1 µM, 17 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Activation of human 20S proteosome at trypsin-like site assessed as maximum fold change in substrate degradation using Boc-LLR-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by spectrometric analysis relative to control
Assay data:8 Tested
Activation of human 20S proteosome at trypsin-like site assessed as substrate degradation using Boc-LLR-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by spectrometric analysis
Activation of human 20S proteosome at caspase-like site assessed as maximum fold change in substrate degradation using Z-LLE-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by spectrometric analysis relative to control
Assay data:6 Tested
Activation of human 20S proteosome at caspase-like site assessed as substrate degradation using Z-LLE-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by spectrometric analysis
Assay data:6 Active, 17 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Activation of human 20S proteosome assessed as maximum fold change in substrate degradation using Suc-LLVY-AMC/Z-LLE-AMC/Boc-LLR-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by spectrometric analysis relative to control
Assay data:9 Tested
Activation of human 20S proteosome assessed as substrate degradation using Suc-LLVY-AMC/Z-LLE-AMC/Boc-LLR-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by spectrometric analysis
Inhibition of 20S proteasome subunit beta-2c (unknown origin) using Ac-KQL-AMC as substrate and measured after 30 mins
Assay data:3 Tested
Inhibition of 20S proteasome subunit beta-2i (unknown origin) using Ac-KQL-AMC as substrate and measured after 30 mins
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