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, and disease-associated mutations (1-4). For example, targeting of opiod receptors by opiates such as morphine is a widespread clinical application for GPCR modulation in pain management. The recently more ..
Tested Compound:
Depositor Specified Assays
Show more |
| AID | Name | Type | Probe | Comment |
|---|---|---|---|---|
| 1861 | Fluorescence-based primary cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). | screening | Primary screen (GPR7 antagonists in singlicate) | |
| 1880 | Summary of probe development efforts to identify antagonists of the G-protein coupled receptor 7 (GPR7). | summary | 2 | Summary (GPR7 antagonists) |
| 1952 | Fluorescence-based confirmation cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). | screening | Confirmation screen (GPR& antagonists in triplicate) | |
| 2148 | Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput screening assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). | screening | Counterscreen (MCHR1 antagonists in triplicate) | |
| 2251 | Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). | confirmatory | Dose response (GPR7 antagonists in triplicate) | |
| 2257 | Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). | confirmatory | Dose response counterscreen (MCHR1 antagonists in triplicate) | |
| 463250 | Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1) | confirmatory | Dose response counterscreen (MCHR1 antagonists in triplicate) | |
| 463251 | Late-stage fluorescence-based dose response cell-based screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7) | confirmatory | Dose response (GPR7 antagonists in triplicate) | |
| 463253 | Late-stage luminescence-based cell-based dose response assay to identify antagonists of the G-protein coupled receptor 7 (GPR7): Cytotoxicity assay | confirmatory | Dose response counterscreen (Cytotoxicity in triplicate) | |
| 485339 | Late-stage fluorescence-based dose response cell-based screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7): Intracellular calcium release | confirmatory | Dose response (GPR7 antagonists in triplicate) | |
| 504886 | Late-stage results from the probe development effort to identify antagonists of the G-protein coupled receptor 7 (GPR7): luminescence-based cell-based dose response counterscreen assay to determine cytotoxicity of antagonist compounds Set 2 | confirmatory | ||
| 588568 | Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1) Set 4 | confirmatory | ||
| 540365 | Late-stage fluorescence-based dose response cell-based screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7) Set 3 | confirmatory | ||
| 588581 | Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1) Set 6 | confirmatory | ||
| 540371 | Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1) Set 3 | confirmatory | ||
| 504868 | Late-stage fluorescence-based dose response cell-based screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7) Set 2 | confirmatory | ||
| 588326 | Late-stage results from the probe development effort to identify antagonists of the G-protein coupled receptor 7 (GPR7): luminescence-based cell-based dose response counterscreen assay to determine cytotoxicity of antagonist compounds Set 3 | confirmatory | ||
| 588564 | Late-stage fluorescence-based dose response cell-based screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7) Set 4 | confirmatory | ||
| 588562 | Late-stage fluorescence-based cell-based screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7): percent inhibition | other | ||
| 588563 | Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1) Set 5 | confirmatory | ||
| 588566 | Late-stage fluorescence-based dose response cell-based screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7) Set 5 | confirmatory | ||
| 504889 | Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1) Set 2 | confirmatory | ||
| 588583 | Late-stage fluorescence-based dose response cell-based screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7) Set 6 | confirmatory |
Description:
Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center
Affiliation: The Scripps Research Institute, TSRI
Assay Provider: Olivier Civelli, University of California, Irvine
Network: Molecular Library Probe Production Centers Network (MLPCN)
Grant Proposal Number 1-R03-DA026557-01
Grant Proposal PI: Olivier Civelli
External Assay ID: GPR7_ANT_RICERCA HITPROFILING SCREEN_2X%INH
Name: Late-stage counterscreen panel assay for GPR7 antagonists: Ricerca HitProfilingScreen + CYP450
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, and disease-associated mutations (1-4). For example, targeting of opiod receptors by opiates such as morphine is a widespread clinical application for GPCR modulation in pain management. The recently de-orphanized GPR7 (5) is localized predominantly in the cerebellum and prefrontal cortex (6), with additional expression in the pituitary, hippocampus, amygdala, and spinal cord (7-9). GPR7 is highly conserved in humans and rodents (6), and exhibits structural features of both GPCRs and somatostatin receptors (7). Studies identifying the energy-regulating neuropeptides Neuropeptide W (NPW) and Neuropeptide B (NPB) as endogenous ligands of GPR7 (5, 10), and the development of hyperphagia and obesity in male GPR7 knockout mice (11, 12), implicate GPR7 in feeding behavior. Additional studies identifying GPR7 expression in peripheral Schwann cells (13) and increased GPR7 expression in rat models and human patients with inflammation-associated neuropathic pain (11, 13), suggest a role for GPR7 in mediating the inflammatory pain response. The identification of modulators of GPR7 will provide useful tools to elucidate the diverse roles of this receptor in central neuropeptide signaling and nociception in general.
References:
1. Pan, H.L., Wu, Z.Z., Zhou, H.Y., Chen, S.R., Zhang, H.M., and Li, D.P., Modulation of pain transmission by G-protein-coupled receptors. Pharmacol Ther, 2008. 117(1): p. 141-61.
2. Lagerstrom, M.C. and Schioth, H.B., Structural diversity of G protein-coupled receptors and significance for drug discovery. Nat Rev Drug Discov, 2008. 7(4): p. 339-57.
3. Thompson, M.D., Cole, D.E., and Jose, P.A., Pharmacogenomics of G protein-coupled receptor signaling: insights from health and disease. Methods Mol Biol, 2008. 448: p. 77-107.
4. Bosier, B. and Hermans, E., Versatility of GPCR recognition by drugs: from biological implications to therapeutic relevance. Trends Pharmacol Sci, 2007. 28(8): p. 438-46.
5. Tanaka, H., Yoshida, T., Miyamoto, N., Motoike, T., Kurosu, H., Shibata, K., Yamanaka, A., Williams, S.C., Richardson, J.A., Tsujino, N., Garry, M.G., Lerner, M.R., King, D.S., O'Dowd, B.F., Sakurai, T., and Yanagisawa, M., Characterization of a family of endogenous neuropeptide ligands for the G protein-coupled receptors GPR7 and GPR8. Proc Natl Acad Sci U S A, 2003. 100(10): p. 6251-6.
6. O'Dowd, B.F., Scheideler, M.A., Nguyen, T., Cheng, R., Rasmussen, J.S., Marchese, A., Zastawny, R., Heng, H.H., Tsui, L.C., Shi, X., and et al., The cloning and chromosomal mapping of two novel human opioid-somatostatin-like receptor genes, GPR7 and GPR8, expressed in discrete areas of the brain. Genomics, 1995. 28(1): p. 84-91.
7. Brezillon, S., Lannoy, V., Franssen, J.D., Le Poul, E., Dupriez, V., Lucchetti, J., Detheux, M., and Parmentier, M., Identification of natural ligands for the orphan G protein-coupled receptors GPR7 and GPR8. J Biol Chem, 2003. 278(2): p. 776-83.
8. Singh, G., Maguire, J.J., Kuc, R.E., Fidock, M., and Davenport, A.P., Identification and cellular localisation of NPW1 (GPR7) receptors for the novel neuropeptide W-23 by [125I]-NPW radioligand binding and immunocytochemistry. Brain Res, 2004. 1017(1-2): p. 222-6.
9. Lee, D.K., Nguyen, T., Porter, C.A., Cheng, R., George, S.R., and O'Dowd, B.F., Two related G protein-coupled receptors: the distribution of GPR7 in rat brain and the absence of GPR8 in rodents. Brain Res Mol Brain Res, 1999. 71(1): p. 96-103.
10. Fujii, R., Yoshida, H., Fukusumi, S., Habata, Y., Hosoya, M., Kawamata, Y., Yano, T., Hinuma, S., Kitada, C., Asami, T., Mori, M., Fujisawa, Y., and Fujino, M., Identification of a neuropeptide modified with bromine as an endogenous ligand for GPR7. J Biol Chem, 2002. 277(37): p. 34010-6.
11. Kelly, M.A., Beuckmann, C.T., Williams, S.C., Sinton, C.M., Motoike, T., Richardson, J.A., Hammer, R.E., Garry, M.G., and Yanagisawa, M., Neuropeptide B-deficient mice demonstrate hyperalgesia in response to inflammatory pain. Proc Natl Acad Sci U S A, 2005. 102(28): p. 9942-7.
12. Ishii, M., Fei, H., and Friedman, J.M., Targeted disruption of GPR7, the endogenous receptor for neuropeptides B and W, leads to metabolic defects and adult-onset obesity. Proc Natl Acad Sci U S A, 2003. 100(18): p. 10540-5.
13. Zaratin, P.F., Quattrini, A., Previtali, S.C., Comi, G., Hervieu, G., and Scheideler, M.A., Schwann cell overexpression of the GPR7 receptor in inflammatory and painful neuropathies. Mol Cell Neurosci, 2005. 28(1): p. 55-63.
Keywords:
Late stage, late stage AID, powders, GPR7, NPBWR1, G-protein coupled receptor 7, pain, feeding, antagonist, antagonism, inhibitor, inhibition, counterscreen, panel assay, Ricerca, HitProfilingScreen, Sf9 cells, radioligand binding, Scripps, The Scripps Research Institute Molecular Screening Center, SRIMSC, Molecular Libraries Probe Production Centers Network, MLPCN.
Affiliation: The Scripps Research Institute, TSRI
Assay Provider: Olivier Civelli, University of California, Irvine
Network: Molecular Library Probe Production Centers Network (MLPCN)
Grant Proposal Number 1-R03-DA026557-01
Grant Proposal PI: Olivier Civelli
External Assay ID: GPR7_ANT_RICERCA HITPROFILING SCREEN_2X%INH
Name: Late-stage counterscreen panel assay for GPR7 antagonists: Ricerca HitProfilingScreen + CYP450
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, and disease-associated mutations (1-4). For example, targeting of opiod receptors by opiates such as morphine is a widespread clinical application for GPCR modulation in pain management. The recently de-orphanized GPR7 (5) is localized predominantly in the cerebellum and prefrontal cortex (6), with additional expression in the pituitary, hippocampus, amygdala, and spinal cord (7-9). GPR7 is highly conserved in humans and rodents (6), and exhibits structural features of both GPCRs and somatostatin receptors (7). Studies identifying the energy-regulating neuropeptides Neuropeptide W (NPW) and Neuropeptide B (NPB) as endogenous ligands of GPR7 (5, 10), and the development of hyperphagia and obesity in male GPR7 knockout mice (11, 12), implicate GPR7 in feeding behavior. Additional studies identifying GPR7 expression in peripheral Schwann cells (13) and increased GPR7 expression in rat models and human patients with inflammation-associated neuropathic pain (11, 13), suggest a role for GPR7 in mediating the inflammatory pain response. The identification of modulators of GPR7 will provide useful tools to elucidate the diverse roles of this receptor in central neuropeptide signaling and nociception in general.
References:
1. Pan, H.L., Wu, Z.Z., Zhou, H.Y., Chen, S.R., Zhang, H.M., and Li, D.P., Modulation of pain transmission by G-protein-coupled receptors. Pharmacol Ther, 2008. 117(1): p. 141-61.
2. Lagerstrom, M.C. and Schioth, H.B., Structural diversity of G protein-coupled receptors and significance for drug discovery. Nat Rev Drug Discov, 2008. 7(4): p. 339-57.
3. Thompson, M.D., Cole, D.E., and Jose, P.A., Pharmacogenomics of G protein-coupled receptor signaling: insights from health and disease. Methods Mol Biol, 2008. 448: p. 77-107.
4. Bosier, B. and Hermans, E., Versatility of GPCR recognition by drugs: from biological implications to therapeutic relevance. Trends Pharmacol Sci, 2007. 28(8): p. 438-46.
5. Tanaka, H., Yoshida, T., Miyamoto, N., Motoike, T., Kurosu, H., Shibata, K., Yamanaka, A., Williams, S.C., Richardson, J.A., Tsujino, N., Garry, M.G., Lerner, M.R., King, D.S., O'Dowd, B.F., Sakurai, T., and Yanagisawa, M., Characterization of a family of endogenous neuropeptide ligands for the G protein-coupled receptors GPR7 and GPR8. Proc Natl Acad Sci U S A, 2003. 100(10): p. 6251-6.
6. O'Dowd, B.F., Scheideler, M.A., Nguyen, T., Cheng, R., Rasmussen, J.S., Marchese, A., Zastawny, R., Heng, H.H., Tsui, L.C., Shi, X., and et al., The cloning and chromosomal mapping of two novel human opioid-somatostatin-like receptor genes, GPR7 and GPR8, expressed in discrete areas of the brain. Genomics, 1995. 28(1): p. 84-91.
7. Brezillon, S., Lannoy, V., Franssen, J.D., Le Poul, E., Dupriez, V., Lucchetti, J., Detheux, M., and Parmentier, M., Identification of natural ligands for the orphan G protein-coupled receptors GPR7 and GPR8. J Biol Chem, 2003. 278(2): p. 776-83.
8. Singh, G., Maguire, J.J., Kuc, R.E., Fidock, M., and Davenport, A.P., Identification and cellular localisation of NPW1 (GPR7) receptors for the novel neuropeptide W-23 by [125I]-NPW radioligand binding and immunocytochemistry. Brain Res, 2004. 1017(1-2): p. 222-6.
9. Lee, D.K., Nguyen, T., Porter, C.A., Cheng, R., George, S.R., and O'Dowd, B.F., Two related G protein-coupled receptors: the distribution of GPR7 in rat brain and the absence of GPR8 in rodents. Brain Res Mol Brain Res, 1999. 71(1): p. 96-103.
10. Fujii, R., Yoshida, H., Fukusumi, S., Habata, Y., Hosoya, M., Kawamata, Y., Yano, T., Hinuma, S., Kitada, C., Asami, T., Mori, M., Fujisawa, Y., and Fujino, M., Identification of a neuropeptide modified with bromine as an endogenous ligand for GPR7. J Biol Chem, 2002. 277(37): p. 34010-6.
11. Kelly, M.A., Beuckmann, C.T., Williams, S.C., Sinton, C.M., Motoike, T., Richardson, J.A., Hammer, R.E., Garry, M.G., and Yanagisawa, M., Neuropeptide B-deficient mice demonstrate hyperalgesia in response to inflammatory pain. Proc Natl Acad Sci U S A, 2005. 102(28): p. 9942-7.
12. Ishii, M., Fei, H., and Friedman, J.M., Targeted disruption of GPR7, the endogenous receptor for neuropeptides B and W, leads to metabolic defects and adult-onset obesity. Proc Natl Acad Sci U S A, 2003. 100(18): p. 10540-5.
13. Zaratin, P.F., Quattrini, A., Previtali, S.C., Comi, G., Hervieu, G., and Scheideler, M.A., Schwann cell overexpression of the GPR7 receptor in inflammatory and painful neuropathies. Mol Cell Neurosci, 2005. 28(1): p. 55-63.
Keywords:
Late stage, late stage AID, powders, GPR7, NPBWR1, G-protein coupled receptor 7, pain, feeding, antagonist, antagonism, inhibitor, inhibition, counterscreen, panel assay, Ricerca, HitProfilingScreen, Sf9 cells, radioligand binding, Scripps, The Scripps Research Institute Molecular Screening Center, SRIMSC, Molecular Libraries Probe Production Centers Network, MLPCN.
Panel Information
Targets
§ Panel component ID.
| Data Table(All) | Show more |
| PID§ | Name | Substance | Panel Targets | Description | Additional Information | ||
|---|---|---|---|---|---|---|---|
| Active | Inactive | ||||||
| 1 | CYP450, 1A2 | 1 | cytochrome P450, family 1, subfamily A, polypeptide 2 [Homo sapiens] [gi:119619719] | Taxonomy id: 9606 Gene id: 1544 | |||
| 2 | CYP450, 2C19 | 1 | cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] [gi:55665398] | Taxonomy id: 9606 Gene id: 1557 | |||
| 3 | CYP450, 2C9 | 1 | Cytochrome P450, family 2, subfamily C, polypeptide 9 [Homo sapiens] [gi:115529027] | Taxonomy id: 9606 Gene id: 1559 | |||
| 4 | CYP450, 2D6 | 1 | Cytochrome P450, family 2, subfamily D, polypeptide 6 [Homo sapiens] [gi:117558701] | Taxonomy id: 9606 Gene id: 1565 | |||
| 5 | CYP450, 3A4 | 1 | cytochrome P450 family 3 subfamily A polypeptide 4 [Homo sapiens] [gi:115371803] | Taxonomy id: 9606 Gene id: 1576 | |||
| 6 | Adenosine A1 | 1 | adenosine A1 receptor [Homo sapiens] [gi:119611871] | Taxonomy id: 9606 Gene id: 134 | |||
| 7 | Adenosine A2A | 1 | adenosine A2a receptor [Homo sapiens] [gi:119580062] | Taxonomy id: 9606 Gene id: 135 | |||
| 8 | Adrenergic alpha1A | 1 | adrenergic receptor, alpha 1a [Rattus norvegicus] [gi:149030335] | Taxonomy id: 10116 Gene id: 29412 | |||
| 9 | Adrenergic alpha1B | 1 | Adrenergic, alpha-1B-, receptor [Homo sapiens] [gi:187953275] | Taxonomy id: 10116 Gene id: 147 | |||
| 10 | Adrenergic alpha2A | 1 | alpha-2A adrenergic receptor [Homo sapiens] [gi:194353970] | Taxonomy id: 9606 Gene id: 150 | |||
| 11 | Adrenergic beta1 | 1 | adrenergic, beta-1-, receptor [Homo sapiens] [gi:166706747] | Taxonomy id: 9606 Gene id: 153 | |||
| 12 | Adrenergic beta2 | 1 | Adrenergic, beta-2-, receptor, surface [Homo sapiens] [gi:127798637] | Taxonomy id: 9606 Gene id: 154 | |||
| 13 | Calcium Channel L-Type, Dihydropyridine | 1 | voltage-dependent calcium channel subunit alpha-2/delta-1 isoform 2 [Rattus norvegicus] [gi:161086906] | Taxonomy id: 10116 Gene id: 25399 | |||
| 14 | Cannabinoid CB1 | 1 | cannabinoid receptor [Homo sapiens] [gi:67550212] | Taxonomy id: 9606 Gene id: 1268 | |||
| 15 | Dopamine D1 | 1 | Dopamine receptor D1 [Homo sapiens] [gi:67677841] | Taxonomy id: 9606 Gene id: 1812 | |||
| 16 | Dopamine D2S | 1 | dopamine receptor D2 isoform short [Homo sapiens] [gi:197692661] | Taxonomy id: 9606 Gene id: 1813 | |||
| 17 | GABAA, Flunitrazepam, Central | 1 | gamma-aminobutyric acid A receptor, gamma 2 [Rattus norvegicus] [gi:149052302] | Taxonomy id: 10116 Gene id: 29709 | |||
| 18 | GABAA, Muscimol, Central | 1 | testis gamma-aminobutyric acid receptor subunit beta 3 [Rattus norvegicus] [gi:53765741] | Taxonomy id: 10116 Gene id: 24922 | |||
| 19 | Glutamate, NMDA, Phencyclidine | 1 | glutamate receptor, ionotropic, N-methyl D-aspartate 1, isoform CRA_h [Rattus norvegicus] [gi:149039393] | Taxonomy id: 10116 Gene id: 24408 | |||
| 20 | Histamine H1 | 1 | histamine H1 receptor [Homo sapiens] [gi:149158709] | Taxonomy id: 9606 Gene id: 3269 | |||
| 21 | Imidazoline I2, Central | 1 | Taxonomy id: 10116 | ||||
| 22 | Muscarinic M2 | 1 | cholinergic receptor, muscarinic 2 [Homo sapiens] [gi:119604271] | Taxonomy id: 9606 Gene id: 1129 | |||
| 23 | Muscarinic M3 | 1 | Cholinergic receptor, muscarinic 3 [Homo sapiens] [gi:111306506] | Taxonomy id: 9606 Gene id: 1131 | |||
| 24 | Nicotinic Acetylcholine | 1 | cholinergic receptor, nicotinic, alpha 3, isoform CRA_a [Homo sapiens] [gi:119619563] | Taxonomy id: 9606 Gene id: 1136 | |||
| 25 | Nicotinic Acetylcholine alpha 1, Bungarotoxin | 1 | cholinergic receptor, nicotinic, alpha 1 (muscle), isoform CRA_a [Homo sapiens] [gi:119631533] | Taxonomy id: 9606 Gene id: 1134 | |||
| 26 | Opiate mu (OP3, MOP) | 1 | mu-type opioid receptor isoform MOR-1B2 [Homo sapiens] [gi:223718719] | Taxonomy id: 9606 Gene id: 4988 | |||
| 27 | Phorbol Ester | 1 | Taxonomy id: 10090 | ||||
| 28 | Potassium Channel [KATP] | 1 | Taxonomy id: 10036 | ||||
| 29 | Potassium Channel hERG | 1 | voltage-gated potassium channel subfamily H isoform 3.1 [Homo sapiens] [gi:237862038] | Taxonomy id: 9606 Gene id: 3757 | |||
| 30 | Prostanoid EP4 | 1 | Prostaglandin E receptor 4 (subtype EP4) [Homo sapiens] [gi:109731195] | Taxonomy id: 9606 Gene id: 5734 | |||
| 31 | Rolipram | 1 | Taxonomy id: 10116 | ||||
| 32 | Serotonin (5-Hydroxytryptamine) 5-HT2B | 1 | 5-hydroxytryptamine (serotonin) receptor 2B [Homo sapiens] [gi:119591355] | Taxonomy id: 9606 Gene id: 3357 | |||
| 33 | Sigma 1 | 1 | opioid receptor, sigma 1 [Homo sapiens] [gi:123231939] | Taxonomy id: 9606 Gene id: 10280 | |||
| 34 | Sodium Channel, Site 2 | 1 | sodium channel, nonvoltage-gated 1 alpha [Rattus norvegicus] [gi:149049394] | Taxonomy id: 10116 Gene id: 25122 | |||
| 35 | Transporter, Norepinephrine (NET) | 1 | Net [Homo sapiens] [gi:531523] | Taxonomy id: 9606 Gene id: 2004 | |||
§ Panel component ID.
Protocol
Assay Overview:
The purpose of this panel of binding assays performed by Ricerca Biosciences, LLC, is to identify a subset of potential receptors, transporters, ion channels, etc. for which the GPR7 antagonist compound SID 96021160 displays affinity.
Protocol Summary:
Assays for CYP450, 1A2; CYP450, 2C19; CYP450, 2C9; CYP450, 2D6; and CYP450, 3A4 were enzyme assays using human recombinant insect Sf9 cells with 5 uM 3-cyano-7-ethoxycoumarin as substrate (except for CYP450, 3A4, which used 50 uM 7-benzyloxy-4-(trifluoromethyl)-coumarin as substrate). Detection was based on spectrofluorimetric quantitation of the enzymatic product produced. Assays for the other targets were radioligand binding assays.
A response of greater than or equal to 50% inhibition or stimulation is considered active. Negative inhibition represents a stimulation of binding.
List of Reagents:
Reagents were provided by Ricerca Biosciences, LLC.
The purpose of this panel of binding assays performed by Ricerca Biosciences, LLC, is to identify a subset of potential receptors, transporters, ion channels, etc. for which the GPR7 antagonist compound SID 96021160 displays affinity.
Protocol Summary:
Assays for CYP450, 1A2; CYP450, 2C19; CYP450, 2C9; CYP450, 2D6; and CYP450, 3A4 were enzyme assays using human recombinant insect Sf9 cells with 5 uM 3-cyano-7-ethoxycoumarin as substrate (except for CYP450, 3A4, which used 50 uM 7-benzyloxy-4-(trifluoromethyl)-coumarin as substrate). Detection was based on spectrofluorimetric quantitation of the enzymatic product produced. Assays for the other targets were radioligand binding assays.
A response of greater than or equal to 50% inhibition or stimulation is considered active. Negative inhibition represents a stimulation of binding.
List of Reagents:
Reagents were provided by Ricerca Biosciences, LLC.
Result Definitions
| Show more |
| TID | Name | Description | PID§ | Panel Targets | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||||
| 1 | CYP450, 1A2 (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 1 | cytochrome P450, family 1, subfamily A, polypeptide 2 [Homo sapiens] |  | Float | % | |
| 2 | CYP450, 1A2 (Outcome) | The assay outcome, one of Inactive or Active. | 1 | | Outcome | |||
| 3 | CYP450, 2C19 (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 2 | cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] | | Float | % | |
| 4 | CYP450, 2C19 (Outcome) | The assay outcome, one of Inactive or Active. | 2 | | Outcome | |||
| 5 | CYP450, 2C9 (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 3 | Cytochrome P450, family 2, subfamily C, polypeptide 9 [Homo sapiens] | | Float | % | |
| 6 | CYP450, 2C9 (Outcome) | The assay outcome, one of Inactive or Active. | 3 | | Outcome | |||
| 7 | CYP450, 2D6 (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 4 | Cytochrome P450, family 2, subfamily D, polypeptide 6 [Homo sapiens] | | Float | % | |
| 8 | CYP450, 2D6 (Outcome) | The assay outcome, one of Inactive or Active. | 4 | | Outcome | |||
| 9 | CYP450, 3A4 (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 5 | cytochrome P450 family 3 subfamily A polypeptide 4 [Homo sapiens] | | Float | % | |
| 10 | CYP450, 3A4 (Outcome) | The assay outcome, one of Inactive or Active. | 5 | | Outcome | |||
| 11 | Adenosine A1 (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 6 | adenosine A1 receptor [Homo sapiens] | | Float | % | |
| 12 | Adenosine A1 (Outcome) | The assay outcome, one of Inactive or Active. | 6 | | Outcome | |||
| 13 | Adenosine A2A (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 7 | adenosine A2a receptor [Homo sapiens] | | Float | % | |
| 14 | Adenosine A2A (Outcome) | The assay outcome, one of Inactive or Active. | 7 | | Outcome | |||
| 15 | Adrenergic alpha1A (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 8 | adrenergic receptor, alpha 1a [Rattus norvegicus] | | Float | % | |
| 16 | Adrenergic alpha1A (Outcome) | The assay outcome, one of Inactive or Active. | 8 | | Outcome | |||
| 17 | Adrenergic alpha1B (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 9 | Adrenergic, alpha-1B-, receptor [Homo sapiens] | | Float | % | |
| 18 | Adrenergic alpha1B (Outcome) | The assay outcome, one of Inactive or Active. | 9 | | Outcome | |||
| 19 | Adrenergic alpha2A (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 10 | alpha-2A adrenergic receptor [Homo sapiens] | | Float | % | |
| 20 | Adrenergic alpha2A (Outcome) | The assay outcome, one of Inactive or Active. | 10 | | Outcome | |||
| 21 | Adrenergic beta1 (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 11 | adrenergic, beta-1-, receptor [Homo sapiens] | | Float | % | |
| 22 | Adrenergic beta1 (Outcome) | The assay outcome, one of Inactive or Active. | 11 | | Outcome | |||
| 23 | Adrenergic beta2 (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 12 | Adrenergic, beta-2-, receptor, surface [Homo sapiens] | | Float | % | |
| 24 | Adrenergic beta2 (Outcome) | The assay outcome, one of Inactive or Active. | 12 | | Outcome | |||
| 25 | Calcium Channel L-Type, Dihydropyridine (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 13 | voltage-dependent calcium channel subunit alpha-2/delta-1 isoform 2 [Rattus norvegicus] | | Float | % | |
| 26 | Calcium Channel L-Type, Dihydropyridine (Outcome) | The assay outcome, one of Inactive or Active. | 13 | | Outcome | |||
| 27 | Cannabinoid CB1 (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 14 | cannabinoid receptor [Homo sapiens] | | Float | % | |
| 28 | Cannabinoid CB1 (Outcome) | The assay outcome, one of Inactive or Active. | 14 | | Outcome | |||
| 29 | Dopamine D1 (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 15 | Dopamine receptor D1 [Homo sapiens] | | Float | % | |
| 30 | Dopamine D1 (Outcome) | The assay outcome, one of Inactive or Active. | 15 | | Outcome | |||
| 31 | Dopamine D2S (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 16 | dopamine receptor D2 isoform short [Homo sapiens] | | Float | % | |
| 32 | Dopamine D2S (Outcome) | The assay outcome, one of Inactive or Active. | 16 | | Outcome | |||
| 33 | GABAA, Flunitrazepam, Central (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 17 | gamma-aminobutyric acid A receptor, gamma 2 [Rattus norvegicus] | | Float | % | |
| 34 | GABAA, Flunitrazepam, Central (Outcome) | The assay outcome, one of Inactive or Active. | 17 | | Outcome | |||
| 35 | GABAA, Muscimol, Central (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 18 | testis gamma-aminobutyric acid receptor subunit beta 3 [Rattus norvegicus] | | Float | % | |
| 36 | GABAA, Muscimol, Central (Outcome) | The assay outcome, one of Inactive or Active. | 18 | | Outcome | |||
| 37 | Glutamate, NMDA, Phencyclidine (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 19 | glutamate receptor, ionotropic, N-methyl D-aspartate 1, isoform CRA_h [Rattus norvegicus] | | Float | % | |
| 38 | Glutamate, NMDA, Phencyclidine (Outcome) | The assay outcome, one of Inactive or Active. | 19 | | Outcome | |||
| 39 | Histamine H1 (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 20 | histamine H1 receptor [Homo sapiens] | | Float | % | |
| 40 | Histamine H1 (Outcome) | The assay outcome, one of Inactive or Active. | 20 | | Outcome | |||
| 41 | Imidazoline I2, Central (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 21 | | Float | % | ||
| 42 | Imidazoline I2, Central (Outcome) | The assay outcome, one of Inactive or Active. | 21 | | Outcome | |||
| 43 | Muscarinic M2 (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 22 | cholinergic receptor, muscarinic 2 [Homo sapiens] | | Float | % | |
| 44 | Muscarinic M2 (Outcome) | The assay outcome, one of Inactive or Active. | 22 | | Outcome | |||
| 45 | Muscarinic M3 (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 23 | Cholinergic receptor, muscarinic 3 [Homo sapiens] | | Float | % | |
| 46 | Muscarinic M3 (Outcome) | The assay outcome, one of Inactive or Active. | 23 | | Outcome | |||
| 47 | Nicotinic Acetylcholine (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 24 | cholinergic receptor, nicotinic, alpha 3, isoform CRA_a [Homo sapiens] | | Float | % | |
| 48 | Nicotinic Acetylcholine (Outcome) | The assay outcome, one of Inactive or Active. | 24 | | Outcome | |||
| 49 | Nicotinic Acetylcholine alpha 1, Bungarotoxin (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 25 | cholinergic receptor, nicotinic, alpha 1 (muscle), isoform CRA_a [Homo sapiens] | | Float | % | |
| 50 | Nicotinic Acetylcholine alpha 1, Bungarotoxin (Outcome) | The assay outcome, one of Inactive or Active. | 25 | | Outcome | |||
| 51 | Opiate mu (OP3, MOP) (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 26 | mu-type opioid receptor isoform MOR-1B2 [Homo sapiens] | | Float | % | |
| 52 | Opiate mu (OP3, MOP) (Outcome) | The assay outcome, one of Inactive or Active. | 26 | | Outcome | |||
| 53 | Phorbol Ester (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 27 | | Float | % | ||
| 54 | Phorbol Ester (Outcome) | The assay outcome, one of Inactive or Active. | 27 | | Outcome | |||
| 55 | Potassium Channel [KATP] (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 28 | | Float | % | ||
| 56 | Potassium Channel [KATP] (Outcome) | The assay outcome, one of Inactive or Active. | 28 | | Outcome | |||
| 57 | Potassium Channel hERG (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 29 | voltage-gated potassium channel subfamily H isoform 3.1 [Homo sapiens] | | Float | % | |
| 58 | Potassium Channel hERG (Outcome) | The assay outcome, one of Inactive or Active. | 29 | | Outcome | |||
| 59 | Prostanoid EP4 (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 30 | Prostaglandin E receptor 4 (subtype EP4) [Homo sapiens] | | Float | % | |
| 60 | Prostanoid EP4 (Outcome) | The assay outcome, one of Inactive or Active. | 30 | | Outcome | |||
| 61 | Rolipram (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 31 | | Float | % | ||
| 62 | Rolipram (Outcome) | The assay outcome, one of Inactive or Active. | 31 | | Outcome | |||
| 63 | Serotonin (5-Hydroxytryptamine) 5-HT2B (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 32 | 5-hydroxytryptamine (serotonin) receptor 2B [Homo sapiens] | | Float | % | |
| 64 | Serotonin (5-Hydroxytryptamine) 5-HT2B (Outcome) | The assay outcome, one of Inactive or Active. | 32 | | Outcome | |||
| 65 | Sigma 1 (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 33 | opioid receptor, sigma 1 [Homo sapiens] | | Float | % | |
| 66 | Sigma 1 (Outcome) | The assay outcome, one of Inactive or Active. | 33 | | Outcome | |||
| 67 | Sodium Channel, Site 2 (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 34 | sodium channel, nonvoltage-gated 1 alpha [Rattus norvegicus] | | Float | % | |
| 68 | Sodium Channel, Site 2 (Outcome) | The assay outcome, one of Inactive or Active. | 34 | | Outcome | |||
| 69 | Transporter, Norepinephrine (NET) (Inhibition) (10μM**) | Value of % inhibition at 10 uM compound concentration. | 35 | Net [Homo sapiens] | | Float | % | |
| 70 | Transporter, Norepinephrine (NET) (Outcome) | The assay outcome, one of Inactive or Active. | 35 | | Outcome |
** Test Concentration. § Panel component ID.
Additional Information
Grant Number: 1-R03-DA026557-01
Classification
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