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BioAssay: AID 651832

ML326 M5 PAM Competition in Radioligand Binding assays (Eurofins PanLabs)

The purpose of this assay was to follow up on the confirmatory and dose-response testing of the validated lead SAR series to characterize the candidate probe compound (ML326) for ancillary pharmacology in counter screens via the commercial Eurofins PanLabs, Inc radioligand binding assay panels targeting G-protein coupled receptors, neurotransmitter transporters and ion channels. ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Probe(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Probe(1)
 
 
Active(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 651832
Data Source: Vanderbilt Specialized Chemistry Center
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2012-12-03
Hold-until Date: 2013-07-12
Modify Date: 2013-07-12

Data Table ( Complete ):           Active    All
Target
Sequence: muscarinic acetylcholine receptor M5 [Homo sapiens]
Description ..   
Protein Family: Serpentine type 7TM GPCR chemoreceptor Srx

Gene:CHRM5     Related Protein 3D Structures     More BioActivity Data..
BioActive Compound: Chemical Probe: 1    Active: 1
Description:
The purpose of this assay was to follow up on the confirmatory and dose-response testing of the validated lead SAR series to characterize the candidate probe compound (ML326) for ancillary pharmacology in counter screens via the commercial Eurofins PanLabs, Inc radioligand binding assay panels targeting G-protein coupled receptors, neurotransmitter transporters and ion channels.
Protocol
Methods employed in this study have been adapted from the scientific literature by Eurofins PanLabs, Inc to maximize reliability and reproducibility. Reference standards were run as an integral part of each assay to ensure the validity of the results obtained. Assays were performed under conditions described in an extensive "Methods" section available from Eurofins PanLabs, Inc using a 10 uM test concentration of ML326 for radioligand and 30uM test concentration for functional assays. Percent inhibition of target-selective radioligand binding or functional response is reported. Under the Eurofins PanLabs, Inc panel assay conditions, responses with greater than 50% inhibition are considered significant.
Comment
Under the Eurofins PanLabs, Inc panel assay conditions, responses with greater than 50% inhibition are considered significant. Ten out of the 67 assays reported significant inhibitory responses for ML326 in the Eurofins Panlabs panel.
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Adenosine A1 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
2Adenosine A2A Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
3Adenosine A3 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
4Adrenergic alpha1A Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
5Adrenergic alpha1B Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
6Adrenergic alpha1D Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
7Adrenergic beta1 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
8Adrenergic beta2 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
9Androgen _Testosterone AR Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
10Bradykinin B1 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
11Bradykinin B2 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
12Calcium Channel L-Type_ Benzothiazepine Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
13Calcium Channel L-Type_ Dihydropyridine Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
14Calcium Channel N-Type Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
15Cannabinoid CB1 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
16Dopamine D1 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
17Dopamine D2S Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
18Dopamine D3 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
19Dopamine D4.2 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
20Endothelin ETA Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
21Endothelin ETB Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
22Epidermal Growth Factor _EGF Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
23Estrogen ERalpha Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
24GABAA1_ Flunitrazepam_ Central Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
25GABAA1_ Muscimol_ Central Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
26GABAB1A Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
27Glucocorticoid Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
28Glutamate_ Kainate Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
29Glutamate_ NMDA_ Agonism Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
30Glutamate_ NMDA_ Glycine Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
31Glutamate_ NMDA_ Phencyclidine Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
32Histamine H1 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
33Histamine H2 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
34Histamine H3 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
35Imidazoline I2_ Central Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
36Interleukin IL-1 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
37Leukotriene_ Cysteinyl CysLT1 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
38Melatonin MT1 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
39Muscarinic M1 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
40Muscarinic M2 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
41Muscarinic M3 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
42Neuropeptide Y Y1 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
43Neuropeptide Y Y2 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
44Nicotinic Acetylcholine Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
45Nicotinic Acetylcholine alpha1_ Bungarotoxin Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
46Opiate delta _OP1_ DOP Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
47Opiate kappa_OP2_ KOP Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
48Opiate mu_OP3_ MOP Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
49Phorbol Ester Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
50Platelet Activating Factor _PAF Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
51Potassium Channel [KATP] Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
52Potassium Channel hERG Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
53Prostanoid EP4 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
54Purinergic P2X Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
55Purinergic P2Y Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
56Rolipram Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
57Serotonin _5-Hydroxytryptamine 5-HT1A Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
58Serotonin _5-Hydroxytryptamine 5-HT2B Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
59Serotonin _5-Hydroxytryptamine 5-HT3 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
60Sigma sigma1 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
61Sodium Channel_Site 2Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
62Tachykinin NK1 Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
63Thyroid Hormone Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
64Transporter_ Dopamine _DAT Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
65Transporter_ GABA Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
66Transporter_ Norepinephrine _NET Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
67Transporter_ Serotonin _5-Hydroxytryptamine_SERT Biochemical assay results presented as the percent inhibition of specific binding or activity. Primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH). Significant responses (50% inhibition or stimulation for Biochemical assays).Float%
Additional Information
Grant Number: MH077607-01

Data Table (Concise)
Classification
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