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Antagonist activity at human RXFP1 receptor expressed in CHO-K1 cells assessed as cAMP production upto 30 uM in presence of relaxin-3 incubated for 30 mins by TR-FRET assay
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Antagonist activity at human RXFP1 receptor expressed in CHO-K1 cells assessed as cAMP production at 10 to 30 uM in presence of relaxin-3 incubated for 30 mins by TR-FRET assay
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Agonist activity at human RXFP1 receptor expressed in CHO-K1 cells assessed as stimulation of cAMP production incubated for 30 mins by TR-FRET assay
Modulation of human RXFP1 stably expressed in T-REx-CHO-K1 cells assessed as stimulation of cAMP production measured after 45 mins by d2-dye labelled cAMP based HTRF assay
Assay data:6 Active, 6 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 6 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Agonist activity at human RXFP1 expressed in human CHO-K1 cells assessed as inhibition of H2 relaxin-induced cAMP accumulation at 10 uM incubated for 30 mins by TR-FRET assay relative to H2 relaxin
Assay data:22 Tested
PRESTO-Tango GPCRome screening (RXFP1)
SummaryRelated BioAssays by Target
Agonist activity at human RXFP1 expressed in human HEK-293T cells co-transfected with pCRE beta-galactosidase reporter plasmid assessed as inhibition of IBMX-induced cAMP accumulation incubated for 30 mins by HTRF assay
Assay data:2 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 2 Tested
Displacement of Eu3+-labelled H2 relaxin from human RXFP1 expressed in human HEK-293T cells in presence of 10 % FCS by competition binding assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Selectivity index, ratio of EC50 for agonist activity at rat RXFP1 expressed in human HEK296 cells in presence of RSA by HTRF assay to EC50 for EC50 for agonist activity at rat RXFP1 expressed in human HEK296 cells in absence of RSA by HTRF assay
Selectivity ratio of EC50 for agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells in presence of 2 % HSA to EC50 for agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells in absence of HSA
Assay data:8 Tested
Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins in presence of 2 % HSA by HTRF assay relative to control
Assay data:7 Tested
Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins in presence of 2 % HSA by HTRF assay
Assay data:7 Active, 7 Activity ≤ 1 µM, 11 Tested
Agonist activity at rat RXFP1 expressed in human HEK296 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay relative to control
Assay data:3 Tested
Agonist activity at rat RXFP1 expressed in human HEK296 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay
Assay data:3 Active, 2 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay relative to relaxin
Assay data:42 Tested
Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay
Assay data:42 Active, 7 Activity ≤ 1 nM, 42 Activity ≤ 1 µM, 42 Tested
Agonist activity at RXFP1 receptor (unknown origin) expressed in HEK-293T cells cotransfected with beta-galactosidase assessed as cAMP activation at 10 uM by beta-galactosidase reporter gene assay
Assay data:15 Tested
Agonist activity at RXFP1 receptor (unknown origin) expressed in HEK-293T cells cotransfected with beta-galactosidase assessed as cAMP activation by beta-galactosidase reporter gene assay
Assay data:11 Tested
Antagonist activity at human RXFP1 assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by mutRelaxin agonist addition measured after 60 mins by cell based TR-FRET assay
Agonist activity at human RXFP1 expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay relative to forskloin
Assay data:56 Tested
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