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BioAssay: AID 434974

Late-stage radioligand binding assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen

Name: Late-stage radioligand binding assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Unspecified(1)
 
 
AID: 434974
Data Source: The Scripps Research Institute Molecular Screening Center (NOX1_INH_RAD_96_4X%INH_PDSP Screen)
BioAssay Type: Panel, Primary, Primary Screening, Single Concentration Activity Observed
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2010-06-04
Hold-until Date: 2010-08-18
Modify Date: 2010-08-19

Data Table ( Complete ):           All
Target
Tested Compound:
Depositor Specified Assays
Show more
AIDNameTypeProbeComment
1792Luminescence-based primary cell-based high throughput screening assay to identify inhibitors of NADPH oxidase 1 (Nox1): Maybridge Libraryscreening Primary screen (NOX1 inhibitors)
1796Summary of probe development efforts to identify inhibitors of NADPH oxidase 1 (Nox1)summary2 Summary AID (NOX1 inhibitors)
1823Luminescence-based counterscreen for inhibitors of NADPH oxidase 1 (Nox1): biochemical high throughput screening assay to identify inhibitors of luminol (Maybridge Library)screening Counterscreen (luminal)
2532Late stage results from the probe development effort to identify inhibitors of NOX1: HEK/293 IC50confirmatory Dose response (NOX1 inhibitors, HEK/293 cells)
2538Luminescence-based cell-based dose response assay to identify inhibitors of NADPH oxidase 1 (NOX1)confirmatory Dose response screen (NOX1 inhibitors)
2539Late stage results from the probe development effort to identify inhibitors of (NADPH oxidase 1) NOX1: Family selectivityscreening Counterscreen (NOX2, NOX3, NOX4 inhibitors)
2541Luminescence-based cell-based assay to identify inhibitors of NADPH oxidase 1 (NOX1)screening Confirmation screen (NOX1 inhibitors)
2545Late stage results from the probe development effort to identify inhibitors of (NADPH oxidase 1) NOX1: HEK/293 percent inhibitionscreening Confirmation screen (NOX1 inhibitors, HEK/293 cells)
2556Late stage results from the probe development effort to identify inhibitors of (NADPH oxidase 1) NOX1: Xanthine Oxidaseconfirmatory Counterscreen (Xanthine oxidase inhibitors)
2664Late-stage luminescence-based cell-based dose response assay to identify inhibitors of NADPH oxidase 1 (NOX1): Synthesized analogsconfirmatory Primary screen (NOX1 inhibitors, synthesized analogs)
2752Late-stage luminescence-based cell-based dose response assay to identify inhibitors of NADPH oxidase 1 (NOX1): Synthesized analogs 2confirmatory Primary screen (NOX1 inhibitors, synthesized analogs set 2)
2773Late-stage luminescence-based cell-based dose response assay to identify inhibitors of NADPH oxidase 1 (NOX1): Synthesized analogs 3confirmatory Primary screen (NOX1 inhibitors, synthesized analogs set 3)
435013Late stage results from the probe development effort to identify inhibitors of (NADPH oxidase 1) NOX1: Family selectivity: Set 2confirmatory
435009Late stage results from the probe development effort to identify inhibitors of (NADPH oxidase 1) NOX1: Xanthine Oxidase Set 2confirmatory
488778Late-stage microscopic assay to identify inhibitors of NADPH oxidase 1 (NOX1): Inhibition of extracellular matrix degradationother
504381Late-stage radioligand binding assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen Set 2other
504410Late-stage radioligand binding dose response assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen Ki Set 2confirmatory
434993Late-stage microscopic assay to identify inhibitors of NADPH oxidase 1 (NOX1): Inhibition of invadopodia formationother
434997Luminescence-based cell-based dose response assay to identify inhibitors of NADPH oxidase 1 (NOX1): Cherry picks 2confirmatory
435002Late stage results from the probe development effort to identify inhibitors of NOX1: HEK/293 IC50 Set 2confirmatory
463255Late-stage luminescence-based cell-based dose response assay to identify inhibitors of NADPH oxidase 1 (NOX1): Cytotoxicity assay 2confirmatory
434992Late-stage luminescence-based cell-based dose response assay to identify inhibitors of NADPH oxidase 1 (NOX1): Cytotoxicity assayother
Description:
Data Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC)
Center Affiliation: The Scripps Research Institute, TSRI
Assay Provider: Gary Bokoch, TSRI
Network: Molecular Libraries Probe Production Center Network (MLPCN)
Grant Proposal Number: 1 R03 MH083264-01A1
Grant Proposal PI: Gary Bokoch, TSRI
External Assay ID: NOX1_INH_RAD_96_4X%INH_PDSP Screen

Name: Late-stage radioligand binding assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen

Description:

Host defense mechanisms are diverse and include receptor-initiated signaling pathways, antibody and cytokine production, and the generation of reactive oxygen species (ROS) such as hydroxyl radical and hypochlorus acid to kill microorganisms (1). In activated phagocytic cells, the membrane integrated protein gp91phox serves as the catalytic cytochrome b subunit of the respiratory burst oxidase used to generate superoxide in an NADPH-dependent manner for host defense (2). Generation of ROS has also been identified in non-phagocytic cells (3). One important enzyme involved in ROS production in non-leukocyte tissues is NADPH oxidase 1 (NOX1), a homolog of gp91phox. NOX1 is highly expressed in colon epithelial cells where it can generate ROS to interact with normal and pathogenic bacteria (3-5). However, excess ROS production is associated with damage to the intestinal mucosa, particularly in mucosal lesions of inflammatory bowel disease (IBD) (4). Studies showing that NOX1 levels are increased in human prostate cancer (6) and that cells overexpressing NOX1 have a transformed appearance, exhibit anchorage-independent growth, and induce vascularized tumor formation in athymic mice (3, 7), suggest that NOX1 may also play a role in angiogenesis, cell growth, and tumor pathogenesis (8, 9). The identification of inhibitors of NOX1 may lead to potential candidates for excess cell proliferation, cancer, and IBD.

References:

1. Takeya, R. and Sumimoto, H., Molecular mechanism for activation of superoxide-producing NADPH oxidases. Mol Cells, 2003. 16(3): p. 271-7.
2. Cheng, G., Cao, Z., Xu, X., van Meir, E.G., and Lambeth, J.D., Homologs of gp91phox: cloning and tissue expression of Nox3, Nox4, and Nox5. Gene, 2001. 269(1-2): p. 131-40.
3. Suh, Y.A., Arnold, R.S., Lassegue, B., Shi, J., Xu, X., Sorescu, D., Chung, A.B., Griendling, K.K., and Lambeth, J.D., Cell transformation by the superoxide-generating oxidase Mox1. Nature, 1999. 401(6748): p. 79-82.
4. Szanto, I., Rubbia-Brandt, L., Kiss, P., Steger, K., Banfi, B., Kovari, E., Herrmann, F., Hadengue, A., and Krause, K.H., Expression of NOX1, a superoxide-generating NADPH oxidase, in colon cancer and inflammatory bowel disease. J Pathol, 2005. 207(2): p. 164-76.
5. Rokutan, K., Kawahara, T., Kuwano, Y., Tominaga, K., Nishida, K., and Teshima-Kondo, S., Nox enzymes and oxidative stress in the immunopathology of the gastrointestinal tract. Semin Immunopathol, 2008. 30(3): p. 315-27.
6. Lim, S.D., Sun, C., Lambeth, J.D., Marshall, F., Amin, M., Chung, L., Petros, J.A., and Arnold, R.S., Increased Nox1 and hydrogen peroxide in prostate cancer. Prostate, 2005. 62(2): p. 200-7.
7. Arnold, R.S., Shi, J., Murad, E., Whalen, A.M., Sun, C.Q., Polavarapu, R., Parthasarathy, S., Petros, J.A., and Lambeth, J.D., Hydrogen peroxide mediates the cell growth and transformation caused by the mitogenic oxidase Nox1. Proc Natl Acad Sci U S A, 2001. 98(10): p. 5550-5.
8. Ushio-Fukai, M. and Nakamura, Y., Reactive oxygen species and angiogenesis: NADPH oxidase as target for cancer therapy. Cancer Lett, 2008. 266(1): p. 37-52.
9. Kobayashi, S., Nojima, Y., Shibuya, M., and Maru, Y., Nox1 regulates apoptosis and potentially stimulates branching morphogenesis in sinusoidal endothelial cells. Exp Cell Res, 2004. 300(2): p. 455-62.

Keywords:

NOX1, NADPH oxidase 1, cancer, inflammation, 96, inhibitor, inhibition, late stage, Psychoactive Drug Screening Program, PDSP, radioligand, radioligand binding assay, receptor, transporter, ion channel, NIMH, Scripps, The Scripps Research Institute Molecular Screening Center, SRIMSC, Molecular Libraries Probe Production Center Network, MLPCN.
Panel Information
Receptors
    Data Table(All)Show more
PID§NameSubstancePanel TargetsDescriptionAdditional Information
ActiveInactive
1Serotonin receptor 5ht1a15-hydroxytryptamine (serotonin) receptor 1A [Homo sapiens] [gi:119571762]
Taxonomy id: 9606
Gene id: 3350
2Serotonin receptor 5ht1b15-hydroxytryptamine (serotonin) receptor 1B [Homo sapiens] [gi:119569107]
Taxonomy id: 9606
Gene id: 3351
3Serotonin receptor 5ht1d15-hydroxytryptamine (serotonin) receptor 1D [Homo sapiens] [gi:119615443]
Taxonomy id: 9606
Gene id: 3352
4Serotonin receptor 5ht1e15-hydroxytryptamine (serotonin) receptor 1E [Homo sapiens] [gi:10635353]
Taxonomy id: 9606
Gene id: 3354
5Serotonin receptor 5ht2a15-hydroxytryptamine (serotonin) receptor 2A [Homo sapiens] [gi:119629175]
Taxonomy id: 9606
Gene id: 3356
6Serotonin receptor 5ht2b15-hydroxytryptamine (serotonin) receptor 2B [Homo sapiens] [gi:119591355]
Taxonomy id: 9606
Gene id: 3357
7Serotonin receptor 5ht2c15-hydroxytryptamine (serotonin) receptor 2C, isoform CRA_b [Homo sapiens] [gi:119623029]
Taxonomy id: 9606
Gene id: 3358
8Serotonin receptor 5ht315-hydroxytryptamine (serotonin) receptor 3A, isoform CRA_c [Homo sapiens] [gi:119587644]
Taxonomy id: 9606
Gene id: 3359
9Serotonin receptor 5ht5a15-hydroxytryptamine (serotonin) receptor 5A [Homo sapiens] [gi:119624931]
Taxonomy id: 9606
Gene id: 3361
10Serotonin receptor 5ht615-hydroxytryptamine (serotonin) receptor 6 [Homo sapiens] [gi:119615302]
Taxonomy id: 9606
Gene id: 3362
11Serotonin receptor 5ht715-hydroxytryptamine (serotonin) receptor 7 (adenylate cyclase-coupled), isoform CRA_c [Homo sapiens] [gi:119570505]
Taxonomy id: 9606
Gene id: 3363
12Nicotinic receptor A2B21Cholinergic receptor, nicotinic, alpha 2 (neuronal) [Homo sapiens] [gi:158253953]
cholinergic receptor, nicotinic, beta 2 (neuronal) [Homo sapiens] [gi:119573577]
Taxonomy id: 9606
Gene id: 1135
Gene id: 1141
13Nicotinic receptor A2B41Cholinergic receptor, nicotinic, alpha 2 (neuronal) [Homo sapiens] [gi:158253953]
Cholinergic receptor, nicotinic, beta 4 [Homo sapiens] [gi:64654633]
Taxonomy id: 9606
Gene id: 1135
Gene id: 1143
14Nicotinic receptor A3B21Cholinergic receptor, nicotinic, alpha 3 [Homo sapiens] [gi:68534213]
cholinergic receptor, nicotinic, beta 2 (neuronal) [Homo sapiens] [gi:119573577]
Taxonomy id: 9606
Gene id: 1136
Gene id: 1141
15Nicotinic receptor A3B41Cholinergic receptor, nicotinic, alpha 3 [Homo sapiens] [gi:68534213]
Cholinergic receptor, nicotinic, beta 4 [Homo sapiens] [gi:64654633]
Taxonomy id: 9606
Gene id: 1136
Gene id: 1143
16Nicotinic receptor A4B21cholinergic receptor, nicotinic, alpha polypeptide 4 [Homo sapiens] [gi:68248536]
cholinergic receptor, nicotinic, beta 2 (neuronal) [Homo sapiens] [gi:119573577]
Taxonomy id: 9606
Gene id: 1137
Gene id: 1141
17Nicotinic receptor A4B41cholinergic receptor, nicotinic, alpha polypeptide 4 [Homo sapiens] [gi:68248536]
Cholinergic receptor, nicotinic, beta 4 [Homo sapiens] [gi:64654633]
Taxonomy id: 9606
Gene id: 1137
Gene id: 1143
18Adrenergic receptor Alpha1A1Adrenergic, alpha-1A-, receptor [Homo sapiens] [gi:66267329]
Taxonomy id: 9606
Gene id: 148
19Adrenergic receptor Alpha1B1Adrenergic, alpha-1B-, receptor [Homo sapiens] [gi:187953275]
Taxonomy id: 9606
Gene id: 147
20Adrenergic receptor Alpha1D1adrenergic, alpha-1D-, receptor [Homo sapiens] [gi:119630860]
Taxonomy id: 9606
Gene id: 146
21Adrenergic receptor Alpha2A1alpha-2A adrenergic receptor [Homo sapiens] [gi:194353970]
Taxonomy id: 9606
Gene id: 150
22Adrenergic receptor Alpha2B1Adrenergic, alpha-2B-, receptor [Homo sapiens] [gi:187953265]
Taxonomy id: 9606
Gene id: 151
23Adrenergic receptor Alpha2C1adrenergic, alpha-2C-, receptor [Homo sapiens] [gi:166706749]
Taxonomy id: 9606
Gene id: 152
24Adrenergic receptor Beta11adrenergic, beta-1-, receptor [Homo sapiens] [gi:166706747]
Taxonomy id: 9606
Gene id: 153
25Adrenergic receptor Beta21beta 2 adrenergic receptor [Homo sapiens] [gi:22658465]
Taxonomy id: 9606
Gene id: 154
26Adrenergic receptor Beta31adrenergic, beta-3-, receptor [Homo sapiens] [gi:68248548]
Taxonomy id: 9606
Gene id: 155
27BZP Rat Brain Site1Taxonomy id: 10116
28Ca+ Channel1Calcium channel, voltage-dependent, beta 1 subunit [Homo sapiens] [gi:54673627]
Taxonomy id: 9606
Gene id: 782
29Cannabinoid receptor CB11cannabinoid receptor [Homo sapiens] [gi:67550212]
Taxonomy id: 9606
Gene id: 1268
30Cannabinoid receptor CB21cannabinoid receptor 2 [Homo sapiens] [gi:81681157]
Taxonomy id: 9606
Gene id: 1269
31Dopamine receptor D11Dopamine receptor D1 [Homo sapiens] [gi:67677841]
Taxonomy id: 9606
Gene id: 1812
32Dopamine receptor D21Dopamine receptor D2 [Homo sapiens] [gi:18203703]
Taxonomy id: 9606
Gene id: 1813
33Dopamine receptor D31Dopamine receptor D3 [Homo sapiens] [gi:118764187]
Taxonomy id: 9606
Gene id: 1814
34Dopamine receptor D41dopamine receptor D4 [Homo sapiens] [gi:166714265]
Taxonomy id: 9606
Gene id: 1815
35Dopamine receptor D51dopamine receptor D5 [Homo sapiens] [gi:119613085]
Taxonomy id: 9606
Gene id: 1816
36Biogenic amine transporter DAT1dopamine transporter [Homo sapiens] [gi:139522363]
Taxonomy id: 9606
Gene id: 6531
37Opioid receptor DOR1delta-type opioid receptor [Homo sapiens] [gi:63477962]
Taxonomy id: 9606
Gene id: 4985
38Prostaglandin receptor EP31prostaglandin E receotor EP3 subtype 3 isoform [Homo sapiens] [gi:197692663]
Taxonomy id: 9606
Gene id: 5733
39Prostaglandin receptor EP41Prostaglandin E receptor 4 (subtype EP4) [Homo sapiens] [gi:109731195]
Taxonomy id: 9606
Gene id: 5734
40GABA receptor GABAa1gamma-aminobutyric acid receptor type A rho-1 subunit [Homo sapiens] [gi:182911]
Taxonomy id: 9606
Gene id: 2569
41GABA receptor GABAa a11GABA-A receptor alpha 1 subunit [Homo sapiens] [gi:31633]
Taxonomy id: 9606
Gene id: 2554
42Histamine receptor H11histamine H1 receptor [Homo sapiens] [gi:149158709]
Taxonomy id: 9606
Gene id: 3269
43Histamine receptor H21histamine receptor H2 [Homo sapiens] [gi:197692667]
Taxonomy id: 9606
Gene id: 3274
44Histamine receptor H31histamine H3 receptor [Homo sapiens] [gi:194018562]
Taxonomy id: 9606
Gene id: 11255
45Histamine receptor H41histamine H4 receptor [Homo sapiens] [gi:167887581]
Taxonomy id: 9606
Gene id: 59340
46Opioid receptor KOR1kappa opioid receptor [Homo sapiens] [gi:39986053]
Taxonomy id: 9606
Gene id: 4986
47Muscarinic receptor M11Cholinergic receptor, muscarinic 1 [gi:74754970]
Taxonomy id: 9606
Gene id: 1128
48Muscarinic receptor M21cholinergic receptor, muscarinic 2 [Homo sapiens] [gi:119604271]
Taxonomy id: 9606
Gene id: 1129
49Muscarinic receptor M31Cholinergic receptor, muscarinic 3 [Homo sapiens] [gi:111306506]
Taxonomy id: 9606
Gene id: 1131
50Muscarinic receptor M41Cholinergic receptor, muscarinic 4 [Homo sapiens] [gi:187953629]
Taxonomy id: 9606
Gene id: 1132
51Muscarinic receptor M51Cholinergic receptor, muscarinic 5 [gi:74759612]
Taxonomy id: 9606
Gene id: 1133
52Opioid receptor MOR1Mu opioid receptor [gi:74758917]
Taxonomy id: 9606
Gene id: 4988
53Biogenic amine transporter NET1Net [Homo sapiens] [gi:531523]
Taxonomy id: 9606
Gene id: 2004
54Glutamate receptor NMDA PCP site1glutamate receptor, ionotropic, N-methyl D-aspartate 1 [Homo sapiens] [gi:123240318]
Taxonomy id: 9606
Gene id: 2902
55Oxytocin receptor1Oxytocin receptor [Homo sapiens] [gi:187951685]
Taxonomy id: 9606
Gene id: 5021
56GABA receptor PBR1benzodiazepine receptor, peripheral [Rattus norvegicus] [gi:149065749]
Taxonomy id: 10116
Gene id: 24230
57Biogenic amine transporter SERT1serotonin transporter [Homo sapiens] [gi:58700442]
Taxonomy id: 9606
Gene id: 6532
58Sigma receptor 11opioid receptor, sigma 1 [Homo sapiens] [gi:123231939]
Taxonomy id: 9606
Gene id: 10280
59Sigma receptor 21Taxonomy id: 9606
60Vasopressin receptor V1A1arginine vasopressin receptor 1A [Homo sapiens] [gi:119617521]
Taxonomy id: 9606
Gene id: 552
61Vasopressin receptor V1B1arginine vasopressin receptor 1B [Homo sapiens] [gi:74418840]
Taxonomy id: 9606
Gene id: 553
62Vasopressin receptor V21arginine vasopressin receptor 2 [Homo sapiens] [gi:238055929]
Taxonomy id: 9606
Gene id: 554

§ Panel component ID.
Protocol
Assay Overview:

The purpose of this panel of radioligand binding assays performed by the NIMH Psychoactive Drug Screening Program (PDSP) is to identify a subset of potential receptors, transporters, ion channels, etc. for which the NOX1 inhibitor compound SID 92093123 displays affinity.

Protocol Summary:

Test and reference compounds are diluted to 5X final assay concentration (50 μM for a final assay concentration of 10 μM) in the appropriate radioligand binding buffer. Then, 50 μl aliquots of buffer (negative control), test compound, and reference compound (positive control) are added in quadruplicate to the wells of a 96-well plate, each of which contains 50 μl of 5X radioligand and 100 μl of buffer. Finally, receptor-containing, crude membrane fractions are resuspended in an appropriate volume of buffer and dispensed (50 μl per well) into the 96-well plate. Radioligand binding is allowed to equilibrate for 1.5 hours at room temperature, and then bound radioactivity is isolated by filtration onto 0.3% polyethyleneimine-treated, 96-well filter mats using a 96-well Filtermate harverster. The filter mats are dried, then scintillant is melted onto the filters and the radioactivity retained on the filters is counted in a Microbeta scintillation counter. As designed, membrane fractions to which compound CID 717880 binds will bind less radioligand and decrease the radioactivity measured in the assay.

Raw data from the Microbeta counter are analyzed on the PDSP DB. Total bound radioactivity is estimated from quadruplicate wells containing no test or reference compound and adjusted to 100%; non-specifically bound radioactivity is assessed from quadruplicate wells containing 10 μM of a suitable reference compound and adjusted to 0%. The average bound radioactivity in the presence of the test compound is expressed on a percent scale. The percent inhibition of radioligand binding is calculated as follows:

% Inhibition = 100% - % radioactivity bound

Inhibition of > 50% is considered significant. Negative inhibition represents a stimulation of binding.

The PDSP on-line data entry and analysis system calculates the variance of the quadruplicate determinations (for the total, non-specific, and test compound binding values) and variances greater than 20% are flagged for further inspection and assays are repeated if necessary. Additionally, % inhibition values that are greater than the total binding (i.e., 100%) by at least 20% are also flagged for inspection; such results could indicate allosteric modulation of radioligand binding.

List of Reagents:

Reagents were provided by the NIMH Psychoactive Drug Screening Program.
Result Definitions
Show more
TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Serotonin 5ht1a (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.15-hydroxytryptamine (serotonin) receptor 1A [Homo sapiens]Float%
2Serotonin 5ht1a (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.1Outcome
3Serotonin 5ht1b (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.25-hydroxytryptamine (serotonin) receptor 1B [Homo sapiens]Float%
4Serotonin 5ht1b (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.2Outcome
5Serotonin 5ht1d (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.35-hydroxytryptamine (serotonin) receptor 1D [Homo sapiens]Float%
6Serotonin 5ht1d (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.3Outcome
7Serotonin 5ht1e (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.45-hydroxytryptamine (serotonin) receptor 1E [Homo sapiens]Float%
8Serotonin 5ht1e (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.4Outcome
9Serotonin 5ht2a (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.55-hydroxytryptamine (serotonin) receptor 2A [Homo sapiens]Float%
10Serotonin 5ht2a (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.5Outcome
11Serotonin 5ht2b (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.65-hydroxytryptamine (serotonin) receptor 2B [Homo sapiens]Float%
12Serotonin 5ht2b (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.6Outcome
13Serotonin 5ht2c (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.75-hydroxytryptamine (serotonin) receptor 2C, isoform CRA_b [Homo sapiens]Float%
14Serotonin 5ht2c (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.7Outcome
15Serotonin 5ht3 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.85-hydroxytryptamine (serotonin) receptor 3A, isoform CRA_c [Homo sapiens]Float%
16Serotonin 5ht3 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.8Outcome
17Serotonin 5ht5a (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.95-hydroxytryptamine (serotonin) receptor 5A [Homo sapiens]Float%
18Serotonin 5ht5a (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.9Outcome
19Serotonin 5ht6 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.105-hydroxytryptamine (serotonin) receptor 6 [Homo sapiens]Float%
20Serotonin 5ht6 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.10Outcome
21Serotonin 5ht7 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.115-hydroxytryptamine (serotonin) receptor 7 (adenylate cyclase-coupled), isoform CRA_c [Homo sapiens]Float%
22Serotonin 5ht7 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.11Outcome
23Nicotinic A2B2 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.12Cholinergic receptor, nicotinic, alpha 2 (neuronal) [Homo sapiens]
cholinergic receptor, nicotinic, beta 2 (neuronal) [Homo sapiens]
Float%
24Nicotinic A2B2 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.12Outcome
25Nicotinic A2B4 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.13Cholinergic receptor, nicotinic, alpha 2 (neuronal) [Homo sapiens]
Cholinergic receptor, nicotinic, beta 4 [Homo sapiens]
Float%
26Nicotinic A2B4 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.13Outcome
27Nicotinic A3B2 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.14Cholinergic receptor, nicotinic, alpha 3 [Homo sapiens]
cholinergic receptor, nicotinic, beta 2 (neuronal) [Homo sapiens]
Float%
28Nicotinic A3B2 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.14Outcome
29Nicotinic A3B4 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.15Cholinergic receptor, nicotinic, alpha 3 [Homo sapiens]
Cholinergic receptor, nicotinic, beta 4 [Homo sapiens]
Float%
30Nicotinic A3B4 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.15Outcome
31Nicotinic A4B2 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.16cholinergic receptor, nicotinic, alpha polypeptide 4 [Homo sapiens]
cholinergic receptor, nicotinic, beta 2 (neuronal) [Homo sapiens]
Float%
32Nicotinic A4B2 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.16Outcome
33Nicotinic A4B4 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.17cholinergic receptor, nicotinic, alpha polypeptide 4 [Homo sapiens]
Cholinergic receptor, nicotinic, beta 4 [Homo sapiens]
Float%
34Nicotinic A4B4 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.17Outcome
35Adrenergic Alpha1A (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.18Adrenergic, alpha-1A-, receptor [Homo sapiens]Float%
36Adrenergic Alpha1A (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.18Outcome
37Adrenergic Alpha1B (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.19Adrenergic, alpha-1B-, receptor [Homo sapiens]Float%
38Adrenergic Alpha1B (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.19Outcome
39Adrenergic Alpha1D (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.20adrenergic, alpha-1D-, receptor [Homo sapiens]Float%
40Adrenergic Alpha1D (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.20Outcome
41Adrenergic Alpha2A (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.21alpha-2A adrenergic receptor [Homo sapiens]Float%
42Adrenergic Alpha2A (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.21Outcome
43Adrenergic Alpha2B (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.22Adrenergic, alpha-2B-, receptor [Homo sapiens]Float%
44Adrenergic Alpha2B (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.22Outcome
45Adrenergic Alpha2C (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.23adrenergic, alpha-2C-, receptor [Homo sapiens]Float%
46Adrenergic Alpha2C (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.23Outcome
47Adrenergic Beta1 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.24adrenergic, beta-1-, receptor [Homo sapiens]Float%
48Adrenergic Beta1 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.24Outcome
49Adrenergic Beta2 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.25beta 2 adrenergic receptor [Homo sapiens]Float%
50Adrenergic Beta2 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.25Outcome
51Adrenergic Beta3 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.26adrenergic, beta-3-, receptor [Homo sapiens]Float%
52Adrenergic Beta3 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.26Outcome
53BZP Rat Brain Site (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.27Float%
54BZP Rat Brain Site (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.27Outcome
55Ca+ Channel (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.28Calcium channel, voltage-dependent, beta 1 subunit [Homo sapiens]Float%
56Ca+ Channel (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.28Outcome
57Cannabinoid CB1 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.29cannabinoid receptor [Homo sapiens]Float%
58Cannabinoid CB1 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.29Outcome
59Cannabinoid CB2 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.30cannabinoid receptor 2 [Homo sapiens]Float%
60Cannabinoid CB2 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.30Outcome
61Dopamine D1 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.31Dopamine receptor D1 [Homo sapiens]Float%
62Dopamine D1 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.31Outcome
63Dopamine D2 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.32Dopamine receptor D2 [Homo sapiens]Float%
64Dopamine D2 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.32Outcome
65Dopamine D3 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.33Dopamine receptor D3 [Homo sapiens]Float%
66Dopamine D3 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.33Outcome
67Dopamine D4 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.34dopamine receptor D4 [Homo sapiens]Float%
68Dopamine D4 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.34Outcome
69Dopamine D5 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.35dopamine receptor D5 [Homo sapiens]Float%
70Dopamine D5 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.35Outcome
71Biogenic amine transporter DAT (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.36dopamine transporter [Homo sapiens]Float%
72Biogenic amine transporter DAT (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.36Outcome
73Opioid DOR (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.37delta-type opioid receptor [Homo sapiens]Float%
74Opioid DOR (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.37Outcome
75Prostaglandin EP3 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.38prostaglandin E receotor EP3 subtype 3 isoform [Homo sapiens]Float%
76Prostaglandin EP3 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.38Outcome
77Prostaglandin EP4 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.39Prostaglandin E receptor 4 (subtype EP4) [Homo sapiens]Float%
78Prostaglandin EP4 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.39Outcome
79GABA GabAa (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.40gamma-aminobutyric acid receptor type A rho-1 subunit [Homo sapiens]Float%
80GABA GabAa (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.40Outcome
81GABA GABAa a1 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.41GABA-A receptor alpha 1 subunit [Homo sapiens]Float%
82GABA GABAa a1 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.41Outcome
83Histamine H1 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.42histamine H1 receptor [Homo sapiens]Float%
84Histamine H1 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.42Outcome
85Histamine H2 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.43histamine receptor H2 [Homo sapiens]Float%
86Histamine H2 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.43Outcome
87Histamine H3 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.44histamine H3 receptor [Homo sapiens]Float%
88Histamine H3 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.44Outcome
89Histamine H4 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.45histamine H4 receptor [Homo sapiens]Float%
90Histamine H4 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.45Outcome
91Opioid KOR (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.46kappa opioid receptor [Homo sapiens]Float%
92Opioid KOR (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.46Outcome
93Muscarinic M1 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.47Cholinergic receptor, muscarinic 1Float%
94Muscarinic M1 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.47Outcome
95Muscarinic M2 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.48cholinergic receptor, muscarinic 2 [Homo sapiens]Float%
96Muscarinic M2 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.48Outcome
97Muscarinic M3 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.49Cholinergic receptor, muscarinic 3 [Homo sapiens]Float%
98Muscarinic M3 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.49Outcome
99Muscarinic M4 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.50Cholinergic receptor, muscarinic 4 [Homo sapiens]Float%
100Muscarinic M4 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.50Outcome
101Muscarinic M5 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.51Cholinergic receptor, muscarinic 5Float%
102Muscarinic M5 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested (NT).51Outcome
103Opioid MOR (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.52Mu opioid receptorFloat%
104Opioid MOR (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.52Outcome
105Biogenic amine transporter NET (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.53Net [Homo sapiens]Float%
106Biogenic amine transporter NET (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.53Outcome
107Glutamate NMDA PCP site (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.54glutamate receptor, ionotropic, N-methyl D-aspartate 1 [Homo sapiens]Float%
108Glutamate NMDA PCP site (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.54Outcome
109Oxytocin receptor (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.55Oxytocin receptor [Homo sapiens]Float%
110Oxytocin receptor (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.55Outcome
111GABA PBR (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.56benzodiazepine receptor, peripheral [Rattus norvegicus]Float%
112GABA PBR (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.56Outcome
113Biogenic amine transporter SERT (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.57serotonin transporter [Homo sapiens]Float%
114Biogenic amine transporter SERT (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.57Outcome
115Sigma 1 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.58opioid receptor, sigma 1 [Homo sapiens]Float%
116Sigma 1 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.58Outcome
117Sigma 2 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.59Float%
118Sigma 2 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.59Outcome
119Vasopressin V1A (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.60arginine vasopressin receptor 1A [Homo sapiens]Float%
120Vasopressin V1A (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.60Outcome
121Vasopressin V1B (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.61arginine vasopressin receptor 1B [Homo sapiens]Float%
122Vasopressin V1B (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.61Outcome
123Vasopressin V2 (Inhibition) (10μM**)Value of % Inhibition at 10 uM inhibitor concentration; average of four measurements.62arginine vasopressin receptor 2 [Homo sapiens]Float%
124Vasopressin V2 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.62Outcome

** Test Concentration. § Panel component ID.
Additional Information
Grant Number: 1 R03 MH083264-01A1

Classification
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