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LMPTP Primary Screening Protocol from US Patent US10626094: "Inhibitors of low molecular weight protein tyrosine phosphatase and uses thereof"
Assay data:260 Active, 52 Activity ≤ 1 µM, 332 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Activation of human TREK-1 channel expressed in CHO cells at 10 uM by patch clamp electrophysiology method
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Activation of human TREK-1 expressed in CHO cells at 10 uM in presence of ML335 by patch clamp electrophysiology method
Assay data:2 Active, 2 Tested
Inhibition of human TREK-2 expressed in Xenopus laevis oocytes assessed as inhibition of channel current at 10 uM at +40mV holding potential by two-electrode voltage clamp assay
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of human TREK-1 expressed in Xenopus laevis oocytes assessed as inhibition of channel current at 10 uM at +40mV holding potential by two-electrode voltage clamp assay
TREK1 Assay from Article 10.1111/cbdd.12810: "Identification of the first in silico-designed TREK1 antagonists that block channel currents dose dependently."
Assay data:18 Active, 7 Activity ≤ 1 µM, 28 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of human TREK1 at intermediate transition state expressed in CHO cells by whole-cell patch-clamp electrophysiological method
Assay data:3 Active, 3 Tested
Effect on channel conductance of human TREK1 expressed in CHO cells by single-channel recordings based by inside-out patch method
Inhibition of human TREK1 at intermediate transition state expressed in CHO cells assessed as decrease in probability of TREK1 channel being in open state by single-channel recordings based by inside-out patch method
Inhibition of human TREK1 T211A mutant at intermediate transition state expressed in CHO cells by whole-cell patch-clamp electrophysiological method
Inhibition of human TREK1 M291A mutant at intermediate transition state expressed in CHO cells by whole-cell patch-clamp electrophysiological method
Inhibition of human TREK1 W295A mutant at intermediate transition state expressed in CHO cells by whole-cell patch-clamp electrophysiological method
Inhibition of human TREK1 V288A mutant at intermediate transition state expressed in CHO cells by whole-cell patch-clamp electrophysiological method
Inhibition of human TREK1 S290A mutant at intermediate transition state expressed in CHO cells by whole-cell patch-clamp electrophysiological method
Assay data:2 Active, 3 Tested
Inhibition of human TREK1 D294A mutant at intermediate transition state expressed in CHO cells by whole-cell patch-clamp electrophysiological method
Assay data:1 Active, 3 Tested
Inhibition of human TREK2 at intermediate transition state expressed in CHO cells by whole-cell patch-clamp electrophysiological method
Inhibition of human TREK1 R207A mutant at intermediate transition state expressed in CHO cells by whole-cell patch-clamp electrophysiological method
Assay data:1 Active, 2 Tested
Inhibition of human TREK1 in open state expressed in CHO cells in presence of 10 uM TREK1 activator arachidonic acid by whole-cell patch-clamp electrophysiological method
Activation of human TREK1 at 30 uM by thallium flux mobilization assay relative to control
Assay data:33 Tested
Activation of human TREK1 at 10 uM by thallium flux mobilization assay relative to control
Assay data:4 Tested
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