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 ..
Related BioAssays
Related BioAssays
Target
BioActive Compounds: 11
Depositor Specified Assays
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.
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
Calcium Assay Dose-Response for M5 Positive Allosteric Modulator (PAM)
§ Panel component ID.
| Data Table(Active) Data Table(All) | Show more |
| PID§ | Name | Substance | Panel Targets | Description | Additional Information | ||
|---|---|---|---|---|---|---|---|
| Active | Inactive | ||||||
| 1 | M1 | muscarinic M1 receptor (rat) [gi:202660] | muscarinic M1 receptor (rat) | Taxonomy id: 10116 | |||
| 2 | M2 | muscarinic M2 receptor (human) [gi:20302971] | muscarinic M2 receptor (human) | Taxonomy id: 9606 | |||
| 3 | M3 | muscarinic M3 receptor (human) [gi:20302973] | muscarinic M3 receptor (human) | Taxonomy id: 9606 | |||
| 4 | M4 | muscarinic M4 receptor (rat) [gi:202666] | muscarinic M4 receptor (rat) | Taxonomy id: 10116 | |||
| 5 | M5 | muscarinic M5 receptor (human) [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'.
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
| Show more |
| TID | Name | Description | PID§ | Panel Targets | Annotation | Histogram | Type | Unit |
|---|---|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||||
| Score | The BioAssay activity ranking score |  | Integer | |||||
| 1 | muscarinic M1 receptor (rat) gene_ID† | muscarinic M1 receptor (rat) gene_ID | 1 | muscarinic M1 receptor (rat) | String | |||
| 2 | muscarinic M1 receptor (rat) protein gi | muscarinic M1 receptor (rat) protein gi | 1 | Protein target gi | String | |||
| 3 | muscarinic M1 receptor (rat) tax_id | muscarinic M1 receptor (rat) tax_id | 1 | Target taxonomy ID | String | |||
| 4 | M1 Conc1 Rep1 (0.01μM**) | Value with M1 for replicate 1 at 0.01 micromolar | 1 | | Float | |||
| 5 | M1 Conc2 Rep1 (0.03μM**) | Value with M1 for replicate 1 at 0.0316 micromolar | 1 | | Float | |||
| 6 | M1 Conc3 Rep1 (0.1μM**) | Value with M1 for replicate 1 at 0.1 micromolar | 1 | | Float | |||
| 7 | M1 Conc4 Rep1 (0.32μM**) | Value with M1 for replicate 1 at 0.316 micromolar | 1 | | Float | |||
| 8 | M1 Conc5 Rep1 (1μM**) | Value with M1 for replicate 1 at 1 micromolar | 1 | | Float | |||
| 9 | M1 Conc6 Rep1 (3.16μM**) | Value with M1 for replicate 1 at 3.16 micromolar | 1 | | Float | |||
| 10 | M1 Conc7 Rep1 (10μM**) | Value with M1 for replicate 1 at 10 micromolar | 1 | | Float | |||
| 11 | M1 Conc8 Rep1 (31.6μM**) | Value with M1 for replicate 1 at 31.6 micromolar | 1 | | Float | |||
| 12 | M1 Conc1 Rep2 (0.01μM**) | Value with M1 for replicate 2 at 0.01 micromolar | 1 | | Float | |||
| 13 | M1 Conc2 Rep2 (0.03μM**) | Value with M1 for replicate 2 at 0.0316 micromolar | 1 | | Float | |||
| 14 | M1 Conc3 Rep2 (0.1μM**) | Value with M1 for replicate 2 at 0.1 micromolar | 1 | | Float | |||
| 15 | M1 Conc4 Rep2 (0.32μM**) | Value with M1 for replicate 2 at 0.316 micromolar | 1 | | Float | |||
| 16 | M1 Conc5 Rep2 (1μM**) | Value with M1 for replicate 2 at 1 micromolar | 1 | | Float | |||
| 17 | M1 Conc6 Rep2 (3.16μM**) | Value with M1 for replicate 2 at 3.16 micromolar | 1 | | Float | |||
| 18 | M1 Conc7 Rep2 (10μM**) | Value with M1 for replicate 2 at 10 micromolar | 1 | | Float | |||
| 19 | M1 Conc8 Rep2 (31.6μM**) | Value with M1 for replicate 2 at 31.6 micromolar | 1 | | Float | |||
| 20 | M1 Conc1 Rep3 (0.01μM**) | Value with M1 for replicate 3 at 0.01 micromolar | 1 | | Float | |||
| 21 | M1 Conc2 Rep3 (0.03μM**) | Value with M1 for replicate 3 at 0.0316 micromolar | 1 | | Float | |||
| 22 | M1 Conc3 Rep3 (0.1μM**) | Value with M1 for replicate 3 at 0.1 micromolar | 1 | | Float | |||
| 23 | M1 Conc4 Rep3 (0.32μM**) | Value with M1 for replicate 3 at 0.316 micromolar | 1 | | Float | |||
| 24 | M1 Conc5 Rep3 (1μM**) | Value with M1 for replicate 3 at 1 micromolar | 1 | | Float | |||
| 25 | M1 Conc6 Rep3 (3.16μM**) | Value with M1 for replicate 3 at 3.16 micromolar | 1 | | Float | |||
| 26 | M1 Conc7 Rep3 (10μM**) | Value with M1 for replicate 3 at 10 micromolar | 1 | | Float | |||
| 27 | M1 Conc8 Rep3 (31.62μM**) | Value with M1 for replicate 3 at 31.6 micromolar | 1 | | Float | |||
| 28 | M1 Bottom | Calculated Bottom with M1 | 1 | | Float | |||
| 29 | M1 Top | Calculated Top with M1 | 1 | | Float | |||
| 30 | M1 LogEC50 | Calculated LogEC50 with M1 | 1 | | Float | |||
| 31 | M1 Hillslope | Calculated Hillslope with M1 | 1 | | Float | |||
| 32 | M1 EC50 | Calculated EC50 with M1 | 1 | | Float | μM | ||
| 33 | M1 Std Error Bottom | Calculated Std Error Bottom with M1 | 1 | | Float | |||
| 34 | M1 Std Error Top | Calculated Std Error Top with M1 | 1 | | Float | |||
| 35 | M1 Std Error LogEC50 | Calculated Std Error LogEC50 with M1 | 1 | | Float | |||
| 36 | M1 Std Error Hillslope | Calculated Std Error Hillslope with M1 | 1 | | Float | |||
| 37 | M1 95% CI Bottom | Calculated 95% CI Bottom with M1 | 1 | String | ||||
| 38 | M1 95% CI Top | Calculated 95% CI Top with M1 | 1 | String | ||||
| 39 | M1 95% CI LogEC50 | Calculated 95% CI LogEC50 with M1 | 1 | String | ||||
| 40 | M1 95% CI Hillslope | Calculated 95% CI Hillslope with M1 | 1 | String | ||||
| 41 | M1 95% CI EC50 | Calculated 95% CI EC50 with M1 | 1 | String | ||||
| 42 | M1 Deg Freedom | Calculated Deg Freedom with M1 | 1 | | Integer | |||
| 43 | M1 R-Squared | Calculated R-Squared with M1 | 1 | | Float | |||
| 44 | M1 Abs Sum Squares | Calculated Abs Sum Squares with M1 | 1 | | Float | |||
| 45 | muscarinic M2 receptor (human) gene_ID† | muscarinic M2 receptor (human) gene_ID | 1 | String | ||||
| 46 | muscarinic M2 receptor (human) protein gi | muscarinic M2 receptor (human) protein gi | 2 | muscarinic M2 receptor (human) | Protein target gi | String | ||
| 47 | muscarinic M2 receptor (human) tax_id | muscarinic M2 receptor (human) tax_id | 2 | Target taxonomy ID | String | |||
| 48 | M2 Conc1 Rep1 (0.01μM**) | Value with M2 for replicate 1 at 0.01 micromolar | 2 | | Float | |||
| 49 | M2 Conc2 Rep1 (0.03μM**) | Value with M2 for replicate 1 at 0.0316 micromolar | 2 | | Float | |||
| 50 | M2 Conc3 Rep1 (0.1μM**) | Value with M2 for replicate 1 at 0.1 micromolar | 2 | | Float | |||
| 51 | M2 Conc4 Rep1 (0.32μM**) | Value with M2 for replicate 1 at 0.316 micromolar | 2 | | Float | |||
| 52 | M2 Conc5 Rep1 (1μM**) | Value with M2 for replicate 1 at 1 micromolar | 2 | | Float | |||
| 53 | M2 Conc6 Rep1 (3.16μM**) | Value with M2 for replicate 1 at 3.16 micromolar | 2 | | Float | |||
| 54 | M2 Conc7 Rep1 (10μM**) | Value with M2 for replicate 1 at 10 micromolar | 2 | | Float | |||
| 55 | M2 Conc8 Rep1 (31.62μM**) | Value with M2 for replicate 1 at 31.6 micromolar | 2 | | Float | |||
| 56 | M2 Conc1 Rep2 (0.01μM**) | Value with M2 for replicate 2 at 0.01 micromolar | 2 | | Float | |||
| 57 | M2 Conc2 Rep2 (0.03μM**) | Value with M2 for replicate 2 at 0.0316 micromolar | 2 | | Float | |||
| 58 | M2 Conc3 Rep2 (0.1μM**) | Value with M2 for replicate 2 at 0.1 micromolar | 2 | | Float | |||
| 59 | M2 Conc4 Rep2 (0.32μM**) | Value with M2 for replicate 2 at 0.316 micromolar | 2 | | Float | |||
| 60 | M2 Conc5 Rep2 (1μM**) | Value with M2 for replicate 2 at 1 micromolar | 2 | | Float | |||
| 61 | M2 Conc6 Rep2 (3.16μM**) | Value with M2 for replicate 2 at 3.16 micromolar | 2 | | Float | |||
| 62 | M2 Conc7 Rep2 (10μM**) | Value with M2 for replicate 2 at 10 micromolar | 2 | | Float | |||
| 63 | M2 Conc8 Rep2 (31.62μM**) | Value with M2 for replicate 2 at 31.6 micromolar | 2 | | Float | |||
| 64 | M2 Conc1 Rep3 (0.01μM**) | Value with M2 for replicate 3 at 0.01 micromolar | 2 | | Float | |||
| 65 | M2 Conc2 Rep3 (0.03μM**) | Value with M2 for replicate 3 at 0.0316 micromolar | 2 | | Float | |||
| 66 | M2 Conc3 Rep3 (0.1μM**) | Value with M2 for replicate 3 at 0.1 micromolar | 2 | | Float | |||
| 67 | M2 Conc4 Rep3 (0.32μM**) | Value with M2 for replicate 3 at 0.316 micromolar | 2 | | Float | |||
| 68 | M2 Conc5 Rep3 (1μM**) | Value with M2 for replicate 3 at 1 micromolar | 2 | | Float | |||
| 69 | M2 Conc6 Rep3 (3.16μM**) | Value with M2 for replicate 3 at 3.16 micromolar | 2 | | Float | |||
| 70 | M2 Conc7 Rep3 (10μM**) | Value with M2 for replicate 3 at 10 micromolar | 2 | | Float | |||
| 71 | M2 Conc8 Rep3 (31.62μM**) | Value with M2 for replicate 3 at 31.6 micromolar | 2 | | Float | |||
| 72 | M2 Conc1 Rep4 (0.01μM**) | Value with M2 for replicate 4 at 0.01 micromolar | 2 | | Float | |||
| 73 | M2 Conc2 Rep4 (0.03μM**) | Value with M2 for replicate 4 at 0.0316 micromolar | 2 | | Float | |||
| 74 | M2 Conc3 Rep4 (0.1μM**) | Value with M2 for replicate 4 at 0.1 micromolar | 2 | | Float | |||
| 75 | M2 Conc4 Rep4 (0.32μM**) | Value with M2 for replicate 4 at 0.316 micromolar | 2 | | Float | |||
| 76 | M2 Conc5 Rep4 (1μM**) | Value with M2 for replicate 4 at 1 micromolar | 2 | | Float | |||
| 77 | M2 Conc6 Rep4 (3.16μM**) | Value with M2 for replicate 4 at 3.16 micromolar | 2 | | Float | |||
| 78 | M2 Conc7 Rep4 (10μM**) | Value with M2 for replicate 4 at 10 micromolar | 2 | | Float | |||
| 79 | M2 Conc8 Rep4 (31.62μM**) | Value with M2 for replicate 4 at 31.6 micromolar | 2 | | Float | |||
| 80 | M2 Conc1 Rep5 (0.01μM**) | Value with M2 for replicate 5 at 0.01 micromolar | 2 | | Float | |||
| 81 | M2 Conc2 Rep5 (0.03μM**) | Value with M2 for replicate 5 at 0.0316 micromolar | 2 | | Float | |||
| 82 | M2 Conc3 Rep5 (0.1μM**) | Value with M2 for replicate 5 at 0.1 micromolar | 2 | | Float | |||
| 83 | M2 Conc4 Rep5 (0.32μM**) | Value with M2 for replicate 5 at 0.316 micromolar | 2 | | Float | |||
| 84 | M2 Conc5 Rep5 (1μM**) | Value with M2 for replicate 5 at 1 micromolar | 2 | | Float | |||
| 85 | M2 Conc6 Rep5 (3.16μM**) | Value with M2 for replicate 5 at 3.16 micromolar | 2 | | Float | |||
| 86 | M2 Conc7 Rep5 (10μM**) | Value with M2 for replicate 5 at 10 micromolar | 2 | | Float | |||
| 87 | M2 Conc8 Rep5 (31.62μM**) | Value with M2 for replicate 5 at 31.6 micromolar | 2 | | Float | |||
| 88 | M2 Curve | Comment describing resulting curve fit by Prism | 2 | String | ||||
| 89 | muscarinic M3 receptor (human) gene_ID† | muscarinic M3 receptor (human) gene_ID | 3 | muscarinic M3 receptor (human) | String | |||
| 90 | muscarinic M3 receptor (human) protein gi | muscarinic M3 receptor (human) protein gi | 3 | Protein target gi | String | |||
| 91 | muscarinic M3 receptor (human) tax_id | muscarinic M3 receptor (human) tax_id | 3 | Target taxonomy ID | String | |||
| 92 | M3 Conc1 Rep1 (0.01μM**) | Value with M3 for replicate 1 at 0.01 micromolar | 3 | | Float | |||
| 93 | M3 Conc2 Rep1 (0.03μM**) | Value with M3 for replicate 1 at 0.0316 micromolar | 3 | | Float | |||
| 94 | M3 Conc3 Rep1 (0.1μM**) | Value with M3 for replicate 1 at 0.1 micromolar | 3 | | Float | |||
| 95 | M3 Conc4 Rep1 (0.32μM**) | Value with M3 for replicate 1 at 0.316 micromolar | 3 | | Float | |||
| 96 | M3 Conc5 Rep1 (1μM**) | Value with M3 for replicate 1 at 1 micromolar | 3 | | Float | |||
| 97 | M3 Conc6 Rep1 (3.16μM**) | Value with M3 for replicate 1 at 3.16 micromolar | 3 | | Float | |||
| 98 | M3 Conc7 Rep1 (10μM**) | Value with M3 for replicate 1 at 10 micromolar | 3 | | Float | |||
| 99 | M3 Conc8 Rep1 (31.62μM**) | Value with M3 for replicate 1 at 31.6 micromolar | 3 | | Float | |||
| 100 | M3 Conc1 Rep2 (0.01μM**) | Value with M3 for replicate 2 at 0.01 micromolar | 3 | | Float | |||
| 101 | M3 Conc2 Rep2 (0.03μM**) | Value with M3 for replicate 2 at 0.0316 micromolar | 3 | | Float | |||
| 102 | M3 Conc3 Rep2 (0.1μM**) | Value with M3 for replicate 2 at 0.1 micromolar | 3 | | Float | |||
| 103 | M3 Conc4 Rep2 (0.32μM**) | Value with M3 for replicate 2 at 0.316 micromolar | 3 | | Float | |||
| 104 | M3 Conc5 Rep2 (1μM**) | Value with M3 for replicate 2 at 1 micromolar | 3 | | Float | |||
| 105 | M3 Conc6 Rep2 (3.16μM**) | Value with M3 for replicate 2 at 3.16 micromolar | 3 | | Float | |||
| 106 | M3 Conc7 Rep2 (10μM**) | Value with M3 for replicate 2 at 10 micromolar | 3 | | Float | |||
| 107 | M3 Conc8 Rep2 (31.62μM**) | Value with M3 for replicate 2 at 31.6 micromolar | 3 | | Float | |||
| 108 | M3 Conc1 Rep3 (0.01μM**) | Value with M3 for replicate 3 at 0.01 micromolar | 3 | | Float | |||
| 109 | M3 Conc2 Rep3 (0.03μM**) | Value with M3 for replicate 3 at 0.0316 micromolar | 3 | | Float | |||
| 110 | M3 Conc3 Rep3 (0.1μM**) | Value with M3 for replicate 3 at 0.1 micromolar | 3 | | Float | |||
| 111 | M3 Conc4 Rep3 (0.32μM**) | Value with M3 for replicate 3 at 0.316 micromolar | 3 | | Float | |||
| 112 | M3 Conc5 Rep3 (1μM**) | Value with M3 for replicate 3 at 1 micromolar | 3 | | Float | |||
| 113 | M3 Conc6 Rep3 (3.16μM**) | Value with M3 for replicate 3 at 3.16 micromolar | 3 | | Float | |||
| 114 | M3 Conc7 Rep3 (10μM**) | Value with M3 for replicate 3 at 10 micromolar | 3 | | Float | |||
| 115 | M3 Conc8 Rep3 (31.62μM**) | Value with M3 for replicate 3 at 31.6 micromolar | 3 | | Float | |||
| 116 | M3 Conc1 Rep4 (0.01μM**) | Value with M3 for replicate 4 at 0.01 micromolar | 3 | | Float | |||
| 117 | M3 Conc2 Rep4 (0.03μM**) | Value with M3 for replicate 4 at 0.0316 micromolar | 3 | | Float | |||
| 118 | M3 Conc3 Rep4 (0.1μM**) | Value with M3 for replicate 4 at 0.1 micromolar | 3 | | Float | |||
| 119 | M3 Conc4 Rep4 (0.32μM**) | Value with M3 for replicate 4 at 0.316 micromolar | 3 | | Float | |||
| 120 | M3 Conc5 Rep4 (1μM**) | Value with M3 for replicate 4 at 1 micromolar | 3 | | Float | |||
| 121 | M3 Conc6 Rep4 (3.16μM**) | Value with M3 for replicate 4 at 3.16 micromolar | 3 | | Float | |||
| 122 | M3 Conc7 Rep4 (10μM**) | Value with M3 for replicate 4 at 10 micromolar | 3 | | Float | |||
| 123 | M3 Conc8 Rep4 (31.62μM**) | Value with M3 for replicate 4 at 31.6 micromolar | 3 | | Float | |||
| 124 | M3 Bottom | Calculated Bottom with M3 | 3 | | Float | |||
| 125 | M3 Top | Calculated Top with M3 | 3 | | Float | |||
| 126 | M3 LogEC50 | Calculated LogEC50 with M3 | 3 | | Float | |||
| 127 | M3 Hillslope | Calculated Hillslope with M3 | 3 | | Float | |||
| 128 | M3 EC50 | Calculated EC50 with M3 | 3 | | Float | μM | ||
| 129 | M3 Std Error Bottom | Calculated Std Error Bottom with M3 | 3 | | Float | |||
| 130 | M3 Std Error Top | Calculated Std Error Top with M3 | 3 | | Float | |||
| 131 | M3 Std Error LogEC50 | Calculated Std Error LogEC50 with M3 | 3 | | Float | |||
| 132 | M3 Std Error Hillslope | Calculated Std Error Hillslope with M3 | 3 | | Float | |||
| 133 | M3 95% CI Bottom | Calculated 95% CI Bottom with M3 | 3 | String | ||||
| 134 | M3 95% CI Top | Calculated 95% CI Top with M3 | 3 | String | ||||
| 135 | M3 95% CI LogEC50 | Calculated 95% CI LogEC50 with M3 | 3 | String | ||||
| 136 | M3 95% CI Hillslope | Calculated 95% CI Hillslope with M3 | 3 | String | ||||
| 137 | M3 95% CI EC50 | Calculated 95% CI EC50 with M3 | 3 | String | ||||
| 138 | M3 Deg Freedom | Calculated Deg Freedom with M3 | 3 | | Integer | |||
| 139 | M3 R-Squared | Calculated R-Squared with M3 | 3 | | Float | |||
| 140 | M3 Abs Sum Squares | Calculated Abs Sum Squares with M3 | 3 | | Float | |||
| 141 | muscarinic M4 receptor (rat) gene_ID† | muscarinic M4 receptor (rat) gene_ID | 4 | muscarinic M4 receptor (rat) | String | |||
| 142 | muscarinic M4 receptor (rat) protein gi | muscarinic M4 receptor (rat) protein gi | 4 | Protein target gi | String | |||
| 143 | muscarinic M4 receptor (rat) tax_id | muscarinic M4 receptor (rat) tax_id | 4 | Target taxonomy ID | String | |||
| 144 | M4 Conc1 Rep1 (0.01μM**) | Value with M4 for replicate 1 at 0.01 micromolar | 4 | | Float | |||
| 145 | M4 Conc2 Rep1 (0.03μM**) | Value with M4 for replicate 1 at 0.0316 micromolar | 4 | | Float | |||
| 146 | M4 Conc3 Rep1 (0.1μM**) | Value with M4 for replicate 1 at 0.1 micromolar | 4 | | Float | |||
| 147 | M4 Conc4 Rep1 (0.32μM**) | Value with M4 for replicate 1 at 0.316 micromolar | 4 | | Float | |||
| 148 | M4 Conc5 Rep1 (1μM**) | Value with M4 for replicate 1 at 1 micromolar | 4 | | Float | |||
| 149 | M4 Conc6 Rep1 (3.16μM**) | Value with M4 for replicate 1 at 3.16 micromolar | 4 | | Float | |||
| 150 | M4 Conc7 Rep1 (10μM**) | Value with M4 for replicate 1 at 10 micromolar | 4 | | Float | |||
| 151 | M4 Conc8 Rep1 (31.62μM**) | Value with M4 for replicate 1 at 31.6 micromolar | 4 | | Float | |||
| 152 | M4 Conc1 Rep2 (0.01μM**) | Value with M4 for replicate 2 at 0.01 micromolar | 4 | | Float | |||
| 153 | M4 Conc2 Rep2 (0.03μM**) | Value with M4 for replicate 2 at 0.0316 micromolar | 4 | | Float | |||
| 154 | M4 Conc3 Rep2 (0.1μM**) | Value with M4 for replicate 2 at 0.1 micromolar | 4 | | Float | |||
| 155 | M4 Conc4 Rep2 (0.32μM**) | Value with M4 for replicate 2 at 0.316 micromolar | 4 | | Float | |||
| 156 | M4 Conc5 Rep2 (1μM**) | Value with M4 for replicate 2 at 1 micromolar | 4 | | Float | |||
| 157 | M4 Conc6 Rep2 (3.16μM**) | Value with M4 for replicate 2 at 3.16 micromolar | 4 | | Float | |||
| 158 | M4 Conc7 Rep2 (10μM**) | Value with M4 for replicate 2 at 10 micromolar | 4 | | Float | |||
| 159 | M4 Conc8 Rep2 (31.62μM**) | Value with M4 for replicate 2 at 31.6 micromolar | 4 | | Float | |||
| 160 | M4 Conc1 Rep3 (0.01μM**) | Value with M4 for replicate 3 at 0.01 micromolar | 4 | | Float | |||
| 161 | M4 Conc2 Rep3 (0.03μM**) | Value with M4 for replicate 3 at 0.0316 micromolar | 4 | | Float | |||
| 162 | M4 Conc3 Rep3 (0.1μM**) | Value with M4 for replicate 3 at 0.1 micromolar | 4 | | Float | |||
| 163 | M4 Conc4 Rep3 (0.32μM**) | Value with M4 for replicate 3 at 0.316 micromolar | 4 | | Float | |||
| 164 | M4 Conc5 Rep3 (1μM**) | Value with M4 for replicate 3 at 1 micromolar | 4 | | Float | |||
| 165 | M4 Conc6 Rep3 (3.16μM**) | Value with M4 for replicate 3 at 3.16 micromolar | 4 | | Float | |||
| 166 | M4 Conc7 Rep3 (10μM**) | Value with M4 for replicate 3 at 10 micromolar | 4 | | Float | |||
| 167 | M4 Conc8 Rep3 (31.62μM**) | Value with M4 for replicate 3 at 31.6 micromolar | 4 | | Float | |||
| 168 | M4 Conc1 Rep4 (0.01μM**) | Value with M4 for replicate 4 at 0.01 micromolar | 4 | | Float | |||
| 169 | M4 Conc2 Rep4 (0.03μM**) | Value with M4 for replicate 4 at 0.0316 micromolar | 4 | | Float | |||
| 170 | M4 Conc3 Rep4 (0.1μM**) | Value with M4 for replicate 4 at 0.1 micromolar | 4 | | Float | |||
| 171 | M4 Conc4 Rep4 (0.32μM**) | Value with M4 for replicate 4 at 0.316 micromolar | 4 | | Float | |||
| 172 | M4 Conc5 Rep4 (1μM**) | Value with M4 for replicate 4 at 1 micromolar | 4 | | Float | |||
| 173 | M4 Conc6 Rep4 (3.16μM**) | Value with M4 for replicate 4 at 3.16 micromolar | 4 | | Float | |||
| 174 | M4 Conc7 Rep4 (10μM**) | Value with M4 for replicate 4 at 10 micromolar | 4 | | Float | |||
| 175 | M4 Conc8 Rep4 (31.62μM**) | Value with M4 for replicate 4 at 31.6 micromolar | 4 | | Float | |||
| 176 | M4 Curve | Comment describing resulting curve fit by Prism | 4 | String | ||||
| 177 | muscarinic M5 receptor (human) gene_ID† | muscarinic M5 receptor (human) gene_ID | 5 | muscarinic M5 receptor (human) | String | |||
| 178 | muscarinic M5 receptor (human) protein gi | muscarinic M5 receptor (human) protein gi | 5 | Protein target gi | String | |||
| 179 | muscarinic M5 receptor (human) tax_id | muscarinic M5 receptor (human) tax_id | 5 | | Float | |||
| 180 | M5 Conc1 Rep1 (0.01μM**) | Value with M5 for replicate 1 at 0.01 micromolar | 5 | | Float | |||
| 181 | M5 Conc2 Rep1 (0.03μM**) | Value with M5 for replicate 1 at 0.0316 micromolar | 5 | | Float | |||
| 182 | M5 Conc3 Rep1 (0.1μM**) | Value with M5 for replicate 1 at 0.1 micromolar | 5 | | Float | |||
| 183 | M5 Conc4 Rep1 (0.32μM**) | Value with M5 for replicate 1 at 0.316 micromolar | 5 | | Float | |||
| 184 | M5 Conc5 Rep1 (1μM**) | Value with M5 for replicate 1 at 1 micromolar | 5 | | Float | |||
| 185 | M5 Conc6 Rep1 (3.16μM**) | Value with M5 for replicate 1 at 3.16 micromolar | 5 | | Float | |||
| 186 | M5 Conc7 Rep1 (10μM**) | Value with M5 for replicate 1 at 10 micromolar | 5 | | Float | |||
| 187 | M5 Conc8 Rep1 (31.62μM**) | Value with M5 for replicate 1 at 31.6 micromolar | 5 | | Float | |||
| 188 | M5 Conc1 Rep2 (0.01μM**) | Value with M5 for replicate 2 at 0.01 micromolar | 5 | | Float | |||
| 189 | M5 Conc2 Rep2 (0.03μM**) | Value with M5 for replicate 2 at 0.0316 micromolar | 5 | | Float | |||
| 190 | M5 Conc3 Rep2 (0.1μM**) | Value with M5 for replicate 2 at 0.1 micromolar | 5 | | Float | |||
| 191 | M5 Conc4 Rep2 (0.32μM**) | Value with M5 for replicate 2 at 0.316 micromolar | 5 | | Float | |||
| 192 | M5 Conc5 Rep2 (1μM**) | Value with M5 for replicate 2 at 1 micromolar | 5 | | Float | |||
| 193 | M5 Conc6 Rep2 (3.16μM**) | Value with M5 for replicate 2 at 3.16 micromolar | 5 | | Float | |||
| 194 | M5 Conc7 Rep2 (10μM**) | Value with M5 for replicate 2 at 10 micromolar | 5 | | Float | |||
| 195 | M5 Conc8 Rep2 (31.62μM**) | Value with M5 for replicate 2 at 31.6 micromolar | 5 | | Float | |||
| 196 | M5 Conc1 Rep3 (0.01μM**) | Value with M5 for replicate 3 at 0.01 micromolar | 5 | | Float | |||
| 197 | M5 Conc2 Rep3 (0.03μM**) | Value with M5 for replicate 3 at 0.0316 micromolar | 5 | | Float | |||
| 198 | M5 Conc3 Rep3 (0.1μM**) | Value with M5 for replicate 3 at 0.1 micromolar | 5 | | Float | |||
| 199 | M5 Conc4 Rep3 (0.32μM**) | Value with M5 for replicate 3 at 0.316 micromolar | 5 | | Float | |||
| 200 | M5 Conc5 Rep3 (1μM**) | Value with M5 for replicate 3 at 1 micromolar | 5 | | Float | |||
| 201 | M5 Conc6 Rep3 (3.16μM**) | Value with M5 for replicate 3 at 3.16 micromolar | 5 | | Float | |||
| 202 | M5 Conc7 Rep3 (10μM**) | Value with M5 for replicate 3 at 10 micromolar | 5 | | Float | |||
| 203 | M5 Conc8 Rep3 (31.62μM**) | Value with M5 for replicate 3 at 31.6 micromolar | 5 | | Float | |||
| 204 | M5 Conc1 Rep4 (0.01μM**) | Value with M5 for replicate 4 at 0.01 micromolar | 5 | | Float | |||
| 205 | M5 Conc2 Rep4 (0.03μM**) | Value with M5 for replicate 4 at 0.0316 micromolar | 5 | | Float | |||
| 206 | M5 Conc3 Rep4 (0.1μM**) | Value with M5 for replicate 4 at 0.1 micromolar | 5 | | Float | |||
| 207 | M5 Conc4 Rep4 (0.32μM**) | Value with M5 for replicate 4 at 0.316 micromolar | 5 | | Float | |||
| 208 | M5 Conc5 Rep4 (1μM**) | Value with M5 for replicate 4 at 1 micromolar | 5 | | Float | |||
| 209 | M5 Conc6 Rep4 (3.16μM**) | Value with M5 for replicate 4 at 3.16 micromolar | 5 | | Float | |||
| 210 | M5 Conc7 Rep4 (10μM**) | Value with M5 for replicate 4 at 10 micromolar | 5 | | Float | |||
| 211 | M5 Conc8 Rep4 (31.62μM**) | Value with M5 for replicate 4 at 31.6 micromolar | 5 | | Float | |||
| 212 | M5 Conc1 Rep5 (0.01μM**) | Value with M5 for replicate 5 at 0.01 micromolar | 5 | | Float | |||
| 213 | M5 Conc2 Rep5 (0.03μM**) | Value with M5 for replicate 5 at 0.0316 micromolar | 5 | | Float | |||
| 214 | M5 Conc3 Rep5 (0.1μM**) | Value with M5 for replicate 5 at 0.1 micromolar | 5 | | Float | |||
| 215 | M5 Conc4 Rep5 (0.32μM**) | Value with M5 for replicate 5 at 0.316 micromolar | 5 | | Float | |||
| 216 | M5 Conc5 Rep5 (1μM**) | Value with M5 for replicate 5 at 1 micromolar | 5 | | Float | |||
| 217 | M5 Conc6 Rep5 (3.16μM**) | Value with M5 for replicate 5 at 3.16 micromolar | 5 | | Float | |||
| 218 | M5 Conc7 Rep5 (10μM**) | Value with M5 for replicate 5 at 10 micromolar | 5 | | Float | |||
| 219 | M5 Conc8 Rep5 (31.62μM**) | Value with M5 for replicate 5 at 31.6 micromolar | 5 | | Float | |||
| 220 | M5 Bottom | Calculated Bottom with M5 | 5 | | Float | |||
| 221 | M5 Top | Calculated Top with M5 | 5 | | Float | |||
| 222 | M5 LogEC50 | Calculated LogEC50 with M5 | 5 | | Float | |||
| 223 | M5 Hillslope | Calculated Hillslope with M5 | 5 | | Float | |||
| 224 | M5 EC50* | Calculated EC50 with M5 | 5 | | Float | μM | ||
| 225 | M5 Std Error Bottom | Calculated Std Error Bottom with M5 | 5 | | Float | |||
| 226 | M5 Std Error Top | Calculated Std Error Top with M5 | 5 | | Float | |||
| 227 | M5 Std Error LogEC50 | Calculated Std Error LogEC50 with M5 | 5 | | Float | |||
| 228 | M5 Std Error Hillslope | Calculated Std Error Hillslope with M5 | 5 | | Float | |||
| 229 | M5 95% CI Bottom | Calculated 95% CI Bottom with M5 | 5 | String | ||||
| 230 | M5 95% CI Top | Calculated 95% CI Top with M5 | 5 | String | ||||
| 231 | M5 95% CI LogEC50 | Calculated 95% CI LogEC50 with M5 | 5 | String | ||||
| 232 | M5 95% CI Hillslope | Calculated 95% CI Hillslope with M5 | 5 | String | ||||
| 233 | M5 95% CI EC50 | Calculated 95% CI EC50 with M5 | 5 | String | ||||
| 234 | M5 Deg Freedom | Calculated Deg Freedom with M5 | 5 | | Integer | |||
| 235 | M5 R-Squared | Calculated R-Squared with M5 | 5 | | Float | |||
| 236 | M5 Abs Sum Squares | Calculated Abs Sum Squares with M5 | 5 | | Float |
† RNAi Target. * Activity Concentration. ** Test Concentration. § Panel component ID.
Additional Information
Grant Number: MH077606
Classification
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