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BioAssay: AID 623933

ML298, ML299 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 compounds (ML298 and ML299) 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(2)
 
 
Active(2)
 
 
 Tested Substances
 Tested Substances
All(2)
 
 
Active(2)
 
 
 Related BioAssays
 Related BioAssays
AID: 623933
Data Source: Vanderbilt Specialized Chemistry Center (ML298_ML299_Ricerca_Binding)
Depositor Category: NIH Molecular Libraries Probe Production Network
Deposit Date: 2012-03-29
Hold-until Date: 2013-03-28
Modify Date: 2013-03-29

Data Table ( Complete ):           View Active Data    View All Data
BioActive Compounds: 2
Related Experiments
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AIDNameTypeProbeComment
588854Summary AID for PLD inhibitor development projectSummary3 depositor-specified cross reference: Summary AID for PLD inhibitor development project
624000PLD2 purified enzyme concentration response (PLD2_Assay_3B_Lib32)Confirmatory depositor-specified cross reference
624001PLD1 purified enzyme concentration response (PLD1_Assay_3A_Lib32)Confirmatory depositor-specified cross reference
624003PLD1 Cellular concentration response (PLD1_Assay_2A_Lib32)Confirmatory depositor-specified cross reference
624004PLD2 Cellular concentration response (PLD2_Assay_2B_Lib32)Confirmatory depositor-specified cross reference
624008PLD1 Cellular isoenzyme activity (PLD1_Assay_1A_Lib32)Screening depositor-specified cross reference
624009PLD2 Cellular isoenzyme activity (PLD2_Assay_1B_Lib32)Screening depositor-specified cross reference
602143Cellular PLD2 isoenzyme activity assays at a set concentrationScreening same project related to Summary assay
602144Cellular PLD1 isoenzyme activity assays at set concentrationScreening same project related to Summary assay
602147Cellular PLD2 concentration responseConfirmatory same project related to Summary assay
602149PLD2 purified enzyme concentration responseConfirmatory same project related to Summary assay
602150PLD1 purified enzyme concentration responseConfirmatory same project related to Summary assay
602151Cellular PLD1 concentration responseConfirmatory same project related to Summary assay
602153ML270, ML271, ML272 Competition in Radioligand Binding assays (Ricerca)Other same project related to Summary assay
602175Developing isoenzyme selective inhibitors of phospholipase D as an antiviral therapeutic - Secondary Assay PanelOther same project related to Summary assay
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 compounds (ML298 and ML299) 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 ML298 and ML299 for radioligand competition 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
Moderate ancillary pharmacology was observed with both ML298 and ML299 probes. Significant inhibition was reported at the following targets:


PLD-2 Selective Probe (ML298)
Adrenergic alpha1B 61%
Adrenergic beta1 69%
Calcium Channel L-Type, Benzothiazepine 65%
Calcium Channel L-Type, Dihydropyridine 66%
Dopamine D2S 94%
Dopamine D4.2 101%
Histamine H1 61%
Opiate kappa(OP2, KOP) 94%
Opiate mu(OP3, MOP) 69%
Potassium Channel hERG 78%
Serotonin (5-Hydroxytryptamine) 5-HT1A 54%
Serotonin (5-Hydroxytryptamine) 5-HT2B 65%
Sigma sigma1 71%
Transporter, Dopamine (DAT) 52%
Transporter, Norepinephrine (NET) 58%

PLD-dual Probe (ML299)
Calcium Channel L-Type, Benzothiazepine 52%
Calcium Channel L-Type, Dihydropyridine 59%
Dopamine D2S Receptor 57%
Dopamine D3 Receptor 54%
Dopamine D4.2 58%
Opiate Receptor kappa(OP2, KOP) 86%
Opiate Receptor mu(OP3, MOP) 85%
Potassium Channel hERG 85%
Tachykinin NK1 Receptor 51%
Transporter, Dopamine (DAT) 74%
Transporter, Norepinephrine (NET) 86%
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1Adenosine_A1Percent inhibition of specific binding or activity. Integer%
2Adenosine_A2aPercent inhibition of specific binding or activity. Integer%
3Adenosine_A3 Percent inhibition of specific binding or activity. Integer%
4Adrenergic_alpha1A Percent inhibition of specific binding or activity. Integer%
5Adrenergic_alpha1B Percent inhibition of specific binding or activity. Integer%
6Adrenergic_alpha1DPercent inhibition of specific binding or activity. Integer%
7Adrenergic_alpha2APercent inhibition of specific binding or activity. Integer%
8Adrenergic_beta1Percent inhibition of specific binding or activity. Integer%
9Adrenergic_beta2Percent inhibition of specific binding or activity. Integer%
10Androgen_Testosterone_AR Percent inhibition of specific binding or activity. Integer%
11Bradykinin_B1Percent inhibition of specific binding or activity. Integer%
12Bradykinin_B2Percent inhibition of specific binding or activity. Integer%
13Calcium_Channel_Ltype_BenzothiazepinePercent inhibition of specific binding or activity. Integer%
14Calcium_Channel_Ltype_Dihydropyridine Percent inhibition of specific binding or activity. Integer%
15Calcium Channel N-Type Percent inhibition of specific binding or activity. Integer%
16Cannabinoid_CB1 Percent inhibition of specific binding or activity. Integer%
17Dopamine_D1 Percent inhibition of specific binding or activity. Integer%
18Dopamine_D2SPercent inhibition of specific binding or activity. Integer%
19Dopamine_D3Percent inhibition of specific binding or activity. Integer%
20Dopamine_D4,2 Percent inhibition of specific binding or activity. Integer%
21Endothelin_EtaPercent inhibition of specific binding or activity. Integer%
22Endothelin_ETbPercent inhibition of specific binding or activity. Integer%
23Epidermal_Growth_Factor_EGF Percent inhibition of specific binding or activity. Integer%
24Estrogen_ER_alphaPercent inhibition of specific binding or activity. Integer%
25GABA_A_Flunitrazepam_Central Percent inhibition of specific binding or activity. Integer%
26GABA_A_Muscimol_Central Percent inhibition of specific binding or activity. Integer%
27GABA_B_1APercent inhibition of specific binding or activity. Integer%
28Glucocorticoid Percent inhibition of specific binding or activity. Integer%
29Glutamate_Kainate Percent inhibition of specific binding or activity. Integer%
30Glutamate_NMDA_Agonism Percent inhibition of specific binding or activity. Integer%
31Glutamate_NMDA_Glycine Percent inhibition of specific binding or activity. Integer%
32Glutamate_NMDA_Phencyclidine Percent inhibition of specific binding or activity. Integer%
33Histamine_H1 Percent inhibition of specific binding or activity. Integer%
34Histamine_H2 Percent inhibition of specific binding or activity. Integer%
35 Histamine_H3 Percent inhibition of specific binding or activity. Integer%
36Imidazoline_I2_Central Percent inhibition of specific binding or activity. Integer%
37Interleukin_IL1 Percent inhibition of specific binding or activity. Integer%
38Leukotriene_Cysteinyl_CysLT1 Percent inhibition of specific binding or activity. Integer%
39Melatonin_MT1 Percent inhibition of specific binding or activity. Integer%
40Muscarinic_M1 Percent inhibition of specific binding or activity. Integer%
41Muscarinic_M2 Percent inhibition of specific binding or activity. Integer%
42Muscarinic_M3Percent inhibition of specific binding or activity. Integer%
43NeuropeptideY_Y1 Percent inhibition of specific binding or activity. Integer%
44NeuropeptideY_Y2 Percent inhibition of specific binding or activity. Integer%
45Nicotinic_Acetylcholine Percent inhibition of specific binding or activity. Integer%
46Nicotinic_Acetylcholine_alpha1_BungarotoxinPercent inhibition of specific binding or activity. Integer%
47Opiate_delta1_OP1_DOP Percent inhibition of specific binding or activity. Integer%
48Opiate_kappa_OP2_KOPPercent inhibition of specific binding or activity. Integer%
49Opiate_mu_OP3_MOP Percent inhibition of specific binding or activity. Integer%
50Phorbol_Ester Percent inhibition of specific binding or activity. Integer%
51Platelet_Activating_Factor_PAF Percent inhibition of specific binding or activity. Integer%
52Potassium_Channel_K_ATP Percent inhibition of specific binding or activity. Integer%
53Potassium_Channel_hERG Percent inhibition of specific binding or activity. Integer%
54Prostanoid_EP4 Percent inhibition of specific binding or activity. Integer%
55Purinergic_P2XYPercent inhibition of specific binding or activity. Integer%
56Purinergic_P2YPercent inhibition of specific binding or activity. Integer%
57Rolipram Percent inhibition of specific binding or activity. Integer%
58Serotonin_5HT1APercent inhibition of specific binding or activity. Integer%
59Serotonin_5HT2B Percent inhibition of specific binding or activity. Integer%
60Serotonin_5HT3 Percent inhibition of specific binding or activity. Integer%
61Sigma_rho1 Percent inhibition of specific binding or activity. Integer%
62Tachykinin_NK1Percent inhibition of specific binding or activity. Integer%
63Thyroid_HormonePercent inhibition of specific binding or activity. Integer%
64Transporter_Dopamine_DAT Percent inhibition of specific binding or activity. Integer%
65Transporter_GABAPercent inhibition of specific binding or activity. Integer%
66Transporter_Norepinephrine_NETPercent inhibition of specific binding or activity. Integer%
67Transporter_Serotonin_5-Hydroxytryptamine_SERT Percent inhibition of specific binding or activity. Integer%
Additional Information
Grant Number: P01 ES013125

Data Table (Concise)
Data Table ( Complete ):     View Active Data    View All Data
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