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Summary
Agonist activity at human CLpP (57 to 277 amino acids) expressed in Escherichia coli assessed as induction of casein degradation using FITC-labelled casein as substrate
Assay data:6 Tested
SummaryPubMed CitationRelated BioAssays by Target
Potency index, ratio of ONC201 Kd to test compound Kd for binding affinity to human CLpP
Assay data:1 Tested
Binding affinity to human CLpP assessed as change in enthalpy by ITC method
Assay data:2 Tested
Binding affinity to human CLpP assessed as change in entropy by ITC method
Binding affinity to human CLpP assessed as dissociation constant by ITC method
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to CLpP in human HCT-116 cells assessed as protein stabilization at 10 uM incubated for 30 mins followed by heating at 46 to 74 degree celcius for 3 mins CETSA based Western blot analysis
Assay data:1 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Binding affinity to human CLpP (57 to 277 amino acids) expressed in Escherichia coli assessed as change in melting temperature at 100 uM incubated for 30 mins by DSF assay
Agonist activity at human CLpP (57 to 277 amino acids) expressed in Escherichia coli using fluorogenic peptide AC-WLA-AMC as substrate incubated for 10 mins by fluorescence based assay
Assay data:43 Active, 33 Activity ≤ 1 µM, 52 Tested
Inhibition of human ClpP expressed in Escherichia coli SG1146 cells using N-acetyl-Trp-Leu-Ala-AMC as substrate incubated for 1 hr and measured at 20 secs time interval for 90 mins by fluorescence assay
Assay data:2 Active, 11 Tested
Inhibition of C-terminal recombinant human ClpP expressed in Escherichia coli Rosetta2 (DE3) cells using Suc-Leu-Tyr-AMC as substrate incubated for 15 mins and measured for 90 mins by fluorescence assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of C-terminal recombinant human ClpP (57 to 277 amino acids) expressed in Escherichia coli Rosetta2 cells using Suc-Leu-Tyr-AMC as substrate incubated for 1 hr and measured for 90 mins by fluorescence assay
Assay data:1 Active, 1 Tested
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