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Inhibition of human GABA-B receptor at 10 uM relative to control
Assay data:1 Active, 3 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Positive allosteric modulation of GABA-B receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS binding by [35S]GTPgammaS binding assay
Assay data:14 Active, 14 Activity ≤ 1 µM, 14 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Positive allosteric modulation of GABA-B receptor (unknown origin) assessed as fold increase in stimulation of [35S]GTPgammaS binding at 10 uM by [35S]GTPgammaS binding assay
Assay data:16 Tested
SummaryPubMed CitationRelated BioAssays by Target
Binding Assay from US Patent US10556914: "Substituted isoxazolopyridazinones and isothiazolopyridazinones and methods of use"
Assay data:88 Active, 36 Activity ≤ 1 µM, 100 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Agonist activity at human GABAB expressed in HEK293T cells co-transfected with human CaV2.2 channel assessed as inhibition of CaV2.2-mediated Ba2+ peak-current amplitude at -80 to 10 mV holding potential after 72 hrs by whole cell patch clamp assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Agonist activity at human GABAB expressed in HEK293T cells co-transfected with human CaV2.2-beta3 channel assessed as inhibition of CaV2.2-mediated Ba2+ peak-current amplitude at 100 nM at -80 to 10 mV holding potential after 72 hrs by whole cell patch clamp assay relative to control
Assay data:3 Tested
Agonist activity at human GABAB expressed in HEK293T cells co-transfected with human CaV2.2-alpha2delta1 channel assessed as inhibition of CaV2.2-mediated Ba2+ peak-current amplitude at 100 nM at -80 to 10 mV holding potential after 72 hrs by whole cell patch clamp assay relative to control
Agonist activity at human GABAB expressed in HEK293T cells co-transfected with human CaV2.2-alpha1B channel assessed as inhibition of CaV2.2-mediated Ba2+ peak-current amplitude at 100 nM at -80 to 10 mV holding potential after 72 hrs by whole cell patch clamp assay relative to control
Inhibition of GABA-B receptor (unknown origin) at 0.1 to 1 uM
Assay data:1 Tested
Activation of human GABAB1/GABAB2 expressed in HEK293 cells co-transfected with rat CaV2.2 channel assessed as reduction in CaV2.2-mediated peak-current amplitude in response to depolarizing pulse at 1 nM in presence of with 10 uM baclofen by whole cell patch clamp assay relative to control
Activation of human GABAB1/GABAB2 expressed in HEK293 cells co-transfected with rat CaV2.2 channel assessed as reduction in CaV2.2-mediated peak-current amplitude in response to depolarizing pulse at 10 uM by whole cell patch clamp assay relative to control
Assay data:2 Tested
Activation of human GABAB1/GABAB2 expressed in HEK293 cells co-transfected with rat CaV2.2 channel assessed as reduction in CaV2.2-mediated peak-current amplitude in response to depolarizing pulse at 1 nM by whole cell patch clamp assay relative to control
Activation of human GABAB1/GABAB2 expressed in HEK293 cells co-transfected with rat CaV2.2 channel assessed as reduction in CaV2.2-mediated Ba2+ peak-current amplitude in response to depolarizing pulse in presence of 1 uM GABAB receptor antagonist CGP55845 by whole cell patch clamp assay
Activation of human GABAB1/GABAB2 expressed in HEK293 cells co-transfected with rat CaV2.2 channel assessed as reduction in CaV2.2-mediated peak-current amplitude in response to the depolarizing pulse by whole cell patch clamp assay
Assay data:7 Active, 1 Activity ≤ 1 nM, 9 Activity ≤ 1 µM, 9 Tested
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
Positive allosteric modulator activity at GABA-B receptor (unknown origin) assessed as potentiation of 1 uM GABA-induced [35S]GTPgammaS binding
Assay data:1 Active, 1 Tested
Positive allosteric modulator activity at GABA-B receptor (unknown origin) assessed as potentiation of GABA-induced [35S]GTPgammaS binding
Assay data:5 Tested
Potency index, ratio of EC50 for racemic baclofen to EC50 for test compound for agonist activity at human recombinant GABA-B receptor
Agonist activity at human recombinant GABA-B receptor
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Displacement of [3H]CGP54626 from GABA-B receptor (unknown origin) by radioligand binding assay
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