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BioAssay: AID 504381

Late-stage radioligand binding assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen Set 2

Name: Late-stage radioligand binding assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen Set 2 ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Unspecified(1)
 
 
AID: 504381
Data Source: The Scripps Research Institute Molecular Screening Center (NOX1_INH_RAD_96_4X%INH_PDSP SCREEN_SET 2)
BioAssay Type: Panel
Depositor Category: NIH Molecular Libraries Probe Production Network, Assay Provider
Deposit Date: 2011-02-28

Data Table ( Complete ):           All
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 in singlicate)
1796Summary of probe development efforts to identify inhibitors of NADPH oxidase 1 (Nox1)summary2 Summary (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 in singlicate)
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)
2808Late-stage luminescence-based cell-based dose response assay to identify inhibitors of NADPH oxidase 1 (NOX1): Purchased analogsconfirmatory Primary screen (NOX1 inhibitors, purchased analogs)
2819Late-stage luminescence-based cell-based dose response assay to identify inhibitors of NADPH oxidase 1 (NOX1): Purchased analogs 2confirmatory Primary screen (NOX1 inhibitors, purchased analogs set 2)
434974Late-stage radioligand binding assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screenscreening Psychoactive Drug Screening Program primary screen (NOX1 inhibitors)
434953Late-stage radioligand binding dose response assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen Kiscreening Psychoactive Drug Screening Program secondary screen (NOX1 inhibitors)
434992Late-stage luminescence-based cell-based dose response assay to identify inhibitors of NADPH oxidase 1 (NOX1): Cytotoxicity assayother Late stage dose response (Cytotoxicity)
434993Late-stage microscopic assay to identify inhibitors of NADPH oxidase 1 (NOX1): Inhibition of invadopodia formationother Late stage microscopic assay (Invadopodia inhibition)
434997Luminescence-based cell-based dose response assay to identify inhibitors of NADPH oxidase 1 (NOX1): Cherry picks 2confirmatory Dose response (NOX1 inhibitors, cherry picks 2)
435002Late stage results from the probe development effort to identify inhibitors of NOX1: HEK/293 IC50 Set 2confirmatory Late stage dose response (NOX1 inhibitors, HEK/293 cells set 2)
435009Late stage results from the probe development effort to identify inhibitors of (NADPH oxidase 1) NOX1: Xanthine Oxidase Set 2confirmatory Late stage dose response (NOX1 inhibitors, xanthine oxidase set 2)
435013Late stage results from the probe development effort to identify inhibitors of (NADPH oxidase 1) NOX1: Family selectivity: Set 2confirmatory Late stage dose response (NOX1 inhibitors, family selectivity set 2)
463255Late-stage luminescence-based cell-based dose response assay to identify inhibitors of NADPH oxidase 1 (NOX1): Cytotoxicity assay 2confirmatory Late stage dose response counterscreen (Cytotoxicity assay 2)
488778Late-stage microscopic assay to identify inhibitors of NADPH oxidase 1 (NOX1): Inhibition of extracellular matrix degradationother Late stage (ECM degradation inhibitors)
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_SET 2

Name: Late-stage radioligand binding assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen Set 2

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, powders, 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
12Adrenergic receptor Alpha1A1Adrenergic, alpha-1A-, receptor [Homo sapiens] [gi:66267329]
Taxonomy id: 9606
Gene id: 148
13Adrenergic receptor Alpha1B1Adrenergic, alpha-1B-, receptor [Homo sapiens] [gi:187953275]
Taxonomy id: 9606
Gene id: 147
14Adrenergic receptor Alpha1D1adrenergic, alpha-1D-, receptor [Homo sapiens] [gi:119630860]
Taxonomy id: 9606
Gene id: 146
15Adrenergic receptor Beta11adrenergic, beta-1-, receptor [Homo sapiens] [gi:166706747]
Taxonomy id: 9606
Gene id: 153
16Adrenergic receptor Beta21beta 2 adrenergic receptor [Homo sapiens] [gi:22658465]
Taxonomy id: 9606
Gene id: 154
17Adrenergic receptor Beta31adrenergic, beta-3-, receptor [Homo sapiens] [gi:68248548]
Taxonomy id: 9606
Gene id: 155
18BZP Rat Brain Site1Taxonomy id: 10116
19Dopamine receptor D11Dopamine receptor D1 [Homo sapiens] [gi:67677841]
Taxonomy id: 9606
Gene id: 1812
20Dopamine receptor D21Dopamine receptor D2 [Homo sapiens] [gi:18203703]
Taxonomy id: 9606
Gene id: 1813
21Dopamine receptor D31Dopamine receptor D3 [Homo sapiens] [gi:118764187]
Taxonomy id: 9606
Gene id: 1814
22Dopamine receptor D41dopamine receptor D4 [Homo sapiens] [gi:166714265]
Taxonomy id: 9606
Gene id: 1815
23Dopamine receptor D51dopamine receptor D5 [Homo sapiens] [gi:119613085]
Taxonomy id: 9606
Gene id: 1816
24Biogenic amine transporter DAT1dopamine transporter [Homo sapiens] [gi:139522363]
Taxonomy id: 9606
Gene id: 6531
25Opioid receptor DOR1delta-type opioid receptor [Homo sapiens] [gi:63477962]
Taxonomy id: 9606
Gene id: 4985
26GABA receptor GABAa1gamma-aminobutyric acid receptor type A rho-1 subunit [Homo sapiens] [gi:182911]
Taxonomy id: 9606
Gene id: 2569
27Histamine receptor H11histamine H1 receptor [Homo sapiens] [gi:149158709]
Taxonomy id: 9606
Gene id: 3269
28Histamine receptor H21histamine receptor H2 [Homo sapiens] [gi:197692667]
Taxonomy id: 9606
Gene id: 3274
29Histamine receptor H31histamine H3 receptor [Homo sapiens] [gi:194018562]
Taxonomy id: 9606
Gene id: 11255
30Histamine receptor H41histamine H4 receptor [Homo sapiens] [gi:167887581]
Taxonomy id: 9606
Gene id: 59340
31Opioid receptor KOR1kappa opioid receptor [Homo sapiens] [gi:39986053]
Taxonomy id: 9606
Gene id: 4986
32Muscarinic receptor M11Cholinergic receptor, muscarinic 1 [gi:74754970]
Taxonomy id: 9606
Gene id: 1128
33Muscarinic receptor M21cholinergic receptor, muscarinic 2 [Homo sapiens] [gi:119604271]
Taxonomy id: 9606
Gene id: 1129
34Muscarinic receptor M31Cholinergic receptor, muscarinic 3 [Homo sapiens] [gi:111306506]
Taxonomy id: 9606
Gene id: 1131
35Muscarinic receptor M41Cholinergic receptor, muscarinic 4 [Homo sapiens] [gi:187953629]
Taxonomy id: 9606
Gene id: 1132
36Muscarinic receptor M51Cholinergic receptor, muscarinic 5 [gi:74759612]
Taxonomy id: 9606
Gene id: 1133
37Opioid receptor MOR1Mu opioid receptor [gi:74758917]
Taxonomy id: 9606
Gene id: 4988
38Biogenic amine transporter NET1Net [Homo sapiens] [gi:531523]
Taxonomy id: 9606
Gene id: 2004
39Biogenic amine transporter SERT1serotonin transporter [Homo sapiens] [gi:58700442]
Taxonomy id: 9606
Gene id: 6532
40Sigma receptor 11opioid receptor, sigma 1 [Homo sapiens] [gi:123231939]
Taxonomy id: 9606
Gene id: 10280
41Sigma receptor 21Taxonomy id: 9606

§ 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 57287864 displays affinity.

Protocol Summary:

Test and reference compounds are diluted to 5X final assay concentration (50 uM for a final assay concentration of 10 uM) in the appropriate radioligand binding buffer. Then, 50 uL 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 uL of 5X radioligand and 100 uL of buffer. Finally, receptor-containing, crude membrane fractions are resuspended in an appropriate volume of buffer and dispensed (50 mul 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 substance SID 57287864 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 uM 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 activator 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 activator 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 activator 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 activator 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 activator 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 activator 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 activator 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 activator 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 activator 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 activator 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 activator 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
23Adrenergic Alpha1A (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.12Adrenergic, alpha-1A-, receptor [Homo sapiens]Float%
24Adrenergic Alpha1A (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.12Outcome
25Adrenergic Alpha1B (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.13Adrenergic, alpha-1B-, receptor [Homo sapiens]Float%
26Adrenergic Alpha1B (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.13Outcome
27Adrenergic Alpha1D (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.14adrenergic, alpha-1D-, receptor [Homo sapiens]Float%
28Adrenergic Alpha1D (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.14Outcome
29Adrenergic Beta1 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.15adrenergic, beta-1-, receptor [Homo sapiens]Float%
30Adrenergic Beta1 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.15Outcome
31Adrenergic Beta2 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.16beta 2 adrenergic receptor [Homo sapiens]Float%
32Adrenergic Beta2 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.16Outcome
33Adrenergic Beta3 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.17adrenergic, beta-3-, receptor [Homo sapiens]Float%
34Adrenergic Beta3 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.17Outcome
35BZP Rat Brain Site (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.18Float%
36BZP Rat Brain Site (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.18Outcome
37Dopamine D1 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.19Dopamine receptor D1 [Homo sapiens]Float%
38Dopamine D1 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.19Outcome
39Dopamine D2 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.20Dopamine receptor D2 [Homo sapiens]Float%
40Dopamine D2 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.20Outcome
41Dopamine D3 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.21Dopamine receptor D3 [Homo sapiens]Float%
42Dopamine D3 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.21Outcome
43Dopamine D4 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.22dopamine receptor D4 [Homo sapiens]Float%
44Dopamine D4 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.22Outcome
45Dopamine D5 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.23dopamine receptor D5 [Homo sapiens]Float%
46Dopamine D5 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.23Outcome
47Biogenic amine transporter DAT (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.24dopamine transporter [Homo sapiens]Float%
48Biogenic amine transporter DAT (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.24Outcome
49Opioid DOR (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.25delta-type opioid receptor [Homo sapiens]Float%
50Opioid DOR (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.25Outcome
51GABA GABAa (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.26gamma-aminobutyric acid receptor type A rho-1 subunit [Homo sapiens]Float%
52GABA GABAa (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.26Outcome
53Histamine H1 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.27histamine H1 receptor [Homo sapiens]Float%
54Histamine H1 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.27Outcome
55Histamine H2 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.28histamine receptor H2 [Homo sapiens]Float%
56Histamine H2 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.28Outcome
57Histamine H3 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.29histamine H3 receptor [Homo sapiens]Float%
58Histamine H3 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.29Outcome
59Histamine H4 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.30histamine H4 receptor [Homo sapiens]Float%
60Histamine H4 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.30Outcome
61Opioid KOR (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.31kappa opioid receptor [Homo sapiens]Float%
62Opioid KOR (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.31Outcome
63Muscarinic M1 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.32Cholinergic receptor, muscarinic 1Float%
64Muscarinic M1 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.32Outcome
65Muscarinic M2 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.33cholinergic receptor, muscarinic 2 [Homo sapiens]Float%
66Muscarinic M2 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.33Outcome
67Muscarinic M3 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.34Cholinergic receptor, muscarinic 3 [Homo sapiens]Float%
68Muscarinic M3 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.34Outcome
69Muscarinic M4 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.35Cholinergic receptor, muscarinic 4 [Homo sapiens]Float%
70Muscarinic M4 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.35Outcome
71Muscarinic M5 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.36Cholinergic receptor, muscarinic 5Float%
72Muscarinic M5 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.36Outcome
73Opioid MOR (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.37Mu opioid receptorFloat%
74Opioid MOR (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.37Outcome
75Biogenic amine transporter NET (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.38Net [Homo sapiens]Float%
76Biogenic amine transporter NET (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.38Outcome
77Biogenic amine transporter SERT (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.39serotonin transporter [Homo sapiens]Float%
78Biogenic amine transporter SERT (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.39Outcome
79Sigma 1 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.40opioid receptor, sigma 1 [Homo sapiens]Float%
80Sigma 1 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.40Outcome
81Sigma 2 (Inhibition) (10μM**)Value of % Inhibition at 10 uM activator concentration; average of four measurements.41Float%
82Sigma 2 (Outcome)The Assay outcome, one of Active, Inactive or Not Tested.41Outcome

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

Classification
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