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BioAssay: AID 2204

Discovery of Novel Allosteric Modulators of the Muscarinic Receptor M5: Calcium Flux Assay

Muscarinic acetylcholine receptors are family A GPCRs comprised of five distinct mammalian subtypes (mAChR1-5 or M1-M5), which are expressed differentially throughout the body and play an important role in a variety of physiological processes. Among the mAChRs, M1 and M4 have been historically considered attractive targets for small molecule treatments of numerous CNS disorders such as more ..
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 Tested Compounds
 Tested Compounds
All(11)
 
 
Active(11)
 
 
 Tested Substances
 Tested Substances
All(11)
 
 
Active(11)
 
 
AID: 2204
Data Source: Vanderbilt Screening Center for GPCRs, Ion Channels and Transporters (M5 PAM Ca CRCs)
BioAssay Type: Panel, Confirmatory, Concentration-Response Relationship Observed
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2009-12-14
Modify Date: 2014-01-30

Data Table ( Complete ):           Active    All
Target
BioActive Compounds: 11
Depositor Specified Assays
AIDNameTypeComment
2416Discovery of Novel Allosteric Modulators of the Muscarinic Receptor M5summary
2665Discovery of Novel Allosteric Modulators of the Muscarinic Receptor M5: SAR with Acetylcholinescreening
Description:
Assay Provider: P. Jeffrey Conn
Assay Provider Affiliation: Vanderbilt University

Muscarinic acetylcholine receptors are family A GPCRs comprised of five distinct mammalian subtypes (mAChR1-5 or M1-M5), which are expressed differentially throughout the body and play an important role in a variety of physiological processes. Among the mAChRs, M1 and M4 have been historically considered attractive targets for small molecule treatments of numerous CNS disorders such as Alzheimer's disease and schizophrenia due to their respective localization and involvement in regulation of certain aspects of learning, memory, sleep, motor control, reward, and pain, among others. However, discovery of subtype-selective small molecules has proven highly difficult due to the conservation of the orthosteric binding-site across the mAChRs. This has contributed to the failure of muscarinic agonists in clinical trials and has also hampered pharmacological investigation into the role(s) of each mAChR in basic neurobiology.

Among the mAChRs, M5 has remained perhaps the most challenging to investigate pharmacologically due in part to its extremely low expression level and a complete lack of M5-selective ligands. Interestingly, studies using M5-KO mice suggest that M5 is the sole mediator of acetylcholine-induced cerebrovasodilation, which has led to the hypothesis that an M5 activator would have therapeutic efficacy in treatment of cerebrovascular dementias and ischemic stroke. Furthermore, M5-KO mice show dramatically reduced reward responses to drugs of abuse, consistent with its putative localization on midbrain dopaminergic neurons of the nigrostriatal and mesolimbic pathways. This suggests that M5 antagonism or negative modulation may have utility in treatment of illicit drug addiction and withdrawal. Despite these and other related findings from M5-KO mice, there remains a strong need for small molecule tools to probe M5 function and test M5-related hypotheses in order to advance the state of the mAChR research field and provide critical proof-of-concept studies for drug discovery aims.
Panel Information
Panel Assay with Multiple Targets/Outcomes
    Data Table(Active)    Data Table(All)Show more
PID§NameSubstancePanel TargetsDescriptionAdditional Information
ActiveInactive
1M1muscarinic acetylcholine receptor m1 [Rattus norvegicus] [gi:202660]
muscarinic M1 receptor (rat)Taxonomy id: 10116
2M2muscarinic acetylcholine receptor M2 [Homo sapiens] [gi:20302971]
muscarinic M2 receptor (human)Taxonomy id: 9606
3M3muscarinic acetylcholine receptor M3 [Homo sapiens] [gi:20302973]
muscarinic M3 receptor (human)Taxonomy id: 9606
4M4muscarinic acetylcholine receptor m4, partial [Rattus norvegicus] [gi:202666]
muscarinic M4 receptor (rat)Taxonomy id: 10116
5M5muscarinic acetylcholine receptor M5 [Homo sapiens] [gi:20373106]
muscarinic M5 receptor (human)Taxonomy id: 9606

§ Panel component ID.
Protocol
CHO-K1 cells stably transfected with rat M1, human M2/Gqi5, human M3, rat M4/Gqi5, or human M5 were loaded with calcium indicator dye (2mM Fluo-4 AM) for 45-60 min at 37 degrees C. Dye was removed and replaced with assay buffer, pH 7.4 (1X HBSS (Hanks' Balanced Salt Solution), supplemented with 20 mM HEPES and 2.5 mM probenecid). All compounds were serially diluted in assay buffer for a final 2X stock in 0.6% DMSO. This stock was then added to the assay plate for a final DMSO concentration of 0.3%. Acetylcholine EC20 was prepared at a 10X stock solution in assay buffer prior to addition to assay plates. Calcium mobilization was measured at 25 degrees C using a FLEXstation II (Molecular Devices, Sunnyvale, CA) according to the following protocol. Cells were preincubated with test compound (or vehicle) for 1.5 min prior to the addition of the agonist, acetylcholine. Cells were then stimulated for 50 sec with a submaximal concentration (EC20). The signal amplitude was first normalized to baseline and then as a percentage of the maximal response to acetylcholine. EC50 values for each compound were determined using GraphPad Prism (4.0c), which fit curves using standard non-linear regression (variable slope).

These compounds had EC50s less than 10 micromolar for the muscarinic M5 receptor in the calcium flux assay, and therefore, 'Outcome' was assigned as 'Active'. Compound SID 85285464 had no selectivity preference for M5 compared to the other subtypes and was assigned 'Score' of '50'. Compound SID 85285486 was more than 60-fold selective for M5 over the other subtypes, and thus assigned a 'Score' of '100'.
Result Definitions
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TIDNameDescriptionPID§Panel TargetsAnnotationHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1muscarinic M1 receptor (rat) gene_IDmuscarinic M1 receptor (rat) gene_ID1muscarinic acetylcholine receptor m1 [Rattus norvegicus]String
2muscarinic M1 receptor (rat) protein gimuscarinic M1 receptor (rat) protein gi1Protein target giString
3muscarinic M1 receptor (rat) tax_idmuscarinic M1 receptor (rat) tax_id1Target taxonomy IDString
4M1 Conc1 Rep1 (0.01μM**)Value with M1 for replicate 1 at 0.01 micromolar1Float
5M1 Conc2 Rep1 (0.03μM**)Value with M1 for replicate 1 at 0.0316 micromolar1Float
6M1 Conc3 Rep1 (0.1μM**)Value with M1 for replicate 1 at 0.1 micromolar1Float
7M1 Conc4 Rep1 (0.32μM**)Value with M1 for replicate 1 at 0.316 micromolar1Float
8M1 Conc5 Rep1 (1μM**)Value with M1 for replicate 1 at 1 micromolar1Float
9M1 Conc6 Rep1 (3.16μM**)Value with M1 for replicate 1 at 3.16 micromolar1Float
10M1 Conc7 Rep1 (10μM**)Value with M1 for replicate 1 at 10 micromolar1Float
11M1 Conc8 Rep1 (31.6μM**)Value with M1 for replicate 1 at 31.6 micromolar1Float
12M1 Conc1 Rep2 (0.01μM**)Value with M1 for replicate 2 at 0.01 micromolar1Float
13M1 Conc2 Rep2 (0.03μM**)Value with M1 for replicate 2 at 0.0316 micromolar1Float
14M1 Conc3 Rep2 (0.1μM**)Value with M1 for replicate 2 at 0.1 micromolar1Float
15M1 Conc4 Rep2 (0.32μM**)Value with M1 for replicate 2 at 0.316 micromolar1Float
16M1 Conc5 Rep2 (1μM**)Value with M1 for replicate 2 at 1 micromolar1Float
17M1 Conc6 Rep2 (3.16μM**)Value with M1 for replicate 2 at 3.16 micromolar1Float
18M1 Conc7 Rep2 (10μM**)Value with M1 for replicate 2 at 10 micromolar1Float
19M1 Conc8 Rep2 (31.6μM**)Value with M1 for replicate 2 at 31.6 micromolar1Float
20M1 Conc1 Rep3 (0.01μM**)Value with M1 for replicate 3 at 0.01 micromolar1Float
21M1 Conc2 Rep3 (0.03μM**)Value with M1 for replicate 3 at 0.0316 micromolar1Float
22M1 Conc3 Rep3 (0.1μM**)Value with M1 for replicate 3 at 0.1 micromolar1Float
23M1 Conc4 Rep3 (0.32μM**)Value with M1 for replicate 3 at 0.316 micromolar1Float
24M1 Conc5 Rep3 (1μM**)Value with M1 for replicate 3 at 1 micromolar1Float
25M1 Conc6 Rep3 (3.16μM**)Value with M1 for replicate 3 at 3.16 micromolar1Float
26M1 Conc7 Rep3 (10μM**)Value with M1 for replicate 3 at 10 micromolar1Float
27M1 Conc8 Rep3 (31.62μM**)Value with M1 for replicate 3 at 31.6 micromolar1Float
28M1 BottomCalculated Bottom with M11Float
29M1 TopCalculated Top with M11Float
30M1 LogEC50Calculated LogEC50 with M11Float
31M1 HillslopeCalculated Hillslope with M11Float
32M1 EC50Calculated EC50 with M11FloatμM
33M1 Std Error BottomCalculated Std Error Bottom with M11Float
34M1 Std Error TopCalculated Std Error Top with M11Float
35M1 Std Error LogEC50Calculated Std Error LogEC50 with M11Float
36M1 Std Error HillslopeCalculated Std Error Hillslope with M11Float
37M1 95% CI BottomCalculated 95% CI Bottom with M11String
38M1 95% CI TopCalculated 95% CI Top with M11String
39M1 95% CI LogEC50Calculated 95% CI LogEC50 with M11String
40M1 95% CI HillslopeCalculated 95% CI Hillslope with M11String
41M1 95% CI EC50Calculated 95% CI EC50 with M11String
42M1 Deg FreedomCalculated Deg Freedom with M11Integer
43M1 R-SquaredCalculated R-Squared with M11Float
44M1 Abs Sum SquaresCalculated Abs Sum Squares with M11Float
45muscarinic M2 receptor (human) gene_IDmuscarinic M2 receptor (human) gene_ID2muscarinic acetylcholine receptor M2 [Homo sapiens]String
46muscarinic M2 receptor (human) protein gimuscarinic M2 receptor (human) protein gi2Protein target giString
47muscarinic M2 receptor (human) tax_idmuscarinic M2 receptor (human) tax_id2Target taxonomy IDString
48M2 Conc1 Rep1 (0.01μM**)Value with M2 for replicate 1 at 0.01 micromolar2Float
49M2 Conc2 Rep1 (0.03μM**)Value with M2 for replicate 1 at 0.0316 micromolar2Float
50M2 Conc3 Rep1 (0.1μM**)Value with M2 for replicate 1 at 0.1 micromolar2Float
51M2 Conc4 Rep1 (0.32μM**)Value with M2 for replicate 1 at 0.316 micromolar2Float
52M2 Conc5 Rep1 (1μM**)Value with M2 for replicate 1 at 1 micromolar2Float
53M2 Conc6 Rep1 (3.16μM**)Value with M2 for replicate 1 at 3.16 micromolar2Float
54M2 Conc7 Rep1 (10μM**)Value with M2 for replicate 1 at 10 micromolar2Float
55M2 Conc8 Rep1 (31.62μM**)Value with M2 for replicate 1 at 31.6 micromolar2Float
56M2 Conc1 Rep2 (0.01μM**)Value with M2 for replicate 2 at 0.01 micromolar2Float
57M2 Conc2 Rep2 (0.03μM**)Value with M2 for replicate 2 at 0.0316 micromolar2Float
58M2 Conc3 Rep2 (0.1μM**)Value with M2 for replicate 2 at 0.1 micromolar2Float
59M2 Conc4 Rep2 (0.32μM**)Value with M2 for replicate 2 at 0.316 micromolar2Float
60M2 Conc5 Rep2 (1μM**)Value with M2 for replicate 2 at 1 micromolar2Float
61M2 Conc6 Rep2 (3.16μM**)Value with M2 for replicate 2 at 3.16 micromolar2Float
62M2 Conc7 Rep2 (10μM**)Value with M2 for replicate 2 at 10 micromolar2Float
63M2 Conc8 Rep2 (31.62μM**)Value with M2 for replicate 2 at 31.6 micromolar2Float
64M2 Conc1 Rep3 (0.01μM**)Value with M2 for replicate 3 at 0.01 micromolar2Float
65M2 Conc2 Rep3 (0.03μM**)Value with M2 for replicate 3 at 0.0316 micromolar2Float
66M2 Conc3 Rep3 (0.1μM**)Value with M2 for replicate 3 at 0.1 micromolar2Float
67M2 Conc4 Rep3 (0.32μM**)Value with M2 for replicate 3 at 0.316 micromolar2Float
68M2 Conc5 Rep3 (1μM**)Value with M2 for replicate 3 at 1 micromolar2Float
69M2 Conc6 Rep3 (3.16μM**)Value with M2 for replicate 3 at 3.16 micromolar2Float
70M2 Conc7 Rep3 (10μM**)Value with M2 for replicate 3 at 10 micromolar2Float
71M2 Conc8 Rep3 (31.62μM**)Value with M2 for replicate 3 at 31.6 micromolar2Float
72M2 Conc1 Rep4 (0.01μM**)Value with M2 for replicate 4 at 0.01 micromolar2Float
73M2 Conc2 Rep4 (0.03μM**)Value with M2 for replicate 4 at 0.0316 micromolar2Float
74M2 Conc3 Rep4 (0.1μM**)Value with M2 for replicate 4 at 0.1 micromolar2Float
75M2 Conc4 Rep4 (0.32μM**)Value with M2 for replicate 4 at 0.316 micromolar2Float
76M2 Conc5 Rep4 (1μM**)Value with M2 for replicate 4 at 1 micromolar2Float
77M2 Conc6 Rep4 (3.16μM**)Value with M2 for replicate 4 at 3.16 micromolar2Float
78M2 Conc7 Rep4 (10μM**)Value with M2 for replicate 4 at 10 micromolar2Float
79M2 Conc8 Rep4 (31.62μM**)Value with M2 for replicate 4 at 31.6 micromolar2Float
80M2 Conc1 Rep5 (0.01μM**)Value with M2 for replicate 5 at 0.01 micromolar2Float
81M2 Conc2 Rep5 (0.03μM**)Value with M2 for replicate 5 at 0.0316 micromolar2Float
82M2 Conc3 Rep5 (0.1μM**)Value with M2 for replicate 5 at 0.1 micromolar2Float
83M2 Conc4 Rep5 (0.32μM**)Value with M2 for replicate 5 at 0.316 micromolar2Float
84M2 Conc5 Rep5 (1μM**)Value with M2 for replicate 5 at 1 micromolar2Float
85M2 Conc6 Rep5 (3.16μM**)Value with M2 for replicate 5 at 3.16 micromolar2Float
86M2 Conc7 Rep5 (10μM**)Value with M2 for replicate 5 at 10 micromolar2Float
87M2 Conc8 Rep5 (31.62μM**)Value with M2 for replicate 5 at 31.6 micromolar2Float
88M2 CurveComment describing resulting curve fit by Prism2String
89muscarinic M3 receptor (human) gene_IDmuscarinic M3 receptor (human) gene_ID3muscarinic acetylcholine receptor M3 [Homo sapiens]String
90muscarinic M3 receptor (human) protein gimuscarinic M3 receptor (human) protein gi3Protein target giString
91muscarinic M3 receptor (human) tax_idmuscarinic M3 receptor (human) tax_id3Target taxonomy IDString
92M3 Conc1 Rep1 (0.01μM**)Value with M3 for replicate 1 at 0.01 micromolar3Float
93M3 Conc2 Rep1 (0.03μM**)Value with M3 for replicate 1 at 0.0316 micromolar3Float
94M3 Conc3 Rep1 (0.1μM**)Value with M3 for replicate 1 at 0.1 micromolar3Float
95M3 Conc4 Rep1 (0.32μM**)Value with M3 for replicate 1 at 0.316 micromolar3Float
96M3 Conc5 Rep1 (1μM**)Value with M3 for replicate 1 at 1 micromolar3Float
97M3 Conc6 Rep1 (3.16μM**)Value with M3 for replicate 1 at 3.16 micromolar3Float
98M3 Conc7 Rep1 (10μM**)Value with M3 for replicate 1 at 10 micromolar3Float
99M3 Conc8 Rep1 (31.62μM**)Value with M3 for replicate 1 at 31.6 micromolar3Float
100M3 Conc1 Rep2 (0.01μM**)Value with M3 for replicate 2 at 0.01 micromolar3Float
101M3 Conc2 Rep2 (0.03μM**)Value with M3 for replicate 2 at 0.0316 micromolar3Float
102M3 Conc3 Rep2 (0.1μM**)Value with M3 for replicate 2 at 0.1 micromolar3Float
103M3 Conc4 Rep2 (0.32μM**)Value with M3 for replicate 2 at 0.316 micromolar3Float
104M3 Conc5 Rep2 (1μM**)Value with M3 for replicate 2 at 1 micromolar3Float
105M3 Conc6 Rep2 (3.16μM**)Value with M3 for replicate 2 at 3.16 micromolar3Float
106M3 Conc7 Rep2 (10μM**)Value with M3 for replicate 2 at 10 micromolar3Float
107M3 Conc8 Rep2 (31.62μM**)Value with M3 for replicate 2 at 31.6 micromolar3Float
108M3 Conc1 Rep3 (0.01μM**)Value with M3 for replicate 3 at 0.01 micromolar3Float
109M3 Conc2 Rep3 (0.03μM**)Value with M3 for replicate 3 at 0.0316 micromolar3Float
110M3 Conc3 Rep3 (0.1μM**)Value with M3 for replicate 3 at 0.1 micromolar3Float
111M3 Conc4 Rep3 (0.32μM**)Value with M3 for replicate 3 at 0.316 micromolar3Float
112M3 Conc5 Rep3 (1μM**)Value with M3 for replicate 3 at 1 micromolar3Float
113M3 Conc6 Rep3 (3.16μM**)Value with M3 for replicate 3 at 3.16 micromolar3Float
114M3 Conc7 Rep3 (10μM**)Value with M3 for replicate 3 at 10 micromolar3Float
115M3 Conc8 Rep3 (31.62μM**)Value with M3 for replicate 3 at 31.6 micromolar3Float
116M3 Conc1 Rep4 (0.01μM**)Value with M3 for replicate 4 at 0.01 micromolar3Float
117M3 Conc2 Rep4 (0.03μM**)Value with M3 for replicate 4 at 0.0316 micromolar3Float
118M3 Conc3 Rep4 (0.1μM**)Value with M3 for replicate 4 at 0.1 micromolar3Float
119M3 Conc4 Rep4 (0.32μM**)Value with M3 for replicate 4 at 0.316 micromolar3Float
120M3 Conc5 Rep4 (1μM**)Value with M3 for replicate 4 at 1 micromolar3Float
121M3 Conc6 Rep4 (3.16μM**)Value with M3 for replicate 4 at 3.16 micromolar3Float
122M3 Conc7 Rep4 (10μM**)Value with M3 for replicate 4 at 10 micromolar3Float
123M3 Conc8 Rep4 (31.62μM**)Value with M3 for replicate 4 at 31.6 micromolar3Float
124M3 BottomCalculated Bottom with M33Float
125M3 TopCalculated Top with M33Float
126M3 LogEC50Calculated LogEC50 with M33Float
127M3 HillslopeCalculated Hillslope with M33Float
128M3 EC50Calculated EC50 with M33FloatμM
129M3 Std Error BottomCalculated Std Error Bottom with M33Float
130M3 Std Error TopCalculated Std Error Top with M33Float
131M3 Std Error LogEC50Calculated Std Error LogEC50 with M33Float
132M3 Std Error HillslopeCalculated Std Error Hillslope with M33Float
133M3 95% CI BottomCalculated 95% CI Bottom with M33String
134M3 95% CI TopCalculated 95% CI Top with M33String
135M3 95% CI LogEC50Calculated 95% CI LogEC50 with M33String
136M3 95% CI HillslopeCalculated 95% CI Hillslope with M33String
137M3 95% CI EC50Calculated 95% CI EC50 with M33String
138M3 Deg FreedomCalculated Deg Freedom with M33Integer
139M3 R-SquaredCalculated R-Squared with M33Float
140M3 Abs Sum SquaresCalculated Abs Sum Squares with M33Float
141muscarinic M4 receptor (rat) gene_IDmuscarinic M4 receptor (rat) gene_ID4muscarinic acetylcholine receptor m4, partial [Rattus norvegicus]String
142muscarinic M4 receptor (rat) protein gimuscarinic M4 receptor (rat) protein gi4Protein target giString
143muscarinic M4 receptor (rat) tax_idmuscarinic M4 receptor (rat) tax_id4Target taxonomy IDString
144M4 Conc1 Rep1 (0.01μM**)Value with M4 for replicate 1 at 0.01 micromolar4Float
145M4 Conc2 Rep1 (0.03μM**)Value with M4 for replicate 1 at 0.0316 micromolar4Float
146M4 Conc3 Rep1 (0.1μM**)Value with M4 for replicate 1 at 0.1 micromolar4Float
147M4 Conc4 Rep1 (0.32μM**)Value with M4 for replicate 1 at 0.316 micromolar4Float
148M4 Conc5 Rep1 (1μM**)Value with M4 for replicate 1 at 1 micromolar4Float
149M4 Conc6 Rep1 (3.16μM**)Value with M4 for replicate 1 at 3.16 micromolar4Float
150M4 Conc7 Rep1 (10μM**)Value with M4 for replicate 1 at 10 micromolar4Float
151M4 Conc8 Rep1 (31.62μM**)Value with M4 for replicate 1 at 31.6 micromolar4Float
152M4 Conc1 Rep2 (0.01μM**)Value with M4 for replicate 2 at 0.01 micromolar4Float
153M4 Conc2 Rep2 (0.03μM**)Value with M4 for replicate 2 at 0.0316 micromolar4Float
154M4 Conc3 Rep2 (0.1μM**)Value with M4 for replicate 2 at 0.1 micromolar4Float
155M4 Conc4 Rep2 (0.32μM**)Value with M4 for replicate 2 at 0.316 micromolar4Float
156M4 Conc5 Rep2 (1μM**)Value with M4 for replicate 2 at 1 micromolar4Float
157M4 Conc6 Rep2 (3.16μM**)Value with M4 for replicate 2 at 3.16 micromolar4Float
158M4 Conc7 Rep2 (10μM**)Value with M4 for replicate 2 at 10 micromolar4Float
159M4 Conc8 Rep2 (31.62μM**)Value with M4 for replicate 2 at 31.6 micromolar4Float
160M4 Conc1 Rep3 (0.01μM**)Value with M4 for replicate 3 at 0.01 micromolar4Float
161M4 Conc2 Rep3 (0.03μM**)Value with M4 for replicate 3 at 0.0316 micromolar4Float
162M4 Conc3 Rep3 (0.1μM**)Value with M4 for replicate 3 at 0.1 micromolar4Float
163M4 Conc4 Rep3 (0.32μM**)Value with M4 for replicate 3 at 0.316 micromolar4Float
164M4 Conc5 Rep3 (1μM**)Value with M4 for replicate 3 at 1 micromolar4Float
165M4 Conc6 Rep3 (3.16μM**)Value with M4 for replicate 3 at 3.16 micromolar4Float
166M4 Conc7 Rep3 (10μM**)Value with M4 for replicate 3 at 10 micromolar4Float
167M4 Conc8 Rep3 (31.62μM**)Value with M4 for replicate 3 at 31.6 micromolar4Float
168M4 Conc1 Rep4 (0.01μM**)Value with M4 for replicate 4 at 0.01 micromolar4Float
169M4 Conc2 Rep4 (0.03μM**)Value with M4 for replicate 4 at 0.0316 micromolar4Float
170M4 Conc3 Rep4 (0.1μM**)Value with M4 for replicate 4 at 0.1 micromolar4Float
171M4 Conc4 Rep4 (0.32μM**)Value with M4 for replicate 4 at 0.316 micromolar4Float
172M4 Conc5 Rep4 (1μM**)Value with M4 for replicate 4 at 1 micromolar4Float
173M4 Conc6 Rep4 (3.16μM**)Value with M4 for replicate 4 at 3.16 micromolar4Float
174M4 Conc7 Rep4 (10μM**)Value with M4 for replicate 4 at 10 micromolar4Float
175M4 Conc8 Rep4 (31.62μM**)Value with M4 for replicate 4 at 31.6 micromolar4Float
176M4 CurveComment describing resulting curve fit by Prism4String
177muscarinic M5 receptor (human) gene_IDmuscarinic M5 receptor (human) gene_ID5muscarinic acetylcholine receptor M5 [Homo sapiens]String
178muscarinic M5 receptor (human) protein gimuscarinic M5 receptor (human) protein gi5Protein target giString
179muscarinic M5 receptor (human) tax_idmuscarinic M5 receptor (human) tax_id5Float
180M5 Conc1 Rep1 (0.01μM**)Value with M5 for replicate 1 at 0.01 micromolar5Float
181M5 Conc2 Rep1 (0.03μM**)Value with M5 for replicate 1 at 0.0316 micromolar5Float
182M5 Conc3 Rep1 (0.1μM**)Value with M5 for replicate 1 at 0.1 micromolar5Float
183M5 Conc4 Rep1 (0.32μM**)Value with M5 for replicate 1 at 0.316 micromolar5Float
184M5 Conc5 Rep1 (1μM**)Value with M5 for replicate 1 at 1 micromolar5Float
185M5 Conc6 Rep1 (3.16μM**)Value with M5 for replicate 1 at 3.16 micromolar5Float
186M5 Conc7 Rep1 (10μM**)Value with M5 for replicate 1 at 10 micromolar5Float
187M5 Conc8 Rep1 (31.62μM**)Value with M5 for replicate 1 at 31.6 micromolar5Float
188M5 Conc1 Rep2 (0.01μM**)Value with M5 for replicate 2 at 0.01 micromolar5Float
189M5 Conc2 Rep2 (0.03μM**)Value with M5 for replicate 2 at 0.0316 micromolar5Float
190M5 Conc3 Rep2 (0.1μM**)Value with M5 for replicate 2 at 0.1 micromolar5Float
191M5 Conc4 Rep2 (0.32μM**)Value with M5 for replicate 2 at 0.316 micromolar5Float
192M5 Conc5 Rep2 (1μM**)Value with M5 for replicate 2 at 1 micromolar5Float
193M5 Conc6 Rep2 (3.16μM**)Value with M5 for replicate 2 at 3.16 micromolar5Float
194M5 Conc7 Rep2 (10μM**)Value with M5 for replicate 2 at 10 micromolar5Float
195M5 Conc8 Rep2 (31.62μM**)Value with M5 for replicate 2 at 31.6 micromolar5Float
196M5 Conc1 Rep3 (0.01μM**)Value with M5 for replicate 3 at 0.01 micromolar5Float
197M5 Conc2 Rep3 (0.03μM**)Value with M5 for replicate 3 at 0.0316 micromolar5Float
198M5 Conc3 Rep3 (0.1μM**)Value with M5 for replicate 3 at 0.1 micromolar5Float
199M5 Conc4 Rep3 (0.32μM**)Value with M5 for replicate 3 at 0.316 micromolar5Float
200M5 Conc5 Rep3 (1μM**)Value with M5 for replicate 3 at 1 micromolar5Float
201M5 Conc6 Rep3 (3.16μM**)Value with M5 for replicate 3 at 3.16 micromolar5Float
202M5 Conc7 Rep3 (10μM**)Value with M5 for replicate 3 at 10 micromolar5Float
203M5 Conc8 Rep3 (31.62μM**)Value with M5 for replicate 3 at 31.6 micromolar5Float
204M5 Conc1 Rep4 (0.01μM**)Value with M5 for replicate 4 at 0.01 micromolar5Float
205M5 Conc2 Rep4 (0.03μM**)Value with M5 for replicate 4 at 0.0316 micromolar5Float
206M5 Conc3 Rep4 (0.1μM**)Value with M5 for replicate 4 at 0.1 micromolar5Float
207M5 Conc4 Rep4 (0.32μM**)Value with M5 for replicate 4 at 0.316 micromolar5Float
208M5 Conc5 Rep4 (1μM**)Value with M5 for replicate 4 at 1 micromolar5Float
209M5 Conc6 Rep4 (3.16μM**)Value with M5 for replicate 4 at 3.16 micromolar5Float
210M5 Conc7 Rep4 (10μM**)Value with M5 for replicate 4 at 10 micromolar5Float
211M5 Conc8 Rep4 (31.62μM**)Value with M5 for replicate 4 at 31.6 micromolar5Float
212M5 Conc1 Rep5 (0.01μM**)Value with M5 for replicate 5 at 0.01 micromolar5Float
213M5 Conc2 Rep5 (0.03μM**)Value with M5 for replicate 5 at 0.0316 micromolar5Float
214M5 Conc3 Rep5 (0.1μM**)Value with M5 for replicate 5 at 0.1 micromolar5Float
215M5 Conc4 Rep5 (0.32μM**)Value with M5 for replicate 5 at 0.316 micromolar5Float
216M5 Conc5 Rep5 (1μM**)Value with M5 for replicate 5 at 1 micromolar5Float
217M5 Conc6 Rep5 (3.16μM**)Value with M5 for replicate 5 at 3.16 micromolar5Float
218M5 Conc7 Rep5 (10μM**)Value with M5 for replicate 5 at 10 micromolar5Float
219M5 Conc8 Rep5 (31.62μM**)Value with M5 for replicate 5 at 31.6 micromolar5Float
220M5 BottomCalculated Bottom with M55Float
221M5 TopCalculated Top with M55Float
222M5 LogEC50Calculated LogEC50 with M55Float
223M5 HillslopeCalculated Hillslope with M55Float
224M5 EC50*Calculated EC50 with M55FloatμM
225M5 Std Error BottomCalculated Std Error Bottom with M55Float
226M5 Std Error TopCalculated Std Error Top with M55Float
227M5 Std Error LogEC50Calculated Std Error LogEC50 with M55Float
228M5 Std Error HillslopeCalculated Std Error Hillslope with M55Float
229M5 95% CI BottomCalculated 95% CI Bottom with M55String
230M5 95% CI TopCalculated 95% CI Top with M55String
231M5 95% CI LogEC50Calculated 95% CI LogEC50 with M55String
232M5 95% CI HillslopeCalculated 95% CI Hillslope with M55String
233M5 95% CI EC50Calculated 95% CI EC50 with M55String
234M5 Deg FreedomCalculated Deg Freedom with M55Integer
235M5 R-SquaredCalculated R-Squared with M55Float
236M5 Abs Sum SquaresCalculated Abs Sum Squares with M55Float

RNAi Target. * Activity Concentration. ** Test Concentration. § Panel component ID.
Additional Information
Grant Number: MH077606

Classification
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