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hERG Inhibition Assay from US Patent US20230295159: "ATX INHIBITOR, AND PREPARATION METHOD THEREFOR AND USE THEREOF"
Assay data:5 Tested
SummaryRelated BioAssays by DepositorRelated BioAssays by Target
ATX Enzyme Activity Inhibition Assay from US Patent US20230295159: "ATX INHIBITOR, AND PREPARATION METHOD THEREFOR AND USE THEREOF"
Assay data:28 Active, 28 Activity ≤ 1 µM, 29 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Bioactivity Assay from US Patent US11591342: "Heterocyclic compound, application thereof and pharmaceutical composition comprising same"
Assay data:45 Active, 44 Activity ≤ 1 µM, 46 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µM
Inhibition of rat ATX lysoPLD activity using LPC as substrate assessed as reduction in choline release measured after 60 mins by HVA fluorescence based analysis
Assay data:16 Active, 13 Activity ≤ 1 µM, 19 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Assay data:9 Active, 1 Activity ≤ 1 µM, 18 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Cytotoxicity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Assay data:5 Active, 1 Activity ≤ 1 µM, 18 Tested
Cytotoxicity against human H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Assay data:4 Active, 18 Tested
SummaryCompounds, ActivePubMed Citation
Cytotoxicity against human NCI-H1581 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Assay data:6 Active, 18 Tested
Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human MCF-7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Assay data:7 Active, 18 Tested
Negative allosteric modulation activity against human ATX using FS-3 as substrate preincubated for 45 mins followed by substrate addition and measured every 30 mins by multi-mode microplate reader
Assay data:24 Active, 25 Activity ≤ 1 µM, 25 Tested
Antifibrotic activity against BLM induced C57BL/6J mouse lung fibrosis model assessed as recovery of body weight at 60 mg/kg, ip pretreated with compound administered once daily for 3 days followed by BLM treatment and measured after 28 days
Assay data:1 Active, 1 Tested
Downregulation of TNF-alpha expression in lung tissue of BLM induced C57BL/6J mouse lung fibrosis model assessed as fold reduction in TNF-alpha expression level at 60 mg/kg, ip by qRT-PCR analysis
Assay data:1 Tested
SummaryPubMed Citation
Downregulation of IL-6 expression in lung tissue of BLM induced C57BL/6J mouse lung fibrosis model assessed as fold reduction in IL-6 expression level at 60 mg/kg, ip by qRT-PCR analysis
Downregulation of TGF-beta expression in lung tissue of BLM induced C57BL/6J mouse lung fibrosis model assessed as fold reduction in TGF-beta expression level at 60 mg/kg, ip by qRT-PCR analysis
In vivo inhibition of ATX in lung homogenate of BLM induced C57BL/6J mouse lung fibrosis model assessed as reduction in ATX activity using FS-3 as substrate at 60 mg/kg, ip by fluorescence based microplate reader analysis (Rvb = 7.78%)
Assay data:2 Tested
Antifibrotic activity against BLM induced C57BL/6J mouse lung fibrosis model assessed as improvement in lung architecture by measuring appearance of conterminous fibrotic walls at 60 mg/kg, ip pretreated with compound administered once daily for 3 days followed by BLM treatment and measured after 28 days by hematoxylin and eosin staining based microscopic analysis
Antifibrotic activity against BLM induced C57BL/6J mouse lung fibrosis model assessed as improvement in lung architecture by measuring appearance of fibrotic lesions at 60 mg/kg, ip pretreated with compound administered once daily for 3 days followed by BLM treatment and measured after 28 days by hematoxylin and eosin staining based microscopic analysis
Antifibrotic activity against BLM induced C57BL/6J mouse lung fibrosis model assessed as improvement in lung architecture by measuring appearance of conterminous fibrotic walls at 60 mg/kg, ip pretreated with compound administered once daily for 3 days followed by BLM treatment and measured after 28 days by Masson staining based microscopic analysis
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