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Protac activity at IAP/BRD4 in human SK-MEL-28 cells assessed as induction of BRD4 degradation at 0.1 to 10 uM measured after 24 hrs by Western blotting analysis
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
PROTAC activity at IAP/BTK in human THP-1 cells assessed as reduction in BTK level incubated for 16 hrs by immunoblot analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Protac activity at XIAP/BCR-ABL in human K562 cells assessed as induction of BCR-ABL protein degradation measured after 6 hrs by Western blot analysis
Protac activity at XIAP (unknown origin)/ERalpha (unknown origin) assessed as protein degradation
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Antagonist activity at x-IAP1 (unknown origin)
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Fluorescence Polarization (FP) Assays from US Patent US20230295181: "INHIBITOR OF APOPTOSIS (IAP) PROTEIN ANTAGONISTS"
Assay data:6 Active, 6 Activity ≤ 1 µM, 6 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Binding affinity to XIAP BIR3 domain (unknown origin)
Assay data:1 Active, 1 Tested
Inhibition of XIAP BIR3 domain (unknown origin) at 155 uM relative to control
Inhibition of XIAP BIR3 domain (unknown origin) at 1000 uM relative to control
Inhibition of XIAP BIR3 domain (unknown origin) at 495 uM relative to control
Inhibition of XIAP BIR3 domain (unknown origin)
Assay data:6 Active, 6 Activity ≤ 1 µM, 7 Tested
Binding affinity to N-terminal His-tagged XIAP-BIR3 domain (253 to 347 residues) (unknown origin) expressed in Escherichia coli BL21 assessed as covalent adduct formation by measuring change in melting temperature at 20 uM incubated for 2 hrs followed by heating at 40 to 70 degree C for 30 mins by SYPRO orange dye based thermal shift assay
Binding affinity to N-terminal His-tagged XIAP-BIR3 domain (253 to 347 residues) (unknown origin) expressed in Escherichia coli BL21 assessed as non-covalent stabilization by measuring change in melting temperature at 20 uM incubated for 2 hrs followed by heating at 40 to 70 degree C for 30 mins by SYPRO orange dye based thermal shift assay
Antagonist activity at N-terminal His-tagged XIAP-BIR3 domain (253 to 347 residues)(unknown origin) expressed in Escherichia coli BL21 at protein:compound concentration ratio of 1:2 incubated for 2 hrs by SDS-PAGE analysis
Antagonist activity at N-terminal His-tagged XIAP-BIR3 domain (253 to 347 residues)(unknown origin) expressed in Escherichia coli BL21 using AVPIAQKSEK-biotinylated peptide as substrate preincubated for 2 hrs with protein followed by substrate addition measured after 2 hrs by DELFIA assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Antagonist activity at N-terminal His-tagged XIAP-BIR3 domain (253 to 347 residues)(unknown origin) expressed in Escherichia coli BL21 using AVPIAQKSEK-biotinylated peptide as substrate incubated for 2 hrs by DELFIA assay
Assay data:9 Active, 9 Activity ≤ 1 µM, 12 Tested
Biological Assay from US Patent US11111270: "Inhibitor of apoptosis protein (IAP) antagonists"
Assay data:39 Tested
SummaryRelated BioAssays by Target
Biological Assay 1: affinity of compounds to cIAP1-BIR3, cIAP2-BIR3, XIAP-BIR3 from US Patent US10508103: "Benzimidazole-linked indole compound acting as novel divalent IAP antagonist"
Assay data:29 Active, 29 Activity ≤ 1 µM, 29 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
TR-FRET Assays for XIAP BIR3 from US Patent US10398702: "Dimeric compounds"
Assay data:27 Active, 27 Activity ≤ 1 µM, 27 Tested
TR-FRET Assays for XIAP BIR2 from US Patent US10398702: "Dimeric compounds"
Assay data:21 Active, 17 Activity ≤ 1 µM, 27 Tested
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