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Inhibition of the Organic Cation Transporter 3 (OCT3, SLC22A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by MPP+ uptake in HEK-293 JumpIN-SLC22A3 cells (PubChem AID: 1745861)
Assay data:4 Active, 2 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Substrate uptake at human OCT3 overexpressed in HEK293 cells incubated for 2 mins by LC-MS/MS analysis
Assay data:5 Active, 5 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of human OCT3 mediated methylscopolamine uptake overexpressed in HEK293 cells at 20 uM incubated for 5 mins by HPLC-MS/MS analysis relative to control
Assay data:5 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of human OCT3 mediated N-Ethyllidocaine uptake overexpressed in HEK293 cells at 20 uM incubated for 5 mins by HPLC-MS/MS analysis relative to control
Assay data:4 Tested
Inhibition of human OCT3 mediated Famotidine uptake overexpressed in HEK293 cells at 20 uM incubated for 5 mins by HPLC-MS/MS analysis relative to control
Inhibition of human OCT3 mediated (S,S)-Ethambutol uptake overexpressed in HEK293 cells at 20 uM incubated for 5 mins by HPLC-MS/MS analysis relative to control
Inhibition of human OCT3 mediated ASP+ uptake overexpressed in HEK293 cells at 20 uM incubated for 5 mins by HPLC-MS/MS analysis relative to control
Substrate activity at human OCT3 overexpressed in HEK293 cells at 2.5 uM incubated for 2 mins by LC-MS/MS analysis
Assay data:5 Active, 7 Tested
Inhibition of OCT3 (unknown origin) overexpressed in HEK293 cells assessed as intracellular accumulation of ASP+ incubated for 2 mins by Analyst AD plate reader method relative to control
Assay data:7 Tested
Inhibition of human OCT3 overexpressed in HEK293 cells assessed as intracellularly accumulation of ASP+ at 20 uM incubated for 5 mins by HPLC-MS/MS analysis relative to control
Assay data:2 Active, 14 Tested
Substrate activity at human OCT3 overexpressed in HEK293 cells assessed as uptake ratio incubated for 2 mins by LC-MS/MS analysis
Assay data:15 Tested
Impedance-based transport assay for SLC22A3 using HEK293 JumpIn SLC22A3 OE cells
Assay data:5 Active, 2 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Substrate activity at OCT3 in human Caco2 cells assessed as protein-mediated drug uptake at 0.5 mM measured after 10 mins in presence of OCT1 substrate metformin by UPLC-MS/MS analysis
Assay data:2 Tested
Substrate activity at OCT3 in human Caco2 cells assessed as protein-mediated drug uptake at 0.5 mM measured after 10 mins in absence of OCT1 substrate metformin by UPLC-MS/MS analysis
Substrate activity at human OCT3 expressed in HEK293 cells assessed as increase in compound uptake up to 200 uM incubated for 2 mins by LC-MS/MS analysis based Michaelis-Menten plot analysis relative to control empty vector transfected cells
Assay data:1 Tested
Substrate activity at human OCT3 expressed in HEK293 cells assessed as increase in compound uptake by measuring Km incubated for 2 mins by LC-MS/MS analysis based Michaelis-Menten plot analysis relative to control empty vector transfected cells
Assay data:3 Tested
Substrate activity at human OCT3 expressed in HEK293 cells assessed as increase in compound uptake by measuring Vmax incubated for 2 mins by LC-MS/MS analysis based Michaelis-Menten plot analysis relative to control empty vector transfected cells
Competitive inhibition of human OCT3 expressed in HEK293 cells in presence of varying concentration of MPP+ by Lineweaver-Burk plot analysis
Assay data:1 Active, 1 Tested
Competitive inhibition of human OCT3 expressed in HEK293 cells up to 10 uM in presence of varying concentration of MPP+ by Lineweaver-Burk plot analysis
Competitive inhibition of human OCT3 expressed in HEK293 cells up to 25 uM in presence of varying concentration of MPP+ by Lineweaver-Burk plot analysis
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