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BioAssay: AID 652084

Late-stage results from the probe development effort to identify antagonists of OPRK1: fluorescence-based cell-based dose response assay, Set 2.

Name: Late-stage results from the probe development effort to identify antagonists of OPRK1: fluorescence-based cell-based dose response assay, Set 2. ..more
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 Tested Compounds
 Tested Compounds
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Active(1)
 
 
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 Tested Substances
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Active(1)
 
 
AID: 652084
Data Source: The Scripps Research Institute Molecular Screening Center (OPRK1_ANT_FRET_384_4XIC50_SET2)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2013-03-05
Hold-until Date: 2013-10-21
Modify Date: 2013-10-21

Data Table ( Complete ):           View Active Data    View All Data
Target
BioActive Compound: 1
Related Experiments
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AIDNameTypeComment
652031Maybridge screen to identify antagonists of kappa opioid receptor 1 (OPRK1): fluorescence-based cell-based assayScreeningdepositor-specified cross reference: Maybridge screen (OPRK1 inhibitors in singlicate)
652032Late-stage results from the probe development effort to identify antagonists of OPRK1: fluorescence-based cell-based dose response assayConfirmatorydepositor-specified cross reference: Late-stage dose response (OPRK1 antagonists in quadruplicate)
652033Late-stage results from the probe development effort to identify antagonists of OPRK1: fluorescence-based cell-based dose response OPRD1 counterscreenConfirmatorydepositor-specified cross reference: Late-stage dose response counterscreen (OPRD1 antagonists in quadruplicate)
652034Late-stage results from the probe development effort to identify antagonists of OPRK1: luminescence-based cell-based dose response OPRM1 counterscreenConfirmatorydepositor-specified cross reference: Late-stage dose response counterscreen (OPRM1 antagonists in quadruplicate)
652045Summary of the probe development efforts to identify antagonists of the kappa 1 (OPRK1) opioid receptorSummarydepositor-specified cross reference: Summary (OPRK1 antagonists)
652108Late-stage results from the probe development effort to identify antagonists of OPRK1: In vivo tail flick assayOtherdepositor-specified cross reference
652075Late-stage results from the probe development effort to identify antagonists of OPRK1: radiometric-based biochemical hERG counterscreen assayOthersame project related to Summary assay
652076Late-stage results from the probe development effort to identify antagonists of OPRK1: LCMS-based biochemical cytochrome P450 inhibition assayOthersame project related to Summary assay
652077Late-stage fluorescence-based cell-based dose response assay for antagonists of kappa opioid receptor 1 (OPRK1)Confirmatorysame project related to Summary assay
652078Late-stage results from the probe development effort to identify antagonists of OPRK1: LCMS-based pharmacokinetic plasma protein binding assayOthersame project related to Summary assay
652079Late-stage counterscreen for antagonists of kappa opioid receptor 1 (OPRK1): fluorescence-based cell-based dose response assay to identify antagonists of Sphingosine 1-Phosphate Receptor 1 (S1P1)Confirmatorysame project related to Summary assay
652080Late-stage results from the probe development effort to identify antagonists of OPRK1: fluorescence-based cell-based dose response OPRD1 counterscreen, Set 2Confirmatorysame project related to Summary assay
652081Late-stage results from the probe development effort to identify antagonists of OPRK1: luminescence-based cell-based dose response OPRM1 counterscreen, Set 2Confirmatorysame project related to Summary assay
652082Fluorescence-based cell-based confirmation assay for antagonists of kappa opioid receptor 1 (OPRK1)Othersame project related to Summary assay
652083Late-stage results from the probe development effort to identify antagonists of OPRK1: CEREP radiometric-based biochemical counterscreen panel assayOthersame project related to Summary assay
652085Late-stage results from the probe development effort to identify antagonists of OPRK1: LCMS-based in vivo plasma and brain levelsOthersame project related to Summary assay
652086Late-stage results from the probe development effort to identify antagonists of OPRK1: luminescence-based cell-based dose response counterscreen assay to determine cytotoxicity of test compoundsConfirmatorysame project related to Summary assay
652087Counterscreen for antagonists of kappa opioid receptor 1 (OPRK1): fluorescence-based cell-based assay to identify antagonists of Sphingosine 1-Phosphate Receptor 1 (S1P1)Othersame project related to Summary assay
652088Late-stage results from the probe development effort to identify antagonists of OPRK1: LCMS-based biochemical hepatic microsome stability assayOthersame project related to Summary assay
652113Late-stage results from the probe development effort to identify antagonists of OPRK1: LCMS-based parallel artificial membrane permeability (PAMPA) assayOthersame project related to Summary assay
Description:
Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC)
Affiliation: The Scripps Research Institute, TSRI
Assay Provider: Lakshmi A. Devi, Mount Sinai School of Medicine
Network: Molecular Library Probe Production Centers Network (MLPCN)
Grant Proposal Number: R03NS053751
Grant Proposal PI: Lakshmi A. Devi, Mount Sinai School of Medicine
External Assay ID: OPRK1_ANT_FRET_384_4XIC50_SET2

Name: Late-stage results from the probe development effort to identify antagonists of OPRK1: fluorescence-based cell-based dose response assay, Set 2.

Description:

Potent and selective OPRK antagonists will be useful for studying the mechanisms involved in OPRK-mediated analgesia and may have therapeutic value as novel analgesics with an improved side effect profile to currently available drugs. Studies have identified a role for dynorphin and OPRK stimulation in neuropathic pain (1). The dynorphins act as endogenous agonists at the opioid receptors, including OPRK (2), and the increased dynorphin expression in neuropathic pain also leads to a sustained activation of OPRK (1, 3). The mechanisms and neural circuits in OPRK-mediated analgesia are active areas of study; it is hoped those studies will assist in the development of novel analgesics that bypass OPRK-mediated depression (4-5). A role for dynorphin/OPRK in modulating drug addiction has been proposed (for review, see (6-7)). The function of dynorphin/OPRK systems in addiction appears to be diverse, and may modulate drug-seeking behavior depending on factors such as drug history, pattern of intake, and stress (for review, see (6)). The availability of potent and selective OPRK ligands may help unravel these mechanisms, as well as prove to be of therapeutic utility. Evidence from preclinical studies indicates that the dynorphin/OPRK system may be dysregulated in affective psychiatric disorders (for review, see (6, 8)). However, solid evidence from clinical studies is lacking. There is increasing evidence for a potential involvement of dynorphin/OPRK in schizophrenia; OPRK agonists appear to induce symptoms in humans and animals that are present in schizophrenia (8-10). Thus, the availability of new research tools such as potent and selective OPRK antagonists will facilitate understanding the physiological and pathophysiological mechanisms of dynorphin/OPRK systems and their roles in psychiatric disease in humans.

References:

1. Xu, M., et al., Neuropathic pain activates the endogenous kappa opioid system in mouse spinal cord and induces opioid receptor tolerance. J Neurosci, 2004. 24(19): p. 4576-84.
2. Chavkin, C., I.F. James, and A. Goldstein, Dynorphin is a specific endogenous ligand of the kappa opioid receptor. Science, 1982. 215(4531): p. 413-5.
3. Xu, M., et al., Sciatic nerve ligation-induced proliferation of spinal cord astrocytes is mediated by kappa opioid activation of p38 mitogen-activated protein kinase. J Neurosci, 2007. 27(10): p. 2570-81.
4. Al-Hasani, R. and M.R. Bruchas, Molecular mechanisms of opioid receptor-dependent signaling and behavior. Anesthesiology, 2011. 115(6): p. 1363-81.
5. Muschamp, J.W., A. Van't Veer, and W.A. Carlezon, Jr., Tracking down the molecular substrates of stress: new roles for p38alpha MAPK and kappa-opioid receptors. Neuron, 2011. 71(3): p. 383-5.
6. Tejeda, H.A., T.S. Shippenberg, and R. Henriksson, The dynorphin/kappa-opioid receptor system and its role in psychiatric disorders. Cell Mol Life Sci, 2012. 69(6): p. 857-96.
7. Yoo, J.H., I. Kitchen, and A. Bailey, The endogenous opioid system in cocaine addiction: what lessons have opioid peptide and receptor knockout mice taught us? Br J Pharmacol, 2012. 166(7): p. 1993-2014.
8. Schwarzer, C., 30 years of dynorphins--new insights on their functions in neuropsychiatric diseases. Pharmacol Ther, 2009. 123(3): p. 353-70.
9. Bortolato, M. and M.V. Solbrig, The price of seizure control: dynorphins in interictal and postictal psychosis. Psychiatry Res, 2007. 151(1-2): p. 139-43.
10. Sheffler, D.J. and B.L. Roth, Salvinorin A: the "magic mint" hallucinogen finds a molecular target in the kappa opioid receptor. Trends Pharmacol Sci, 2003. 24(3): p. 107-9.

Keywords:

Late stage, late stage AID, OPRK1, kappa, opioid, receptor, GPCR, beta-arrestin, U2OS, Tango trade mark, beta-lactamase, FRET, FRET-enabled substrate, TEV, TEV protease, beta-arrestin, EC80 challenge, SNC80, antagonist, inhibitor, inhibit, pain, analgesic, dynorphin, neuropathic pain, drug addiction, addiction, 384, Scripps, The Scripps Research Institute Molecular Screening Center, SRIMSC, Molecular Libraries Probe Production Centers Network, MLPCN.
Protocol
Assay Overview:

The purpose of this assay is to confirm the potency of test synthesized compounds. This assay uses Tango OPRK1-bla U2OS cells which express OPRK1 linked to a GAL4-VP16 transcription factor via a TEV protease site. The cells also express a Beta-arrestin/TEV protease fusion protein and a Beta-lactamase (BLA) reporter gene under the control of a UAS response element. Stimulation of the OPRK1 receptor by agonist causes migration of the Beta-arrestin fusion protein to the GPCR, and through proteolysis liberates GAL4-VP16 from the receptor. The liberated VP16-GAL4 migrates to the nucleus, where it induces transcription of the BLA gene. BLA expression is monitored by measuring fluorescence resonance energy transfer (FRET) of a cleavable, fluorogenic, cell-permeable BLA substrate. As designed, test compounds that act as OPRK1 antagonists will inhibit agonist activation and migration of the fusion protein, thus preventing proteolysis of GAL4-VP16 and BLA transcription, leading to no increase in well FRET. Compounds were tested in either quadulplicat or octuplet using a 12-point, 1:3 dilution series starting at a nominal concentration of 10 uM.

Protocol Summary:

The Tango OPRK1-U20S dividing cell line was routinely cultured in 150 mm dishes at 37 C, 5% CO2 and 95% relative humidity (RH). The growth medium consisted of McCoys 5A Media supplemented with 10% v/v dialyzed fetal bovine serum, 25 mM HEPES, 0.1 mM non-essential amino acids, 1 mM sodium pyruvate, and 1X antibiotic mix (penicillin streptomycin). On day 1 of the assay, 16,000 cells in 10 uL of assay media (DMEM-Glutamax with sodium pyruvate, 10% fetal bovine serum stripped with charcoal-dextran, 25 mM HEPES, 0.1 mM non-essential amino acids, and antibiotic mix (penicillin streptomycin) were seeded into each well of a 384-well plate. On Day 2, 50 nl of test compound in DMSO were added to the appropriate wells and plates were incubated for 30 minutes at 37 C, 5% CO2 and 95% RH. Next, 0.6 uL of 111 nM U50488 OPRK1 Agonist (EC80 Challenge; final concentration 6 nM) or DMSO in assay medium was added to appropriate wells and incubated 4 hours at 37 C, 5% CO2 and 95% RH. 2.5 uL of LiveBLazer trade mark FRET B/G (CCF4-AM) loading mix (prepared according to manufacturer's instructions; 6 uL solution A, 60 uL Solution B, 904 uL Solution C, and 30 uL Solution D) were added to each well, and plates incubated at room temperature in the dark for 2 hours. Well fluorescence was measured on Perkin Elmer's Envision using an Excitation filter 409 nm, Emission filters at 460 nm and 590 nm, bottom read.

Percent Inhibition was calculated from the median ratio as follows:

%_Inhibition = 1 - ( ( FI_Test_Compound - Median_FI_HighControl ) / ( Median_FI_Low_Control - Median_FI_High_Control ) ) * 100

Where:

FI is defined as Fluorescence Intensity at 460 nm/Fluorescence Intensity at 530 nm.
Test_Compound is defined as wells containing test compound.
Low_Control (0% inhibition) is defined as wells containing U50488 EC80 challenge
High Control (100% inhibition) is defined as wells containing DMSO.

For each test compound, percent inhibition was plotted against the log of the compound concentration. A three parameter equation describing a sigmoidal dose-response curve was then fitted using GraphPad Prism (GraphPad Software Inc) normalized from 0 to 100 for each assay. The software-generated IC50 values were reported. In cases where the highest concentration tested (i.e. 50 uM) did not result in greater than 50% inhibition, the IC50 was determined manually as greater than 50 uM.

PubChem Activity Outcome and Score:

Compounds with an IC50 of 10 uM or less were considered active. Compounds with an IC50 of greater than 10 uM were considered inactive.

Any compound with a percent activity value < 50% at all test concentrations was assigned an activity score of zero. Any compound with a percent activity value >= 50% at any test concentration was assigned an activity score greater than zero.

Activity score was then ranked by the potency of the compounds with fitted curves, with the most potent compounds assigned the highest activity scores.

The PubChem Activity Score range for active compounds is 100-100. There are no inactive compounds.

List of Reagents:

Tango trade mark OPRK1-bla U20S Cells (Invitrogen K1576)
McCoy's 5A Medium, (Invitrogen, part 16600-082)
Dialyzed Fetal Bovine Serum, (Invitrogen, part 26400-036)
Non Essential Amino Acids 100X (Invitrogen, part 11140-050)
HEPES (pH 7.3) 1M, (Invitrogen, part 15630-080)
Sodium Pyruvate 100X (Invitrogen, part 11360-070)
Penicillin Streptomycin, (Invitrogen, part 15640)
Trypsin 0.25% EDTA (Invitrogen, part 25200056)
DPBS without Calcium /Magnesium (Invitrogen, part 14190-136)
DMEM, High Glucose,GlutaMAX (Invitrogen, part 10569-010)
Fetal Bovine Serum, Charcoal Stripped (Invitrogen, part 12676-011)
DMSO Dry (Sigma, part D2650)
U50488 OPRK1 Agonist MW410.29 (Tocris 67198-19-0)
GNTI dihydrochloride OPRK1 Antagonist MW571.5 (Tocris 1282)
Nor-Binaltorphimine dihydrochloride MW770.75 (Tocris 0347)
384 black low profile, clear bottom, low volume plate (Greiner, part 788092)
Low profile plate lids (Greiner, part 656190)
LiveBLAzer trade mark-FRET/BG Loading Mix (Invitrogen, part K1030
Comment
This assay was performed by the SRIMSC with powder samples of synthesized test compounds.
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay: CurveFit [1]: Equation: = [Baseline Response] + ( [Maximal Response] - [Baseline Response] ) / ( 1 + 10 ^ ( ( [LogEC50] - Log( [Concentration] * 10^-6) ) * [Hill Slope] ) )
Assay: Dictionary: Version: 0.1
From PubChem:
Assay Format: Cell-based
Assay Cell Type: U-2 OS
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1IC50*The concentration at which 50 percent of the activity in the antagonist assay is observed; (IC50) shown in nanomolar.FloatμM
2Log IC50The Log of IC50Float
3Hill SlopeThe Hill SlopeFloat
4Maximal ResponseThe maximal or asymptotic response above the baseline as concentration increases without bound.Float
5Baseline ResponseAdjustable baseline of the curve fit, minimal response value.Float
6R squaredThe value of R squaredFloat
7Inhibition at 10 uM [1] (10μM**)Value of % inhibition at 10 uM compound concentration; replicate [1]Float%
8Inhibition at 10 uM [2] (10μM**)Value of % inhibition at 10 uM compound concentration; replicate [2]Float%
9Inhibition at 10 uM [3] (10μM**)Value of % inhibition at 10 uM compound concentration; replicate [3]Float%
10Inhibition at 10 uM [4] (10μM**)Value of % inhibition at 10 uM compound concentration; replicate [4]Float%
11Inhibition at 10 uM [5] (10μM**)Value of % inhibition at 10 uM compound concentration; replicate [5]Float%
12Inhibition at 10 uM [6] (10μM**)Value of % inhibition at 10 uM compound concentration; replicate [6]Float%
13Inhibition at 10 uM [7] (10μM**)Value of % inhibition at 10 uM compound concentration; replicate [7]Float%
14Inhibition at 10 uM [8] (10μM**)Value of % inhibition at 10 uM compound concentration; replicate [8]Float%
15Inhibition at 3.33 uM [1] (3.33μM**)Value of % inhibition at 3.33 uM compound concentration; replicate [1]Float%
16Inhibition at 3.33 uM [2] (3.33μM**)Value of % inhibition at 3.33 uM compound concentration; replicate [2]Float%
17Inhibition at 3.33 uM [3] (3.33μM**)Value of % inhibition at 3.33 uM compound concentration; replicate [3]Float%
18Inhibition at 3.33 uM [4] (3.33μM**)Value of % inhibition at 3.33 uM compound concentration; replicate [4]Float%
19Inhibition at 3.33 uM [5] (3.33μM**)Value of % inhibition at 3.33 uM compound concentration; replicate [5]Float%
20Inhibition at 3.33 uM [6] (3.33μM**)Value of % inhibition at 3.33 uM compound concentration; replicate [6]Float%
21Inhibition at 3.33 uM [7] (3.33μM**)Value of % inhibition at 3.33 uM compound concentration; replicate [7]Float%
22Inhibition at 3.33 uM [8] (3.33μM**)Value of % inhibition at 3.33 uM compound concentration; replicate [8]Float%
23Inhibition at 1.11 uM [1] (1.11μM**)Value of % inhibition at 1.11 uM compound concentration; replicate [1]Float%
24Inhibition at 1.11 uM [2] (1.11μM**)Value of % inhibition at 1.11 uM compound concentration; replicate [2]Float%
25Inhibition at 1.11 uM [3] (1.11μM**)Value of % inhibition at 1.11 uM compound concentration; replicate [3]Float%
26Inhibition at 1.11 uM [4] (1.11μM**)Value of % inhibition at 1.11 uM compound concentration; replicate [4]Float%
27Inhibition at 1.11 uM [5] (1.11μM**)Value of % inhibition at 1.11 uM compound concentration; replicate [5]Float%
28Inhibition at 1.11 uM [6] (1.11μM**)Value of % inhibition at 1.11 uM compound concentration; replicate [6]Float%
29Inhibition at 1.11 uM [7] (1.11μM**)Value of % inhibition at 1.11 uM compound concentration; replicate [7]Float%
30Inhibition at 1.11 uM [8] (1.11μM**)Value of % inhibition at 1.11 uM compound concentration; replicate [8]Float%
31Inhibition at 0.37 uM [1] (0.37μM**)Value of % inhibition at 0.37 uM compound concentration; replicate [1]Float%
32Inhibition at 0.37 uM [2] (0.37μM**)Value of % inhibition at 0.37 uM compound concentration; replicate [2]Float%
33Inhibition at 0.37 uM [3] (0.37μM**)Value of % inhibition at 0.37 uM compound concentration; replicate [3]Float%
34Inhibition at 0.37 uM [4] (0.37μM**)Value of % inhibition at 0.37 uM compound concentration; replicate [4]Float%
35Inhibition at 0.37 uM [5] (0.37μM**)Value of % inhibition at 0.37 uM compound concentration; replicate [5]Float%
36Inhibition at 0.37 uM [6] (0.37μM**)Value of % inhibition at 0.37 uM compound concentration; replicate [6]Float%
37Inhibition at 0.37 uM [7] (0.37μM**)Value of % inhibition at 0.37 uM compound concentration; replicate [7]Float%
38Inhibition at 0.37 uM [8] (0.37μM**)Value of % inhibition at 0.37 uM compound concentration; replicate [8]Float%
39Inhibition at 0.123 uM [1] (0.123μM**)Value of % inhibition at 0.123 uM compound concentration; replicate [1]Float%
40Inhibition at 0.123 uM [2] (0.123μM**)Value of % inhibition at 0.123 uM compound concentration; replicate [2]Float%
41Inhibition at 0.123 uM [3] (0.123μM**)Value of % inhibition at 0.123 uM compound concentration; replicate [3]Float%
42Inhibition at 0.123 uM [4] (0.123μM**)Value of % inhibition at 0.123 uM compound concentration; replicate [4]Float%
43Inhibition at 0.123 uM [5] (0.123μM**)Value of % inhibition at 0.123 uM compound concentration; replicate [5]Float%
44Inhibition at 0.123 uM [6] (0.123μM**)Value of % inhibition at 0.123 uM compound concentration; replicate [6]Float%
45Inhibition at 0.123 uM [7] (0.123μM**)Value of % inhibition at 0.123 uM compound concentration; replicate [7]Float%
46Inhibition at 0.123 uM [8] (0.123μM**)Value of % inhibition at 0.123 uM compound concentration; replicate [8]Float%
47Inhibition at 0.0411 uM [1] (0.0411μM**)Value of % inhibition at 0.0411 uM compound concentration; replicate [1]Float%
48Inhibition at 0.0411 uM [2] (0.0411μM**)Value of % inhibition at 0.0411 uM compound concentration; replicate [2]Float%
49Inhibition at 0.0411 uM [3] (0.0411μM**)Value of % inhibition at 0.0411 uM compound concentration; replicate [3]Float%
50Inhibition at 0.0411 uM [4] (0.0411μM**)Value of % inhibition at 0.0411 uM compound concentration; replicate [4]Float%
51Inhibition at 0.0411 uM [5] (0.0411μM**)Value of % inhibition at 0.0411 uM compound concentration; replicate [5]Float%
52Inhibition at 0.0411 uM [6] (0.0411μM**)Value of % inhibition at 0.0411 uM compound concentration; replicate [6]Float%
53Inhibition at 0.0411 uM [7] (0.0411μM**)Value of % inhibition at 0.0411 uM compound concentration; replicate [7]Float%
54Inhibition at 0.0411 uM [8] (0.0411μM**)Value of % inhibition at 0.0411 uM compound concentration; replicate [8]Float%
55Inhibition at 0.0137 uM [1] (0.0137μM**)Value of % inhibition at 0.0137 uM compound concentration; replicate [1]Float%
56Inhibition at 0.0137 uM [2] (0.0137μM**)Value of % inhibition at 0.0137 uM compound concentration; replicate [2]Float%
57Inhibition at 0.0137 uM [3] (0.0137μM**)Value of % inhibition at 0.0137 uM compound concentration; replicate [3]Float%
58Inhibition at 0.0137 uM [4] (0.0137μM**)Value of % inhibition at 0.0137 uM compound concentration; replicate [4]Float%
59Inhibition at 0.0137 uM [5] (0.0137μM**)Value of % inhibition at 0.0137 uM compound concentration; replicate [5]Float%
60Inhibition at 0.0137 uM [6] (0.0137μM**)Value of % inhibition at 0.0137 uM compound concentration; replicate [6]Float%
61Inhibition at 0.0137 uM [7] (0.0137μM**)Value of % inhibition at 0.0137 uM compound concentration; replicate [7]Float%
62Inhibition at 0.0137 uM [8] (0.0137μM**)Value of % inhibition at 0.0137 uM compound concentration; replicate [8]Float%
63Inhibition at 0.00457 uM [1] (0.00457μM**)Value of % inhibition at 0.00457 uM compound concentration; replicate [1]Float%
64Inhibition at 0.00457 uM [2] (0.00457μM**)Value of % inhibition at 0.00457 uM compound concentration; replicate [2]Float%
65Inhibition at 0.00457 uM [3] (0.00457μM**)Value of % inhibition at 0.00457 uM compound concentration; replicate [3]Float%
66Inhibition at 0.00457 uM [4] (0.00457μM**)Value of % inhibition at 0.00457 uM compound concentration; replicate [4]Float%
67Inhibition at 0.00457 uM [5] (0.00457μM**)Value of % inhibition at 0.00457 uM compound concentration; replicate [5]Float%
68Inhibition at 0.00457 uM [6] (0.00457μM**)Value of % inhibition at 0.00457 uM compound concentration; replicate [6]Float%
69Inhibition at 0.00457 uM [7] (0.00457μM**)Value of % inhibition at 0.00457 uM compound concentration; replicate [7]Float%
70Inhibition at 0.00457 uM [8] (0.00457μM**)Value of % inhibition at 0.00457 uM compound concentration; replicate [8]Float%
71Inhibition at 0.00152 uM [1] (0.00152μM**)Value of % inhibition at 0.00152 uM compound concentration; replicate [1]Float%
72Inhibition at 0.00152 uM [2] (0.00152μM**)Value of % inhibition at 0.00152 uM compound concentration; replicate [2]Float%
73Inhibition at 0.00152 uM [3] (0.00152μM**)Value of % inhibition at 0.00152 uM compound concentration; replicate [3]Float%
74Inhibition at 0.00152 uM [4] (0.00152μM**)Value of % inhibition at 0.00152 uM compound concentration; replicate [4]Float%
75Inhibition at 0.00152 uM [5] (0.00152μM**)Value of % inhibition at 0.00152 uM compound concentration; replicate [5]Float%
76Inhibition at 0.00152 uM [6] (0.00152μM**)Value of % inhibition at 0.00152 uM compound concentration; replicate [6]Float%
77Inhibition at 0.00152 uM [7] (0.00152μM**)Value of % inhibition at 0.00152 uM compound concentration; replicate [7]Float%
78Inhibition at 0.00152 uM [8] (0.00152μM**)Value of % inhibition at 0.00152 uM compound concentration; replicate [8]Float%
79Inhibition at 0.000508 uM [1] (0.000508μM**)Value of % inhibition at 0.000508 uM compound concentration; replicate [1]Float%
80Inhibition at 0.000508 uM [2] (0.000508μM**)Value of % inhibition at 0.000508 uM compound concentration; replicate [2]Float%
81Inhibition at 0.000508 uM [3] (0.000508μM**)Value of % inhibition at 0.000508 uM compound concentration; replicate [3]Float%
82Inhibition at 0.000508 uM [4] (0.000508μM**)Value of % inhibition at 0.000508 uM compound concentration; replicate [4]Float%
83Inhibition at 0.000508 uM [5] (0.000508μM**)Value of % inhibition at 0.000508 uM compound concentration; replicate [5]Float%
84Inhibition at 0.000508 uM [6] (0.000508μM**)Value of % inhibition at 0.000508 uM compound concentration; replicate [6]Float%
85Inhibition at 0.000508 uM [7] (0.000508μM**)Value of % inhibition at 0.000508 uM compound concentration; replicate [7]Float%
86Inhibition at 0.000508 uM [8] (0.000508μM**)Value of % inhibition at 0.000508 uM compound concentration; replicate [8]Float%
87Inhibition at 0.000169 uM [1] (0.000169μM**)Value of % inhibition at 0.000169 uM compound concentration; replicate [1]Float%
88Inhibition at 0.000169 uM [2] (0.000169μM**)Value of % inhibition at 0.000169 uM compound concentration; replicate [2]Float%
89Inhibition at 0.000169 uM [3] (0.000169μM**)Value of % inhibition at 0.000169 uM compound concentration; replicate [3]Float%
90Inhibition at 0.000169 uM [4] (0.000169μM**)Value of % inhibition at 0.000169 uM compound concentration; replicate [4]Float%
91Inhibition at 0.000169 uM [5] (0.000169μM**)Value of % inhibition at 0.000169 uM compound concentration; replicate [5]Float%
92Inhibition at 0.000169 uM [6] (0.000169μM**)Value of % inhibition at 0.000169 uM compound concentration; replicate [6]Float%
93Inhibition at 0.000169 uM [7] (0.000169μM**)Value of % inhibition at 0.000169 uM compound concentration; replicate [7]Float%
94Inhibition at 0.000169 uM [8] (0.000169μM**)Value of % inhibition at 0.000169 uM compound concentration; replicate [8]Float%
95Inhibition at 0.0000565 uM [1] (5.65e-05μM**)Value of % inhibition at 0.0000565 uM compound concentration; replicate [1]Float%
96Inhibition at 0.0000565 uM [2] (5.65e-05μM**)Value of % inhibition at 0.0000565 uM compound concentration; replicate [2]Float%
97Inhibition at 0.0000565 uM [3] (5.65e-05μM**)Value of % inhibition at 0.0000565 uM compound concentration; replicate [3]Float%
98Inhibition at 0.0000565 uM [4] (5.65e-05μM**)Value of % inhibition at 0.0000565 uM compound concentration; replicate [4]Float%
99Inhibition at 0.0000565 uM [5] (5.65e-05μM**)Value of % inhibition at 0.0000565 uM compound concentration; replicate [5]Float%
100Inhibition at 0.0000565 uM [6] (5.65e-05μM**)Value of % inhibition at 0.0000565 uM compound concentration; replicate [6]Float%
101Inhibition at 0.0000565 uM [7] (5.65e-05μM**)Value of % inhibition at 0.0000565 uM compound concentration; replicate [7]Float%
102Inhibition at 0.0000565 uM [8] (5.65e-05μM**)Value of % inhibition at 0.0000565 uM compound concentration; replicate [8]Float%

* Activity Concentration. ** Test Concentration.
Additional Information
Grant Number: R03NS053751

Data Table (Concise)
Data Table ( Complete ):     View Active Data    View All Data
Classification
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