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ATX Inhibitory Selectivity Test from Article 10.1021/cb400150c: "Screening and X-ray crystal structure-based optimization of autotaxin (ENPP2) inhibitors, using a newly developed fluorescence probe."
Assay data:14 Active, 10 Activity ≤ 1 µM, 19 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Biochemical Assay from US Patent US9796719: "Compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders"
Assay data:101 Active, 98 Activity ≤ 1 µM, 102 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Potency index, ratio of IC50 for GLPG1690 to IC50 for test compound for inhibition of autotaxin in mouse plasma assessed as reduction in LPA (18:2) production incubated for 2 hrs LC-MS-/MS analysis
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of autotaxin in mouse plasma assessed as reduction in LPA (18:2) production incubated for 2 hrs LC-MS-/MS analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of ATX in mouse plasma assessed as reduction in LPA prodution after 3 hrs by LC-MS/MS analysis
Assay data:3 Tested
Inhibition of ATX in mouse plasma assessed as reduction in LPA prodution at 10 uM after 3 hrs by LC-MS/MS analysis
Assay data:11 Active, 30 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of ATX in mouse plasma after 2 hrs by LC-MS/MS analysis
Assay data:34 Active, 32 Activity ≤ 1 µM, 51 Tested
Inhibition of mouse ATX expressed in one-cell stage zebra fish embryos assessed as rescue of cardia bifida phenotype at 10 uM incubated for 12 to 24 hrs post fertilization in presence of Ki16425 by whole mount in situ hybridization based microscopic analysis relative to control
Assay data:6 Tested
Inhibition of mouse ATX using TG-mTMP as substrate after 2 hrs by fluorometric analysis
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Inhibition of ATX in mouse plasma assessed as reduction in LPA 18:2 production after 2 hrs by LC-MS/MS analysis
Inhibition of recombinant mouse ATX expressed in HEK293 cells using LPC 17:0 as substrate after 30 mins by LC-MS/MS method
Inhibition of recombinant mouse ATX expressed in HEK293 cells using FS3 as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins
Inhibition of mouse ATX-beta using LPC 18:0 as substrate by Amplex Red PLD assay
Assay data:7 Active, 5 Activity ≤ 1 µM, 7 Tested
Inhibition of mouse ATX-beta using LPC 16:0 as substrate by Amplex Red PLD assay
Assay data:15 Active, 9 Activity ≤ 1 µM, 25 Tested
Inhibition of ATX in paclitaxel-resistant mouse 4T1 cells assessed as potentiation of paclitaxel-induced antiproliferative activity by measuring reduction in cell viability at 5 uM measured after 3 days by CellTiter blue assay
Assay data:2 Tested
Inhibition of ATX in mouse 4T1 cells assessed as potentiation of paclitaxel-induced antiproliferative activity by measuring paclitaxel LD50 at 3 uM preincubated for 24 hrs followed by paclitaxel addition measured after 48 hrs by CellTiter blue assay (Rvb = 202 nM)
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Mouse autotaxin (LPA synthesis)
Assay data:1 Active, 1 Tested
Inhibition of recombinant mouse ATX using lysophosphatidylcholine as substrate by choline release assay
Inhibition of ATX in mouse plasma assessed as inhibition of LPA production after 2 hrs by LC-MS/MS analysis
Assay data:1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Genome-wide siRNA screen of genes regulating the Lipopolysaccharide-induced NF-kappaB and TNF-alpha responses in mouse macrophages_Primary screen NFkB readout
Assay data:762 Active, 16821 Tested
SummaryRelated BioAssays by Same Project
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