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Inhibition of MRGPRX2 receptor (unknown origin) upto 10000 nM
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Selectivity interaction (FLIPR assay) EUB0000353a MRGPRX2
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Selectivity interaction (FLIPR assay) EUB0000345a MRGPRX2
SummaryRelated BioAssays by Target
Affinity On-target Cellular interaction (PRESTO-Tango concentration response assay (by the NIMH-PDSP)) EUB0000353a MRGPRX2
Affinity On-target Cellular interaction (PRESTO-Tango concentration response assay (by the NIMH-PDSP)) EUB0000345a MRGPRX2
Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay
Assay data:29 Active, 22 Activity ≤ 1 µM, 61 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells assessed as maximal efficacy at 5 uM in presence of BAM8-22 by Fluo4-dye based FLIPR assay relative to control
Assay data:61 Tested
Antagonist activity at MRGPRX2 (unknown origin) expressed in HEK293 cells assessed as inhibition of C48/80-induced Ca2+- mobilization
Assay data:2 Tested
Antagonist activity at MRGPRX2 (unknown origin) expressed in HEK293 cells assessed as inhibition of calcium mobilization at upto 10 uM
Assay data:3 Active, 3 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Agonist activity at MRGPRX2 (unknown origin) expressed in HEK293 cells assessed as induction of G(o) dissociation by measuring luminescent decay at 32 uM by NanoBiT-G-protein dissociation assay
Assay data:2 Active, 2 Tested
Agonist activity at MRGPRX2 (unknown origin) expressed in HEK293 cells assessed as induction of G(o) dissociation by measuring luminescent decay at 10 uM by NanoBiT-G-protein dissociation assay
Assay data:1 Active, 1 Tested
Agonistic activity at MRGPRX2 (unknown origin)
Antagonist activity at human MRGPRX2 expressed in HEK293 cells co-expressing mouse Galpha15 assessed as inhibition of Cortistatin-14 induced Ca2+ mobilization preincubated for 30 mins followed by Cortistatin-14 addition by FLIPRtetra-calcium mobilization assay
Assay data:1 Active, 6 Activity ≤ 1 µM, 6 Tested
Agonist activity at human MRGPRX1 expressed in HEK293 cells upto 100 uM in absence of BAM8-22 by Fluo-dye based FLIPR assay
Positive allosteric modulator activity at human MRGPRX1 transfected in HEK293 cells assessed as maximal efficacy in presence of BAM8-22 by Fulo4AM dye based FLIPR assay relative to control
Assay data:18 Tested
Positive allosteric modulator activity at human MRGPRX1 transfected in HEK293 cells in presence of BAM8-22 by Fulo4AM dye based FLIPR assay
Assay data:15 Active, 8 Activity ≤ 1 µM, 20 Tested
Positive allosteric modulator activity at human MRGPRX2 transfected in HEK293 cells at 5 uM in presence of C48/80 by Fluo-4 AM-based FLIPR assay
PRESTO-Tango Assay from Article 10.1038/nchembio.2334: "In silico design of novel probes for the atypical opioid receptor MRGPRX2."
Assay data:13 Active, 2 Activity ≤ 1 µM, 32 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Intracellular Calcium Mobilization Assay from Article 10.1038/nchembio.2334: "In silico design of novel probes for the atypical opioid receptor MRGPRX2."
Assay data:15 Active, 4 Activity ≤ 1 µM, 26 Tested
FLIPR assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
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