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BioAssay: AID 623927

ML292 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 positive allosteric modulator (PAM) of metabotropic glutamate receptor, subtype 4 (mGlu4) probe (ML292) 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: 623927
Data Source: Vanderbilt Specialized Chemistry Center (ML292_Riserca_Binding)
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2012-03-29
Hold-until Date: 2013-03-27
Modify Date: 2013-03-27

Data Table ( Complete ):           Active    All
Target
Sequence: metabotropic glutamate receptor 4 [Homo sapiens]
Description ..   
Protein Family: 7 transmembrane sweet-taste receptor of 3 GCPR

Gene:GRM4     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 positive allosteric modulator (PAM) of metabotropic glutamate receptor, subtype 4 (mGlu4) probe (ML292) 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 ML292 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 was one significant inhibitory responses reported for ML292 in the Riscerca panel (Norepinephrine transporter, 80%). Therefore, the ML292 probe was assigned an Activity Score of 10 / 100 for mild off target activity in the Ricerca Binding Panel assay.
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
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).Float%
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).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_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).Float%
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).Float%
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).Float%
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).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_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).Float%
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).Float%
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).Float%
14Calcium_Channel_Ltype_DihydropyridineBiochemical 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-TypeBiochemical 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_D1Biochemical 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_D2SBiochemical 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_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).Float%
19Dopamine_D4,2Biochemical 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%
20Endothelin_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).Float%
21Endothelin_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).Float%
22Epidermal_Growth_Factor_EGFBiochemical 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_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).Float%
24G_Protein_Coupled_Receptor_GPR103Biochemical 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%
25GABA_A_Flunitrazepam_CentralBiochemical 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%
26GABA_A_Muscimol_CentralBiochemical 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%
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).Float%
28GlucocorticoidBiochemical 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_KainateBiochemical 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_AgonismBiochemical 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_GlycineBiochemical 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_PhencyclidineBiochemical 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_H1Biochemical 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_H2Biochemical 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%
35 Histamine_H3Biochemical 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_CentralBiochemical 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_IL1Biochemical 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_CysLT1Biochemical 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_MT1Biochemical 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_M1Biochemical 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_M2Biochemical 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_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).Float%
43NeuropeptideY_Y1Biochemical 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%
44NeuropeptideY_Y2Biochemical 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_AcetylcholineBiochemical 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_D1_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).Float%
47Opiate_delta1_OP1_DOPBiochemical 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_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).Float%
49Opiate_mu_OP3_MOPBiochemical 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_EsterBiochemical 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_PAFBiochemical 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_K_ATPBiochemical 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_hERGBiochemical 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_EP4Biochemical 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_P2XBiochemical 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_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).Float%
57RolipramBiochemical 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_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).Float%
59Serotonin_5HT3Biochemical 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_rho1Biochemical 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_rho2Biochemical 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_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).Float%
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).Float%
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).Float%
65Transporter_Dopamine_DATBiochemical 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_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).Float%
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).Float%
68Transporter_Serotonin_5-Hydroxytryptamine_SERTBiochemical 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: NS053536-01

Data Table (Concise)
Classification
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