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BioAssay: AID 588753

ML254 and ML273 Competition in Radioligand Binding assays (Riserca)

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 (ML254 and ML273) for ancillary pharmacology in counter screens via the commercial Reserca 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(2)
 
 
Inactive(2)
 
 
 Tested Substances
 Tested Substances
All(2)
 
 
Inactive(2)
 
 
AID: 588753
Data Source: Vanderbilt Specialized Chemistry Center (ML254_Riscerca_Binding)
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2011-10-30
Hold-until Date: 2012-10-25
Modify Date: 2012-10-27

Data Table ( Complete ):           All
Target
Tested Compounds:
Depositor Specified Assays
AIDNameTypeComment
588721Optimization of novel mGluR5 positive allosteric modulators (PAM)ssummaryOptimization of novel mGluR5 positive allosteric modulators (PAM)s.
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 (ML254 and ML273) for ancillary pharmacology in counter screens via the commercial Reserca 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 ML254 and ML273 for radioligand competition and 30uM test concentration for functional assays. Percent inhibition of target-selective radioligand binding or functional response is reported.
Comment
Under the Ricerca Biosciences, LLC panel assay conditions, responses with greater than 50% inhibition are considered significant. Of note, there were no significant inhibitory responses were reported for ML254 and ML273 in the Riscerca panel.
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Adenosine_A1Biochemical 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).Integer%
2Adenosine_A2aBiochemical 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).Integer%
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).Integer%
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).Integer%
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).Integer%
6Adrenergic_alpha1DBiochemical 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).Integer%
7Adrenergic_alpha2ABiochemical 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).Integer%
8Adrenergic_beta1Biochemical 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).Integer%
9Adrenergic_beta2Biochemical 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).Integer%
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).Integer%
11Bradykinin_B1Biochemical 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).Integer%
12Bradykinin_B2Biochemical 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).Integer%
13Calcium_Channel_Ltype_BenzothiazepineBiochemical 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).Integer%
14Calcium_Channel_Ltype_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).Integer%
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).Integer%
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).Integer%
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).Integer%
18Dopamine_D25Biochemical 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).Integer%
19Dopamine_D3Biochemical 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).Integer%
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).Integer%
21Endothelin_EtaBiochemical 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).Integer%
22Endothelin_ETbBiochemical 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).Integer%
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).Integer%
24Estrogen_ER_alphaBiochemical 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).Integer%
25GABA_A_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).Integer%
26GABA_A_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).Integer%
27GABA_B_1ABiochemical 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).Integer%
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).Integer%
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).Integer%
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).Integer%
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).Integer%
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).Integer%
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).Integer%
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).Integer%
35 Histamine_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).Integer%
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).Integer%
37Interleukin_IL1 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).Integer%
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).Integer%
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).Integer%
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).Integer%
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).Integer%
42Muscarinic_M3Biochemical 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).Integer%
43NeuropeptideY_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).Integer%
44NeuropeptideY_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).Integer%
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).Integer%
46Nicotinic_Acetylcholine_alpha1_BungarotoxinBiochemical 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).Integer%
47Opiate_delta1_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).Integer%
48Opiate_kappa_OP2_KOPBiochemical 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).Integer%
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).Integer%
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).Integer%
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).Integer%
52Potassium_Channel_K_ATP 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).Integer%
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).Integer%
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).Integer%
55Purinergic_P2XYBiochemical 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).Integer%
56Purinergic_P2YBiochemical 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).Integer%
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).Integer%
58Serotonin_5HT1ABiochemical 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).Integer%
59Serotonin_5HT2B 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).Integer%
60Serotonin_5HT3 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).Integer%
61Sigma_rho1 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).Integer%
62Sodium_Channel_Site2Biochemical 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).Integer%
63Tachykinin_NK1Biochemical 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).Integer%
64Thyroid_HormoneBiochemical 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).Integer%
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).Integer%
66Transporter_GABABiochemical 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).Integer%
67Transporter_Norepinephrine_NETBiochemical 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).Integer%
68Transporter_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).Integer%
Additional Information
Grant Number: R01 MH062646

Data Table (Concise)
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