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Substrate uptake by the Glycine Transporter-2 (GlyT2, SLC6A5) as assessed by the fluorescent FLIPR membrane potential dye in HEK-293 JumpIN-SLC6A5 cells (PubChem AID: 1794825)
Assay data:1 Tested
SummaryRelated BioAssays by Target
Membrane potential based assay for SLC6A5 using HEK-293 SLC6A5 OE cells
Assay data:1 Active, 1 Tested
SummaryCompounds, ActiveRelated BioAssays by DepositorRelated BioAssays by Target
Reversible inhibition of recombinant human GlyT2a expressed in Xenopus laevis oocytes assessed as recovery of transport current at IC50 followed by compound wash out followed by glycine re-application at 5 mins intervals throughout wash time course and measured after 25 mins by two-electrode voltage clamp electrophysiology
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Slow reversible inhibition of recombinant human GlyT2a expressed in Xenopus laevis oocytes assessed as recovery of transport current at IC50 followed by compound wash out followed by glycine re-application at 5 mins intervals throughout wash time course and measured after 30 mins by two-electrode voltage clamp electrophysiology
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of full length human GlyT2 expressed in FreeStyle 293-F suspension cells incubated for 30 mins before [3H]glycine addition and measured after 30 mins by liquid scintillation counting method
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of recombinant human GlyT2a expressed in Xenopus laevis oocytes assessed as reduction in channel current at 1 uM by two-electrode voltage clamp electrophysiology
Reversible non-competitive inhibition of human GlyT2a expressed in Xenopus laevis oocytes by two-electrode voltage clamp electrophysiology
Assay data:5 Active, 3 Activity ≤ 1 µM, 6 Tested
Reversible inhibition of recombinant human GlyT2 expressed in HEK293 cells assessed as reduction in [3H]-glycine uptake after 2 hrs by top count assay
Inhibition of recombinant human GlyT2
Inhibition of recombinant human GlyT2a expressed in Xenopus laevis oocytes assessed as reduction in channel current by two-electrode voltage clamp electrophysiology relative to control
Assay data:35 Tested
Inhibition of recombinant human GlyT2a expressed in Xenopus laevis oocytes assessed as reduction in channel current by two-electrode voltage clamp electrophysiology
Assay data:31 Active, 25 Activity ≤ 1 µM, 35 Tested
Inhibition of recombinant human GlyT2a expressed in Xenopus laevis oocytes assessed as reduction in channel current at 10 nM by two-electrode voltage clamp electrophysiology
Inhibition of recombinant human GlyT2a expressed in Xenopus laevis oocytes assessed as reduction in channel current at 30 nM by two-electrode voltage clamp electrophysiology
Inhibition of human GlyT2 expressed in porcine aorta epithelial cells assessed as reduction in [3H]-Glycine uptake at pH 7.5 by scintillation spectroscopy
Assay data:4 Active, 3 Activity ≤ 1 µM, 5 Tested
Inhibition of human glycine transporter-2 expressed in HEK293 cells assessed as reduction in [14C]glycine uptake preincubated for 10 mins followed by [14C]glycine addition measured after 3 hrs by scintillation proximity assay
Assay data:34 Tested
Inhibition of human GlyT2 stably expressed in CHO cells assessed as reduction in [3H]glycine uptake incubated for 10 mins by liquid scintillation counting method
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
Inhibition of GlyT2 (unknown origin)
Inhibition of human GlyT-2
Inhibition of human GlyT-2 expressed in HEK293 cells assessed as reduction in [3H]-glycine uptake
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