Bookmark and Share
BioAssay: AID 1788

Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Ancillary Activity

The M1 muscarinic receptor is thought to be an important therapeutic target in schizophrenia. A cell-based fluorometric calcium assay was developed for high throughput screening. This assay was used to identify compounds with high selectivity for the M1 receptor subtype that act at an allosteric site on the receptor, thus providing increased specificity for this single receptor subtype. It is anticipated that these compounds will provide important tools for the study of muscarinic receptor function in the CNS. ..more
_
   
 Tested Compounds
 Tested Compounds
All(1)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Unspecified(1)
 
 
AID: 1788
Data Source: Vanderbilt Screening Center for GPCRs, Ion Channels and Transporters (JC001_MDS_agonist)
BioAssay Type: Panel
Depositor Category: NIH Molecular Libraries Screening Center Network
BioAssay Version:
Deposit Date: 2009-05-27
Modify Date: 2009-09-11

Data Table ( Complete ):           View All Data
Target
Sequence: cholinergic receptor, muscarinic 1 [Homo sapiens]
Description ..   
Protein Family: Serpentine type 7TM GPCR chemoreceptor Srx

Gene:CHRM1     Related Protein 3D Structures     More BioActivity Data..
Tested Compound:
Related Experiments
Show more
AIDNameTypeProbeComment
626Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary ScreenScreening depositor-specified cross reference: Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen
1488Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation AssayOther depositor-specified cross reference: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay
1798Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Probe SummarySummary1 depositor-specified cross reference
1470Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS binding at M1Confirmatory same project related to Summary assay
1508Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5Confirmatory same project related to Summary assay
1741Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Counterscreen with M4 ReceptorOther same project related to Summary assay
1743Discovery of novel allosteric modulators of the M1 muscarinic receptor: Y381A Mutant M1 ReceptorConfirmatory same project related to Summary assay
1744Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Activity against Muscarinic PanelConfirmatory same project related to Summary assay
1757Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M4Confirmatory same project related to Summary assay
1764Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3Confirmatory same project related to Summary assay
1767Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2Confirmatory same project related to Summary assay
Description:
Assay Provider: P. Jeffrey Conn
Assay Provider Affiliation: Vanderbilt University
Grant Title: Discovery of novel allosteric modulators of the M1 muscarinic receptor
Grant Number: 1 R03 MH077606-01

The M1 muscarinic receptor is thought to be an important therapeutic target in schizophrenia. A cell-based fluorometric calcium assay was developed for high throughput screening. This assay was used to identify compounds with high selectivity for the M1 receptor subtype that act at an allosteric site on the receptor, thus providing increased specificity for this single receptor subtype. It is anticipated that these compounds will provide important tools for the study of muscarinic receptor function in the CNS.

Agents that enhance cholinergic transmission or activate muscarinic acetylcholine receptors (mAChRs) have been developed to ameliorate the loss of cognitive function in patients with Alzheimer's Disease (AD). While cholinergic agents have been partially successful in improving cognitive function in AD patients, the most exciting findings coming from clinical studies with these agents have been the demonstration of efficacy in reducing psychotic symptoms in patients with AD and other neurodegenerative disorders. Interestingly, the M1/M4 preferring mAChR agonist, xanomeline, also induces a robust antipsychotic effect in schizophrenic patients, suggesting that mAChR agonists may have broad utility in reducing psychotic symptoms in patients suffering from schizophrenia and certain neurodegenerative disorders.

Evidence suggests that the antipsychotic effects of cholinergic agents may be mediated by the M1 mAChR subtype. However, previous compounds developed to selectively activate M1 receptors have failed in clinical development due to a lack of true specificity for M1 and adverse effects associated with activation of other mAChR subtypes. Furthermore, the lack of highly selective compounds has made it impossible to definitively determine whether the behavioral and clinical effects of these compounds are mediated by M1 and the M4 receptor subtype is also a viable candidate for mediating the antipsychotic effects.

Previous attempts to develop agonists and antagonists that are highly selective for M1 or other specific mAChR subtypes have failed because of the high conservation of the ACh binding site and difficulty in developing compounds that are truly specific. However, in recent years, major advances have been made in discovery of highly selective antagonists of other G protein-coupled receptors (GPCRs) that act at allosteric sites rather than the orthosteric neurotransmitter binding site [1, 2]. These compounds induce a noncompetitive blockade of receptor function and tend to be highly selective for the targeted receptor. Even more promising for discovery of M1-selective agonists, novel compounds have now been discovered that act at an allosteric site on M1 receptor rather than the orthosteric ACh-binding site to induce a robust activation of the receptor and provide high receptor subtype specificity [3, 4].

1.May, L.T. and A. Christopoulos, Allosteric modulators of G-protein-coupled receptors. Curr Opin Pharmacol, 2003. 3(5): p. 551-6.
2.Gasparini, F., R. Kuhn, and J.P. Pin, Allosteric modulators of group1 metabotropic glutamate receptors: novel subtype-selective ligands and therapeutic perspectives. Curr Opin Pharmacol, 2002. 2(1): p. 43-9.
3.Spalding, T.A., et al., Discovery of an ectopic activation site on the M(1) muscarinic receptor. Mol Pharmacol, 2002. 61(6): p. 1297-302.
4.Sur, C., et al., N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates Nmethyl-D-aspartate receptor activity. Proc Natl Acad Sci USA, 2003. 100(23): p. 13674-9.
Panel Information
M1 muscarinic receptor: Agonist Ancillary Activity
    Data Table(All)Show more
PID§NameSubstancePanel TargetsDescriptionAdditional Information
ActiveInactive
1Adenosine A1 (human)1adenosine A1 receptor [Homo sapiens] [gi:4501947]
Taxonomy id: 9606
Gene id: 134
2Adenosine A2 (human)1adenosine A2a receptor [Homo sapiens] [gi:5921992]
Taxonomy id: 9606
Gene id: 135
3Adenosine A3 (human)1adenosine A3 receptor [Homo sapiens] [gi:4262078]
Taxonomy id: 9606
Gene id: 140
4Adrenergic a1A (rat)1adrenergic, alpha-1A-, receptor [Rattus norvegicus] [gi:148747171]
Taxonomy id: 10116
Gene id: 29412
5Adrenergic a1B (rat)1adrenergic, alpha-1B-, receptor [Rattus norvegicus] [gi:47575853]
Taxonomy id: 10116
Gene id: 24173
6Adrenergic a1D (human)1alpha-1D-adrenergic receptor [Homo sapiens] [gi:4501957]
Taxonomy id: 9606
Gene id: 146
7Adrenergic a2A (human)1alpha-2A-adrenergic receptor [Homo sapiens] [gi:194353970]
Taxonomy id: 9606
Gene id: 150
8Adrenergic b1 (human)1beta-1-adrenergic receptor [Homo sapiens] [gi:4557265]
Taxonomy id: 9606
Gene id: 153
9Adrenergic b2 (human)1adrenergic, beta-2-, receptor, surface [Homo sapiens] [gi:4501969]
Taxonomy id: 9606
Gene id: 154
10Androgen (testosterone)AR (rat)1androgen receptor [Rattus norvegicus] [gi:6978535]
Taxonomy id: 10116
Gene id: 24208
11Bradykinin B1 (human)1bradykinin receptor B1 [Homo sapiens] [gi:20544172]
Taxonomy id: 9606
Gene id: 623
12Bradykinin B2 (human)1bradykinin receptor B2 [Homo sapiens] [gi:4557359]
Taxonomy id: 9606
Gene id: 624
13Calcium channel L -type, benzothiazepine (rat)1Taxonomy id: 10116
14Calcium channel L -type, dihydropyridine (rat)1calcium channel, voltage-dependent, alpha2/delta subunit 1 isoform 1 [Rattus norvegicus] [gi:31542335]
Taxonomy id: 10116
Gene id: 25399
15Calcium channel N-type (rat)1calcium channel, voltage-dependent, N type, alpha 1B subunit [Rattus norvegicus] [gi:25453410]
Taxonomy id: 10116
Gene id: 257648
16Dopamine D 1 (human)1dopamine receptor D1 [Homo sapiens] [gi:4503383]
Taxonomy id: 9606
Gene id: 1812
17Dopamine D 2S (human)1dopamine receptor D2 isoform short [Homo sapiens] [gi:17986270]
Taxonomy id: 9606
Gene id: 1813
18Dopamine D 4.2 (human)1dopamine receptor D4 [Homo sapiens] [gi:32483397]
Taxonomy id: 9606
Gene id: 1815
19Dopamine D3 (human)1dopamine receptor D3 isoform a [Homo sapiens] [gi:89191861]
Taxonomy id: 9606
Gene id: 1814
20Endothelin ETA (human)1endothelin receptor type A [Homo sapiens] [gi:4503465]
Taxonomy id: 9606
Gene id: 1909
21Endothelin ETB (human)1endothelin receptor type B isoform 1 precursor [Homo sapiens] [gi:4557547]
Taxonomy id: 9606
Gene id: 1910
22Epidermal Growth Factor (EGF) (human)1epidermal growth factor (beta-urogastrone) [Homo sapiens] [gi:166362728]
Taxonomy id: 9606
Gene id: 1950
23Estrogen ER a (human)1estrogen receptor alpha isoform 1 [Homo sapiens] [gi:62821794]
Taxonomy id: 9606
Gene id: 2099
24G protein-coupled receptor GPR103 (human)1G protein-coupled receptor 103 [Homo sapiens] [gi:157738685]
Taxonomy id: 9606
Gene id: 84109
25GABA B1A (human)1gamma-aminobutyric acid (GABA) B receptor 1 isoform a precursor [Homo sapiens] [gi:10835015]
Taxonomy id: 9606
Gene id: 2550
26GABAAFlunitrazepam, central (rat)1Taxonomy id: 10116
27GABAAMuscimol, central (rat)1gamma-aminobutyric acid (GABA) A receptor, gamma 2 [Rattus norvegicus] [gi:34328527]
Taxonomy id: 10116
Gene id: 29709
28Glucocorticoid (human)1nuclear receptor subfamily 3, group C, member 1 isoform alpha [Homo sapiens] [gi:66528611]
Taxonomy id: 9606
Gene id: 2908
29Glutamate, Kainate (rat)1glutamate receptor, ionotropic, kainate 1 isoform 2 precursor [Rattus norvegicus] [gi:8393481]
Taxonomy id: 10116
Gene id: 29559
30Glutamate, NMDA, Agonism (rat)1glutamate receptor, ionotropic, N-methyl D-aspartate 1 [Rattus norvegicus] [gi:8393484]
Taxonomy id: 10116
Gene id: 24408
31Glutamate, NMDA, Glycine (rat)1glutamate receptor, ionotropic, N-methyl D-aspartate 2B [Rattus norvegicus] [gi:6980984]
Taxonomy id: 10116
Gene id: 24410
32Glutamate, NMDA, Phencyclidine (rat)1glutamate receptor, ionotropic, NMDA2A (epsilon 1) [Mus musculus] [gi:41680705]
Taxonomy id: 10116
Gene id: 14811
33Histamine H1 (human)1histamine receptor H1 [Homo sapiens] [gi:149158709]
Taxonomy id: 9606
Gene id: 3269
34Histamine H2 (human)1histamine receptor H2 isoform 2 [Homo sapiens] [gi:13435405]
Taxonomy id: 9606
Gene id: 3274
35Histamine H3 (human)1histamine receptor H3 [Homo sapiens] [gi:194018562]
Taxonomy id: 9606
Gene id: 11255
36Imidazoline I2, central (rat)1PREDICTED: similar to nischarin [Rattus norvegicus] [gi:109503022]
Taxonomy id: 10116
Gene id: 306255
37Interleukin IL-1 (mouse)1interleukin 1 receptor, type I isoform 1 [Mus musculus] [gi:6680417]
Taxonomy id: 10090
Gene id: 16177
38Leukotriene, Cysteinyl CysLT1 (human)1cysteinyl leukotriene receptor 1 [Homo sapiens] [gi:5729798]
Taxonomy id: 9606
Gene id: 10800
39Melatonin MT1 (human)1melatonin receptor 1A [Homo sapiens] [gi:5174593]
Taxonomy id: 9606
Gene id: 4543
40Muscarinic M1 (human)1cholinergic receptor, muscarinic 1 [Homo sapiens] [gi:37622910]
Taxonomy id: 9606
Gene id: 1128
41Muscarinic M2 (human)1cholinergic receptor, muscarinic 2 [Homo sapiens] [gi:4502817]
Taxonomy id: 9606
Gene id: 1129
42Muscarinic M3 (human)1cholinergic receptor, muscarinic 3 [Homo sapiens] [gi:4502819]
Taxonomy id: 9606
Gene id: 1131
43Neuropeptide Y Y1 (human)1neuropeptide Y receptor Y1 [Homo sapiens] [gi:4505445]
Taxonomy id: 9606
Gene id: 4886
44Neuropeptide Y Y2 (human)1neuropeptide Y receptor Y2 [Homo sapiens] [gi:4505447]
Taxonomy id: 9606
Gene id: 4887
45Nicotinic Acetylcholine (human)1cholinergic receptor, nicotinic, alpha 3 [Homo sapiens] [gi:19923122]
Taxonomy id: 9606
Gene id: 1136
46Nicotinic Acetylcholine 1 a , Bungarotoxin (human)1nicotinic cholinergic receptor alpha 1 isoform b precursor [Homo sapiens] [gi:4557457]
Taxonomy id: 9606
Gene id: 1134
47Opiate d (OP1, DOP) (human)1opioid receptor, delta 1 [Homo sapiens] [gi:63477962]
Taxonomy id: 9606
Gene id: 4985
48Opiate k (OP2, KOP) (human)1opioid receptor, kappa 1 [Homo sapiens] [gi:39725940]
Taxonomy id: 9606
Gene id: 4986
49Opiate m (OP3, MOP) (human)1opioid receptor, mu 1 isoform MOR-1 [Homo sapiens] [gi:117940060]
Taxonomy id: 9606
Gene id: 4988
50Phorbol Ester (mouse)1Taxonomy id: 10090
51Platelet Activating Factor (PAF) (human)1Taxonomy id: 9606
52Potassium Channel [K ATP] (hamster)1RecName: Full=G protein-activated inward rectifier potassium channel 2; AltName: Full=GIRK2; AltName: Full=Potassium channel, inwardly rectifying subfamily J member 6; AltName: Full=Inward rectifier K(+) channel Kir3.2; AltName: Full=KATP-2 [gi:1352488]
Taxonomy id: 10036
53Potassium Channel hERG (human)1voltage-gated potassium channel, subfamily H, member 2 isoform a [Homo sapiens] [gi:4557729]
Taxonomy id: 9606
Gene id: 3757
54Prostanoid EP4 (human)1prostaglandin E receptor 4, subtype EP4 [Homo sapiens] [gi:4506259]
Taxonomy id: 9606
Gene id: 5734
55Purinergic P2X (rabbit)1
56Purinergic P2Y (rat)1purinergic receptor P2Y, G-protein coupled 1 [Rattus norvegicus] [gi:25742733]
Taxonomy id: 10116
Gene id: 25265
57Rolipram (rat)1Taxonomy id: 10116
58Serotonin (5-Hydroxytryptamine) 5-HT1A (human)15-hydroxytryptamine (serotonin) receptor 1A [Homo sapiens] [gi:55956923]
Taxonomy id: 9606
Gene id: 3350
59Serotonin (5-Hydroxytryptamine) 5-HT3 (human)15-hydroxytryptamine (serotonin) receptor 3A isoform b precursor [Homo sapiens] [gi:253735700]
Taxonomy id: 9606
Gene id: 3359
60Sigma s1 (human)1sigma non-opioid intracellular receptor 1 isoform 1 [Homo sapiens] [gi:5032117]
Taxonomy id: 9606
Gene id: 10280
61Sigma s2 (rat)1opioid receptor, sigma 1 [Rattus norvegicus] [gi:13591888]
Taxonomy id: 10116
Gene id: 29336
62Sodium Channel, Site 2 (rat)1sodium channel, voltage-gated, type I, alpha [Rattus norvegicus] [gi:13540709]
Taxonomy id: 10116
Gene id: 81574
63Tachykinin NK1 (human)1tachykinin receptor 1 isoform long [Homo sapiens] [gi:4507343]
Taxonomy id: 9606
Gene id: 6869
64Thyroid Hormone (rat)1c-erbA-alpha2 isoform TRalpha2 [Rattus norvegicus] [gi:63079703]
Taxonomy id: 10116
Gene id: 81812
65Transporter, Dopamine (DAT) (human)1solute carrier family 6 (neurotransmitter transporter, dopamine), member 3 [Homo sapiens] [gi:4507041]
Taxonomy id: 9606
Gene id: 6531
66Transporter, GABA (rat)1vesicular inhibitory amino acid transporter [Rattus norvegicus] [gi:13929106]
Taxonomy id: 10116
Gene id: 83612
67Transporter, Norepinephrine (NET) (human)1solute carrier family 6 member 2 [Homo sapiens] [gi:4557046]
Taxonomy id: 9606
Gene id: 6530
68Transporter, Serotonin (5-Hydroxytryptamine) (SERT) (human)1solute carrier family 6 member 4 [Homo sapiens] [gi:4507043]
Taxonomy id: 9606
Gene id: 6532

§ Panel component ID.
Protocol
The purpose of this assay was to test the lead compound against a broad panel of targets to determine ancillary activity.

MDS Pharma (The Triad, 2200 Renaissance Blvd, Suite 400, King of Prussia, PA 19406-2755) performed a Lead Profiling Screen of GPCRs, ion channels and transporters against the compound at 10uM concentration. The compond possessed a superior ancillary profile with only three activities >50% at 10 uM, and was thus declared an MLSCN probe.
Result Definitions
Show more
TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity Outcome1adenosine A1 receptor [Homo sapiens]Outcome
2Adenosine A1 (human) (10μM**)% Inhibition at Adenosine A1 (human) as reported by MDS1Integer%
3Activity Outcome2adenosine A2a receptor [Homo sapiens]Outcome
4Adenosine A2 (human) (10μM**)% Inhibition at Adenosine A2 (human) as reported by MDS2Integer%
5Activity Outcome3adenosine A3 receptor [Homo sapiens]Outcome
6Adenosine A3 (human) (10μM**)% Inhibition at Adenosine A3 (human) as reported by MDS3Integer%
7Activity Outcome4adrenergic, alpha-1A-, receptor [Rattus norvegicus]Outcome
8Adrenergic a1A (rat) (10μM**)% Inhibition at Adrenergic a1A (rat) as reported by MDS4Integer%
9Activity Outcome5adrenergic, alpha-1B-, receptor [Rattus norvegicus]Outcome
10Adrenergic a1B (rat) (10μM**)% Inhibition at Adrenergic a1B (rat) as reported by MDS5Integer%
11Activity Outcome6alpha-1D-adrenergic receptor [Homo sapiens]Outcome
12Adrenergic a1D (human) (10μM**)% Inhibition at Adrenergic a1D (human) as reported by MDS6Integer%
13Activity Outcome7alpha-2A-adrenergic receptor [Homo sapiens]Outcome
14Adrenergic a2A (human) (10μM**)% Inhibition at Adrenergic a2A (human) as reported by MDS7Integer%
15Activity Outcome8beta-1-adrenergic receptor [Homo sapiens]Outcome
16Adrenergic b1 (human) (10μM**)% Inhibition at Adrenergic b1 (human) as reported by MDS8Integer%
17Activity Outcome9adrenergic, beta-2-, receptor, surface [Homo sapiens]Outcome
18Adrenergic b2 (human) (10μM**)% Inhibition at Adrenergic b2 (human) as reported by MDS9Integer%
19Activity Outcome10androgen receptor [Rattus norvegicus]Outcome
20Androgen (testosterone)AR (rat) (10μM**)% Inhibition at Androgen (testosterone)AR (rat) as reported by MDS10Integer%
21Activity Outcome11bradykinin receptor B1 [Homo sapiens]Outcome
22Bradykinin B1 (human) (10μM**)% Inhibition at Bradykinin B1 (human) as reported by MDS11Integer%
23Activity Outcome12bradykinin receptor B2 [Homo sapiens]Outcome
24Bradykinin B2 (human) (10μM**)% Inhibition at Bradykinin B2 (human) as reported by MDS12Integer%
25Activity Outcome13Outcome
26Calcium channel L -type, benzothiazepine (rat) (10μM**)% Inhibition at Calcium channel L -type, benzothiazepine (rat) as reported by MDS13Integer%
27Activity Outcome14calcium channel, voltage-dependent, alpha2/delta subunit 1 isoform 1 [Rattus norvegicus]Outcome
28Calcium channel L -type, dihydropyridine (rat) (10μM**)% Inhibition at Calcium channel L -type, dihydropyridine (rat) as reported by MDS14Integer%
29Activity Outcome15calcium channel, voltage-dependent, N type, alpha 1B subunit [Rattus norvegicus]Outcome
30Calcium channel N-type (rat) (10μM**)% Inhibition at Calcium channel N-type (rat) as reported by MDS15Integer%
31Activity Outcome16dopamine receptor D1 [Homo sapiens]Outcome
32Dopamine D 1 (human) (10μM**)% Inhibition at Dopamine D 1 (human) as reported by MDS16Integer%
33Activity Outcome17dopamine receptor D2 isoform short [Homo sapiens]Outcome
34Dopamine D 2S (human) (10μM**)% Inhibition at Dopamine D 2S (human) as reported by MDS17Integer%
35Activity Outcome18dopamine receptor D4 [Homo sapiens]Outcome
36Dopamine D 4.2 (human) (10μM**)% Inhibition at Dopamine D 4.2 (human) as reported by MDS18Integer%
37Activity Outcome19dopamine receptor D3 isoform a [Homo sapiens]Outcome
38Dopamine D3 (human) (10μM**)% Inhibition at Dopamine D3 (human) as reported by MDS19Integer%
39Activity Outcome20endothelin receptor type A [Homo sapiens]Outcome
40Endothelin ETA (human) (10μM**)% Inhibition at Endothelin ETA (human) as reported by MDS20Integer%
41Activity Outcome21endothelin receptor type B isoform 1 precursor [Homo sapiens]Outcome
42Endothelin ETB (human) (10μM**)% Inhibition at Endothelin ETB (human) as reported by MDS21Integer%
43Activity Outcome22epidermal growth factor (beta-urogastrone) [Homo sapiens]Outcome
44Epidermal Growth Factor (EGF) (human) (10μM**)% Inhibition at Epidermal Growth Factor (EGF) (human) as reported by MDS22Integer%
45Activity Outcome23estrogen receptor alpha isoform 1 [Homo sapiens]Outcome
46Estrogen ER a (human) (10μM**)% Inhibition at Estrogen ER a (human) as reported by MDS23Integer%
47Activity Outcome24G protein-coupled receptor 103 [Homo sapiens]Outcome
48G protein-coupled receptor GPR103 (human) (10μM**)% Inhibition at G protein-coupled receptor GPR103 (human) as reported by MDS24Integer%
49Activity Outcome25gamma-aminobutyric acid (GABA) B receptor 1 isoform a precursor [Homo sapiens]Outcome
50GABA B1A (human) (10μM**)% Inhibition at GABA B1A (human) as reported by MDS25Integer%
51Activity Outcome26Outcome
52GABAAFlunitrazepam, central (rat) (10μM**)% Inhibition at GABAAFlunitrazepam, central (rat) as reported by MDS26Integer%
53Activity Outcome27gamma-aminobutyric acid (GABA) A receptor, gamma 2 [Rattus norvegicus]Outcome
54GABAAMuscimol, central (rat) (10μM**)% Inhibition at GABAAMuscimol, central (rat) as reported by MDS27Integer%
55Activity Outcome28nuclear receptor subfamily 3, group C, member 1 isoform alpha [Homo sapiens]Outcome
56Glucocorticoid (human) (10μM**)% Inhibition at Glucocorticoid (human) as reported by MDS28Integer%
57Activity Outcome29glutamate receptor, ionotropic, kainate 1 isoform 2 precursor [Rattus norvegicus]Outcome
58Glutamate, Kainate (rat) (10μM**)% Inhibition at Glutamate, Kainate (rat) as reported by MDS29Integer%
59Activity Outcome30glutamate receptor, ionotropic, N-methyl D-aspartate 1 [Rattus norvegicus]Outcome
60Glutamate, NMDA, Agonism (rat) (10μM**)% Inhibition at Glutamate, NMDA, Agonism (rat) as reported by MDS30Integer%
61Activity Outcome31glutamate receptor, ionotropic, N-methyl D-aspartate 2B [Rattus norvegicus]Outcome
62Glutamate, NMDA, Glycine (rat) (10μM**)% Inhibition at Glutamate, NMDA, Glycine (rat) as reported by MDS31Integer%
63Activity Outcome32glutamate receptor, ionotropic, NMDA2A (epsilon 1) [Mus musculus]Outcome
64Glutamate, NMDA, Phencyclidine (rat) (10μM**)% Inhibition at Glutamate, NMDA, Phencyclidine (rat) as reported by MDS32Integer%
65Activity Outcome33histamine receptor H1 [Homo sapiens]Outcome
66Histamine H1 (human) (10μM**)% Inhibition at Histamine H1 (human) as reported by MDS33Integer%
67Activity Outcome34histamine receptor H2 isoform 2 [Homo sapiens]Outcome
68Histamine H2 (human) (10μM**)% Inhibition at Histamine H2 (human) as reported by MDS34Integer%
69Activity Outcome35histamine receptor H3 [Homo sapiens]Outcome
70Histamine H3 (human) (10μM**)% Inhibition at Histamine H3 (human) as reported by MDS35Integer%
71Activity Outcome36PREDICTED: similar to nischarin [Rattus norvegicus]Outcome
72Imidazoline I2, central (rat) (10μM**)% Inhibition at Imidazoline I2, central (rat) as reported by MDS36Integer%
73Activity Outcome37interleukin 1 receptor, type I isoform 1 [Mus musculus]Outcome
74Interleukin IL-1 (mouse) (10μM**)% Inhibition at Interleukin IL-1 (mouse) as reported by MDS37Integer%
75Activity Outcome38cysteinyl leukotriene receptor 1 [Homo sapiens]Outcome
76Leukotriene, Cysteinyl CysLT1 (human) (10μM**)% Inhibition at Leukotriene, Cysteinyl CysLT1 (human) as reported by MDS38Integer%
77Activity Outcome39melatonin receptor 1A [Homo sapiens]Outcome
78Melatonin MT1 (human) (10μM**)% Inhibition at Melatonin MT1 (human) as reported by MDS39Integer%
79Activity Outcome40cholinergic receptor, muscarinic 1 [Homo sapiens]Outcome
80Muscarinic M1 (human) (10μM**)% Inhibition at Muscarinic M1 (human) as reported by MDS40Integer%
81Activity Outcome41cholinergic receptor, muscarinic 2 [Homo sapiens]Outcome
82Muscarinic M2 (human) (10μM**)% Inhibition at Muscarinic M2 (human) as reported by MDS41Integer%
83Activity Outcome42cholinergic receptor, muscarinic 3 [Homo sapiens]Outcome
84Muscarinic M3 (human) (10μM**)% Inhibition at Muscarinic M3 (human) as reported by MDS42Integer%
85Activity Outcome43neuropeptide Y receptor Y1 [Homo sapiens]Outcome
86Neuropeptide Y Y1 (human) (10μM**)% Inhibition at Neuropeptide Y Y1 (human) as reported by MDS43Integer%
87Activity Outcome44neuropeptide Y receptor Y2 [Homo sapiens]Outcome
88Neuropeptide Y Y2 (human) (10μM**)% Inhibition at Neuropeptide Y Y2 (human) as reported by MDS44Integer%
89Activity Outcome45cholinergic receptor, nicotinic, alpha 3 [Homo sapiens]Outcome
90Nicotinic Acetylcholine (human) (10μM**)% Inhibition at Nicotinic Acetylcholine (human) as reported by MDS45Integer%
91Activity Outcome46nicotinic cholinergic receptor alpha 1 isoform b precursor [Homo sapiens]Outcome
92Nicotinic Acetylcholine 1 a , Bungarotoxin (human) (10μM**)% Inhibition at Nicotinic Acetylcholine 1 a , Bungarotoxin (human) as reported by MDS46Integer%
93Activity Outcome47opioid receptor, delta 1 [Homo sapiens]Outcome
94Opiate d (OP1, DOP) (human) (10μM**)% Inhibition at Opiate d (OP1, DOP) (human) as reported by MDS47Integer%
95Activity Outcome48opioid receptor, kappa 1 [Homo sapiens]Outcome
96Opiate k (OP2, KOP) (human) (10μM**)% Inhibition at Opiate k (OP2, KOP) (human) as reported by MDS48Integer%
97Activity Outcome49opioid receptor, mu 1 isoform MOR-1 [Homo sapiens]Outcome
98Opiate m (OP3, MOP) (human) (10μM**)% Inhibition at Opiate m (OP3, MOP) (human) as reported by MDS49Integer%
99Activity Outcome50Outcome
100Phorbol Ester (mouse) (10μM**)% Inhibition at Phorbol Ester (mouse) as reported by MDS50Integer%
101Activity Outcome51Outcome
102Platelet Activating Factor (PAF) (human) (10μM**)% Inhibition at Platelet Activating Factor (PAF) (human) as reported by MDS51Integer%
103Activity Outcome52RecName: Full=G protein-activated inward rectifier potassium channel 2; AltName: Full=GIRK2; AltName: Full=Potassium channel, inwardly rectifying subfamily J member 6; AltName: Full=Inward rectifier K(+) channel Kir3.2; AltName: Full=KATP-2Outcome
104Potassium Channel [K ATP] (hamster) (10μM**)% Inhibition at Potassium Channel [K ATP] (hamster) as reported by MDS52Integer%
105Activity Outcome53voltage-gated potassium channel, subfamily H, member 2 isoform a [Homo sapiens]Outcome
106Potassium Channel hERG (human) (10μM**)% Inhibition at Potassium Channel hERG (human) as reported by MDS53Integer%
107Activity Outcome54prostaglandin E receptor 4, subtype EP4 [Homo sapiens]Outcome
108Prostanoid EP4 (human) (10μM**)% Inhibition at Prostanoid EP4 (human) as reported by MDS54Integer%
109Activity Outcome55Outcome
110Purinergic P2X (rabbit) (10μM**)% Inhibition at Purinergic P2X (rabbit) as reported by MDS55Integer%
111Activity Outcome56purinergic receptor P2Y, G-protein coupled 1 [Rattus norvegicus]Outcome
112Purinergic P2Y (rat) (10μM**)% Inhibition at Purinergic P2Y (rat) as reported by MDS56Integer%
113Activity Outcome57Outcome
114Rolipram (rat) (10μM**)% Inhibition at Rolipram (rat) as reported by MDS57Integer%
115Activity Outcome585-hydroxytryptamine (serotonin) receptor 1A [Homo sapiens]Outcome
116Serotonin (5-Hydroxytryptamine) 5-HT1A (human) (10μM**)% Inhibition at Serotonin (5-Hydroxytryptamine) 5-HT1A (human) as reported by MDS58Integer%
117Activity Outcome595-hydroxytryptamine (serotonin) receptor 3A isoform b precursor [Homo sapiens]Outcome
118Serotonin (5-Hydroxytryptamine) 5-HT3 (human) (10μM**)% Inhibition at Serotonin (5-Hydroxytryptamine) 5-HT3 (human) as reported by MDS59Integer%
119Activity Outcome60sigma non-opioid intracellular receptor 1 isoform 1 [Homo sapiens]Outcome
120Sigma s1 (human) (10μM**)% Inhibition at Sigma s1 (human) as reported by MDS60Integer%
121Activity Outcome61opioid receptor, sigma 1 [Rattus norvegicus]Outcome
122Sigma s2 (rat) (10μM**)% Inhibition at Sigma s2 (rat) as reported by MDS61Integer%
123Activity Outcome62sodium channel, voltage-gated, type I, alpha [Rattus norvegicus]Outcome
124Sodium Channel, Site 2 (rat) (10μM**)% Inhibition at Sodium Channel, Site 2 (rat) as reported by MDS62Integer%
125Activity Outcome63tachykinin receptor 1 isoform long [Homo sapiens]Outcome
126Tachykinin NK1 (human) (10μM**)% Inhibition at Tachykinin NK1 (human) as reported by MDS63Integer%
127Activity Outcome64c-erbA-alpha2 isoform TRalpha2 [Rattus norvegicus]Outcome
128Thyroid Hormone (rat) (10μM**)% Inhibition at Thyroid Hormone (rat) as reported by MDS64Integer%
129Activity Outcome65solute carrier family 6 (neurotransmitter transporter, dopamine), member 3 [Homo sapiens]Outcome
130Transporter, Dopamine (DAT) (human) (10μM**)% Inhibition at Transporter, Dopamine (DAT) (human) as reported by MDS65Integer%
131Activity Outcome66vesicular inhibitory amino acid transporter [Rattus norvegicus]Outcome
132Transporter, GABA (rat) (10μM**)% Inhibition at Transporter, GABA (rat) as reported by MDS66Integer%
133Activity Outcome67solute carrier family 6 member 2 [Homo sapiens]Outcome
134Transporter, Norepinephrine (NET) (human) (10μM**)% Inhibition at Transporter, Norepinephrine (NET) (human) as reported by MDS67Integer%
135Activity Outcome68solute carrier family 6 member 4 [Homo sapiens]Outcome
136Transporter, Serotonin (5-Hydroxytryptamine) (SERT) (human) (10μM**)% Inhibition at Transporter, Serotonin (5-Hydroxytryptamine) (SERT) (human) as reported by MDS68Integer%

** Test Concentration. § Panel component ID.
Additional Information
Grant Number: 1 R03 MH077606-01

Classification
PageFrom: