Bookmark and Share
BioAssay: AID 1744

Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Activity against Muscarinic Panel

The M1 muscarinic receptor is thought to be an important therapeutic target in schizophrenia. A cell-based fluorometric calcium assay was developed for high throughput screening. This assay was used to identify compounds with high selectivity for the M1 receptor subtype that act at an allosteric site on the receptor, thus providing increased specificity for this single receptor subtype. It is anticipated that these compounds will provide important tools for the study of muscarinic receptor function in the CNS. ..more
_
   
 Tested Compounds
 Tested Compounds
All(8)
 
 
Active(8)
 
 
 Tested Substances
 Tested Substances
All(8)
 
 
Active(8)
 
 
AID: 1744
Data Source: Vanderbilt Screening Center for GPCRs, Ion Channels and Transporters (JC001_CaPanel)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: NIH Molecular Libraries Screening Center Network
Deposit Date: 2009-05-12
Modify Date: 2010-06-24

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: cholinergic receptor, muscarinic 1 [Rattus norvegicus]
Description ..   
Protein Family: Olfactory receptor

Gene:CHRM1     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 8
Related Experiments
Show more
AIDNameTypeProbeComment
626Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary ScreenScreening depositor-specified cross reference
1488Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation AssayOther depositor-specified cross reference
1741Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Counterscreen with M4 ReceptorOther depositor-specified cross reference
1798Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Probe SummarySummary1 depositor-specified cross reference
1470Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS binding at M1Confirmatory same project related to Summary assay
1508Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5Confirmatory same project related to Summary assay
1743Discovery of novel allosteric modulators of the M1 muscarinic receptor: Y381A Mutant M1 ReceptorConfirmatory same project related to Summary assay
1757Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M4Confirmatory same project related to Summary assay
1764Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3Confirmatory same project related to Summary assay
1767Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2Confirmatory same project related to Summary assay
1788Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Ancillary ActivityOther same project related to Summary assay
Description:
Assay Provider: P. Jeffrey Conn
Assay Provider Affiliation: Vanderbilt University
Grant Title: Discovery of novel allosteric modulators of the M1 muscarinic receptor
Grant Number: 1 R03 MH077606-01

The M1 muscarinic receptor is thought to be an important therapeutic target in schizophrenia. A cell-based fluorometric calcium assay was developed for high throughput screening. This assay was used to identify compounds with high selectivity for the M1 receptor subtype that act at an allosteric site on the receptor, thus providing increased specificity for this single receptor subtype. It is anticipated that these compounds will provide important tools for the study of muscarinic receptor function in the CNS.

Agents that enhance cholinergic transmission or activate muscarinic acetylcholine receptors (mAChRs) have been developed to ameliorate the loss of cognitive function in patients with Alzheimer's Disease (AD). While cholinergic agents have been partially successful in improving cognitive function in AD patients, the most exciting findings coming from clinical studies with these agents have been the demonstration of efficacy in reducing psychotic symptoms in patients with AD and other neurodegenerative disorders. Interestingly, the M1/M4 preferring mAChR agonist, xanomeline, also induces a robust antipsychotic effect in schizophrenic patients, suggesting that mAChR agonists may have broad utility in reducing psychotic symptoms in patients suffering from schizophrenia and certain neurodegenerative disorders.

Evidence suggests that the antipsychotic effects of cholinergic agents may be mediated by the M1 mAChR subtype. However, previous compounds developed to selectively activate M1 receptors have failed in clinical development due to a lack of true specificity for M1 and adverse effects associated with activation of other mAChR subtypes. Furthermore, the lack of highly selective compounds has made it impossible to definitively determine whether the behavioral and clinical effects of these compounds are mediated by M1 and the M4 receptor subtype is also a viable candidate for mediating the antipsychotic effects.

Previous attempts to develop agonists and antagonists that are highly selective for M1 or other specific mAChR subtypes have failed because of the high conservation of the ACh binding site and difficulty in developing compounds that are truly specific. However, in recent years, major advances have been made in discovery of highly selective antagonists of other G protein-coupled receptors (GPCRs) that act at allosteric sites rather than the orthosteric neurotransmitter binding site [1, 2]. These compounds induce a noncompetitive blockade of receptor function and tend to be highly selective for the targeted receptor. Even more promising for discovery of M1-selective agonists, novel compounds have now been discovered that act at an allosteric site on M1 receptor rather than the orthosteric ACh-binding site to induce a robust activation of the receptor and provide high receptor subtype specificity [3, 4].

1.May, L.T. and A. Christopoulos, Allosteric modulators of G-protein-coupled receptors. Curr Opin Pharmacol, 2003. 3(5): p. 551-6.
2.Gasparini, F., R. Kuhn, and J.P. Pin, Allosteric modulators of group1 metabotropic glutamate receptors: novel subtype-selective ligands and therapeutic perspectives. Curr Opin Pharmacol, 2002. 2(1): p. 43-9.
3.Spalding, T.A., et al., Discovery of an ectopic activation site on the M(1) muscarinic receptor. Mol Pharmacol, 2002. 61(6): p. 1297-302.
4.Sur, C., et al., N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates Nmethyl-D-aspartate receptor activity. Proc Natl Acad Sci USA, 2003. 100(23): p. 13674-9.
Protocol
The purpose of this screen was to test compounds of interest against the muscarinic panel (M1, M2, M3, M4 and M5) for their ability to modulate calcium flux.
Experimental Protocol:
Stable CHO-K1 cell lines expressing rat M1, human M2-Gqi5, human M3, rat M4-Gqi5, or human M5 were plated into 96-well Costar optical bottom assay plates at a concentration of 50K cells/well in 100 microliters of Ham's F-12 media. Cells were incubated overnight at 37 degrees C (5% CO2). The following day, medium was removed from cells and they were incubated in 50 microliters of Fluo-4 AM diluted in assay buffer (HBSS containing 20 mM HEPES and 2.5 mM probenecid, pH 7.4) for 1 hour at 37 degrees C. Dye was removed and replaced with 45 microliters of assay buffer. Test compounds were serially diluted in DMSO-matched assay buffer at 2X concentration and 45 microliters was applied to a cell-containing assay plate in an automated format using the Flexstation (Molecular Devices). Calcium flux was measured over time as an increase in fluorescence (fold over basal), and the max minus min values for each well were copied into a custom excel template, which normalized the data as a % of maximum response elicited by a high concentration of ACh control. This data was then copied into Prism (version 4.0c), which fit the data to a sigmoidal dose-response model with variable slopes using no constraints or weighting.
Result Definitions
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1M1 Value1 at 0.01 micromolar (0.01μM**)normalized activity at 0.01 micromolar for replicate 1 with M1 cell lineFloat
2M1 Value1 at 0.03 micromolar (0.03μM**)normalized activity at 0.03 micromolar for replicate 1 with M1 cell lineFloat
3M1 Value1 at 0.10 micromolar (0.1μM**)normalized activity at 0.10 micromolar for replicate 1 with M1 cell lineFloat
4M1 Value1 at 0.301 micromolar (0.301μM**)normalized activity at 0.301 micromolar for replicate 1 with M1 cell lineFloat
5M1 Value1 at 1.0 micromolar (1μM**)normalized activity at 1 micromolar for replicate 1 with M1 cell lineFloat
6M1 Value1 at 3.0 micromolar (3μM**)normalized activity at 3 micromolar for replicate 1 with M1 cell lineFloat
7M1 Value1 at 10.0 micromolar (10μM**)normalized activity at 10 micromolar for replicate 1 with M1 cell lineFloat
8M1 Value1 at 30.0 micromolar (30μM**)normalized activity at 30 micromolar for replicate 1 with M1 cell lineFloat
9M1 Value2 at 0.01 micromolar (0.01μM**)normalized activity at 0.01 micromolar for replicate 2 with M1 cell lineFloat
10M1 Value2 at 0.03 micromolar (0.03μM**)normalized activity at 0.03 micromolar for replicate 2 with M1 cell lineFloat
11M1 Value2 at 0.10 micromolar (0.1μM**)normalized activity at 0.10 micromolar for replicate 2 with M1 cell lineFloat
12M1 Value2 at 0.301 micromolar (0.301μM**)normalized activity at 0.301 micromolar for replicate 2 with M1 cell lineFloat
13M1 Value2 at 1.0 micromolar (1μM**)normalized activity at 1 micromolar for replicate 2 with M1 cell lineFloat
14M1 Value2 at 3.0 micromolar (3μM**)normalized activity at 3 micromolar for replicate 2 with M1 cell lineFloat
15M1 Value2 at 10.0 micromolar (10μM**)normalized activity at 10 micromolar for replicate 2 with M1 cell lineFloat
16M1 Value2 at 30.0 micromolar (30μM**)normalized activity at 30 micromolar for replicate 2 with M1 cell lineFloat
17M1 Value3 at 0.01 micromolar (0.01μM**)normalized activity at 0.01 micromolar for replicate 3 with M1 cell lineFloat
18M1 Value3 at 0.03 micromolar (0.03μM**)normalized activity at 0.03 micromolar for replicate 3 with M1 cell lineFloat
19M1 Value3 at 0.10 micromolar (0.1μM**)normalized activity at 0.10 micromolar for replicate 3 with M1 cell lineFloat
20M1 Value3 at 0.301 micromolar (0.301μM**)normalized activity at 0.301 micromolar for replicate 3 with M1 cell lineFloat
21M1 Value3 at 1.0 micromolar (1μM**)normalized activity at 1 micromolar for replicate 3 with M1 cell lineFloat
22M1 Value3 at 3.0 micromolar (3μM**)normalized activity at 3 micromolar for replicate 3 with M1 cell lineFloat
23M1 Value3 at 10.0 micromolar (10μM**)normalized activity at 10 micromolar for replicate 3 with M1 cell lineFloat
24M1 Value3 at 30.0 micromolar (30μM**)normalized activity at 30 micromolar for replicate 3 with M1 cell lineFloat
25M1 Fit ResultSigmoidal dose-reponse' reported when fit model without weighting or contraints. 'No fit' reported when Prism reported ambiguous, not converge or interupted. M1 cell line tested.String
26M1 BottomPrism best fit value for bottom of curve for M1Float
27M1 TopPrism best fit value for top of curve for M1Float
28M1 LogEC50Prism best fit value for LogEC50 for M1Float
29M1 HillSlopePrism best fit value for Hill Slope for M1Float
30M1 EC50*Prism best fit value for EC50 for M1FloatμM
31M1 Std. Error BottomCalculated standard error for the Bottom value for M1Float
32M1 Std. ErrorTopCalculated standard error for the Top value for M1String
33M1 Std. Error LogEC50Calculated standard error for the LogEC50 value for M1String
34M1 Std. Error HillSlopeCalculated standard error for the HillSlope value for M1String
35M1 95% Confidence Intervals BottomPrism-calculated 95% confidence intervals for the Bottom value for M1String
36M1 95% Confidence Intervals TopPrism-calculated 95% confidence intervals for the Top value for M1String
37M1 95% Confidence Intervals LogEC50Prism-calculated 95% confidence intervals for the LogEC50 value for M1String
38M1 95% Confidence Intervals HillSlopePrism-calculated 95% confidence intervals for the HillSlope value for M1String
39M1 95% Confidence Intervals EC50Prism-calculated 95% confidence intervals for the EC50 value for M1String
40M1 Degrees of FreedomNumber of degrees of freedom in this model for M1Integer
41M1 RsquaredCoefficient of determination for this data set for M1Float
42M1 AbsSumOfSquaresAbsolute sum of squares of the residuals for M1Float
43M1 StddevResidualsStandard deviation of the residuals for M1Float
44M1 NumPointsNumber of points analyzed for M1Integer
45M2 Value1 at 0.01 micromolar (0.01μM**)normalized activity at 0.01 micromolar for replicate 1 with M2 cell lineFloat
46M2 Value1 at 0.03 micromolar (0.03μM**)normalized activity at 0.03 micromolar for replicate 1 with M2 cell lineFloat
47M2 Value1 at 0.10 micromolar (0.1μM**)normalized activity at 0.10 micromolar for replicate 1 with M2 cell lineFloat
48M2 Value1 at 0.301 micromolar (0.301μM**)normalized activity at 0.301 micromolar for replicate 1 with M2 cell lineFloat
49M2 Value1 at 1.0 micromolar (1μM**)normalized activity at 1 micromolar for replicate 1 with M2 cell lineFloat
50M2 Value1 at 3.0 micromolar (3μM**)normalized activity at 3 micromolar for replicate 1 with M2 cell lineFloat
51M2 Value1 at 10.0 micromolar (10μM**)normalized activity at 10 micromolar for replicate 1 with M2 cell lineFloat
52M2 Value1 at 30.0 micromolar (30μM**)normalized activity at 30 micromolar for replicate 1 with M2 cell lineFloat
53M2 Value2 at 0.01 micromolar (0.01μM**)normalized activity at 0.01 micromolar for replicate 2 with M2 cell lineFloat
54M2 Value2 at 0.03 micromolar (0.03μM**)normalized activity at 0.03 micromolar for replicate 2 with M2 cell lineFloat
55M2 Value2 at 0.10 micromolar (0.1μM**)normalized activity at 0.10 micromolar for replicate 2 with M2 cell lineFloat
56M2 Value2 at 0.301 micromolar (0.301μM**)normalized activity at 0.301 micromolar for replicate 2 with M2 cell lineFloat
57M2 Value2 at 1.0 micromolar (1μM**)normalized activity at 1 micromolar for replicate 2 with M2 cell lineFloat
58M2 Value2 at 3.0 micromolar (3μM**)normalized activity at 3 micromolar for replicate 2 with M2 cell lineFloat
59M2 Value2 at 10.0 micromolar (10μM**)normalized activity at 10 micromolar for replicate 2 with M2 cell lineFloat
60M2 Value2 at 30.0 micromolar (30μM**)normalized activity at 30 micromolar for replicate 2 with M2 cell lineFloat
61M2 Value3 at 0.01 micromolar (0.01μM**)normalized activity at 0.01 micromolar for replicate 3 with M2 cell lineFloat
62M2 Value3 at 0.03 micromolar (0.03μM**)normalized activity at 0.03 micromolar for replicate 3 with M2 cell lineFloat
63M2 Value3 at 0.10 micromolar (0.1μM**)normalized activity at 0.10 micromolar for replicate 3 with M2 cell lineFloat
64M2 Value3 at 0.301 micromolar (0.301μM**)normalized activity at 0.301 micromolar for replicate 3 with M2 cell lineFloat
65M2 Value3 at 1.0 micromolar (1μM**)normalized activity at 1 micromolar for replicate 3 with M2 cell lineFloat
66M2 Value3 at 3.0 micromolar (3μM**)normalized activity at 3 micromolar for replicate 3 with M2 cell lineFloat
67M2 Value3 at 10.0 micromolar (10μM**)normalized activity at 10 micromolar for replicate 3 with M2 cell lineFloat
68M2 Value3 at 30.0 micromolar (30μM**)normalized activity at 30 micromolar for replicate 3 with M2 cell lineFloat
69M2 Fit ResultSigmoidal dose-reponse' reported when fit model without weighting or contraints. 'No fit' reported when Prism reported ambiguous, not converge or interupted. M2 cell line tested.String
70M2 NumPointsNumber of points analyzed for M2Integer
71M3 Value1 at 0.01 micromolar (0.01μM**)normalized activity at 0.01 micromolar for replicate 1 with M3 cell lineFloat
72M3 Value1 at 0.03 micromolar (0.03μM**)normalized activity at 0.03 micromolar for replicate 1 with M3 cell lineFloat
73M3 Value1 at 0.10 micromolar (0.1μM**)normalized activity at 0.10 micromolar for replicate 1 with M3 cell lineFloat
74M3 Value1 at 0.301 micromolar (0.301μM**)normalized activity at 0.301 micromolar for replicate 1 with M3 cell lineFloat
75M3 Value1 at 1.0 micromolar (1μM**)normalized activity at 1 micromolar for replicate 1 with M3 cell lineFloat
76M3 Value1 at 3.0 micromolar (3μM**)normalized activity at 3 micromolar for replicate 1 with M3 cell lineFloat
77M3 Value1 at 10.0 micromolar (10μM**)normalized activity at 10 micromolar for replicate 1 with M3 cell lineFloat
78M3 Value1 at 30.0 micromolar (30μM**)normalized activity at 30 micromolar for replicate 1 with M3 cell lineFloat
79M3 Value2 at 0.01 micromolar (0.01μM**)normalized activity at 0.01 micromolar for replicate 2 with M3 cell lineFloat
80M3 Value2 at 0.03 micromolar (0.03μM**)normalized activity at 0.03 micromolar for replicate 2 with M3 cell lineFloat
81M3 Value2 at 0.10 micromolar (0.1μM**)normalized activity at 0.10 micromolar for replicate 2 with M3 cell lineFloat
82M3 Value2 at 0.301 micromolar (0.301μM**)normalized activity at 0.301 micromolar for replicate 2 with M3 cell lineFloat
83M3 Value2 at 1.0 micromolar (1μM**)normalized activity at 1 micromolar for replicate 2 with M3 cell lineFloat
84M3 Value2 at 3.0 micromolar (3μM**)normalized activity at 3 micromolar for replicate 2 with M3 cell lineFloat
85M3 Value2 at 10.0 micromolar (10μM**)normalized activity at 10 micromolar for replicate 2 with M3 cell lineFloat
86M3 Value2 at 30.0 micromolar (30μM**)normalized activity at 30 micromolar for replicate 2 with M3 cell lineFloat
87M3 Value3 at 0.01 micromolar (0.01μM**)normalized activity at 0.01 micromolar for replicate 3 with M3 cell lineFloat
88M3 Value3 at 0.03 micromolar (0.03μM**)normalized activity at 0.03 micromolar for replicate 3 with M3 cell lineFloat
89M3 Value3 at 0.10 micromolar (0.1μM**)normalized activity at 0.10 micromolar for replicate 3 with M3 cell lineFloat
90M3 Value3 at 0.301 micromolar (0.301μM**)normalized activity at 0.301 micromolar for replicate 3 with M3 cell lineFloat
91M3 Value3 at 1.0 micromolar (1μM**)normalized activity at 1 micromolar for replicate 3 with M3 cell lineFloat
92M3 Value3 at 3.0 micromolar (3μM**)normalized activity at 3 micromolar for replicate 3 with M3 cell lineFloat
93M3 Value3 at 10.0 micromolar (10μM**)normalized activity at 10 micromolar for replicate 3 with M3 cell lineFloat
94M3 Value3 at 30.0 micromolar (30μM**)normalized activity at 30 micromolar for replicate 3 with M3 cell lineFloat
95M3 Fit ResultSigmoidal dose-reponse' reported when fit model without weighting or contraints. 'No fit' reported when Prism reported ambiguous, not converge or interupted. M3 cell line tested.String
96M3 NumPointsNumber of points analyzed for M3Integer
97M4 Value1 at 0.01 micromolar (0.01μM**)normalized activity at 0.01 micromolar for replicate 1 with M4 cell lineFloat
98M4 Value1 at 0.03 micromolar (0.03μM**)normalized activity at 0.03 micromolar for replicate 1 with M4 cell lineFloat
99M4 Value1 at 0.10 micromolar (0.1μM**)normalized activity at 0.10 micromolar for replicate 1 with M4 cell lineFloat
100M4 Value1 at 0.301 micromolar (0.301μM**)normalized activity at 0.301 micromolar for replicate 1 with M4 cell lineFloat
101M4 Value1 at 1.0 micromolar (1μM**)normalized activity at 1 micromolar for replicate 1 with M4 cell lineFloat
102M4 Value1 at 3.0 micromolar (3μM**)normalized activity at 3 micromolar for replicate 1 with M4 cell lineFloat
103M4 Value1 at 10.0 micromolar (10μM**)normalized activity at 10 micromolar for replicate 1 with M4 cell lineFloat
104M4 Value1 at 30.0 micromolar (30μM**)normalized activity at 30 micromolar for replicate 1 with M4 cell lineFloat
105M4 Value2 at 0.01 micromolar (0.01μM**)normalized activity at 0.01 micromolar for replicate 2 with M4 cell lineFloat
106M4 Value2 at 0.03 micromolar (0.03μM**)normalized activity at 0.03 micromolar for replicate 2 with M4 cell lineFloat
107M4 Value2 at 0.10 micromolar (0.1μM**)normalized activity at 0.10 micromolar for replicate 2 with M4 cell lineFloat
108M4 Value2 at 0.301 micromolar (0.301μM**)normalized activity at 0.301 micromolar for replicate 2 with M4 cell lineFloat
109M4 Value2 at 1.0 micromolar (1μM**)normalized activity at 1 micromolar for replicate 2 with M4 cell lineFloat
110M4 Value2 at 3.0 micromolar (3μM**)normalized activity at 3 micromolar for replicate 2 with M4 cell lineFloat
111M4 Value2 at 10.0 micromolar (10μM**)normalized activity at 10 micromolar for replicate 2 with M4 cell lineFloat
112M4 Value2 at 30.0 micromolar (30μM**)normalized activity at 30 micromolar for replicate 2 with M4 cell lineFloat
113M4 Value3 at 0.01 micromolar (0.01μM**)normalized activity at 0.01 micromolar for replicate 3 with M4 cell lineFloat
114M4 Value3 at 0.03 micromolar (0.03μM**)normalized activity at 0.03 micromolar for replicate 3 with M4 cell lineFloat
115M4 Value3 at 0.10 micromolar (0.1μM**)normalized activity at 0.10 micromolar for replicate 3 with M4 cell lineFloat
116M4 Value3 at 0.301 micromolar (0.301μM**)normalized activity at 0.301 micromolar for replicate 3 with M4 cell lineFloat
117M4 Value3 at 1.0 micromolar (1μM**)normalized activity at 1 micromolar for replicate 3 with M4 cell lineFloat
118M4 Value3 at 3.0 micromolar (3μM**)normalized activity at 3 micromolar for replicate 3 with M4 cell lineFloat
119M4 Value3 at 10.0 micromolar (10μM**)normalized activity at 10 micromolar for replicate 3 with M4 cell lineFloat
120M4 Value3 at 30.0 micromolar (30μM**)normalized activity at 30 micromolar for replicate 3 with M4 cell lineFloat
121M4 Fit ResultSigmoidal dose-reponse' reported when fit model without weighting or contraints. 'No fit' reported when Prism reported ambiguous, not converge or interupted. M4 cell line tested.String
122M4 NumPointsNumber of points analyzed for M4Integer
123M5 Value1 at 0.01 micromolar (0.01μM**)normalized activity at 0.01 micromolar for replicate 1 with M5 cell lineFloat
124M5 Value1 at 0.03 micromolar (0.03μM**)normalized activity at 0.03 micromolar for replicate 1 with M5 cell lineFloat
125M5 Value1 at 0.10 micromolar (0.1μM**)normalized activity at 0.10 micromolar for replicate 1 with M5 cell lineFloat
126M5 Value1 at 0.301 micromolar (0.301μM**)normalized activity at 0.301 micromolar for replicate 1 with M5 cell lineFloat
127M5 Value1 at 1.0 micromolar (1μM**)normalized activity at 1 micromolar for replicate 1 with M5 cell lineFloat
128M5 Value1 at 3.0 micromolar (3μM**)normalized activity at 3 micromolar for replicate 1 with M5 cell lineFloat
129M5 Value1 at 10.0 micromolar (10μM**)normalized activity at 10 micromolar for replicate 1 with M5 cell lineFloat
130M5 Value1 at 30.0 micromolar (30μM**)normalized activity at 30 micromolar for replicate 1 with M5 cell lineFloat
131M5 Value2 at 0.01 micromolar (0.01μM**)normalized activity at 0.01 micromolar for replicate 2 with M5 cell lineFloat
132M5 Value2 at 0.03 micromolar (0.03μM**)normalized activity at 0.03 micromolar for replicate 2 with M5 cell lineFloat
133M5 Value2 at 0.10 micromolar (0.1μM**)normalized activity at 0.10 micromolar for replicate 2 with M5 cell lineFloat
134M5 Value2 at 0.301 micromolar (0.301μM**)normalized activity at 0.301 micromolar for replicate 2 with M5 cell lineFloat
135M5 Value2 at 1.0 micromolar (1μM**)normalized activity at 1 micromolar for replicate 2 with M5 cell lineFloat
136M5 Value2 at 3.0 micromolar (3μM**)normalized activity at 3 micromolar for replicate 2 with M5 cell lineFloat
137M5 Value2 at 10.0 micromolar (10μM**)normalized activity at 10 micromolar for replicate 2 with M5 cell lineFloat
138M5 Value2 at 30.0 micromolar (30μM**)normalized activity at 30 micromolar for replicate 2 with M5 cell lineFloat
139M5 Value3 at 0.01 micromolar (0.01μM**)normalized activity at 0.01 micromolar for replicate 3 with M5 cell lineFloat
140M5 Value3 at 0.03 micromolar (0.03μM**)normalized activity at 0.03 micromolar for replicate 3 with M5 cell lineFloat
141M5 Value3 at 0.10 micromolar (0.1μM**)normalized activity at 0.10 micromolar for replicate 3 with M5 cell lineFloat
142M5 Value3 at 0.301 micromolar (0.301μM**)normalized activity at 0.301 micromolar for replicate 3 with M5 cell lineFloat
143M5 Value3 at 1.0 micromolar (1μM**)normalized activity at 1 micromolar for replicate 3 with M5 cell lineFloat
144M5 Value3 at 3.0 micromolar (3μM**)normalized activity at 3 micromolar for replicate 3 with M5 cell lineFloat
145M5 Value3 at 10.0 micromolar (10μM**)normalized activity at 10 micromolar for replicate 3 with M5 cell lineFloat
146M5 Value3 at 30.0 micromolar (30μM**)normalized activity at 30 micromolar for replicate 3 with M5 cell lineFloat
147M5 Fit ResultSigmoidal dose-reponse' reported when fit model without weighting or contraints. 'No fit' reported when Prism reported ambiguous, not converge or interupted. M5 cell line tested.String
148M5 NumPointsNumber of points analyzed for M5Integer

* Activity Concentration. ** Test Concentration.
Additional Information
Grant Number: 1 R03 MH077606-01

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