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BioAssay: AID 1921

Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator: Ancillary Activity

Grant Title: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM) ..more
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 Tested Compounds
 Tested Compounds
All(2)
 
 
Active(2)
 
 
 Tested Substances
 Tested Substances
All(2)
 
 
Active(2)
 
 
AID: 1921
Data Source: Vanderbilt Screening Center for GPCRs, Ion Channels and Transporters (rM4_PAM_ancillary)
BioAssay Type: Panel
Depositor Category: NIH Molecular Libraries Screening Center Network
BioAssay Version:
Deposit Date: 2009-09-04
Modify Date: 2009-10-10

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: cholinergic receptor, muscarinic 4 [Rattus norvegicus]
Description ..   

Gene:CHRM4     Conserved Domain     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 2
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
643Discovery of Novel Allosteric Agonists of the M4 Muscarinic Receptor: Confirmation ScreenOther depositor-specified cross reference: Discovery of Novel Allosteric Agonists of the M4 Muscarinic Receptor: Confirmation Screen
2616Chemical optimization of in vitro pharmacology and DMPK properties of the highly selective mAChR 4 (M4) Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor ActivitySummary depositor-specified cross reference
625Discovery of Novel Allosteric Agonists of the M4 Muscarinic Receptor: Primary ScreenScreening same project related to Summary assay
1923Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Analog PotencyConfirmatory same project related to Summary assay
1928Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Analog Fold-shift Selectivity at hM5Confirmatory same project related to Summary assay
1929Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Analog Foldshift Selectivity with hM3Confirmatory same project related to Summary assay
1930Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Fold-shift Selectivity with hM2Confirmatory same project related to Summary assay
1932Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Analog Fold-shift Selectivity at rM1Confirmatory same project related to Summary assay
1938Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator (PAM): Analog Dose Response with rM4Confirmatory same project related to Summary assay
1939Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator (PAM): NMS Competition at rM4Confirmatory same project related to Summary assay
449767Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Foldshift of AcetylcholineOther same project related to Summary assay
449769Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Analog Fold-shift Selectivity at rM4Confirmatory same project related to Summary assay
449770Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Foldshift of Acetylcholine with human M4Confirmatory same project related to Summary assay
588743Chemical optimization of the highly selective mAChR 4 (M4) Positive Allosteric Modulator (PAM) SeriesConfirmatory same project related to Summary assay
588744Human M1 PAM Extended Characterization CounterScreen (CRC)Confirmatory same project related to Summary assay
588745Human M3 PAM Extended Characterization CounterScreen (CRC)Confirmatory same project related to Summary assay
588746Human M2 PAM Extended Characterization CounterScreen (CRC)Confirmatory same project related to Summary assay
588747Human M5 PAM Extended Characterization CounterScreen (CRC)Confirmatory same project related to Summary assay
588748Rat M2 PAM Extended Characterization CounterScreen (CRC)Confirmatory same project related to Summary assay
588749Rat M1 PAM Extended Characterization CounterScreen (CRC)Confirmatory same project related to Summary assay
588750Rat M3 PAM Extended Characterization CounterScreen (CRC)Confirmatory same project related to Summary assay
588751Rat M4 PAM Extended Characterization CounterScreen (CRC)Confirmatory same project related to Summary assay
588752Rat M5 PAM Extended Characterization CounterScreen (CRC)Confirmatory same project related to Summary assay
588755Human M4 PAM Extended Characterization Fold ShiftOther same project related to Summary assay
588758ML253 Competition in Radioligand Binding assays (Riserca)Other same project related to Summary assay
623924Chemical optimization of in vitro pharmacology and DMPK properties of the highly selective mAChR 4 (M4) Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity (hM1 CounterScreen)Confirmatory same project related to Summary assay
623925Chemical optimization of in vitro pharmacology and DMPK properties of the highly selective mAChR 4 (M4) Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity (hM2 CounterScreen)Confirmatory same project related to Summary assay
623926Chemical optimization of in vitro pharmacology and DMPK properties of the highly selective mAChR 4 (M4) Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity (hM3 CounterScreen)Confirmatory same project related to Summary assay
623938Chemical optimization of in vitro pharmacology and DMPK properties of the highly selective mAChR 4 (M4) Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity (hM4 Calcium Potency)Confirmatory1 same project related to Summary assay
623939Chemical optimization of in vitro pharmacology and DMPK properties of the highly selective mAChR 4 (M4) Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity (hM5 CounterScreen)Confirmatory same project related to Summary assay
623940Chemical optimization of in vitro pharmacology and DMPK properties of the highly selective mAChR 4 (M4) Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity (rM1 CounterScreen)Confirmatory same project related to Summary assay
623941Chemical optimization of in vitro pharmacology and DMPK properties of the highly selective mAChR 4 (M4) Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity (rM2 CounterScreen)Confirmatory same project related to Summary assay
623943Chemical optimization of in vitro pharmacology and DMPK properties of the highly selective mAChR 4 (M4) Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity (rM3 CounterScreen)Confirmatory same project related to Summary assay
623945Chemical optimization of in vitro pharmacology and DMPK properties of the highly selective mAChR 4 (M4) Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity (rM4 CounterScreen)Confirmatory1 same project related to Summary assay
623946Chemical optimization of in vitro pharmacology and DMPK properties of the highly selective mAChR 4 (M4) Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity (rM5 CounterScreen)Confirmatory same project related to Summary assay
623948Chemical optimization of in vitro pharmacology and DMPK properties of the highly selective mAChR 4 (M4) Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity (hM4 Fold Shift)Other1 same project related to Summary assay
Description:
Assay Provider: Colleen Niswender
Assay Provider Affiliation: Vanderbilt University
Grant Title: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM)
Grant Number: MH077607-1

To date, five muscarinic acetylcholine receptor (mAChR) subtypes have been identified (M1-M5) and play important roles in mediating the actions of ACh in the peripheral and central nervous systems. Of these, M1 and M4 are the most heavily expressed in the CNS and represent attractive therapeutic targets for cognition, Alzheimer's disease, and schizophrenia. In contrast, the adverse effects of cholinergic agents are thought to be primarily due to activation of peripheral M2 and M3 mAChRs. Due to the high sequence homology and conservation of the orthosteric ACh binding site among the mAChR subtypes, development of chemical agents that are selective for a single subtype has been largely unsuccessful, and in the absence of highly selective activators of M4, it has been impossible to test the role of selective M4 activation. Clinical trials with xanomeline, a M1/M4-preferring orthosteric agonist, demonstrated efficacy as both a cognition-enhancing agent and an antipsychotic agent. In follow-up studies in rats, xanomeline displayed an antipsychotic-like profile comparable to clozapine. However, a long standing question concerned whether or not the antipsychotic efficacy or antipsychotic-like activity in animal models is mediated by activation of M1, M4, or a combination of both receptors. Data from mAChR knockout mice led to the suggestion that a selective M1 agonist would be beneficial for cognition, whereas an M4 agonist would provide antipsychotic activity for the treatment of schizophrenia. This proposal is further supported by recent studies demonstrating that M4 receptors modulate the dynamics of cholinergic and dopaminergic neurotransmission and that loss of M4 function results in a state of dopamine yperfunction. These data, coupled with findings that schizophrenic patients have altered hippocampal M4 but not M1 receptor expression, suggest that selective activators of M4 may provide a novel treatment strategy for schizophrenia patients. However, multiple studies suggest that M1 may also play an important role in the antipsychotic effects of mAChR agonists and that the relative contributions of M1 and M4 to the antipsychotic efficacy of xanomeline or antipsychotic-like effects of this compound in animal models are not known. However, highly selective centrally penetrant activators of either M1 or M4 have not been available, making it impossible to determine the in vivo effects of selective activation of these receptors.
Panel Information
M4 Positive Allosteric Modulator: Ancillary Activity
    Data Table(Active)    Data Table(All)Show more
PID§NameSubstancePanel TargetsDescriptionAdditional Information
ActiveInactive
1adenosine A1 receptor [Homo sapiens] [gi:4501947]
Taxonomy id: 9606
Gene id: 134
2adenosine A2a receptor [Homo sapiens] [gi:5921992]
Taxonomy id: 9606
Gene id: 135
3adenosine A3 receptor [Homo sapiens] [gi:4262078]
Taxonomy id: 9606
Gene id: 140
4adrenergic, alpha-1A-, receptor [Rattus norvegicus] [gi:148747171]
Taxonomy id: 10116
Gene id: 29412
5adrenergic, alpha-1B-, receptor [Rattus norvegicus] [gi:47575853]
Taxonomy id: 10116
Gene id: 24173
6alpha-1D-adrenergic receptor [Homo sapiens] [gi:4501957]
Taxonomy id: 9606
Gene id: 146
7alpha-2A-adrenergic receptor [Homo sapiens] [gi:194353970]
Taxonomy id: 9606
Gene id: 150
8beta-1-adrenergic receptor [Homo sapiens] [gi:4557265]
Taxonomy id: 9606
Gene id: 153
9adrenergic, beta-2-, receptor, surface [Homo sapiens] [gi:4501969]
Taxonomy id: 9606
Gene id: 154
10androgen receptor [Rattus norvegicus] [gi:6978535]
Taxonomy id: 10116
Gene id: 24208
11bradykinin receptor B1 [Homo sapiens] [gi:20544172]
Taxonomy id: 9606
Gene id: 623
12bradykinin receptor B2 [Homo sapiens] [gi:4557359]
Taxonomy id: 9606
Gene id: 624
13Taxonomy id: 10116
14calcium channel, voltage-dependent, alpha2/delta subunit 1 isoform 1 [Rattus norvegicus] [gi:31542335]
Taxonomy id: 10116
Gene id: 25399
15calcium channel, voltage-dependent, N type, alpha 1B subunit [Rattus norvegicus] [gi:25453410]
Taxonomy id: 10116
Gene id: 257648
16dopamine receptor D1 [Homo sapiens] [gi:4503383]
Taxonomy id: 9606
Gene id: 1812
17dopamine receptor D2 isoform short [Homo sapiens] [gi:17986270]
Taxonomy id: 9606
Gene id: 1813
18dopamine receptor D4 [Homo sapiens] [gi:32483397]
Taxonomy id: 9606
Gene id: 1815
19dopamine receptor D3 isoform a [Homo sapiens] [gi:89191861]
Taxonomy id: 9606
Gene id: 1814
20endothelin receptor type A isoform a precursor [Homo sapiens] [gi:4503465]
Taxonomy id: 9606
Gene id: 1909
21endothelin receptor type B isoform 1 precursor [Homo sapiens] [gi:4557547]
Taxonomy id: 9606
Gene id: 1910
22Taxonomy id: 9606
23estrogen receptor alpha isoform 1 [Homo sapiens] [gi:62821794]
Taxonomy id: 9606
Gene id: 2099
24G protein-coupled receptor 103 [Homo sapiens] [gi:157738685]
Taxonomy id: 9606
Gene id: 84109
25gamma-aminobutyric acid (GABA) B receptor 1 isoform a precursor [Homo sapiens] [gi:10835015]
Taxonomy id: 9606
Gene id: 2550
26Taxonomy id: 10116
27gamma-aminobutyric acid (GABA) A receptor, gamma 2 precursor [Rattus norvegicus] [gi:34328527]
Taxonomy id: 10116
Gene id: 29709
28glucocorticoid receptor isoform alpha [Homo sapiens] [gi:66528611]
Taxonomy id: 9606
Gene id: 2908
29glutamate receptor, ionotropic, kainate 1 isoform 2 precursor [Rattus norvegicus] [gi:8393481]
Taxonomy id: 10116
Gene id: 29559
30glutamate receptor, ionotropic, N-methyl D-aspartate 1 precursor [Rattus norvegicus] [gi:8393484]
Taxonomy id: 10116
Gene id: 24408
31glutamate receptor, ionotropic, N-methyl D-aspartate 2B precursor [Rattus norvegicus] [gi:6980984]
Taxonomy id: 10116
Gene id: 24410
32glutamate receptor, ionotropic, NMDA2A (epsilon 1) precursor [Mus musculus] [gi:41680705]
Taxonomy id: 10116
Gene id: 14811
33histamine receptor H1 [Homo sapiens] [gi:149158709]
Taxonomy id: 9606
Gene id: 3269
34histamine receptor H2 isoform 2 [Homo sapiens] [gi:13435405]
Taxonomy id: 9606
Gene id: 3274
35Taxonomy id: 9606
36PREDICTED: similar to nischarin [Rattus norvegicus] [gi:109503022]
Taxonomy id: 10116
Gene id: 306255
37interleukin 1 receptor, type I isoform 1 [Mus musculus] [gi:6680417]
Taxonomy id: 10090
Gene id: 16177
38cysteinyl leukotriene receptor 1 [Homo sapiens] [gi:5729798]
Taxonomy id: 9606
Gene id: 10800
39melatonin receptor 1A [Homo sapiens] [gi:5174593]
Taxonomy id: 9606
Gene id: 4543
40cholinergic receptor, muscarinic 1 [Homo sapiens] [gi:37622910]
Taxonomy id: 9606
Gene id: 1128
41cholinergic receptor, muscarinic 2 [Homo sapiens] [gi:4502817]
Taxonomy id: 9606
Gene id: 1129
42cholinergic receptor, muscarinic 3 [Homo sapiens] [gi:4502819]
Taxonomy id: 9606
Gene id: 1131
43neuropeptide Y receptor Y1 [Homo sapiens] [gi:4505445]
Taxonomy id: 9606
Gene id: 4886
44neuropeptide Y receptor Y2 [Homo sapiens] [gi:4505447]
Taxonomy id: 9606
Gene id: 4887
45cholinergic receptor, nicotinic, alpha 3 precursor [Homo sapiens] [gi:19923122]
Taxonomy id: 9606
Gene id: 1136
46nicotinic cholinergic receptor alpha 1 isoform b precursor [Homo sapiens] [gi:4557457]
Taxonomy id: 9606
Gene id: 1134
47opioid receptor, delta 1 [Homo sapiens] [gi:63477962]
Taxonomy id: 9606
Gene id: 4985
48opioid receptor, kappa 1 [Homo sapiens] [gi:39725940]
Taxonomy id: 9606
Gene id: 4986
49opioid receptor, mu 1 isoform MOR-1 [Homo sapiens] [gi:117940060]
Taxonomy id: 9606
Gene id: 4988
50Taxonomy id: 10090
51Taxonomy id: 9606
52RecName: 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
53voltage-gated potassium channel, subfamily H, member 2 isoform a [Homo sapiens] [gi:4557729]
Taxonomy id: 9606
Gene id: 3757
54
55
56purinergic receptor P2Y, G-protein coupled 1 [Rattus norvegicus] [gi:25742733]
Taxonomy id: 10116
Gene id: 25265
57Taxonomy id: 10116
585-hydroxytryptamine (serotonin) receptor 1A [Homo sapiens] [gi:55956923]
Taxonomy id: 9606
Gene id: 3350
59Taxonomy id: 9606
60sigma non-opioid intracellular receptor 1 isoform 1 [Homo sapiens] [gi:5032117]
Taxonomy id: 9606
Gene id: 10280
61opioid receptor, sigma 1 [Rattus norvegicus] [gi:13591888]
Taxonomy id: 10116
Gene id: 29336
62sodium channel, voltage-gated, type I, alpha [Rattus norvegicus] [gi:13540709]
Taxonomy id: 10116
Gene id: 81574
63tachykinin receptor 1 isoform long [Homo sapiens] [gi:4507343]
Taxonomy id: 9606
Gene id: 6869
64c-erbA-alpha2 isoform TRalpha2 [Rattus norvegicus] [gi:63079703]
Taxonomy id: 10116
Gene id: 81812
65solute carrier family 6 (neurotransmitter transporter, dopamine), member 3 [Homo sapiens] [gi:4507041]
Taxonomy id: 9606
Gene id: 6531
66vesicular inhibitory amino acid transporter [Rattus norvegicus] [gi:13929106]
Taxonomy id: 10116
Gene id: 83612
67solute carrier family 6 member 2 [Homo sapiens] [gi:4557046]
Taxonomy id: 9606
Gene id: 6530
68solute 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.
Categorized Comment - additional comments and annotations
From PubChem:
Assay Test Type: In vitro/In vivo
Result Definitions
Show more
TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1Adenosine A1 (human) (10μM**)% Inhibition at Adenosine A1 (human) as reported by MDS1adenosine A1 receptor [Homo sapiens]Integer%
2Adenosine A2 (human) (10μM**)% Inhibition at Adenosine A2 (human) as reported by MDS2adenosine A2a receptor [Homo sapiens]Integer%
3Adenosine A3 (human) (10μM**)% Inhibition at Adenosine A3 (human) as reported by MDS3adenosine A3 receptor [Homo sapiens]Integer%
4Adrenergic a1A (rat) (10μM**)% Inhibition at Adrenergic a1A (rat) as reported by MDS4adrenergic, alpha-1A-, receptor [Rattus norvegicus]Integer%
5Adrenergic a1B (rat) (10μM**)% Inhibition at Adrenergic a1B (rat) as reported by MDS5adrenergic, alpha-1B-, receptor [Rattus norvegicus]Integer%
6Adrenergic a1D (human) (10μM**)% Inhibition at Adrenergic a1D (human) as reported by MDS6alpha-1D-adrenergic receptor [Homo sapiens]Integer%
7Adrenergic a2A (human) (10μM**)% Inhibition at Adrenergic a2A (human) as reported by MDS7alpha-2A-adrenergic receptor [Homo sapiens]Integer%
8Adrenergic b1 (human) (10μM**)% Inhibition at Adrenergic b1 (human) as reported by MDS8beta-1-adrenergic receptor [Homo sapiens]Integer%
9Adrenergic b2 (human) (10μM**)% Inhibition at Adrenergic b2 (human) as reported by MDS9adrenergic, beta-2-, receptor, surface [Homo sapiens]Integer%
10Androgen (testosterone)AR (rat) (10μM**)% Inhibition at Androgen (testosterone)AR (rat) as reported by MDS10androgen receptor [Rattus norvegicus]Integer%
11Bradykinin B1 (human) (10μM**)% Inhibition at Bradykinin B1 (human) as reported by MDS11bradykinin receptor B1 [Homo sapiens]Integer%
12Bradykinin B2 (human) (10μM**)% Inhibition at Bradykinin B2 (human) as reported by MDS12bradykinin receptor B2 [Homo sapiens]Integer%
13Calcium channel L -type, benzothiazepine (rat) (10μM**)% Inhibition at Calcium channel L -type, benzothiazepine (rat) as reported by MDS13Integer%
14Calcium channel L -type, dihydropyridine (rat) (10μM**)% Inhibition at Calcium channel L -type, dihydropyridine (rat) as reported by MDS14calcium channel, voltage-dependent, alpha2/delta subunit 1 isoform 1 [Rattus norvegicus]Integer%
15Calcium channel N-type (rat) (10μM**)% Inhibition at Calcium channel N-type (rat) as reported by MDS15calcium channel, voltage-dependent, N type, alpha 1B subunit [Rattus norvegicus]Integer%
16Dopamine D 1 (human) (10μM**)% Inhibition at Dopamine D 1 (human) as reported by MDS16dopamine receptor D1 [Homo sapiens]Integer%
17Dopamine D 2S (human) (10μM**)% Inhibition at Dopamine D 2S (human) as reported by MDS17dopamine receptor D2 isoform short [Homo sapiens]Integer%
18Dopamine D 4.2 (human) (10μM**)% Inhibition at Dopamine D 4.2 (human) as reported by MDS18dopamine receptor D4 [Homo sapiens]Integer%
19Dopamine D3 (human) (10μM**)% Inhibition at Dopamine D3 (human) as reported by MDS19dopamine receptor D3 isoform a [Homo sapiens]Integer%
20Endothelin ETA (human) (10μM**)% Inhibition at Endothelin ETA (human) as reported by MDS20endothelin receptor type A isoform a precursor [Homo sapiens]Integer%
21Endothelin ETB (human) (10μM**)% Inhibition at Endothelin ETB (human) as reported by MDS21endothelin receptor type B isoform 1 precursor [Homo sapiens]Integer%
22Epidermal Growth Factor (EGF) (human) (10μM**)% Inhibition at Epidermal Growth Factor (EGF) (human) as reported by MDS22Integer%
23Estrogen ER a (human) (10μM**)% Inhibition at Estrogen ER a (human) as reported by MDS23estrogen receptor alpha isoform 1 [Homo sapiens]Integer%
24G protein-coupled receptor GPR103 (human) (10μM**)% Inhibition at G protein-coupled receptor GPR103 (human) as reported by MDS24G protein-coupled receptor 103 [Homo sapiens]Integer%
25GABA B1A (human) (10μM**)% Inhibition at GABA B1A (human) as reported by MDS25gamma-aminobutyric acid (GABA) B receptor 1 isoform a precursor [Homo sapiens]Integer%
26GABAAFlunitrazepam, central (rat) (10μM**)% Inhibition at GABAAFlunitrazepam, central (rat) as reported by MDS26Integer%
27GABAAMuscimol, central (rat) (10μM**)% Inhibition at GABAAMuscimol, central (rat) as reported by MDS27gamma-aminobutyric acid (GABA) A receptor, gamma 2 precursor [Rattus norvegicus]Integer%
28Glucocorticoid (human) (10μM**)% Inhibition at Glucocorticoid (human) as reported by MDS28glucocorticoid receptor isoform alpha [Homo sapiens]Integer%
29Glutamate, Kainate (rat) (10μM**)% Inhibition at Glutamate, Kainate (rat) as reported by MDS29glutamate receptor, ionotropic, kainate 1 isoform 2 precursor [Rattus norvegicus]Integer%
30Glutamate, NMDA, Agonism (rat) (10μM**)% Inhibition at Glutamate, NMDA, Agonism (rat) as reported by MDS30glutamate receptor, ionotropic, N-methyl D-aspartate 1 precursor [Rattus norvegicus]Integer%
31Glutamate, NMDA, Glycine (rat) (10μM**)% Inhibition at Glutamate, NMDA, Glycine (rat) as reported by MDS31glutamate receptor, ionotropic, N-methyl D-aspartate 2B precursor [Rattus norvegicus]Integer%
32Glutamate, NMDA, Phencyclidine (rat) (10μM**)% Inhibition at Glutamate, NMDA, Phencyclidine (rat) as reported by MDS32glutamate receptor, ionotropic, NMDA2A (epsilon 1) precursor [Mus musculus]Integer%
33Histamine H1 (human) (10μM**)% Inhibition at Histamine H1 (human) as reported by MDS33histamine receptor H1 [Homo sapiens]Integer%
34Histamine H2 (human) (10μM**)% Inhibition at Histamine H2 (human) as reported by MDS34histamine receptor H2 isoform 2 [Homo sapiens]Integer%
35Histamine H3 (human) (10μM**)% Inhibition at Histamine H3 (human) as reported by MDS35Integer%
36Imidazoline I2, central (rat) (10μM**)% Inhibition at Imidazoline I2, central (rat) as reported by MDS36PREDICTED: similar to nischarin [Rattus norvegicus]Integer%
37Interleukin IL-1 (mouse) (10μM**)% Inhibition at Interleukin IL-1 (mouse) as reported by MDS37interleukin 1 receptor, type I isoform 1 [Mus musculus]Integer%
38Leukotriene, Cysteinyl CysLT1 (human) (10μM**)% Inhibition at Leukotriene, Cysteinyl CysLT1 (human) as reported by MDS38cysteinyl leukotriene receptor 1 [Homo sapiens]Integer%
39Melatonin MT1 (human) (10μM**)% Inhibition at Melatonin MT1 (human) as reported by MDS39melatonin receptor 1A [Homo sapiens]Integer%
40Muscarinic M1 (human) (10μM**)% Inhibition at Muscarinic M1 (human) as reported by MDS40cholinergic receptor, muscarinic 1 [Homo sapiens]Integer%
41Muscarinic M2 (human) (10μM**)% Inhibition at Muscarinic M2 (human) as reported by MDS41cholinergic receptor, muscarinic 2 [Homo sapiens]Integer%
42Muscarinic M3 (human) (10μM**)% Inhibition at Muscarinic M3 (human) as reported by MDS42cholinergic receptor, muscarinic 3 [Homo sapiens]Integer%
43Neuropeptide Y Y1 (human) (10μM**)% Inhibition at Neuropeptide Y Y1 (human) as reported by MDS43neuropeptide Y receptor Y1 [Homo sapiens]Integer%
44Neuropeptide Y Y2 (human) (10μM**)% Inhibition at Neuropeptide Y Y2 (human) as reported by MDS44neuropeptide Y receptor Y2 [Homo sapiens]Integer%
45Nicotinic Acetylcholine (human) (10μM**)% Inhibition at Nicotinic Acetylcholine (human) as reported by MDS45cholinergic receptor, nicotinic, alpha 3 precursor [Homo sapiens]Integer%
46Nicotinic Acetylcholine 1 a , Bungarotoxin (human) (10μM**)% Inhibition at Nicotinic Acetylcholine 1 a , Bungarotoxin (human) as reported by MDS46nicotinic cholinergic receptor alpha 1 isoform b precursor [Homo sapiens]Integer%
47Opiate d (OP1, DOP) (human) (10μM**)% Inhibition at Opiate d (OP1, DOP) (human) as reported by MDS47opioid receptor, delta 1 [Homo sapiens]Integer%
48Opiate k (OP2, KOP) (human) (10μM**)% Inhibition at Opiate k (OP2, KOP) (human) as reported by MDS48opioid receptor, kappa 1 [Homo sapiens]Integer%
49Opiate m (OP3, MOP) (human) (10μM**)% Inhibition at Opiate m (OP3, MOP) (human) as reported by MDS49opioid receptor, mu 1 isoform MOR-1 [Homo sapiens]Integer%
50Phorbol Ester (mouse) (10μM**)% Inhibition at Phorbol Ester (mouse) as reported by MDS50Integer%
51Platelet Activating Factor (PAF) (human) (10μM**)% Inhibition at Platelet Activating Factor (PAF) (human) as reported by MDS51Integer%
52Potassium Channel [K ATP] (hamster) (10μM**)% Inhibition at Potassium Channel [K ATP] (hamster) as reported by MDS52RecName: 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-2Integer%
53Potassium Channel hERG (human) (10μM**)% Inhibition at Potassium Channel hERG (human) as reported by MDS53voltage-gated potassium channel, subfamily H, member 2 isoform a [Homo sapiens]Integer%
54Prostanoid EP4 (human) (10μM**)% Inhibition at Prostanoid EP4 (human) as reported by MDS54Integer%
55Purinergic P2X (rabbit) (10μM**)% Inhibition at Purinergic P2X (rabbit) as reported by MDS55Integer%
56Purinergic P2Y (rat) (10μM**)% Inhibition at Purinergic P2Y (rat) as reported by MDS56purinergic receptor P2Y, G-protein coupled 1 [Rattus norvegicus]Integer%
57Rolipram (rat) (10μM**)% Inhibition at Rolipram (rat) as reported by MDS57Integer%
58Serotonin (5-Hydroxytryptamine) 5-HT1A (human) (10μM**)% Inhibition at Serotonin (5-Hydroxytryptamine) 5-HT1A (human) as reported by MDS585-hydroxytryptamine (serotonin) receptor 1A [Homo sapiens]Integer%
59Serotonin (5-Hydroxytryptamine) 5-HT3 (human) (10μM**)% Inhibition at Serotonin (5-Hydroxytryptamine) 5-HT3 (human) as reported by MDS59Integer%
60Sigma s1 (human) (10μM**)% Inhibition at Sigma s1 (human) as reported by MDS60sigma non-opioid intracellular receptor 1 isoform 1 [Homo sapiens]Integer%
61Sigma s2 (rat) (10μM**)% Inhibition at Sigma s2 (rat) as reported by MDS61opioid receptor, sigma 1 [Rattus norvegicus]Integer%
62Sodium Channel, Site 2 (rat) (10μM**)% Inhibition at Sodium Channel, Site 2 (rat) as reported by MDS62sodium channel, voltage-gated, type I, alpha [Rattus norvegicus]Integer%
63Tachykinin NK1 (human) (10μM**)% Inhibition at Tachykinin NK1 (human) as reported by MDS63tachykinin receptor 1 isoform long [Homo sapiens]Integer%
64Thyroid Hormone (rat) (10μM**)% Inhibition at Thyroid Hormone (rat) as reported by MDS64c-erbA-alpha2 isoform TRalpha2 [Rattus norvegicus]Integer%
65Transporter, Dopamine (DAT) (human) (10μM**)% Inhibition at Transporter, Dopamine (DAT) (human) as reported by MDS65solute carrier family 6 (neurotransmitter transporter, dopamine), member 3 [Homo sapiens]Integer%
66Transporter, GABA (rat) (10μM**)% Inhibition at Transporter, GABA (rat) as reported by MDS66vesicular inhibitory amino acid transporter [Rattus norvegicus]Integer%
67Transporter, Norepinephrine (NET) (human) (10μM**)% Inhibition at Transporter, Norepinephrine (NET) (human) as reported by MDS67solute carrier family 6 member 2 [Homo sapiens]Integer%
68Transporter, Serotonin (5-Hydroxytryptamine) (SERT) (human) (10μM**)% Inhibition at Transporter, Serotonin (5-Hydroxytryptamine) (SERT) (human) as reported by MDS68solute carrier family 6 member 4 [Homo sapiens]Integer%

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

Classification
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