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Inhibition of KSP (unknown origin)
Assay data:2 Active, 3 Tested
SummaryRelated BioAssays by Target
Inhibition of Eg5 ATPase activity (unknown origin)
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Inhibition of Eg5 (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of recombinant GST-tagged human Eg5 assessed as inhibition of microtubule-stimulated ATPase activity preincubated for 30 mins followed by ATP addition and further incubated for 15 mins by ADP-Glo reagent based assay
Assay data:3 Tested
Inhibition of the Kinesin Spindle Protein KSP/Eg5 from US Patent US11806404: "Site specific homogeneous with KSP inhibitors"
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition Assay from US Patent US11071788: "Antibody drug conjugates of kinesin spindel protein (KSP) inhibitors with antiB7H3-antibodies"
Assay data:21 Active, 8 Activity ≤ 1 nM, 21 Activity ≤ 1 µM, 21 Tested
ADP Hunter Plus Assay from Article 10.1111/cbdd.12744: "Discovery of Novel Allosteric Eg5 Inhibitors Through Structure-Based Virtual Screening."
SummaryPubMed CitationRelated BioAssays by Target
In Vitro Assay from US Patent US8748626: "Oxazole and thiazole compounds as KSP inhibitors"
Assay data:8 Active, 1 Activity ≤ 1 nM, 8 Activity ≤ 1 µM, 8 Tested
Microtubule-activated ATPase Kinetic Assay from Article 10.1002/cbic.201402089: "Structure-based design of new KSP-Eg5 inhibitors assisted by a targeted multicomponent reaction."
Assay data:6 Active, 6 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
In Vitro Assay from US Patent US8546434: "Triazole compounds as KSP inhibitors"
Assay data:14 Active, 8 Activity ≤ 1 nM, 14 Activity ≤ 1 µM, 14 Tested
Binding Assay from Article 10.1021/bi1005283: "Novel benzimidazole inhibitors bind to a unique site in the kinesin spindle protein motor domain."
Assay data:6 Active, 1 Activity ≤ 1 µM, 7 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Malachite Green Assay from Article 10.1002/cbic.200500168: "Synthesis and biological evaluation of novel EG5 inhibitors."
Assay data:9 Active, 10 Tested
WT-6x from Article 10.1038/nchembio.2007.34: "ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism."
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
WT-3x from Article 10.1038/nchembio.2007.34: "ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism."
HCT116-D130V 3x biary selected from Article 10.1038/nchembio.2007.34: "ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism."
Assay data:3 Active, 1 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
HCT116-D130V IC95 biaryl selected from Article 10.1038/nchembio.2007.34: "ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism."
HCT116-D130V IC50 biaryl selected from Article 10.1038/nchembio.2007.34: "ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism."
Assay data:3 Active, 2 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 3 Tested
HCT116-D130V not selected from Article 10.1038/nchembio.2007.34: "ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism."
Assay data:3 Active, 2 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
Wild-type 3x biaryl selected from Article 10.1038/nchembio.2007.34: "ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism."
Assay data:3 Active, 2 Activity ≤ 1 µM, 3 Tested
Wild-type IC95 biaryl selected from Article 10.1038/nchembio.2007.34: "ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism."
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