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I2/CENTR/R Eurofins SafetyScreen44 (BI)
Assay data:1 Tested
SummaryRelated BioAssays by Target
Inhibitory Assay from US Patent US8865750: "Small molecule inhibitors of RGS proteins"
Assay data:1 Active, 1 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
I1 CEREP ligand profiling
I2/CENTR/R Eurofins-Panlabs selectivity data (BI)
Binding affinity to Galpha-o (unknown origin) assessed as shifting of protein melting temperature by Sypro-orange dye based differential scanning fluorimetry
Assay data:1 Active, 1 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
Assay data:1 Active, 1 Activity ≤ 1 µM, 179 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of recombinant rat Gi coupled mGlu2 receptor expressed in CHO cells assessed as suppression of L-glutamate-induced decrease in cAMP level pretreated for 1 hr followed by L-glutamate/forskolin addition and measured after 30 mins by FRET assay
Assay data:8 Tested
SummaryPubMed CitationRelated BioAssays by Target
Binding affinity to Galphao (unknown origin) assessed as change in melting temperature by differential scanning fluorimetry
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Human regulator of G-protein signaling 8 (R4 family)
Assay data:3 Active, 3 Tested
High-throughput screen for inhibitors of the GIV GBA-motif interaction with Galpha-i G protein subunits
Assay data:879 Active, 206873 Tested
SummaryCompounds, ActiveRelated BioAssays by DepositorRelated BioAssays by Target
Binding affinity to Galphai1 (unknown origin) coupled with alpha-2 adrenoceptor transfected in HEK293 GloSensor cells assessed as restoration of Fsk/UK14304-induced reduction of cAMP preincubated for 20 mins followed by Fsk/UK14304 induction measured every 2 secs by FLIPR assay
Assay data:2 Tested
Binding affinity to Galphai1 (unknown origin) coupled with alpha-2 adrenoceptor transfected in HEK293 GloSensor cells assessed as restoration of Fsk/UK14304-induced reduction of cAMP at 0.1 to 10 uM preincubated for 20 mins followed by Fsk/UK14304 induction measured every 2 secs by FLIPR assay
Binding affinity to Galphai1 (unknown origin) coupled with alpha-2 adrenoceptor transfected in HEK293 GloSensor cells assessed as restoration of Fsk/UK14304-induced reduction of cAMP at 100 nM preincubated for 20 mins followed by Fsk/UK14304 induction measured every 2 secs by FLIPR assay relative to control
Binding affinity to GDP-bound human Galphai1 expressed in Escherichia coli BL21 in H2O/DMSO-d6 at 500 uM by STD NMR analysis
Assay data:1 Active, 2 Tested
Binding affinity to human Galphai1 expressed in Escherichia coli BL21 assessed as inhibition of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition measured for 30 mins by liquid scintillation counting analysis
Binding affinity to human Galphai1 expressed in Escherichia coli BL21 assessed as inhibition of BODIPY FL GTPgammaS binding by measuring fluorescence reduction at 30 to 300 uM preincubated for 30 mins followed by BODIPY FL GTPgammaS addition measured for 60 mins by real time nucleotide exchange assay relative to vehicle-treated control
Assay data:34 Tested
Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB
Assay data:3916 Active, 206 Activity ≤ 1 nM, 1830 Activity ≤ 1 µM, 3916 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
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