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Binding affinity to C3aR1 (unknown origin) at 10 uM by radioligand binding assay
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
Assay data:14 Active, 11 Activity ≤ 1 µM, 22 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
PRESTO-Tango GPCRome screening (C3AR1)
SummaryRelated BioAssays by Target
Potency index, ratio of SB290157 IC50 to test compound IC50 for antagonist activity at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release
Assay data:3 Tested
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
Displacement of Eu-DTPA-C3a from Galpha16-coupled C3a receptor (unknown origin) expressed in HEK293 cells measured after 60 mins by time-resolved fluorescence assay
Assay data:2 Tested
Potency index, ratio of SB290157 IC50 to test compound IC50 for antagonist activity at C3a receptor in human MDM cells
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
Assay data:24 Active, 18 Activity ≤ 1 µM, 28 Tested
Partial agonist activity at C3a receptor in human MDM cells assessed as induction of intracellular calcium release at higher concentration measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay relative to control
Assay data:7 Tested
Agonist activity at C3a receptor in human MDM cells assessed as induction of intracellular calcium release measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 28 Tested
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
Antagonist activity at C3aR in HMDM assessed as inhibition of agonist-induced Ca2+ release
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Agonist activity at C3aR in HMDM assessed as induction of Ca2+ release
Agonist activity at C3aR in HMDM assessed as induction of Ca2+ release measured for 5 mins by Fluo-3 AM dye-based fluorescence assay
Displacement of 125I-C3a from recombinant human C3aR expressed in HEK293 cell membranes after 3 hrs by scintillation proximity assay
Antagonist activity at human C3aR expressed in RBL-2H3 cells assessed as inhibition of C3a-induced intracellular calcium mobilization
Displacement of 125I-C3a from human C3aR expressed in RBL-2H3 cells
Human C3a receptor (Complement peptide receptors)
Assay data:13 Active, 13 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response at 10 uM measured for 60 secs by fluorescence assay relative to 100 nM C3a
Assay data:24 Tested
Displacement of [125I]-C3a from C3aR in human MDM cells at 20 uM after 60 mins by microbeta scintillation counting analysis
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