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BioAssay: AID 743251

Development of a novel orthosteric Muscarinic 5 (M5) antagonist possessing a hig degree of muscarinic subtype selectivity

Methods employed in this study have been adapted from the scientific literature to maximize reliability and reproducibility.Reference standards were run as an integral part of each assay to ensure the validity of the results obtained. Assays were performed under conditions described in the accompanying "Methods" section of this report.Where presented, IC50 values were determined by a non-linear, more ..
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Active(1)
 
 
AID: 743251
Data Source: Vanderbilt Specialized Chemistry Center (Radioligand Binding assays (Eurofin) ML381 (VU248, PT# 11768..)
BioAssay Type: Panel, Primary, Primary Screening, Single Concentration Activity Observed
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2014-01-14
Hold-until Date: 2014-08-08
Modify Date: 2014-08-09

Data Table ( Complete ):           View Active Data    View All Data
Target
BioActive Compound: 1
Related Experiments
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AIDNameTypeProbeComment
624103Summary of the probe development efforts to identify agonists of the human cholinergic receptor, muscarinic 5 (CHRM5)Summary depositor-specified cross reference
624037Fluorescence-based cell-based primary high throughput screening assay to identify agonists of the human cholinergic receptor, muscarinic 5 (CHRM5)Screening same project related to Summary assay
624038Fluorescence-based cell-based primary high throughput screening assay to identify positive allosteric modulators (PAMs) of the human cholinergic receptor, muscarinic 5 (CHRM5)Screening same project related to Summary assay
624040Fluorescence-based cell-based primary high throughput screening assay to identify antagonists of the human cholinergic receptor, muscarinic 5 (CHRM5)Screening same project related to Summary assay
743025Discovery of Novel Negative Allosteric Modulators (NAM) of Muscarinic Receptor M5: Single Point AssayScreening same project related to Summary assay
743026Discovery of Novel Negative Allosteric Modulators (NAM) of Muscarinic Receptor M5: CRC AssayConfirmatory1 same project related to Summary assay
743096Discovery of Novel Positive Allosteric Modulators (PAMs) of Muscarinic Receptor M5: Counterscreen against human M2Confirmatory same project related to Summary assay
743097Discovery of Novel Positive Allosteric Modulators (PAMs) of Muscarinic Receptor M5: Counterscreen against human M1Confirmatory same project related to Summary assay
743098Discovery of Novel Negative Allosteric Modulators of Muscarinic Receptor M5: Counterscreen against human M1Confirmatory same project related to Summary assay
743099Discovery of Novel Negative Allosteric Modulators of Muscarinic Receptor M5: Counterscreen against human M2Confirmatory same project related to Summary assay
743100Discovery of Novel Positive Allosteric Modulators (PAMs) of Muscarinic Receptor M5: Single Point AssayScreening1 same project related to Summary assay
743101Discovery of Novel Positive Allosteric Modulators (PAMs) of Muscarinic Receptor M5: Counterscreen against human M4Confirmatory same project related to Summary assay
743102Discovery of Novel Positive Allosteric Modulators (PAMs) of Muscarinic Receptor M5: Confirmatory AssayConfirmatory1 same project related to Summary assay
743103Discovery of Negative Allosteric Modulators of Muscarinic Receptor M5: Counterscreen against human M3Confirmatory same project related to Summary assay
743104Discovery of Novel Negative Allosteric Modulators of Muscarinic Receptor M5: Counterscreen against RAT M5Confirmatory same project related to Summary assay
743105Discovery of Novel Negative Allosteric Modulators of Muscarinic Receptor M5: Counterscreen against human M4Confirmatory same project related to Summary assay
743107Discovery of Novel Antagonists of Muscarinic Receptor M5: Single Point AssayScreening same project related to Summary assay
743108Discovery of Novel Antagonists of Muscarinic Receptor M5: Counterscreen against human M1Confirmatory same project related to Summary assay
743109Discovery of Novel Antagonists of Muscarinic Receptor M5: Counterscreen against human M2Confirmatory same project related to Summary assay
743110Discovery of Novel Antagonists of Muscarinic Receptor M5: CRC AssayConfirmatory1 same project related to Summary assay
743111Discovery of Novel Positive Allosteric Modulators (PAMs) of Muscarinic Receptor M5: Counterscreen against RAT M5Confirmatory same project related to Summary assay
743112Discovery of Novel Antagonists of Muscarinic Receptor M5: Counterscreen against RAT M5Confirmatory same project related to Summary assay
743113Discovery of Novel Antagonists of Muscarinic Receptor M5: Counterscreen against human M4Confirmatory same project related to Summary assay
743114Discovery of Antagonists of Muscarinic Receptor M5: Counterscreen against human M3Confirmatory same project related to Summary assay
743115Discovery of Novel Positive Allosteric Modulators (PAMs) of Muscarinic Receptor M5: Counterscreen against human M3Confirmatory same project related to Summary assay
743249 On Hold
743252 On Hold
Description:
Assay Provider: Jeff Conn

Assay Provider Affiliation: Vanderbilt University

Methods employed in this study have been adapted from the scientific literature to maximize reliability and reproducibility.Reference standards were run as an integral part of each assay to ensure the validity of the results obtained. Assays were performed under conditions described in the accompanying "Methods" section of this report.Where presented, IC50 values were determined by a non-linear, least squares regression analysis using MathIQTM (IDBusiness Solutions Ltd., UK). Where inhibition constants (Ki) are presented, the Ki values were calculated using theequation of Cheng and Prusoff (Cheng, Y., Prusoff, W.H., Biochem. Pharmacol. 22:3099-3108, 1973) using theobserved IC50 of the tested compound, the concentration of radioligand employed in the assay, and the historical valuesfor the KD of the ligand (obtained experimentally at Eurofins Panlabs, Inc.). Where presented, the Hill coefficient (nH),defining the slope of the competitive binding curve, was calculated using MathIQTM. Hill coefficients significantly differentthan 1.0, may suggest that the binding displacement does not follow the laws of mass action with a single binding site.Where IC50, Ki, and/or nH data are presented without Standard Error of the Mean (SEM), data are insufficient to be quantitative and the values presented (Ki, IC50 and nH) should be interpreted with caution.
Panel Information
Panel Assay with Multiple Targets/Outcomes
    Data Table(Active)    Data Table(All)Show more
PID§NameSubstancePanel TargetsDescriptionAdditional Information
ActiveInactive
1Eurofin Panel Assays for BMP ProbeADORA1 gene product [Homo sapiens] [gi:4501947]
Radioligand Binding AssayTaxonomy id: 9606
2Eurofin Panel Assays for BMP ProbeADORA2A gene product [Homo sapiens] [gi:5921992]
Radioligand Binding AssayTaxonomy id: 9606
3Eurofin Panel Assays for BMP ProbeADORA3 gene product [Homo sapiens] [gi:4501953]
Radioligand Binding AssayTaxonomy id: 9606
4Eurofin Panel Assays for BMP ProbeAdra1a gene product [Rattus norvegicus] [gi:148747171]
Radioligand Binding AssayTaxonomy id: 10116
5Eurofin Panel Assays for BMP ProbeAdra1b gene product [Rattus norvegicus] [gi:47575853]
Radioligand Binding AssayTaxonomy id: 10116
6Eurofin Panel Assays for BMP ProbeAdra1d gene product [Rattus norvegicus] [gi:13324696]
Radioligand Binding AssayTaxonomy id: 9606
7Eurofin Panel Assays for BMP ProbeADRA2A gene product [Homo sapiens] [gi:194353970]
Radioligand Binding AssayTaxonomy id: 9606
8Eurofin Panel Assays for BMP ProbeADRB1 gene product [Homo sapiens] [gi:4557265]
Radioligand Binding AssayTaxonomy id: 9606
9Eurofin Panel Assays for BMP ProbeADRB2 gene product [Homo sapiens] [gi:4501969]
Radioligand Binding AssayTaxonomy id: 9606
10Eurofin Panel Assays for BMP Probenorepinephrine transporter [Homo sapiens] [gi:4335929]
Radioligand Binding AssayTaxonomy id: 9606
11Eurofin Panel Assays for BMP ProbeBDKRB1 gene product [Homo sapiens] [gi:20544172]
Radioligand Binding AssayTaxonomy id: 9606
12Eurofin Panel Assays for BMP ProbeBDKRB2 gene product [Homo sapiens] [gi:4557359]
Radioligand Binding AssayTaxonomy id: 9606
13Eurofin Panel Assays for BMP ProbeCACNA1C gene product [Homo sapiens] [gi:120433602]
Radioligand Binding AssayTaxonomy id: 10116
14Eurofin Panel Assays for BMP ProbeCACNA1S gene product [Homo sapiens] [gi:110349767]
Radioligand Binding AssayTaxonomy id: 10116
15Eurofin Panel Assays for BMP ProbeCacna1b gene product [Mus musculus] [gi:110225368]
Radioligand Binding AssayTaxonomy id: 10116
16Eurofin Panel Assays for BMP ProbeCNR1 gene product [Homo sapiens] [gi:237681173]
Radioligand Binding AssayTaxonomy id: 9606
17Eurofin Panel Assays for BMP ProbeCNR2 gene product [Homo sapiens] [gi:4502929]
Radioligand Binding AssayTaxonomy id: 9606
18Eurofin Panel Assays for BMP Probedopamine D2 receptor [Homo sapiens] [gi:299687]
Radioligand Binding AssayTaxonomy id: 9606
19Eurofin Panel Assays for BMP Probedopamine D3 receptor [Homo sapiens] [gi:553261]
Radioligand Binding AssayTaxonomy id: 9606
20Eurofin Panel Assays for BMP Probedopamine D4 receptor [Homo sapiens] [gi:1835973]
Radioligand Binding AssayTaxonomy id: 9606
21Eurofin Panel Assays for BMP Probedopamine transporter [Homo sapiens] [gi:256313]
Radioligand Binding AssayTaxonomy id: 9606
22Eurofin Panel Assays for BMP ProbeA-type endothelin receptor [Homo sapiens] [gi:238636]
Radioligand Binding AssayTaxonomy id: 9606
23Eurofin Panel Assays for BMP ProbeEDNRB gene product [Homo sapiens] [gi:4557547]
Radioligand Binding AssayTaxonomy id: 9606
24Eurofin Panel Assays for BMP Probeepidermal growth factor [Homo sapiens] [gi:46242544]
Radioligand Binding AssayTaxonomy id: 9606
25Eurofin Panel Assays for BMP ProbeESR1 gene product [Homo sapiens] [gi:62821794]
Radioligand Binding AssayTaxonomy id: 9606
26Eurofin Panel Assays for BMP ProbeGABA transporter [Homo sapiens] [gi:31658]
Radioligand Binding AssayTaxonomy id: 10116
27Eurofin Panel Assays for BMP ProbeGABAA receptor delta subunit [Rattus norvegicus] [gi:510878]
Radioligand Binding AssayTaxonomy id: 10116
28Eurofin Panel Assays for BMP ProbeGABAB receptor, subunit 1a [Homo sapiens] [gi:3776073]
Radioligand Binding AssayTaxonomy id: 9606
29Eurofin Panel Assays for BMP Probeglucocorticoid receptor [Homo sapiens] [gi:239758]
Radioligand Binding AssayTaxonomy id: 9606
30Eurofin Panel Assays for BMP ProbeGrik3 gene product [Rattus norvegicus] [gi:163659915]
Radioligand Binding AssayTaxonomy id: 10116
31Eurofin Panel Assays for BMP ProbeGrin1 gene product [Rattus norvegicus] [gi:8393484]
Radioligand Binding AssayTaxonomy id: 10116
32Eurofin Panel Assays for BMP ProbeHRH1 gene product [Homo sapiens] [gi:149158709]
Radioligand Binding AssayTaxonomy id: 9606
33Eurofin Panel Assays for BMP Probehistamine H2 receptor [Homo sapiens] [gi:5881576]
Radioligand Binding AssayTaxonomy id: 9606
34Eurofin Panel Assays for BMP ProbeHRH3 gene product [Homo sapiens] [gi:194018562]
Radioligand Binding AssayTaxonomy id: 9606
35Eurofin Panel Assays for BMP ProbeRecName: Full=Nischarin; AltName: Full=Imidazoline receptor 1; Short=I-1; Short=IR1; AltName: Full=Imidazoline-1 receptor; Short=I1R [gi:205829312]
Radioligand Binding AssayTaxonomy id: 10116
36Eurofin Panel Assays for BMP Probeinterleukin 1-beta [Mus musculus] [gi:309398]
Radioligand Binding AssayTaxonomy id: 10090
37Eurofin Panel Assays for BMP ProbeCYSLTR1 gene product [Homo sapiens] [gi:5729798]
Radioligand Binding AssayTaxonomy id: 9606
38Eurofin Panel Assays for BMP ProbeMTNR1A gene product [Homo sapiens] [gi:5174593]
Radioligand Binding AssayTaxonomy id: 9606
39Eurofin Panel Assays for BMP ProbeCHRM1 gene product [Homo sapiens] [gi:37622910]
Radioligand Binding AssayTaxonomy id: 9606
40Eurofin Panel Assays for BMP ProbeCHRM2 gene product [Homo sapiens] [gi:54792115]
Radioligand Binding AssayTaxonomy id: 9606
41Eurofin Panel Assays for BMP ProbeCHRM3 gene product [Homo sapiens] [gi:4502819]
Radioligand Binding AssayTaxonomy id: 9606
42Eurofin Panel Assays for BMP Probetachykinin receptor 1 [Homo sapiens] [gi:38565061]
Radioligand Binding AssayTaxonomy id: 9606
43Eurofin Panel Assays for BMP Probeneuropeptide Y Y1 receptor [Homo sapiens] [gi:1247453]
Radioligand Binding AssayTaxonomy id: 9606
44Eurofin Panel Assays for BMP Probeneuropeptide Y receptor Y2 [Homo sapiens] [gi:29824918]
Radioligand Binding AssayTaxonomy id: 9606
45Eurofin Panel Assays for BMP ProbeRecName: Full=Neuronal acetylcholine receptor subunit alpha-2; Flags: Precursor [gi:308153405]
Radioligand Binding AssayTaxonomy id: 9606
46Eurofin Panel Assays for BMP ProbeCHRNA1 gene product [Homo sapiens] [gi:87567783]
Radioligand Binding AssayTaxonomy id: 9606
47Eurofin Panel Assays for BMP Probedelta opiate receptor [Homo sapiens] [gi:501145]
Radioligand Binding AssayTaxonomy id: 9606
48Eurofin Panel Assays for BMP Probekappa opioid receptor [Homo sapiens] [gi:39986053]
Radioligand Binding AssayTaxonomy id: 9606
49Eurofin Panel Assays for BMP ProbeMu opiate receptor [Homo sapiens] [gi:452073]
Radioligand Binding AssayTaxonomy id: 9606
50Eurofin Panel Assays for BMP ProbeRecName: Full=Serine/threonine-protein kinase D3; AltName: Full=Protein kinase C nu type; AltName: Full=Protein kinase EPK2; AltName: Full=nPKC-nu [gi:12230239]
Radioligand Binding AssayTaxonomy id: 10090
51Eurofin Panel Assays for BMP Probeplatelet activating factor receptor [Homo sapiens] [gi:190015]
Radioligand Binding AssayTaxonomy id: 9606
52Eurofin Panel Assays for BMP Probepotassium channel [Homo sapiens] [gi:619879]
Radioligand Binding AssayTaxonomy id: 9606
53Eurofin Panel Assays for BMP Probepotassium channel HERG [Homo sapiens] [gi:37499017]
Radioligand Binding AssayTaxonomy id: 9606
54Eurofin Panel Assays for BMP ProbePTGER4 gene product [Homo sapiens] [gi:4506259]
Radioligand Binding AssayTaxonomy id: 9606
55Eurofin Panel Assays for BMP ProbePREDICTED: P2X purinoceptor 7 isoform X3 [Oryctolagus cuniculus] [gi:291406943]
Radioligand Binding AssayTaxonomy id: 9986
56Eurofin Panel Assays for BMP ProbeP2ry1 gene product [Rattus norvegicus] [gi:25742733]
Radioligand Binding AssayTaxonomy id: 10116
57Eurofin Panel Assays for BMP ProbePde4a gene product [Rattus norvegicus] [gi:158518444]
Radioligand Binding AssayTaxonomy id: 10116
58Eurofin Panel Assays for BMP Probeserotonin 5-HT1a receptor [Homo sapiens] [gi:36429]
Radioligand Binding AssayTaxonomy id: 9606
59Eurofin Panel Assays for BMP Probeserotonin 1B receptor [Homo sapiens] [gi:219679]
Radioligand Binding AssayTaxonomy id: 9606
60Eurofin Panel Assays for BMP Probeserotonin receptor [Homo sapiens] [gi:3115222]
Radioligand Binding AssayTaxonomy id: 9606
61Eurofin Panel Assays for BMP ProbeSLC6A4 gene product [Homo sapiens] [gi:4507043]
Radioligand Binding AssayTaxonomy id: 9606
62Eurofin Panel Assays for BMP Probesigma 1 receptor [Rattus norvegicus] [gi:5733130]
Radioligand Binding AssayTaxonomy id: 9606
63Eurofin Panel Assays for BMP Probesodium channel [Homo sapiens] [gi:3097314]
Radioligand Binding AssayTaxonomy id: 10116
64Eurofin Panel Assays for BMP Probeandrogen receptor [Homo sapiens] [gi:178882]
Radioligand Binding AssayTaxonomy id: 10116
65Eurofin Panel Assays for BMP Probethyroid hormone receptor [Homo sapiens] [gi:235280]
Radioligand Binding AssayTaxonomy id: 10116

§ Panel component ID.
Protocol
Biochemical assay results are presented as the percent inhibition of specific binding or activity throughout the report. Allother results are expressed in terms of that assay's quantitation method.1:For primary assays, only the lowest concentration with a significant response judged by the assays' criteria, is shownin this summary.2:Where applicable, either the secondary assay results with the lowest dose/concentration meeting the significancecriteria or, if inactive, the highest dose/concentration that did not meet the significance criteria is shown.3:Unless otherwise requested, primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH) are shown where applicable for individual requested assays. In screening packages, primary screening in duplicate with semi-quantitative data (e.g., estimated IC50, Ki and nH) are shown where applicable (concentration range of 4 log units);available secondary functional assays are carried out (30 mM) and MEC or MIC determined only if active in primary assays >50% at 1 log unit below initial test concentration.Significant responses (>/= 50% inhibition or stimulation for Biochemical assays) were noted in the primary assays listed below; No Significant results noted
Result Definitions
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TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Adenosine_A1_Percent_InhibitionPercent Inhibition1ADORA1 gene product [Homo sapiens]Float%
2Adenosine_A1_OutcomeActive/Inactive1Integer
3Adenosine_A2A_Percent_InhibitionPercent Inhibition2ADORA2A gene product [Homo sapiens]Float%
4Adenosine_A2A_OutcomeActive/Inactive2Integer
5Adenosine_A3_Percent_InhibitionPercent Inhibition3ADORA3 gene product [Homo sapiens]Float%
6Adenosine_A3_OutcomeActive/Inactive3Integer
7Adrenergic_alpha1A_Percent_InhibitionPercent Inhibition4Adra1a gene product [Rattus norvegicus]Float%
8Adrenergic_alpha1A_OutcomeActive/Inactive4Integer
9Adrenergic_alpha1B__Percent_InhibitionPercent Inhibition5Adra1b gene product [Rattus norvegicus]Float%
10Adrenergic_alpha1B__OutcomeActive/Inactive5Integer
11Adrenergic_alpha1D_Percent_InhibitionPercent Inhibition6Adra1d gene product [Rattus norvegicus]Float%
12Adrenergic_alpha1D_OutcomeActive/Inactive6Integer
13Adrenergic_alpha2A_Percent_InhibitionPercent Inhibition7ADRA2A gene product [Homo sapiens]Float%
14Adrenergic_alpha2A_OutcomeActive/Inactive7Integer
15Adrenergic_beta1_Percent_InhibitionPercent Inhibition8ADRB1 gene product [Homo sapiens]Float%
16Adrenergic_beta1_OutcomeActive/Inactive8Integer
17Adrenergic_beta2_Percent_InhibitionPercent Inhibition9ADRB2 gene product [Homo sapiens]Float%
18Adrenergic_beta2_OutcomeActive/Inactive9Integer
19Transporter_Norepinephrine_(NET)_Percent_InhibitionPercent Inhibition10norepinephrine transporter [Homo sapiens]Float%
20Transporter_Norepinephrine_(NET)_OutcomeActive/Inactive10Integer
21Bradykinin_B1_Percent_InhibitionPercent Inhibition11BDKRB1 gene product [Homo sapiens]Float%
22Bradykinin_B1_OutcomeActive/Inactive11Integer
23Bradykinin_B2_Percent_InhibitionPercent Inhibition12BDKRB2 gene product [Homo sapiens]Float%
24Bradykinin_B2_OutcomeActive/Inactive12Integer
25Calcium_Channel_L-Type_Benzothiazepine_Percent_InhibitionPercent Inhibition13CACNA1C gene product [Homo sapiens]Float%
26Calcium_Channel_L-Type_Benzothiazepine_OutcomeActive/Inactive13Integer
27Calcium_Channel_L-Type_Dihydropyridine_Percent_InhibitionPercent Inhibition14CACNA1S gene product [Homo sapiens]Float%
28Calcium_Channel_L-Type_Dihydropyridine_OutcomeActive/Inactive14Integer
29Calcium_Channel_N-Type_Percent_InhibitionPercent Inhibition15Cacna1b gene product [Mus musculus]Float%
30Calcium_Channel_N-Type_OutcomeActive/Inactive15Integer
31Cannabinoid_CB1_Percent_InhibitionPercent Inhibition16CNR1 gene product [Homo sapiens]Float%
32Cannabinoid_CB1_OutcomeActive/Inactive16Integer
33Dopamine_D1_Percent_InhibitionPercent Inhibition17CNR2 gene product [Homo sapiens]Float%
34Dopamine_D1_OutcomeActive/Inactive17Integer
35Dopamine_D2S_Percent_InhibitionPercent Inhibition18dopamine D2 receptor [Homo sapiens]Float%
36Dopamine_D2S_OutcomeActive/Inactive18Integer
37Dopamine_D3_Percent_InhibitionPercent Inhibition19dopamine D3 receptor [Homo sapiens]Float%
38Dopamine_D3_OutcomeActive/Inactive19Integer
39Dopamine_D4.2_Percent_InhibitionPercent Inhibition20dopamine D4 receptor [Homo sapiens]Float%
40Dopamine_D4.2_OutcomeActive/Inactive20Integer
41Transporter_Dopamine_(DAT)_Percent_InhibitionPercent Inhibition21dopamine transporter [Homo sapiens]Float%
42Transporter_Dopamine_(DAT)_OutcomeActive/Inactive21Integer
43Endothelin_ETA_Percent_InhibitionPercent Inhibition22A-type endothelin receptor [Homo sapiens]Float%
44Endothelin_ETA_OutcomeActive/Inactive22Integer
45Endothelin_ETB_Percent_InhibitionPercent Inhibition23EDNRB gene product [Homo sapiens]Float%
46Endothelin_ETB_OutcomeActive/Inactive23Integer
47Epidermal_Growth Factor_(EGF)_Percent_InhibitionPercent Inhibition24epidermal growth factor [Homo sapiens]Float%
48Epidermal_Growth Factor_(EGF)_OutcomeActive/Inactive24Integer
49Estrogen_ERalpha_Percent_InhibitionPercent Inhibition25ESR1 gene product [Homo sapiens]Float%
50Estrogen_ERalpha_OutcomeActive/Inactive25Integer
51Transporter_GABA_Percent_InhibitionPercent Inhibition26GABA transporter [Homo sapiens]Float%
52Transporter_GABA_OutcomeActive/Inactive26Integer
53GABAA_Muscimol_Central_Percent_InhibitionPercent Inhibition27GABAA receptor delta subunit [Rattus norvegicus]Float%
54GABAA_Muscimol_Central_OutcomeActive/Inactive27Integer
55GABAB1A_Percent_InhibitionPercent Inhibition28GABAB receptor, subunit 1a [Homo sapiens]Float%
56GABAB1A_OutcomeActive/Inactive28Integer
57Glucocorticoid_Percent_InhibitionPercent Inhibition29glucocorticoid receptor [Homo sapiens]Float%
58Glucocorticoid_OutcomeActive/Inactive29Integer
59Glutamate_Kainate_Percent_InhibitionPercent Inhibition30Grik3 gene product [Rattus norvegicus]Float%
60Glutamate_Kainate_OutcomeActive/Inactive30Integer
61Glutamate_NMDA_Agonism_Percent_InhibitionPercent Inhibition31Grin1 gene product [Rattus norvegicus]Float%
62Glutamate_NMDA_Agonism_OutcomeActive/Inactive31Integer
63Histamine_H1_Percent_InhibitionPercent Inhibition32HRH1 gene product [Homo sapiens]Float%
64Histamine_H1_OutcomeActive/Inactive32Integer
65Histamine_H2_Percent_InhibitionPercent Inhibition33histamine H2 receptor [Homo sapiens]Float%
66Histamine_H2_OutcomeActive/Inactive33Integer
67Histamine_H3_Percent_InhibitionPercent Inhibition34HRH3 gene product [Homo sapiens]Float%
68Histamine_H3_OutcomeActive/Inactive34Integer
69Imidazoline_I2_Central_Percent_InhibitionPercent Inhibition35RecName: Full=Nischarin; AltName: Full=Imidazoline receptor 1; Short=I-1; Short=IR1; AltName: Full=Imidazoline-1 receptor; Short=I1RFloat%
70Imidazoline_I2_Central_OutcomeActive/Inactive35Integer
71Interleukin_IL-1_Percent_InhibitionPercent Inhibition36interleukin 1-beta [Mus musculus]Float%
72Interleukin_IL-1_OutcomeActive/Inactive36Integer
73Leukotriene_Cysteinyl_CysLT1_Percent_InhibitionPercent Inhibition37CYSLTR1 gene product [Homo sapiens]Float%
74Leukotriene_Cysteinyl_CysLT1_OutcomeActive/Inactive37Integer
75Melatonin_MT1_Percent_InhibitionPercent Inhibition38MTNR1A gene product [Homo sapiens]Float%
76Melatonin_MT1_OutcomeActive/Inactive38Integer
77Muscarinic_M1_Percent_InhibitionPercent Inhibition39CHRM1 gene product [Homo sapiens]Float%
78Muscarinic_M1_OutcomeActive/Inactive39Integer
79Muscarinic_M2_Percent_InhibitionPercent Inhibition40CHRM2 gene product [Homo sapiens]Float%
80Muscarinic_M2_OutcomeActive/Inactive40Integer
81Muscarinic_M3_Percent_InhibitionPercent Inhibition41CHRM3 gene product [Homo sapiens]Float%
82Muscarinic_M3_OutcomeActive/Inactive41Integer
83Tachykinin_NK1_Percent_InhibitionPercent Inhibition42tachykinin receptor 1 [Homo sapiens]Float%
84Tachykinin_NK1_OutcomeActive/Inactive42Integer
85Neuropeptide_YY1_Percent_InhibitionPercent Inhibition43neuropeptide Y Y1 receptor [Homo sapiens]Float%
86Neuropeptide_YY1_OutcomeActive/Inactive43Integer
87Neuropeptide_YY2_Percent_InhibitionPercent Inhibition44neuropeptide Y receptor Y2 [Homo sapiens]Float%
88Neuropeptide_YY2_OutcomeActive/Inactive44Integer
89Nicotinic_Acetylcholine_Percent_InhibitionPercent Inhibition45RecName: Full=Neuronal acetylcholine receptor subunit alpha-2; Flags: PrecursorFloat%
90Nicotinic_Acetylcholine_OutcomeActive/Inactive45Integer
91Nicotinic_Acetylcholine_Alpha1_Bungarotoxin_Percent_InhibitionPercent Inhibition46CHRNA1 gene product [Homo sapiens]Float%
92Nicotinic_Acetylcholine_Alpha1_Bungarotoxin_OutcomeActive/Inactive46Integer
93Opiate_delta1 _(OP1, DOP)_Percent_InhibitionPercent Inhibition47delta opiate receptor [Homo sapiens]Float%
94Opiate_delta1 _(OP1, DOP)_OutcomeActive/Inactive47Integer
95Opiate_kappa_(OP2, KOP)_Percent_InhibitionPercent Inhibition48kappa opioid receptor [Homo sapiens]Float%
96Opiate_kappa_(OP2, KOP)_OutcomeActive/Inactive48Integer
97Opiate_mu_(OP3, MOP)_Percent_InhibitionPercent Inhibition49Mu opiate receptor [Homo sapiens]Float%
98Opiate_mu_(OP3, MOP)_OutcomeActive/Inactive49Integer
99Phorbol_Ester_Percent_InhibitionPercent Inhibition50RecName: Full=Serine/threonine-protein kinase D3; AltName: Full=Protein kinase C nu type; AltName: Full=Protein kinase EPK2; AltName: Full=nPKC-nuFloat%
100Phorbol_Ester_OutcomeActive/Inactive50Integer
101Platelet_Activating_Factor _(PAF)_Percent_InhibitionPercent Inhibition51platelet activating factor receptor [Homo sapiens]Float%
102Platelet_Activating_Factor _(PAF)_OutcomeActive/Inactive51Integer
103Potassium_Channel_[KATP]_Percent_InhibitionPercent Inhibition52potassium channel [Homo sapiens]Float%
104Potassium_Channel_[KATP]_OutcomeActive/Inactive52Integer
105Potassium_Channel_hERG_Percent_InhibitionPercent Inhibition53potassium channel HERG [Homo sapiens]Float%
106Potassium_Channel_hERG_OutcomeActive/Inactive53Integer
107Prostanoid_EP4_Percent_InhibitionPercent Inhibition54PTGER4 gene product [Homo sapiens]Float%
108Prostanoid_EP4_OutcomeActive/Inactive54Integer
109Purinergic_P2X_Percent_InhibitionPercent Inhibition55PREDICTED: P2X purinoceptor 7 isoform X3 [Oryctolagus cuniculus]Float%
110Purinergic_P2X_OutcomeActive/Inactive55Integer
111Purinergic_P2Y_Percent_InhibitionPercent Inhibition56P2ry1 gene product [Rattus norvegicus]Float%
112Purinergic_P2Y_OutcomeActive/Inactive56Integer
113Rolipram_Percent_InhibitionPercent Inhibition57Pde4a gene product [Rattus norvegicus]Float%
114Rolipram_OutcomeActive/Inactive57Integer
115Serotonin_(5-Hydroxytryptamine)_5-HT1A_Percent_InhibitionPercent Inhibition58serotonin 5-HT1a receptor [Homo sapiens]Float%
116Serotonin_(5-Hydroxytryptamine)_5-HT1A_OutcomeActive/Inactive58Integer
117Serotonin_(5-Hydroxytryptamine)_5-HT2B_Percent_InhibitionPercent Inhibition59serotonin 1B receptor [Homo sapiens]Float%
118Serotonin_(5-Hydroxytryptamine)_5-HT2B_OutcomeActive/Inactive59Integer
119Serotonin_(5-Hydroxytryptamine)_5-HT3_Percent_InhibitionPercent Inhibition60serotonin receptor [Homo sapiens]Float%
120Serotonin_(5-Hydroxytryptamine)_5-HT3_OutcomeActive/Inactive60Integer
121Transporter_Serotonin_(5-Hydroxytryptamine)_(SERT)_Percent_InhibitionPercent Inhibition61SLC6A4 gene product [Homo sapiens]Float%
122Transporter_Serotonin_(5-Hydroxytryptamine)_(SERT)_OutcomeActive/Inactive61Integer
123Sigma1_Percent_InhibitionPercent Inhibition62sigma 1 receptor [Rattus norvegicus]Float%
124Sigma1_OutcomeActive/Inactive62Integer
125Sodium _Channel_Site_2_Percent_InhibitionPercent Inhibition63sodium channel [Homo sapiens]Float%
126Sodium _Channel_Site_2_OutcomeActive/Inactive63Integer
127Androgen_(Testosterone)_AR_Percent_InhibitionPercent Inhibition64androgen receptor [Homo sapiens]Float%
128Androgen_(Testosterone)_AR_OutcomeActive/Inactive64Integer
129Thyroid_Hormone_Percent_InhibitionPercent Inhibition65thyroid hormone receptor [Homo sapiens]Float%
130Thyroid_Hormone_OutcomeActive/Inactive65Integer
Additional Information
Grant Number: 1X01 MH077606

Classification
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