BDBM50205990 CHEMBL395429 OXYTOCIN
BDBM50332723 Cystathionine Oxytocin CHEMBL1630531
CHEMBL352836 BDBM50056797 Oxytocin Trisulfide
Lanthionine Oxytocin BDBM50332726 CHEMBL1630530
CAS_50-56-6 Oxytocin BDBM86210 NSC_439302
Cys-Tyr-Ile-Gln-Asn-Cys-Pro-Leu-Gly-NH2 1-[19-Amino-13-sec-butyl-10-(2-carbamoyl-ethyl)-7-carbamoylmethyl-16-(4-hydroxy-benzyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaaza-cycloicosane-4-carbonyl]-pyrrolidine-2-carboxylic acid [1-(carbamoylmethyl-carbamoyl)-3-methyl-butyl]-amide CHEMBL265640 1-[19-Amino-13-sec-butyl-10-(2-carbamoyl-ethyl)-7-carbamoylmethyl-16-(4-hydroxy-benzyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaaza-cycloicosane-4-carbonyl]-pyrrolidine-2-carboxylic acid [1-(carbamoylmethyl-carbamoyl)-3-methyl-butyl]-amide(Oxytocin) 1-[19-Amino-13-sec-butyl-10-(2-carbamoyl-ethyl)-7-carbamoylmethyl-16-(4-hydroxy-benzyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaaza-cycloicosane-4-carbonyl]-pyrrolidine-2-carboxylic acid [1-(carbamoylmethyl-carbamoyl)-3-methyl-butyl]-amidec-[Cys-Tyr-Ile-Gln-Asn-Cys]-Pro-Leu-Gly-NH2 BDBM50013775 OXYTOCIN (oxytocin-OT) cyclo[Cys-Tyr-Ile-Gln-Asn-Cys]-Pro-Leu-Gly-NH2
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- ChEMBL_149053 Inhibition of binding of [3H]oxytocin with human oxytocin receptor
- ChEMBL_321073 Displacement of [3H]oxytocin from human Oxytocin receptor
- ChEMBL_652651 Displacement of [3H]oxytocin from human oxytocin receptor
- ChEMBL_661588 Displacement of [3H]-oxytocin from human oxytocin receptor
- ChEMBL_727047 Displacement of [3H]oxytocin from human oxytocin receptor
- ChEMBL_821157 Displacement of [3H]oxytocin from human oxytocin receptor
- ChEMBL_149054 Displacement of 3[H]oxytocin from human oxytocin receptor
- ChEMBL_149058 Inhibition of binding of [3H]oxytocin to rat uterine oxytocin receptor
- ChEMBL_149182 Inhibition of [3H]- oxytocin binding to rat uterine Oxytocin receptor
- ChEMBL_661536 Displacement of [3H]-oxytocin from oxytocin receptor in human uterus tissue
- ChEMBL_661537 Displacement of [3H]-oxytocin from oxytocin receptor in rat uterus tissue
- ChEMBL_449794 Displacement of [3H]oxytocin from human oxytocin receptor expressed in CHO cells
- ChEMBL_661552 Displacement of [3H]-oxytocin from human oxytocin receptor expressed in CHO cells
- ChEMBL_661556 Displacement of [3H]-oxytocin from rat oxytocin receptor expressed in CHO cells
- ChEMBL_748692 Displacement of [3H]oxytocin from human oxytocin receptor expressed in CHO cells
- ChEMBL_145030 Inhibition of radioligand [3H]oxytocin binding at the oxytocin (OT) receptor in rat uterine tissue
- ChEMBL_149056 Compound was tested for its ability to displace [3H]oxytocin from human Oxytocin receptor
- ChEMBL_661577 Displacement of [3H]-oxytocin from human oxytocin receptor expressed in HEK293-EBNA cells
- ChEMBL_661578 Displacement of [3H]-oxytocin from rat oxytocin receptor expressed in HEK293-EBNA cells
- ChEMBL_821172 Antagonist activity at human oxytocin receptor assessed as inhibition of oxytocin binding by FLIPR analysis
- ChEMBL_661561 Antagonist activity at oxytocin receptor in rat uterine strips assessed as inhibition of oxytocin-induced contraction
- ChEMBL_748741 Displacement of radiolabeled oxytocin from human oxytocin receptor expressed in CHO cells by scintillation counting
- ChEMBL_578259 Antagonist activity at oxytocin receptor in Wistar rat uterus assessed as inhibition of oxytocin-induced uterotonic activity treated 1 min prior to oxytocin challenge in absence of Mg2+
- ChEMBL_515097 Binding affinity to oxytocin receptor
- ChEMBL_561007 Binding affinity to oxytocin receptor
- ChEMBL_651959 Antagonist activity at oxytocin receptor
- ChEMBL_864207 Binding affinity to oxytocin receptor
- ChEBML_149062 Compound was tested for its ability to inhibit binding of Oxytocin to its Oxytocin receptor in rat uterine tissue
- ChEMBL_149060 Compound was evaluated for half-maximal inhibition of binding of [3H]oxytocin to Oxytocin receptor in rat uterine tissue
- ChEMBL_149174 Binding affinity against Oxytocin receptor was determined in rat uterine membrane using radioligand [3H]oxytocin
- ChEMBL_515100 Displacement of [3H]oxytocin from human oxytocin receptor expressed in CHO cells by filtration binding assay
- ChEMBL_813470 Displacement of [3H]oxytocin from human oxytocin receptor after 1.5 hrs by liquid scintillation counting
- ChEMBL_540354 Displacement of 3H-oxytocin from human recombinant oxytocin receptor expressed in CHO cells by filtration binding assay
- ChEBML_149046 Binding affinity for human oxytocin receptor
- ChEMBL_149044 Binding affinity for human oxytocin receptor
- ChEMBL_149203 Antagonistic activity against Oxytocin receptor
- ChEMBL_149204 Binding affinity towards oxytocin receptor
- ChEMBL_220998 Binding affinity against oxytocin receptor
- ChEMBL_304139 Effective concentration for human Oxytocin receptor
- ChEMBL_465428 Binding affinity to human oxytocin receptor
- ChEMBL_465438 Binding affinity to recombinant oxytocin receptor
- ChEMBL_590266 Displacement of [3H]oxytocin from human oxytocin receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter
- ChEMBL_326543 Inhibitory activity against human Oxytocin induced intracellular Calcium mobilization in human Oxytocin receptor transfected HEK293-EBNA cells
- ChEMBL_149189 Biological activity against Oxytocin receptor in rat
- ChEMBL_1473360 Displacement of [3H]-oxytocin from human oxytocin receptor expressed in HEK cell membranes after 1 hr by scintillation proximity assay
- ChEMBL_1555978 Displacement of [3H]-oxytocin from human oxytocin receptor expressed in HEK293 cells after 90 mins by microbeta 2 microplate reader analysis
- ChEBML_149179 Binding affinity for rat uterine oxytocin receptor (rOTr)
- ChEBML_149183 Binding affinity against oxytocin receptor in rat uterus
- ChEMBL_149175 Binding affinity for rat oxytocin receptor (OT-R)
- ChEBML_149042 Inhibitory concentration required for antagonist activity against oxytocin receptor
- ChEMBL_1474017 Competitive binding to human oxytocin receptor by radioligand binding assay
- ChEMBL_149043 Binding affinity for cloned human oxytocin receptor (OT-R)
- ChEMBL_321075 Displacement of [3H]oxytocin from human V2 vasopressin receptor
- ChEMBL_321076 Displacement of [3H]oxytocin from human V1b vasopressin receptor
- ChEMBL_321077 Displacement of [3H]oxytocin from human V1a vasopressin receptor
- ChEMBL_1555992 Displacement of [Tyrosyl-2,6-3H]-Oxytocin from recombinant human oxytocin receptor expressed in CHO-DUKX-A2 cells after 180 mins by liquid scintillation counting analysis
- ChEMBL_1474016 Competitive binding to oxytocin receptor (unknown origin) by radioligand binding assay
- ChEMBL_149055 Ability to displace [3H]oxytocin from human OT receptor (hOT)
- ChEMBL_149171 Displacement of [3H]OT from binding to oxytocin receptor of rat uterus
- ChEMBL_149192 In vitro Oxytocin receptor antagonistic activity against rat uterine strips
- ChEMBL_697994 Displacement of [3H]OT from oxytocin receptor expressed in COS1 cells
- ChEBML_193005 Binding affinity against oxytocin receptor (rOTr) in DES pretreated rat uterine
- ChEMBL_149063 Concentration required to displace 50% of [3H]oxytocin from rat uterine receptor.
- ChEMBL_1766336 Displacement of [3H]-oxytocin from OTR receptor in human USMC cell membranes
- ChEMBL_446244 Displacement of [3H]AVP from human oxytocin receptor expressed in CHO cells
- ChEMBL_515099 Antagonist activity at human oxytocin receptor expressed in CHO cells by FLIPR assay
- ChEMBL_609611 Displacement of [3H]AVP from human oxytocin receptor expressed in CHO cells
- ChEMBL_1730147 Antagonist activity at human OXTR expressed in CHOK1 cells assessed as oxytocin-induced beta-arrestin recruitment pre-incubated for 30 mins before oxytocin stimulation for 90 or 180 mins by chemiluminescence method
- ChEBML_149040 Compound was evaluated for its dissociation constant (Kd) to guinea pig myometrial Oxytocin receptor
- ChEBML_149059 Half-maximal inhibition of binding of [3H]oxytocin to OT receptor in rat uterine tissue
- ChEBML_149178 Binding affinity towards rat uterine receptor was determined using [3H]oxytocin as radioligand
- ChEBML_149202 Compound was tested for displacement of 3[H] oxytocin from rat OT receptor (in vitro)
- ChEMBL_149040 Compound was evaluated for its dissociation constant (Kd) to guinea pig myometrial Oxytocin receptor
- ChEMBL_149178 Binding affinity towards rat uterine receptor was determined using [3H]oxytocin as radioligand
- ChEMBL_149202 Compound was tested for displacement of 3[H] oxytocin from rat OT receptor (in vitro)
- ChEMBL_540347 Antagonist activity at human recombinant oxytocin receptor expressed in CHO cells by FLIPR assay
- ChEMBL_578145 Antagonist activity at human cloned oxytocin receptor by cell based beta-lactamase assay
- ChEMBL_604218 Antagonist activity at human cloned oxytocin receptor by cell based beta lactamase assay
- ChEMBL_615224 Antagonist activity at human oxytocin receptor expressed in CHO cells by beta lactamase assay
- ChEMBL_813468 Displacement of [125I]-OVTA from prairie vole Oxytocin receptor after 72 hrs
- ChEBML_1555980 Antagonist activity at human oxytocin receptor expressed in HEK293 cells assessed as inhibition of oxytocin induced IP1 accumulation pretreated for 30 mins measured 1 hr post Ab-Cryptate and IP1-d2 addition by HTRF assay
- ChEMBL_1555980 Antagonist activity at human oxytocin receptor expressed in HEK293 cells assessed as inhibition of oxytocin induced IP1 accumulation pretreated for 30 mins measured 1 hr post Ab-Cryptate and IP1-d2 addition by HTRF assay
- Oxytocin Receptor Antagonist Assay This assay was performed in CHEM-1 cells expressing the human Oxytocin Receptor (hOTR) to determine the inhibitory effect of the compounds of the invention on the human Oxytocin receptor. Oxytocin evokes an increase in intracellular calcium in CHEM-1-hOTR cells which is measured in a fluorescence assay on the FLIPRTETRA using calcium sensitive dyes. Test compounds were assessed for their ability to affect the magnitude of the response to oxytocin, with antagonists showing a concentration-dependent reduction in the oxytocin-mediated fluorescence. Compounds displaying potency at the vasopressin V1a receptor of <100 nM were progressed to selectivity testing against hOTR and were tested in triplicate in a 10-point, 1:3 dilution series starting at a nominal concentration of 3 μM in the assay.CHEM-1-hOTR ready was used to assay frozen cells (Eurofins #HTS090RTA) which are supplied with a proprietary Media Component.
- ChEBML_149050 Binding affinity against cloned human oxytocin receptor from human embryonic kidney cells
- ChEMBL_148874 Inhibition of radioligand [3H]OT binding to oxytocin receptor (OT) in guinea pig myometrium membrane
- ChEMBL_326537 Displacement of [125I]OVTA antagonist from human oxytocin receptor expressed in HEK293-EBNA cells
- ChEMBL_326541 Displacement of [125I]OVTA antagonist from rat oxytocin receptor expressed in HEK293-EBNA cells
- ChEMBL_513959 Antagonist activity at human cloned oxytocin receptor by cell based beta lactamase reporter assay
- ChEMBL_535596 Antagonist activity at human oxytocin receptor by cell based beta-lactamase reporter gene assay
- ChEMBL_540346 Binding affinity to human recombinant oxytocin receptor expressed in CHO cells by fluorescence polarization assay
- ChEMBL_609617 Activity at human oxytocin receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
- ChEMBL_697993 Activity at oxytocin receptor expressed in COS1 cells assessed as IP-one generation by HTRF assay
- ChEMBL_1431801 Agonist activity at human oxytocin receptor expressed CHO cells assessed as calcium flux by FLIPR method
- ChEMBL_743722 Displacement of [3H]AVP from human oxytocin receptor expressed CHO cells after 60 mins
- ChEMBL_864195 Displacement of [3H]-AVP from human oxytocin receptor expressed in CHO cells after 30 mins
- ChEBML_149051 In vivo antagonistic activity against cloned human oxytocin receptor over-expressed in a stable HEK293 cell line
- ChEMBL_1474007 Binding affinity to SNAP-tagged oxytocin receptor (unknown origin) expressed in HEK293 cells by TR-FRET assay
- ChEMBL_149051 In vivo antagonistic activity against cloned human oxytocin receptor over-expressed in a stable HEK293 cell line
- ChEMBL_515103 Displacement of [3H]oxytocin from human vasopressin V2 receptor expressed in CHO cells by filtration binding assay
- ChEMBL_1711200 Antagonist activity at human mammary gland oxytocin receptor expressed in CHO cells assessed as inhibition of agonist-induced intracellular calcium flux preincubated for 20 mins followed by oxytocin addition measured for 5 mins by Fluo-4-AM dye based FLIPR assay
- ChEMBL_373748 Agonist activity at human OTR expressed in CHO cells assessed as inhibition of oxytocin-induced calcium mobilization by FLIPR assay
- ChEMBL_1726373 Displacement of [3H]-oxytocin from human OTR expressed in HEK293 cell membranes after 90 mins by radioligand binding assay
- ChEMBL_1766328 Displacement of [tyrosyl-2,6-3H] oxytocin from OTR (unknown origin) expressed in HEK293 cell membranes incubated for 60 mins
- ChEMBL_1451726 Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay
- ChEMBL_149047 Binding affinity was evaluated by measuring the displacement of [3H]OT (oxytocin) from specific binding sites in uterine tissue obtained from human
- ChEMBL_149048 Binding affinity was evaluated by measuring the displacement of [3H]-OT (oxytocin) from specific binding sites in uterine tissue obtained from human.
- ChEMBL_149052 The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Oxytocin receptor
- ChEMBL_149180 Binding affinity was evaluated by measuring the displacement of [3H]-OT (oxytocin) from specific binding sites in uterine tissue obtained from rats
- ChEMBL_1651553 Displacement of [3H]Oxytocin from human OXTR expressed in CHO cell membranes after 90 mins by liquid scintillation counting method
- ChEMBL_1724090 Displacement of [3H]-oxytocin from human OTR expressed in HEK293 cell membranes after 90 mins by microbeta scintillation counting method
- ChEMBL_149045 Binding affinity against human oxytocin receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
- ChEMBL_149057 Binding affinity against human oxytocin receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
- ChEMBL_1555993 Agonist activity at recombinant human oxytocin receptor expressed in CHO-DUKX-A2 cells assessed as change in intracellular calcium level by FLIPR assay
- ChEMBL_1711191 Displacement of [3H]OT from human mammary gland oxytocin receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
- ChEBML_1681637 Displacement of [Tyrosyl-2,6-3H]Oxytocin from recombinant mouse OTR expressed in CHO-K1 cells after 180 mins by liquid scintillation counting method
- ChEMBL_1474013 Agonist activity at SNAP-tagged oxytocin receptor (unknown origin) expressed in HEK293 cells assessed as intracellular calcium flux after 3 mins by fluorescence assay
- ChEMBL_1583335 Displacement of [3H]8-arginine-vasopressin from human oxytocin receptor expressed in CHO cell membrane incubated for 1 hr by liquid scintillation counting method
- ChEMBL_700576 Antagonist activity at recombinant oxytocin receptor expressed in CHO cells assessed as inhibition of vasopressin-induced calcium release after 10 mins by Fluo4-AM staining
- ChEMBL_743728 Agonist activity at human oxytocin receptor expressed CHO cells assessed as induction of phospholipase C activity after 15 mins by inositol phosphate accumulation assay
- ChEMBL_1474018 Binding affinity to SNAP-tagged oxytocin receptor (unknown origin) expressed in HEK293 cells assessed as association constant after 5 to 120 mins by TR-FRET assay
- ChEMBL_1474023 Binding affinity to SNAP-tagged oxytocin receptor (unknown origin) expressed in HEK293 cells assessed as dissociation constant after 5 to 120 mins by TR-FRET assay
- ChEMBL_1681633 Displacement of [Tyrosyl-2,6-3H]Oxytocin from recombinant human OTR expressed in CHO-DUKX-A2 cells after 180 mins by liquid scintillation counting method
- ChEBML_1583333 Agonist activity at human oxytocin receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 90 sec by fluo-4 dye based FLIPR assay
- ChEMBL_1583333 Agonist activity at human oxytocin receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 90 sec by fluo-4 dye based FLIPR assay
- ChEMBL_1555979 Agonist activity at human oxytocin receptor expressed in HEK293 cells assessed as increase in IP1 accumulation preincubated for 1 hr followed by addition of Ab-Cryptate and IP1-d2 by HTRF assay
- ChEMBL_1711194 Agonist activity at human mammary gland oxytocin receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
- ChEMBL_1766322 Displacement of [Tyrosyl-2,6-3H]oxytocin from recombinant human OTR expressed in CHO-DUKX-A2 cells incubated for 180 mins by scintillation counting based whole cell radioligand binding assay
- ChEMBL_1933582 Agonist activity at human oxytocin receptor expressed in HEK293 cells coexpressing Rluc8-tagged Galphaq, N-terminal GFP-tagged Ggamma2 and Gbeta1 protein incubated for 2 mins by Gq protein activation based BRET assay
- ChEMBL_1933586 Agonist activity at human oxytocin receptor C47A mutant expressed in HEK293 cells coexpressing Rluc8-tagged Galphaq, N-terminal GFP-tagged Ggamma2 and Gbeta1 protein incubated for 2 mins by Gq protein activation based BRET assay
- ChEMBL_1933583 Agonist activity at human oxytocin receptor high affinity site expressed in HEK293 cells coexpressing Rluc8-tagged Galphaq, N-terminal GFP-tagged Ggamma2 and Gbeta1 protein incubated for 2 mins by Gq protein activation based BRET assay
- ChEMBL_1933584 Agonist activity at human oxytocin receptor low affinity site expressed in HEK293 cells coexpressing Rluc8-tagged Galphaq, N-terminal GFP-tagged Ggamma2 and Gbeta1 protein incubated for 2 mins by Gq protein activation based BRET assay
- ChEMBL_1933591 Agonist activity at human oxytocin receptor V43A/C47A double mutant expressed in HEK293 cells coexpressing Rluc8-tagged Galphaq, N-terminal GFP-tagged Ggamma2 and Gbeta1 protein incubated for 2 mins by Gq protein activation based BRET assay
- ChEMBL_1933594 Agonist activity at human oxytocin receptor expressed in HEK293 cells coexpressing Rluc8-tagged Galphaq, N-terminal GFP-tagged Ggamma2 and Gbeta1 protein incubated for 2 mins in presence of TMH1-TAT peptide by Gq protein activation based BRET assay
- ChEMBL_1933595 Agonist activity at human oxytocin receptor expressed in HEK293 cells coexpressing Rluc8-tagged Galphaq, N-terminal GFP-tagged Ggamma2 and Gbeta1 protein incubated for 2 mins in presence of TMH5-TAT peptide by Gq protein activation based BRET assay
- ChEMBL_1933589 Agonist activity at human oxytocin receptor C47A mutant high affinity site expressed in HEK293 cells coexpressing Rluc8-tagged Galphaq, N-terminal GFP-tagged Ggamma2 and Gbeta1 protein incubated for 2 mins by Gq protein activation based BRET assay
- ChEMBL_1933590 Agonist activity at human oxytocin receptor C47A mutant low affinity site expressed in HEK293 cells coexpressing Rluc8-tagged Galphaq, N-terminal GFP-tagged Ggamma2 and Gbeta1 protein incubated for 2 mins by Gq protein activation based BRET assay
- ChEMBL_1933592 Agonist activity at human oxytocin receptor V43A/C47A double mutant high affinity site expressed in HEK293 cells coexpressing Rluc8-tagged Galphaq, N-terminal GFP-tagged Ggamma2 and Gbeta1 protein incubated for 2 mins by Gq protein activation based BRET assay
- ChEMBL_1933593 Agonist activity at human oxytocin receptor V43A/C47A double mutant low affinity site expressed in HEK293 cells coexpressing Rluc8-tagged Galphaq, N-terminal GFP-tagged Ggamma2 and Gbeta1 protein incubated for 2 mins by Gq protein activation based BRET assay
- ChEMBL_1933602 Agonist activity at human oxytocin receptor high affinity site expressed in HEK293 cells coexpressing Rluc8-tagged Galphaq, N-terminal GFP-tagged Ggamma2 and Gbeta1 protein incubated for 2 mins in presence of TMH5-TAT peptide by Gq protein activation based BRET assay
- ChEMBL_1933603 Agonist activity at human oxytocin receptor low affinity site expressed in HEK293 cells coexpressing Rluc8-tagged Galphaq, N-terminal GFP-tagged Ggamma2 and Gbeta1 protein incubated for 2 mins in presence of TMH5-TAT peptide by Gq protein activation based BRET assay
- Fluorescence-based cell-based high throughput dose response assay for agonists of the Oxytocin Receptor (OXTR) Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC) Center Affiliation: The Scripps Research Institute (TSRI) Assay Provider: Michael Jarstfer, University of North Carolina at Chapel Hill (UNC) Network: Molecular Libraries Probe Production Centers Network (MLPCN) Grant Proposal Number: 1 R03 MH085678-01A1 Grant Proposal PI: Michael Jarstfer, UNC External Assay ID: OTR_AG_FLUO8_1536_3XEC50 DRUN Name: Fluorescence-based cell-based high throughput dose response assay for agonists of the Oxytocin Receptor (OXTR). Description: Heterotrimeric G-protein coupled receptors (GPCRs) are major targets for disease therapeutics, due in part to their broad tissue distribution, structural diversity, varied modes of action, disease-associated mutations (1-4). Certain GPCRs are involved in signaling pathways for neuropeptides such as oxytocin, serotonin, and vasopressin, and influence complex social behaviors such as trust, anxiety, and parenting (5). Oxyto
- Fluorescence-based cell-based high throughput dose response assay for potentiators of Oxytocin Receptor (OXTR) Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC) Center Affiliation: The Scripps Research Institute (TSRI) Assay Provider: Michael Jarstfer, University of North Carolina at Chapel Hill (UNC) Network: Molecular Libraries Probe Production Centers Network (MLPCN) Grant Proposal Number: 1 R03 MH085678-01A1 Grant Proposal PI: Michael Jarstfer, UNC External Assay ID: OTR_POT_FLUO8_1536_3XEC50 DRUN Name: Fluorescence-based cell-based high throughput dose response assay for potentiators of Oxytocin Receptor (OXTR). Description: Heterotrimeric G-protein coupled receptors (GPCRs) are major targets for disease therapeutics, due in part to their broad tissue distribution, structural diversity, varied modes of action, disease-associated mutations (1-4). Certain GPCRs are involved in signaling pathways for neuropeptides such as oxytocin, serotonin, and vasopressin, and influence complex social behaviors such as trust, anxiety, and parenting (5). Oxyto
- Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R) Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC) Center Affiliation: The Scripps Research Institute (TSRI) Assay Provider: Michael Jarstfer, University of North Carolina at Chapel Hill (UNC) Network: Molecular Libraries Probe Production Centers Network (MLPCN) Grant Proposal Number: 1 R03 MH085678-01A1 Grant Proposal PI: Michael Jarstfer, UNC External Assay ID: V1R_AG_FLUO8_1536_3XEC50 OXTR DCSRUN Name: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). Description: Heterotrimeric G-protein coupled receptors (GPCRs) are major targets for disease therapeutics, due in part to their broad tissue distribution, structural diversity, varied modes of action, disease-associated mutations (1-4). Certain GPCRs are involved in signaling pathways for neuropeptides such as oxytocin, serotonin, and vasopressin, and influence c
- Counterscreen for vasopressin 1 receptor (V1R) agonists: Fluorescence-based cell-based high throughput dose response assay for agonists of the Oxytocin Receptor (OXTR) Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC) Center Affiliation: The Scripps Research Institute (TSRI) Assay Provider: Michael Jarstfer, University of North Carolina at Chapel Hill (UNC) Network: Molecular Libraries Probe Production Centers Network (MLPCN) Grant Proposal Number: 1 R03 MH085678-01A1 Grant Proposal PI: Michael Jarstfer, UNC External Assay ID: OTR_AG_FLUO8_1536_3XEC50 V1R DCSRUN Name: Counterscreen for vasopressin 1 receptor (V1R) agonists: Fluorescence-based cell-based high throughput dose response assay for agonists of the Oxytocin Receptor (OXTR). Description: Heterotrimeric G-protein coupled receptors (GPCRs) are major targets for disease therapeutics, due in part to their broad tissue distribution, structural diversity, varied modes of action, disease-associated mutations (1-4). Certain GPCRs are involved in signaling pathways for neuropeptides such as oxytocin, serotonin, and vasopressin, and influence complex so
- ChEMBL_1474014 Competitive binding to SNAP-tagged oxytocin receptor (unknown origin) expressed in HEK293 cells incubated for 1 hr at RT followed by 4 hrs at 4 degC by TR-FRET assay in presence of 5-(3-(22-(3-carboxy-4-(3-oxo-3H-xanthen-9-yl)phenyl)-15,22-dioxo-2,5,8,11-tetraoxa-14,21-diazadocosyl)-5-(3-(2-chloro-4-fluorophenoxy)azetidin-1-yl)-4H-1,2,4-triazol-4-yl)-2-methoxypyridinium 2,2,2-trifluoroacetate
- ChEMBL_1474015 Competitive binding to SNAP-tagged oxytocin receptor (unknown origin) expressed in HEK293 cells incubated for 1 hr at RT followed by 4 hrs at 4 degC by TR-FRET assay in presence of 2-(5-(3-(1-(5-(3-(2-chloro-4-fluorophenoxy)azetidin-1-yl)-4-(6-methoxypyridinium-3-yl)-4H-1,2,4-triazol-3-yl)-15-oxo-2,5,8,11-tetraoxa-14-azaoctadecan-18-yl)-1-ethyl-3-methyl-5-sulfoindolin-2-ylidene)penta-1,3-dienyl)-1-ethyl-3,3-dimethyl-3H-indolium-6-sulfonate 2,2,2-trifluoroacetate
- Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R) Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC) Center Affiliation: The Scripps Research Institute (TSRI) Assay Provider: Michael Jarstfer, University of North Carolina at Chapel Hill (UNC) Network: Molecular Libraries Probe Production Centers Network (MLPCN) Grant Proposal Number: 1 R03 MH085678-01A1 Grant Proposal PI: Michael Jarstfer, UNC External Assay ID: V1R_AG_FLUO8_1536_3XEC50 DRUN Name: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). Description: Heterotrimeric G-protein coupled receptors (GPCRs) are major targets for disease therapeutics, due in part to their broad tissue distribution, structural diversity, varied modes of action, disease-associated mutations (1-4). Certain GPCRs are involved in signaling pathways for neuropeptides such as oxytocin, serotonin, and vasopressin, and influence complex social behaviors such as trust, anxiety, and parent