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Inhibition of [14C]-L-leucine uptake at LAT1 in human HT-29 cells after 1 hr by liquid scintillation counting
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Substrate activity at recombinant human LAT1 expressed in Xenopus laevis oocytes assessed as Km by measuring L-[14C]-leucine uptake by Eadie-Hofstee plot method
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of LAT1-mediated [14C]-L-leucine uptake in human MCF7 cells after 5 mins by liquid scintillation counting method
Assay data:3 Tested
Drug uptake in human MCF7 cells assessed as LAT1-mediated drug transportation rate at 3.125 to 100 uM after 10 mins by LC-MS analysis
Assay data:1 Tested
Drug uptake in human MCF7 cells assessed as LAT1-mediated drug transportation rate at 25 to 50 uM after 10 mins by LC-MS analysis
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
Trans-stimulation of human LAT1 expressed in TREx HEK293 cells assessed as induction of [3H]-gabapentin efflux at 200 uM after 3 mins by scintillation counting analysis relative to L-phenylalanine
Assay data:16 Tested
Cis-inhibition of human LAT1 expressed in TREx HEK293 cells at 200 uM assessed as inhibition of [3H]-gabapentin uptake preincubated for 3 mins at 37 degC followed by washing with choline buffer and measured after 3 hrs by scintillation counting analysis relative to BCH
Assay data:17 Tested
Cis-inhibition of human LAT1 expressed in TREx HEK293 cells assessed as inhibition of [3H]-gabapentin uptake preincubated for 3 mins at 37 degC followed by washing with choline buffer and measured after 3 hrs by scintillation counting analysis
Trans-stimulation of human LAT1 expressed in TREx HEK293 cells assessed as induction of [3H]-gabapentin efflux at 200 uM after 3 mins by scintillation counting analysis
Inhibition of recombinant human LAT1
Binding affinity to LAT1 (unknown origin) by in-vitro cell uptake assay
Inhibition of [14C]-L-leucine uptake at LAT1 in human YD-38 cells after 1 hr by liquid scintillation counting
Competitive inhibition of [14C]-L-leucine uptake at LAT1 in human MCF7 cells preincubated for 5 mins followed by addition of substrate measured during 5 mins by liquid scintillation counting
Potency index, ratio of IC50 for 2-amino-2-norbornanecarboxylic acid to IC50 for test compound for inhibition of [14C]-L-leucine uptake at LAT1 in human MCF7 cells
Competitive inhibition of [14C]-L-leucine uptake at LAT1 in human MCF7 cells at 25 uM preincubated for 10 mins followed by addition of substrate measured during 5 mins by liquid scintillation counting
Competitive inhibition of [14C]-L-leucine uptake at LAT1 in human MCF7 cells at 100 uM preincubated for 10 mins followed by addition of substrate measured during 5 mins by liquid scintillation counting
Drug uptake in human MCF7 cells assessed as LAT1 mediated drug transport per mg of protein at 100 uM measured 5 mins after cold wash by HPLC analysis
Drug uptake in human MCF7 cells assessed as LAT1 mediated drug transport per mg of protein at 100 uM measured 30 mins after cold wash by HPLC analysis
Drug uptake in human MCF7 cells assessed as LAT1 mediated drug transport per mg of protein at 100 uM measured 5 mins after warm wash by HPLC analysis
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