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Kinase-Glo Assays from US Patent US20240018138: "PYRIDO[4,3-b]INDOLE DERIVATIVES AND THEIR USE AS PHARMACEUTICALS"
Assay data:24 Active, 16 Activity ≤ 1 µM, 24 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
In Vitro Inhibition Assay from US Patent US20230391786: "cGAS INHIBITORS"
Assay data:322 Active, 322 Activity ≤ 1 µM, 322 Tested
Enzymatic Assay from US Patent US20230348398: "Benzimidazole derivatives"
Assay data:32 Active, 19 Activity ≤ 1 µM, 32 Tested
Inhibition of cGAS (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to cGAS (unknown origin) assessed as dissociation constant
Inhibition of cGAS in human THP-1 cells
Assay data:4 Active, 5 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of human cGAS
Assay data:5 Active, 3 Activity ≤ 1 µM, 5 Tested
Inhibition of human (His6)-SUMO tagged cGAS expressed in Escherichia coli BL21-codonPlus(DE3)-RIL by ATP-biofluorescence assay
Assay data:2 Active, 2 Tested
Inhibition of cGAS (unknown origin) incubated for 1 hr by Typhoon imaging system analysis
Assay data:1 Active, 2 Tested
Inhibition of full-length human cGAS by fluorescence polarization
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Antagonist activity at N-terminal 6XHis tagged human cGAS (155 to 522 residues) expressed in Escherichia coli BL21 DE3 Rosetta 2 in presence of ATP by luciferase based assay
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of cGAS expressed in human THP-1 cells assessed as reduction of IFN-beta expression by ELISA assay
Inhibition of N-terminal 6XHis-SUMO2 fused full length human cGAS (1 to 522 residues) expressed in human THP-1 cells transfected with HT-DNA incubated for 20 mins in presence of ATP by luminescence based analysis
Assay data:1 Active, 3 Tested
Inhibition of full length human cGAS expressed in Escherichia coli BL21 (DE3) incubated for 2 hrs in presence of ATP by RF-MS analysis
Inhibition of human cGAS expressed in human THP-1 cells transfected with HT-DNA incubated for 20 mins in presence of ATP by luminescence based analysis
Assay data:4 Active, 3 Activity ≤ 1 µM, 4 Tested
Inhibition of human cGAS assessed as reduction in 2,3-cGAMP synthesis by measuring ATP consumption incubated for 20 mins by Kinase Glo luminescence assay
Binding affinity to human cGAS assessed as dissociation constant
Inhibition of human cGAS incubated for 1 hr followed by Cy5-labeled cGAMP addition and measured after 1 hr by fluorescence polarization assay
Assay data:1 Active, 1 Tested
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