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BioAssay: AID 2182

Modulation of the Metabotropic Glutamate Receptor mGluR4: Selectivity at mGluR7

Screening Center Name & PI: Vanderbilt Screening Center for GPCRs, Ion Channels and Transporters, C. David Weaver ..more
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 Tested Compounds
 Tested Compounds
All(3)
 
 
Active(1)
 
 
Inactive(2)
 
 
 Tested Substances
 Tested Substances
All(3)
 
 
Active(1)
 
 
Inactive(2)
 
 
AID: 2182
Data Source: Vanderbilt Screening Center for GPCRs, Ion Channels and Transporters (mgluR4 PAM at mgluR7)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: NIH Molecular Libraries Screening Center Network
BioAssay Version:
Deposit Date: 2009-12-07
Modify Date: 2010-10-27

Data Table ( Complete ):           View Active Data    View All Data
Target
BioActive Compound: 1
Related Experiments
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AIDNameTypeProbeComment
2437Modulation of the Metabotropic Glutamate Receptor mGluR4Summary1 depositor-specified cross reference
2807Modulation of the Metabotropic Glutamate Receptor mGluR4: Calcium AssayConfirmatory depositor-specified cross reference
2179Modulation of Metabotropic Glutamate Receptor mGluR4: Rat PAM Fold-ShiftConfirmatory same project related to Summary assay
2180Modulation of Metabotropic Glutmate Receptor mGluR4: Human PAM Fold-ShiftConfirmatory same project related to Summary assay
2181Modulation of the Metabotropic Glutamate Receptor mGluR4: Selectivity at mGluR8Confirmatory same project related to Summary assay
2183Modulation of the Metabotropic Glutamate Receptor mGluR4: Selectivity at mGluR4Confirmatory same project related to Summary assay
2185Modulation of the Metabotropic Glutamate Receptor mGluR4: Rat PAM PotencyConfirmatory same project related to Summary assay
2188Modulation of the Metabotropic Glutamate Receptor mGluR4: Selectivity at mGluR2Confirmatory same project related to Summary assay
2190Modulation of the Metabotropic Glutamate Receptor mGluR4: Selectivity at mGluR3Confirmatory same project related to Summary assay
2191Modulation of the Metabotropic Glutamate Receptor mGluR4: Selectivity at mGluR6Confirmatory same project related to Summary assay
2193Modulation of the Metabotropic Glutamate Receptor mGluR4: Selectivity at mGluR1Confirmatory same project related to Summary assay
2197Modulation of the Metabotropic Glutamate Receptor mGluR4: Potency at human mGluR4Confirmatory same project related to Summary assay
2199Modulation of the Metabotropic Glutamate Receptor mGluR4: Selectivity at mGluR5Confirmatory same project related to Summary assay
488971Rat PAM Fold-shift Assay with mGluR4 GIRKConfirmatory same project related to Summary assay
Description:
Assigned Assay Grant Number: NS053536-01
Screening Center Name & PI: Vanderbilt Screening Center for GPCRs, Ion Channels and Transporters, C. David Weaver
Chemistry Center Name & PI: Vanderbilt Specialized Chemistry Center for Accelerated Probe Development, Craig W. Lindsley
Assay Submitter & Institution: Colleen M. Niswender, Vanderbilt University

The primary pathophysiological change giving rise to the symptoms of Parkinson's disease (PD) is a loss of the dopaminergic neurons in the substantia nigra pars compacta (SNc) that are involved in modulating the function of basal ganglia (BG) nuclei. Unfortunately, traditional therapies for treatment of PD based on dopamine replacement strategies eventually fail in most patients and are associated with numerous side effects. A great deal of effort has been focused on developing a detailed understanding of the circuitry and function of the BG to develop novel, nondopaminergic, approaches for restoring normal BG function in PD patients. Exciting advances suggest that metabotropic glutamate receptors (mGluRs), including the group III mGluRs (mGluR4, -7 and -8), play important roles in regulating transmission through the BG and could serve as targets for novel PD therapeutics (Conn et al., 2005). For instance, mGluR4 activation reduces overactive GABA release at a specific inhibitory BG synapse (Macinnes and Duty, 2008; Marino et al., 2003; Valenti et al., 2003) and reverses motor deficits in a variety of rodent PD models (Konieczny et al., 2007; MacInnes et al., 2004; Marino et al., 2003; Ossowska et al., 2007; Valenti et al., 2003).

To more selectively activate mGluR4 and improve upon the pharmacokinetic liabilities of glutamate analogs, we and others have developed novel positive allosteric modulators (PAMs) which potentiate glutamate function at mGluR4 (Engers et al., 2009; Maj et al., 2003; Marino et al., 2003; Niswender et al., 2008a; Niswender et al., 2008b; Williams et al., 2008); several of these tool compounds exhibit antiparkinsonian and neuroprotective effects in multiple rodent PD models (Battaglia et al., 2006; Marino et al., 2003; Niswender et al., 2008a). Unfortunately, many available compounds have lacked pharmacokinetic properties to make them useful tools for study of mGluR4 function via systemic routes of administration. The probe compound developed here exhibits sufficient potency, efficacy, and pharmacokinetic properties, including brain penetration, to make it a useful compound to progress mGluR4 biology, which will undoubtedly allow the intense study of mGluR4 activation in multiple areas of neuroscience such as psychiatric disorders (Stachowicz et al., 2006; Stachowicz et al., 2004), cancer (Iacovelli et al., 2006), and addiction (Blednov et al., 2004).


References
1. Battaglia G, Busceti CL, Molinaro G, Biagioni F, Traficante A, Nicoletti F and Bruno V (2006) Pharmacological activation of mGlu4 metabotropic glutamate receptors reduces nigrostriatal degeneration in mice treated with 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine. J Neurosci 26(27):7222-7229.
2. Blednov YA, Walker D, Osterndorf-Kahanek E and Harris RA (2004) Mice lacking metabotropic glutamate receptor 4 do not show the motor stimulatory effect of ethanol. Alcohol 34(2-3):251-259.
3. Conn PJ, Battaglia G, Marino MJ and Nicoletti F (2005) Metabotropic glutamate receptors in the basal ganglia motor circuit. Nat Rev Neurosci 6(10):787-798.
4. Engers DW, Niswender CM, Weaver CD, Jadhav S, Menon UN, Zamorano R, Conn PJ, Lindsley CW and Hopkins CR (2009) Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). J Med Chem 52(14):4115-4118.
5. Iacovelli L, Arcella A, Battaglia G, Pazzaglia S, Aronica E, Spinsanti P, Caruso A, De Smaele E, Saran A, Gulino A, D'Onofrio M, Giangaspero F and Nicoletti F (2006) Pharmacological activation of mGlu4 metabotropic glutamate receptors inhibits the growth of medulloblastomas. J Neurosci 26(32):8388-8397.
6. Konieczny J, Wardas J, Kuter K, Pilc A and Ossowska K (2007) The influence of group III metabotropic glutamate receptor stimulation by (1S,3R,4S)-1-aminocyclo-pentane-1,3,4-tricarboxylic acid on the parkinsonian-like akinesia and striatal proenkephalin and prodynorphin mRNA expression in rats. Neuroscience 145(2):611-620.
7. Macinnes N and Duty S (2008) Group III metabotropic glutamate receptors act as hetero-receptors modulating evoked GABA release in the globus pallidus in vivo. Eur J Pharmacol 580(1-2):95-99.
8. MacInnes N, Messenger MJ and Duty S (2004) Activation of group III metabotropic glutamate receptors in selected regions of the basal ganglia alleviates akinesia in the reserpine-treated rat. Br J Pharmacol 141(1):15-22.
9. Maj M, Bruno V, Dragic Z, Yamamoto R, Battaglia G, Inderbitzin W, Stoehr N, Stein T, Gasparini F, Vranesic I, Kuhn R, Nicoletti F and Flor PJ (2003) (-)-PHCCC, a positive allosteric modulator of mGluR4: characterization, mechanism of action, and neuroprotection. Neuropharmacology 45(7):895-906.
10. Marino MJ, Williams DL, Jr., O'Brien JA, Valenti O, McDonald TP, Clements MK, Wang R, DiLella AG, Hess JF, Kinney GG and Conn PJ (2003) Allosteric modulation of group III metabotropic glutamate receptor 4: a potential approach to Parkinson's disease treatment. Proc Natl Acad Sci U S A 100(23):13668-13673.
11. Niswender CM, Johnson KA, Weaver CD, Jones CK, Xiang Z, Luo Q, Rodriguez AL, Marlo JE, de Paulis T, Thompson AD, Days EL, Nalywajko T, Austin CA, Williams MB, Ayala JE, Williams R, Lindsley CW and Conn PJ (2008a) Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4. Mol Pharmacol 74(5):1345-1358.
12. Niswender CM, Lebois EP, Luo Q, Kim K, Muchalski H, Yin H, Conn PJ and Lindsley CW (2008b) Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators. Bioorg Med Chem Lett 18(20):5626-5630.
13. Ossowska K, Konieczny J, Wardas J, Pietraszek M, Kuter K, Wolfarth S and Pilc A (2007) An influence of ligands of metabotropic glutamate receptor subtypes on parkinsonian-like symptoms and the striatopallidal pathway in rats. Amino Acids 32(2):179-188.
14. Stachowicz K, Chojnacka-Wojcik E, Klak K and Pilc A (2006) Anxiolytic-like effects of group III mGlu receptor ligands in the hippocampus involve GABAA signaling. Pharmacol Rep 58(6):820-826.
15. Stachowicz K, Klak K, Klodzinska A, Chojnacka-Wojcik E and Pilc A (2004) Anxiolytic-like effects of PHCCC, an allosteric modulator of mGlu4 receptors, in rats. Eur J Pharmacol 498(1-3):153-156.
16. Valenti O, Marino MJ, Wittmann M, Lis E, DiLella AG, Kinney GG and Conn PJ (2003) Group III metabotropic glutamate receptor-mediated modulation of the striatopallidal synapse. J Neurosci 23(18):7218-7226.
17. Williams R, Niswender CM, Luo Q, Le U, Conn PJ and Lindsley CW (2008) Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead. Bioorg Med Chem Lett.
Protocol
Basic protocol:
1. Cells are plated at a density of 20,000 cells/well 1 day prior to assay in Thallium Assay Media (DMEM + 20mM HEPES, 10% dialyzed FBS, 1mM sodium pyruvate).
2. The following day, media is removed from the cells.
3. 20 ul/well of Fluo Zn dye (0.33 uM) in Assay Buffer (HBSS + 20mM HEPES) is added.
4. The plates are incubated for one hour at RT.
5. Dye is removed from the cells and the cell are washed with Assay Buffer leaving 20uL residual volume.
6. Plates are incubated for 10 minutes at RT.
7. Plates are loaded into a Hamamatsu FDSS.
8. Compounds are tested for selectivity at a 10 uM final concentration (prepared as a 2X stock, 20 ul added per well) and the agonist (LP-4) is added at a 5X concentration (10 ul of agonist added per well, 50 uL total volume). A baseline read is taken for 1.5 seconds, the first addition (compound or DMSO-matched vehicle) occurs at 1.5 seconds and the second addition (agonist) is added at 142 seconds. The read continues for 300 seconds.
Data analysis:
Data were analyzed using Microsoft Excel. Raw data were opened in Excel and each data point in a given trace was divided by the first data point from that trace (static ratio). For experiments in which antagonists/potentiators were added, data were again normalized by dividing each point by the fluorescence value immediately before the agonist addition to correct for any subtle differences in the baseline traces after the compound incubation period. The slope of the fluorescence increase beginning five seconds after thallium/agonist addition and ending fifteen seconds after thallium/agonist addition was calculated. Curves were fitted using a four point logistical equation using Microsoft XLfit (IDBS, Bridgewater, NJ).
This compound was not a positive allosteric modulator of rat mGluR7 and was assigned an 'Outcome' of 'Inactive' and a 'Score' of '0'.
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: Functional
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1L-AP4Rep1_1990_uM (1990μM**)Value for replicate 1 for L-AP4-only at 1990 uM L-AP4Float
2L-AP4Rep2_1990_uM (1990μM**)Value for replicate 2 for L-AP4-only at 1990 uM L-AP4Float
3L-AP4Rep3_1990_uM (1990μM**)Value for replicate 3 for L-AP4-only at 1990 uM L-AP4Float
4L-AP4Rep4_1990_uM (1990μM**)Value for replicate 4 for L-AP4-only at 1990 uM L-AP4Float
5AvgL-AP4_1990_uMAverage for L-AP4-only across all replicates at 1990 uM L-AP4Float
6CompoundL-AP4Rep1_1990_uM (1990μM**)Value for replicate 1 for L-AP4 + compound at 1990 uM L-AP4Float
7CompoundL-AP4Rep2_1990_uM (1990μM**)Value for replicate 2 for L-AP4 + compound at 1990 uM L-AP4Float
8CompoundL-AP4Rep3_1990_uM (1990μM**)Value for replicate 3 for L-AP4 + compound at 1990 uM L-AP4Float
9AvgCompoundL-AP4_1990_uMAverage for L-AP4 + compound across all replicates at 1990 uM L-AP4Float
10L-AP4Rep1_1000_uM (1000μM**)Value for replicate 1 for L-AP4-only at 1000 uM L-AP4Float
11L-AP4Rep2_1000_uM (1000μM**)Value for replicate 2 for L-AP4-only at 1000 uM L-AP4Float
12L-AP4Rep3_1000_uM (1000μM**)Value for replicate 3 for L-AP4-only at 1000 uM L-AP4Float
13L-AP4Rep4_1000_uM (1000μM**)Value for replicate 4 for L-AP4-only at 1000 uM L-AP4Float
14AvgL-AP4_1000_uMAverage for L-AP4-only across all replicates at 1000 uM L-AP4Float
15CompoundL-AP4Rep1_1000_uM (1000μM**)Value for replicate 1 for L-AP4 + compound at 1000 uM L-AP4Float
16CompoundL-AP4Rep2_1000_uM (1000μM**)Value for replicate 2 for L-AP4 + compound at 1000 uM L-AP4Float
17CompoundL-AP4Rep3_1000_uM (1000μM**)Value for replicate 3 for L-AP4 + compound at 1000 uM L-AP4Float
18AvgCompoundL-AP4_1000_uMAverage for L-AP4 + compound across all replicates at 1000 uM L-AP4Float
19L-AP4Rep1_501_uM (501μM**)Value for replicate 1 for L-AP4-only at 501 uM L-AP4Float
20L-AP4Rep2_501_uM (501μM**)Value for replicate 2 for L-AP4-only at 501 uM L-AP4Float
21L-AP4Rep3_501_uM (501μM**)Value for replicate 3 for L-AP4-only at 501 uM L-AP4Float
22L-AP4Rep4_501_uM (501μM**)Value for replicate 4 for L-AP4-only at 501 uM L-AP4Float
23AvgL-AP4_501_uMAverage for L-AP4-only across all replicates at 501 uM L-AP4Float
24CompoundL-AP4Rep1_501_uM (501μM**)Value for replicate 1 for L-AP4 + compound at 501 uM L-AP4Float
25CompoundL-AP4Rep2_501_uM (501μM**)Value for replicate 2 for L-AP4 + compound at 501 uM L-AP4Float
26CompoundL-AP4Re3_501_uM (501μM**)Value for replicate 3 for L-AP4 + compound at 501 uM L-AP4Float
27AvgCompoundL-AP4_501_uMAverage for L-AP4 + compound across all replicates at 501 uM L-AP4Float
28L-AP4Rep1_251_uM (251μM**)Value for replicate 1 for L-AP4-only at 251 uM L-AP4Float
29L-AP4Rep2_251_uM (251μM**)Value for replicate 2 for L-AP4-only at 251 uM L-AP4Float
30L-AP4Rep3_251_uM (251μM**)Value for replicate 3 for L-AP4-only at 251 uM L-AP4Float
31L-AP4Rep4_251_uM (251μM**)Value for replicate 4 for L-AP4-only at 251 uM L-AP4Float
32AvgL-AP4_251_uMAverage for L-AP4-only across all replicates at 251 uM L-AP4Float
33CompoundL-AP4Rep1_251_uM (251μM**)Value for replicate 1 for L-AP4 + compound at 251 uM L-AP4Float
34CompoundL-AP4Rep2_251_uM (251μM**)Value for replicate 2 for L-AP4 + compound at 251 uM L-AP4Float
35CompoundL-AP4Rep3_251_uM (251μM**)Value for replicate 3 for L-AP4 + compound at 251 uM L-AP4Float
36AvgCompoundL-AP4_251_uMAverage for L-AP4 + compound across all replicates at 251 uM L-AP4Float
37L-AP4Rep1_125_uM (125μM**)Value for replicate 1 for L-AP4-only at 125 uM L-AP4Float
38L-AP4Rep2_125_uM (125μM**)Value for replicate 2 for L-AP4-only at 125 uM L-AP4Float
39L-AP4Rep3_125_uM (125μM**)Value for replicate 3 for L-AP4-only at 125 uM L-AP4Float
40L-AP4Rep4_125_uM (125μM**)Value for replicate 4 for L-AP4-only at 125 uM L-AP4Float
41AvgL-AP4_125_uMAverage for L-AP4-only across all replicates at 125 uM L-AP4Float
42CompoundL-AP4Rep1_125_uM (125μM**)Value for replicate 1 for L-AP4 + compound at 125 uM L-AP4Float
43CompoundL-AP4Rep2_125_uM (125μM**)Value for replicate 2 for L-AP4 + compound at 125 uM L-AP4Float
44CompoundL-AP4Rep3_125_uM (125μM**)Value for replicate 3 for L-AP4 + compound at 125 uM L-AP4Float
45AvgCompoundL-AP4_125_uMAverage for L-AP4 + compound across all replicates at 125 uM L-AP4Float
46L-AP4Rep1_63.0_uM (63μM**)Value for replicate 1 for L-AP4-only at 63 uM L-AP4Float
47L-AP4Rep2_63.0_uM (63μM**)Value for replicate 2 for L-AP4-only at 63 uM L-AP4Float
48L-AP4Rep3_63.0_uM (63μM**)Value for replicate 3 for L-AP4-only at 63 uM L-AP4Float
49L-AP4Rep4_63.0_uM (63μM**)Value for replicate 4 for L-AP4-only at 63 uM L-AP4Float
50AvgL-AP4_63.0_uMAverage for L-AP4-only across all replicates at 63 uM L-AP4Float
51CompoundL-AP4Rep1_63.0_uM (63μM**)Value for replicate 1 for L-AP4 + compound at 63 uM L-AP4Float
52CompoundL-AP4Rep2_63.0_uM (63μM**)Value for replicate 2 for L-AP4 + compound at 63 uM L-AP4Float
53CompoundL-AP4Rep3_63.0_uM (63μM**)Value for replicate 3 for L-AP4 + compound at 63 uM L-AP4Float
54AvgCompoundL-AP4_63.0_uMAverage for L-AP4 + compound across all replicates at 63 uM L-AP4Float
55L-AP4Rep1_30.9_uM (30.9μM**)Value for replicate 1 for L-AP4-only at 30.9 uM L-AP4Float
56L-AP4Rep2_30.9_uM (30.9μM**)Value for replicate 2 for L-AP4-only at 30.9 uM L-AP4Float
57L-AP4Rep3_30.9_uM (30.9μM**)Value for replicate 3 for L-AP4-only at 30.9 uM L-AP4Float
58L-AP4Rep4_30.9_uM (30.9μM**)Value for replicate 4 for L-AP4-only at 30.9 uM L-AP4Float
59AvgL-AP4_30.9_uMAverage for L-AP4-only across all replicates at 30.9 uM L-AP4Float
60CompoundL-AP4Rep1_30.9_uM (30.9μM**)Value for replicate 1 for L-AP4 + compound at 30.9 uM L-AP4Float
61CompoundL-AP4Rep2_30.9_uM (30.9μM**)Value for replicate 2 for L-AP4 + compound at 30.9 uM L-AP4Float
62CompoundL-AP4Rep3_30.9_uM (30.9μM**)Value for replicate 3 for L-AP4 + compound at 30.9 uM L-AP4Float
63AvgCompoundL-AP4_30.9_uMAverage for L-AP4 + compound across all replicates at 30.9 uM L-AP4Float
64L-AP4Rep1_15.4_uM (15.4μM**)Value for replicate 1 for L-AP4-only at 15.4 uM L-AP4Float
65L-AP4Rep2_15.4_uM (15.4μM**)Value for replicate 2 for L-AP4-only at 15.4 uM L-AP4Float
66L-AP4Rep3_15.4_uM (15.4μM**)Value for replicate 3 for L-AP4-only at 15.4 uM L-AP4Float
67L-AP4Rep4_15.4_uM (15.4μM**)Value for replicate 4 for L-AP4-only at 15.4 uM L-AP4Float
68AvgL-AP4_15.4_uMAverage for L-AP4-only across all replicates at 15.4 uM L-AP4Float
69CompoundL-AP4Rep1_15.4_uM (15.4μM**)Value for replicate 1 for L-AP4 + compound at 15.4 uM L-AP4Float
70CompoundL-AP4Rep2_15.4_uM (15.4μM**)Value for replicate 2 for L-AP4 + compound at 15.4 uM L-AP4Float
71CompoundL-AP4Rep3_15.4_uM (15.4μM**)Value for replicate 3 for L-AP4 + compound at 15.4 uM L-AP4Float
72AvgCompoundL-AP4_15.4_uMAverage for L-AP4 + compound across all replicates at 15.4 uM L-AP4Float
73L-AP4Rep1_7.76_uM (7.76μM**)Value for replicate 1 for L-AP4-only at 7.76 uM L-AP4Float
74L-AP4Rep2_7.76_uM (7.76μM**)Value for replicate 2 for L-AP4-only at 7.76 uM L-AP4Float
75L-AP4Rep3_7.76_uM (7.76μM**)Value for replicate 3 for L-AP4-only at 7.76 uM L-AP4Float
76L-AP4Rep4_7.76_uM (7.76μM**)Value for replicate 4 for L-AP4-only at 7.76 uM L-AP4Float
77AvgL-AP4_7.76_uMAverage for L-AP4-only across all replicates at 7.76 uM L-AP4Float
78CompoundL-AP4Rep1_7.76_uM (7.76μM**)Value for replicate 1 for L-AP4 + compound at 7.76 uM L-AP4Float
79CompoundL-AP4Rep2_7.76_uM (7.76μM**)Value for replicate 2 for L-AP4 + compound at 7.76 uM L-AP4Float
80CompoundL-AP4Rep3_7.76_uM (7.76μM**)Value for replicate 3 for L-AP4 + compound at 7.76 uM L-AP4Float
81AvgCompoundL-AP4_7.76_uMAverage for L-AP4 + compound across all replicates at 7.76 uM L-AP4Float
82L-AP4Rep1_3.89_uM (3.89μM**)Value for replicate 1 for L-AP4-only at 3.89 uM L-AP4Float
83L-AP4Rep2_3.89_uM (3.89μM**)Value for replicate 2 for L-AP4-only at 3.89 uM L-AP4Float
84L-AP4Rep3_3.89_uM (3.89μM**)Value for replicate 3 for L-AP4-only at 3.89 uM L-AP4Float
85L-AP4Rep4_3.89_uM (3.89μM**)Value for replicate 4 for L-AP4-only at 3.89 uM L-AP4Float
86AvgL-AP4_3.89_uMAverage for L-AP4-only across all replicates at 3.89 uM L-AP4Float
87CompoundL-AP4Rep1_3.89_uM (3.89μM**)Value for replicate 1 for L-AP4 + compound at 3.89 uM L-AP4Float
88CompoundL-AP4Rep2_3.89_uM (3.89μM**)Value for replicate 2 for L-AP4 + compound at 3.89 uM L-AP4Float
89CompoundL-AP4Rep3_3.89_uM (3.89μM**)Value for replicate 3 for L-AP4 + compound at 3.89 uM L-AP4Float
90AvgCompoundL-AP4_3.89_uMAverage for L-AP4 + compound across all replicates at 3.89 uM L-AP4Float
91L-AP4Rep1_1.94_uM (1.94μM**)Value for replicate 1 for L-AP4-only at 1.94 uM L-AP4Float
92L-AP4Rep2_1.94_uM (1.94μM**)Value for replicate 2 for L-AP4-only at 1.94 uM L-AP4Float
93L-AP4Rep3_1.94_uM (1.94μM**)Value for replicate 3 for L-AP4-only at 1.94 uM L-AP4Float
94L-AP4Rep4_1.94_uM (1.94μM**)Value for replicate 4 for L-AP4-only at 1.94 uM L-AP4Float
95AvgL-AP4_1.94_uMAverage for L-AP4-only across all replicates at 1.94 uM L-AP4Float
96CompoundL-AP4Rep1_1.94_uM (1.94μM**)Value for replicate 1 for L-AP4 + compound at 1.94 uM L-AP4Float
97CompoundL-AP4Rep2_1.94_uM (1.94μM**)Value for replicate 2 for L-AP4 + compound at 1.94 uM L-AP4Float
98CompoundL-AP4Rep3_1.94_uM (1.94μM**)Value for replicate 3 for L-AP4 + compound at 1.94 uM L-AP4Float
99AvgCompoundL-AP4_1.94_uMAverage for L-AP4 + compound across all replicates at 1.94 uM L-AP4Float
100L-AP4EC50Calculated L-AP4-only EC50FloatμM
101L-AP4EmaxCalculated L-AP4-only EmaxFloat
102L-AP4EminCalculated L-AP4-only EminFloat
103foldshiftCalculated EC50 fold-shift between L-AP4-only experiment and L-AP4+compound experimentFloat
104CompoundL-AP4EC50*Calculated L-AP4+compound EC50FloatμM
105CompoundL-AP4EmaxCalculated L-AP4+compound EmaxFloat
106CompoundL-AP4EminCalculated L-AP4+compound EminFloat

* Activity Concentration. ** Test Concentration.
Additional Information
Grant Number: NS053536-01

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