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BioAssay: AID 651827

ML332 Competition in Radioligand Binding assays (Ricerca)

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 (ML332) for ancillary pharmacology in counter screens via the commercial Ricerca Biosciences, LLC 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: 651827
Data Source: Vanderbilt Specialized Chemistry Center
Depositor Category: NIH Molecular Libraries Probe Production Network
Deposit Date: 2012-11-30
Hold-until Date: 2013-11-30
Modify Date: 2013-12-02

Data Table ( Complete ):           Active    All
Target
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 (ML332) for ancillary pharmacology in counter screens via the commercial Ricerca Biosciences, LLC 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 Ricerca Biosciences, LLC 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 Ricerca Biosciences, LLC using a 10 uM test concentration of ML332 for radioligand and 30uM test concentration for functional assays. Percent inhibition of target-selective radioligand binding or functional response is reported. Under the Ricerca Biosciences, LLC panel assay conditions, responses with greater than 50% inhibition are considered significant.
Comment
Under the Ricerca Biosciences, LLC panel assay conditions, responses with greater than 50% inhibition are considered significant. There were no significant inhibitory responses reported for ML332 in the Ricerca 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 alpha2A 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 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%
9Adrenergic 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%
10Androgen _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%
11Bradykinin 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%
12Bradykinin 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%
13Calcium 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%
14Calcium 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%
15Calcium 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%
16Cannabinoid 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%
17Dopamine 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%
18Dopamine 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%
19Dopamine 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%
20Dopamine 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%
21Endothelin 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%
22Endothelin 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%
23Epidermal 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%
24Estrogen 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%
25GABAA_ 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%
26GABAA_ 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%
27GABAB1A 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%
28Glucocorticoid 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_ 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%
30Glutamate_ 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%
31Glutamate_ 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%
32Glutamate_ 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%
33Histamine 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%
34Histamine 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%
35Histamine 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%
36Imidazoline 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%
37Interleukin 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%
38Leukotriene_ 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%
39Melatonin 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%
40Muscarinic 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%
41Muscarinic 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%
42Muscarinic 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%
43Neuropeptide 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%
44Neuropeptide 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%
45Nicotinic 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%
46Nicotinic 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%
47Opiate 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%
48Opiate 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%
49Opiate 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%
50Phorbol 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%
51Platelet 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%
52Potassium 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%
53Potassium 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%
54Prostanoid 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%
55Purinergic 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%
56Purinergic 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%
57Rolipram 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-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%
59Serotonin _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%
60Serotonin _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%
61Sigma 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%
62Sodium 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%
63Tachykinin 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%
64Thyroid 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%
65Transporter_ 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%
66Transporter_ 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%
67Transporter_ 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%
68Transporter_ Serotonin _5-Hydroxytryptamine 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: R01 MH062646

Data Table (Concise)
Classification
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