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Substrate activity at OCT1 (unknown origin) assessed as uptake ratio
Assay data:6 Tested
SummaryPubMed CitationRelated BioAssays by Target
Substrate activity at human OCT2 overexpressed in HEK293 cells assessed as uptake ratio incubated for 2 mins by LC-MS/MS analysis
Substrate activity at human OCT1 overexpressed in HEK293 cells at 2.5 uM incubated for 2 mins by LC-MS/MS analysis
Assay data:6 Active, 7 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Substrate activity at human OCT2 overexpressed in HEK293 cells at 2.5 uM incubated for 2 mins by LC-MS/MS analysis
Inhibition of OCT2 mediated (unknown origin) assessed as intracellular accumulation of ASP+ relative to control
Assay data:4 Tested
Inhibition of OCT1 (unknown origin) overexpressed in HEK293 cells assessed as intracellular accumulation of ASP+ measured at 20 uM for 5 mins by Analyst AD plate reader method relative to control
Assay data:8 Tested
Inhibition Assay from US Patent US10689399: "Substituted 3,4,5,6,8,10,14,14a-octahydro-2h-2,6-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazocines and methods for treating viral infections"
Assay data:19 Active, 11 Activity ≤ 1 µM, 23 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition Assay from US Patent US9795602: "Polycyclic-carbamoylpyridone compounds and their pharmaceutical use"
Assay data:4 Active, 1 Activity ≤ 1 µM, 9 Tested
Inhibition of OCT2 (unknown origin) expressed in HEK293 cells
Assay data:1 Tested
Inhibition of OCT1 (unknown origin) expressed in HEK293 cells
Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake by measuring intrinsic clearance incubated for 2 mins by LC-MS/MS analysis
Assay data:22 Tested
Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake by measuring Vmax incubated for 2 mins by LC-MS/MS analysis
Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake by measuring Km incubated for 2 mins by LC-MS/MS analysis
Assay data:5 Active, 22 Tested
Inhibition of human OCT2 assessed as reduction in intracellular probe substrate accumulation upto 100 uM by microplate scintillation counter analysis relative to control
Inhibition of human OCT1 assessed as reduction in intracellular probe substrate accumulation upto 100 uM by microplate scintillation counter analysis relative to control
Inhibition of human OCT2 assessed as reduction in OCT2-mediated metformin transport at 14900 uM relative to control
Inhibition of human OCT1 assessed as reduction in OCT1-mediated metformin transport at 14900 uM relative to control
Inhibition of OCT2 (unknown origin) up to 50 uM
Drug transport in human OCT2 expressed in HEK Flp-In cells at 0.009 uM for 10 mins relative to control
Transport efficiency, ratio of maximal rate of transport to Km for drug transport in human OAT2 expressed in HEK Flp-In cells measured per mg of protein
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