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BioAssay: AID 686925

ML352 Eurofin Panel Assay for Choline Transporter Inhibitor (Probe Compound)

Methods employed in this study have been adapted from the scientific literature 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 the accompanying "Methods" section of this report.Where presented, IC50 values were determined by a non-linear, more ..
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Inactive(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Inactive(1)
 
 
AID: 686925
Data Source: Vanderbilt Specialized Chemistry Center (Radioligand Binding assays (Eurofin) ML352 (VU328-CHT2 ) Cho..)
BioAssay Type: Panel
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2013-04-10
Hold-until Date: 2014-03-17
Modify Date: 2014-03-17

Data Table ( Complete ):           View All Data
Tested Compound:
Related Experiments
AIDNameTypeComment
652262Discovery and structure-activity relationship of a novel choline transporter inhibitor: ML352Summarydepositor-specified cross reference
488997Summary of probe development for inhibitors of the Choline Transporter (CHT)Summarysame project related to Summary assay
652177Discovery and structure-activity relationship of a novel choline transporter inhibitorConfirmatorysame project related to Summary assay
652215Discovery and structure-activity relationship of a novel choline transporter inhibitor, Selectivity StudiesConfirmatorysame project related to Summary assay
Description:
Assay Provider: P Jeffrey Conn

Assay Provider Affiliation: Vanderbilt University

Methods employed in this study have been adapted from the scientific literature 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 the accompanying "Methods" section of this report.Where presented, IC50 values were determined by a non-linear, least squares regression analysis using MathIQTM (IDBusiness Solutions Ltd., UK). Where inhibition constants (Ki) are presented, the Ki values were calculated using the equation of Cheng and Prusoff (Cheng, Y., Prusoff, W.H., Biochem. Pharmacol. 22:3099-3108, 1973) using the observed IC50 of the tested compound, the concentration of radioligand employed in the assay, and the historical valuesfor the KD of the ligand (obtained experimentally at Eurofins Panlabs, Inc.). Where presented, the Hill coefficient (nH),defining the slope of the competitive binding curve, was calculated using MathIQTM. Hill coefficients significantly different than 1.0, may suggest that the binding displacement does not follow the laws of mass action with a single binding site.Where IC50, Ki, and/or nH data are presented without Standard Error of the Mean (SEM), data are insufficient to be quantitative, and the values presented (Ki, IC50, nH) should be interpreted with caution.
Panel Information
Panel Assay with Multiple Targets/Outcomes
    Data Table(All)Show more
PID§NameSubstancePanel TargetsDescriptionAdditional Information
ActiveInactive
1Eurofin Panel Assays for mGlur5 SAM Probe [gi:4501947]
Radioligand Binding AssayTaxonomy id: 9606
2Eurofin Panel Assays for mGlur5 SAM Probe [gi:5921992]
Radioligand Binding AssayTaxonomy id: 9606
3Eurofin Panel Assays for mGlur5 SAM Probe [gi:4501953]
Radioligand Binding AssayTaxonomy id: 9606
4Eurofin Panel Assays for mGlur5 SAM Probe [gi:148747171]
Radioligand Binding AssayTaxonomy id: 10116
5Eurofin Panel Assays for mGlur5 SAM Probe [gi:47575853]
Radioligand Binding AssayTaxonomy id: 10116
6Eurofin Panel Assays for mGlur5 SAM Probe [gi:13324696]
Radioligand Binding AssayTaxonomy id: 9606
7Eurofin Panel Assays for mGlur5 SAM Probe [gi:194353970]
Radioligand Binding AssayTaxonomy id: 9606
8Eurofin Panel Assays for mGlur5 SAM Probe [gi:4557265]
Radioligand Binding AssayTaxonomy id: 9606
9Eurofin Panel Assays for mGlur5 SAM Probe [gi:4501969]
Radioligand Binding AssayTaxonomy id: 9606
10Eurofin Panel Assays for mGlur5 SAM Probe [gi:4335929]
Radioligand Binding AssayTaxonomy id: 9606
11Eurofin Panel Assays for mGlur5 SAM Probe [gi:20544172]
Radioligand Binding AssayTaxonomy id: 9606
12Eurofin Panel Assays for mGlur5 SAM Probe [gi:4557359]
Radioligand Binding AssayTaxonomy id: 9606
13Eurofin Panel Assays for mGlur5 SAM Probe [gi:120433602]
Radioligand Binding AssayTaxonomy id: 10116
14Eurofin Panel Assays for mGlur5 SAM Probe [gi:110349767]
Radioligand Binding AssayTaxonomy id: 10116
15Eurofin Panel Assays for mGlur5 SAM Probe [gi:110225368]
Radioligand Binding AssayTaxonomy id: 10116
16Eurofin Panel Assays for mGlur5 SAM Probe [gi:237681173]
Radioligand Binding AssayTaxonomy id: 9606
17Eurofin Panel Assays for mGlur5 SAM Probe [gi:4502929]
Radioligand Binding AssayTaxonomy id: 9606
18Eurofin Panel Assays for mGlur5 SAM Probe [gi:299687]
Radioligand Binding AssayTaxonomy id: 9606
19Eurofin Panel Assays for mGlur5 SAM Probe [gi:553261]
Radioligand Binding AssayTaxonomy id: 9606
20Eurofin Panel Assays for mGlur5 SAM Probe [gi:1835973]
Radioligand Binding AssayTaxonomy id: 9606
21Eurofin Panel Assays for mGlur5 SAM Probe [gi:256313]
Radioligand Binding AssayTaxonomy id: 9606
22Eurofin Panel Assays for mGlur5 SAM Probe [gi:238636]
Radioligand Binding AssayTaxonomy id: 9606
23Eurofin Panel Assays for mGlur5 SAM Probe [gi:4557547]
Radioligand Binding AssayTaxonomy id: 9606
24Eurofin Panel Assays for mGlur5 SAM Probe [gi:46242544]
Radioligand Binding AssayTaxonomy id: 9606
25Eurofin Panel Assays for mGlur5 SAM Probe [gi:62821794]
Radioligand Binding AssayTaxonomy id: 9606
26Eurofin Panel Assays for mGlur5 SAM Probe [gi:31658]
Radioligand Binding AssayTaxonomy id: 10116
27Eurofin Panel Assays for mGlur5 SAM Probe [gi:510878]
Radioligand Binding AssayTaxonomy id: 10116
28Eurofin Panel Assays for mGlur5 SAM Probe [gi:3776073]
Radioligand Binding AssayTaxonomy id: 9606
29Eurofin Panel Assays for mGlur5 SAM Probe [gi:239758]
Radioligand Binding AssayTaxonomy id: 9606
30Eurofin Panel Assays for mGlur5 SAM Probe [gi:163659915]
Radioligand Binding AssayTaxonomy id: 10116
31Eurofin Panel Assays for mGlur5 SAM Probe [gi:8393484]
Radioligand Binding AssayTaxonomy id: 10116
32Eurofin Panel Assays for mGlur5 SAM Probe [gi:149158709]
Radioligand Binding AssayTaxonomy id: 9606
33Eurofin Panel Assays for mGlur5 SAM Probe [gi:5881576]
Radioligand Binding AssayTaxonomy id: 9606
34Eurofin Panel Assays for mGlur5 SAM Probe [gi:194018562]
Radioligand Binding AssayTaxonomy id: 9606
35Eurofin Panel Assays for mGlur5 SAM Probe [gi:205829312]
Radioligand Binding AssayTaxonomy id: 10116
36Eurofin Panel Assays for mGlur5 SAM Probe [gi:309398]
Radioligand Binding AssayTaxonomy id: 10090
37Eurofin Panel Assays for mGlur5 SAM Probe [gi:5729798]
Radioligand Binding AssayTaxonomy id: 9606
38Eurofin Panel Assays for mGlur5 SAM Probe [gi:5174593]
Radioligand Binding AssayTaxonomy id: 9606
39Eurofin Panel Assays for mGlur5 SAM Probe [gi:37622910]
Radioligand Binding AssayTaxonomy id: 9606
40Eurofin Panel Assays for mGlur5 SAM Probe [gi:54792115]
Radioligand Binding AssayTaxonomy id: 9606
41Eurofin Panel Assays for mGlur5 SAM Probe [gi:4502819]
Radioligand Binding AssayTaxonomy id: 9606
42Eurofin Panel Assays for mGlur5 SAM Probe [gi:38565061]
Radioligand Binding AssayTaxonomy id: 9606
43Eurofin Panel Assays for mGlur5 SAM Probe [gi:1247453]
Radioligand Binding AssayTaxonomy id: 9606
44Eurofin Panel Assays for mGlur5 SAM Probe [gi:29824918]
Radioligand Binding AssayTaxonomy id: 9606
45Eurofin Panel Assays for mGlur5 SAM Probe [gi:308153405]
Radioligand Binding AssayTaxonomy id: 9606
46Eurofin Panel Assays for mGlur5 SAM Probe [gi:87567783]
Radioligand Binding AssayTaxonomy id: 9606
47Eurofin Panel Assays for mGlur5 SAM Probe [gi:501145]
Radioligand Binding AssayTaxonomy id: 9606
48Eurofin Panel Assays for mGlur5 SAM Probe [gi:39986053]
Radioligand Binding AssayTaxonomy id: 9606
49Eurofin Panel Assays for mGlur5 SAM Probe [gi:452073]
Radioligand Binding AssayTaxonomy id: 9606
50Eurofin Panel Assays for mGlur5 SAM Probe [gi:12230239]
Radioligand Binding AssayTaxonomy id: 10090
51Eurofin Panel Assays for mGlur5 SAM Probe [gi:190015]
Radioligand Binding AssayTaxonomy id: 9606
52Eurofin Panel Assays for mGlur5 SAM Probe [gi:619879]
Radioligand Binding AssayTaxonomy id: 9606
53Eurofin Panel Assays for mGlur5 SAM Probe [gi:37499017]
Radioligand Binding AssayTaxonomy id: 9606
54Eurofin Panel Assays for mGlur5 SAM Probe [gi:4506259]
Radioligand Binding AssayTaxonomy id: 9606
55Eurofin Panel Assays for mGlur5 SAM Probe [gi:291406943]
Radioligand Binding AssayTaxonomy id: 9986
56Eurofin Panel Assays for mGlur5 SAM Probe [gi:25742733]
Radioligand Binding AssayTaxonomy id: 10116
57Eurofin Panel Assays for mGlur5 SAM Probe [gi:158518444]
Radioligand Binding AssayTaxonomy id: 10116
58Eurofin Panel Assays for mGlur5 SAM Probe [gi:36429]
Radioligand Binding AssayTaxonomy id: 9606
59Eurofin Panel Assays for mGlur5 SAM Probe [gi:219679]
Radioligand Binding AssayTaxonomy id: 9606
60Eurofin Panel Assays for mGlur5 SAM Probe [gi:3115222]
Radioligand Binding AssayTaxonomy id: 9606
61Eurofin Panel Assays for mGlur5 SAM Probe [gi:4507043]
Radioligand Binding AssayTaxonomy id: 9606
62Eurofin Panel Assays for mGlur5 SAM Probe [gi:5733130]
Radioligand Binding AssayTaxonomy id: 9606
63Eurofin Panel Assays for mGlur5 SAM Probe [gi:3097314]
Radioligand Binding AssayTaxonomy id: 10116
64Eurofin Panel Assays for mGlur5 SAM Probe [gi:178882]
Radioligand Binding AssayTaxonomy id: 10116
65Eurofin Panel Assays for mGlur5 SAM Probe [gi:235280]
Radioligand Binding AssayTaxonomy id: 10116

§ Panel component ID.
Protocol
Biochemical assay results are presented as the percent inhibition of specific binding or activity throughout the report. All other results are expressed in terms of that assay's quantitation method.1:For primary assays, only the lowest concentration with a significant response judged by the assays' criteria, is shown in this summary.2:Where applicable, either the secondary assay results with the lowest dose/concentration meeting the significance criteria or, if inactive, the highest dose/concentration that did not meet the significance criteria is shown.3:Unless otherwise requested, primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH)are shown where applicable for individual requested assays. In screening packages, primary screening in duplicate with semi-quantitative data (e.g., estimated IC50, Ki and nH) are shown where applicable (concentration range of 4 log units);available secondary functional assays are carried out (30 mM) and MEC or MIC determined only if active in primary assays >50% at 1 log unit below initial test concentration.Significant responses (>/= 50% inhibition or stimulation for Biochemical assays) were noted in the primary assays listed below: No Significant Results
Result Definitions
Show more
TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Adenosine_A1_Percent_InhibitionPercent Inhibition1Float%
2Adenosine_A1_OutcomeActive/Inactive1Integer
3Adenosine_A2A_Percent_InhibitionPercent Inhibition2Float%
4Adenosine_A2A_OutcomeActive/Inactive2Integer
5Adenosine_A3_Percent_InhibitionPercent Inhibition3Float%
6Adenosine_A3_OutcomeActive/Inactive3Integer
7Adrenergic_alpha1A_Percent_InhibitionPercent Inhibition4Float%
8Adrenergic_alpha1A_OutcomeActive/Inactive4Integer
9Adrenergic_alpha1B__Percent_InhibitionPercent Inhibition5Float%
10Adrenergic_alpha1B__OutcomeActive/Inactive5Integer
11Adrenergic_alpha1D_Percent_InhibitionPercent Inhibition6Float%
12Adrenergic_alpha1D_OutcomeActive/Inactive6Integer
13Adrenergic_alpha2A_Percent_InhibitionPercent Inhibition7Float%
14Adrenergic_alpha2A_OutcomeActive/Inactive7Integer
15Adrenergic_beta1_Percent_InhibitionPercent Inhibition8Float%
16Adrenergic_beta1_OutcomeActive/Inactive8Integer
17Adrenergic_beta2_Percent_InhibitionPercent Inhibition9Float%
18Adrenergic_beta2_OutcomeActive/Inactive9Integer
19Transporter_Norepinephrine_(NET)_Percent_InhibitionPercent Inhibition10Float%
20Transporter_Norepinephrine_(NET)_OutcomeActive/Inactive10Integer
21Bradykinin_B1_Percent_InhibitionPercent Inhibition11Float%
22Bradykinin_B1_OutcomeActive/Inactive11Integer
23Bradykinin_B2_Percent_InhibitionPercent Inhibition12Float%
24Bradykinin_B2_OutcomeActive/Inactive12Integer
25Calcium_Channel_L-Type_Benzothiazepine_Percent_InhibitionPercent Inhibition13Float%
26Calcium_Channel_L-Type_Benzothiazepine_OutcomeActive/Inactive13Integer
27Calcium_Channel_L-Type_Dihydropyridine_Percent_InhibitionPercent Inhibition14Float%
28Calcium_Channel_L-Type_Dihydropyridine_OutcomeActive/Inactive14Integer
29Calcium_Channel_N-Type_Percent_InhibitionPercent Inhibition15Float%
30Calcium_Channel_N-Type_OutcomeActive/Inactive15Integer
31Cannabinoid_CB1_Percent_InhibitionPercent Inhibition16Float%
32Cannabinoid_CB1_OutcomeActive/Inactive16Integer
33Dopamine_D1_Percent_InhibitionPercent Inhibition17Float%
34Dopamine_D1_OutcomeActive/Inactive17Integer
35Dopamine_D2S_Percent_InhibitionPercent Inhibition18Float%
36Dopamine_D2S_OutcomeActive/Inactive18Integer
37Dopamine_D3_Percent_InhibitionPercent Inhibition19Float%
38Dopamine_D3_OutcomeActive/Inactive19Integer
39Dopamine_D4.2_Percent_InhibitionPercent Inhibition20Float%
40Dopamine_D4.2_OutcomeActive/Inactive20Integer
41Transporter_Dopamine_(DAT)_Percent_InhibitionPercent Inhibition21Float%
42Transporter_Dopamine_(DAT)_OutcomeActive/Inactive21Integer
43Endothelin_ETA_Percent_InhibitionPercent Inhibition22Float%
44Endothelin_ETA_OutcomeActive/Inactive22Integer
45Endothelin_ETB_Percent_InhibitionPercent Inhibition23Float%
46Endothelin_ETB_OutcomeActive/Inactive23Integer
47Epidermal_Growth Factor_(EGF)_Percent_InhibitionPercent Inhibition24Float%
48Epidermal_Growth Factor_(EGF)_OutcomeActive/Inactive24Integer
49Estrogen_ERalpha_Percent_InhibitionPercent Inhibition25Float%
50Estrogen_ERalpha_OutcomeActive/Inactive25Integer
51Transporter_GABA_Percent_InhibitionPercent Inhibition26Float%
52Transporter_GABA_OutcomeActive/Inactive26Integer
53GABAA_Muscimol_Central_Percent_InhibitionPercent Inhibition27Float%
54GABAA_Muscimol_Central_OutcomeActive/Inactive27Integer
55GABAB1A_Percent_InhibitionPercent Inhibition28Float%
56GABAB1A_OutcomeActive/Inactive28Integer
57Glucocorticoid_Percent_InhibitionPercent Inhibition29Float%
58Glucocorticoid_OutcomeActive/Inactive29Integer
59Glutamate_Kainate_Percent_InhibitionPercent Inhibition30Float%
60Glutamate_Kainate_OutcomeActive/Inactive30Integer
61Glutamate_NMDA_Agonism_Percent_InhibitionPercent Inhibition31Float%
62Glutamate_NMDA_Agonism_OutcomeActive/Inactive31Integer
63Histamine_H1_Percent_InhibitionPercent Inhibition32Float%
64Histamine_H1_OutcomeActive/Inactive32Integer
65Histamine_H2_Percent_InhibitionPercent Inhibition33Float%
66Histamine_H2_OutcomeActive/Inactive33Integer
67Histamine_H3_Percent_InhibitionPercent Inhibition34Float%
68Histamine_H3_OutcomeActive/Inactive34Integer
69Imidazoline_I2_Central_Percent_InhibitionPercent Inhibition35Float%
70Imidazoline_I2_Central_OutcomeActive/Inactive35Integer
71Interleukin_IL-1_Percent_InhibitionPercent Inhibition36Float%
72Interleukin_IL-1_OutcomeActive/Inactive36Integer
73Leukotriene_Cysteinyl_CysLT1_Percent_InhibitionPercent Inhibition37Float%
74Leukotriene_Cysteinyl_CysLT1_OutcomeActive/Inactive37Integer
75Melatonin_MT1_Percent_InhibitionPercent Inhibition38Float%
76Melatonin_MT1_OutcomeActive/Inactive38Integer
77Muscarinic_M1_Percent_InhibitionPercent Inhibition39Float%
78Muscarinic_M1_OutcomeActive/Inactive39Integer
79Muscarinic_M2_Percent_InhibitionPercent Inhibition40Float%
80Muscarinic_M2_OutcomeActive/Inactive40Integer
81Muscarinic_M3_Percent_InhibitionPercent Inhibition41Float%
82Muscarinic_M3_OutcomeActive/Inactive41Integer
83Tachykinin_NK1_Percent_InhibitionPercent Inhibition42Float%
84Tachykinin_NK1_OutcomeActive/Inactive42Integer
85Neuropeptide_YY1_Percent_InhibitionPercent Inhibition43Float%
86Neuropeptide_YY1_OutcomeActive/Inactive43Integer
87Neuropeptide_YY2_Percent_InhibitionPercent Inhibition44Float%
88Neuropeptide_YY2_OutcomeActive/Inactive44Integer
89Nicotinic_Acetylcholine_Percent_InhibitionPercent Inhibition45Float%
90Nicotinic_Acetylcholine_OutcomeActive/Inactive45Integer
91Nicotinic_Acetylcholine_Alpha1_Bungarotoxin_Percent_InhibitionPercent Inhibition46Float%
92Nicotinic_Acetylcholine_Alpha1_Bungarotoxin_OutcomeActive/Inactive46Integer
93Opiate_delta1 _(OP1, DOP)_Percent_InhibitionPercent Inhibition47Float%
94Opiate_delta1 _(OP1, DOP)_OutcomeActive/Inactive47Integer
95Opiate_kappa_(OP2, KOP)_Percent_InhibitionPercent Inhibition48Float%
96Opiate_kappa_(OP2, KOP)_OutcomeActive/Inactive48Integer
97Opiate_mu_(OP3, MOP)_Percent_InhibitionPercent Inhibition49Float%
98Opiate_mu_(OP3, MOP)_OutcomeActive/Inactive49Integer
99Phorbol_Ester_Percent_InhibitionPercent Inhibition50Float%
100Phorbol_Ester_OutcomeActive/Inactive50Integer
101Platelet_Activating_Factor _(PAF)_Percent_InhibitionPercent Inhibition51Float%
102Platelet_Activating_Factor _(PAF)_OutcomeActive/Inactive51Integer
103Potassium_Channel_[KATP]_Percent_InhibitionPercent Inhibition52Float%
104Potassium_Channel_[KATP]_OutcomeActive/Inactive52Integer
105Potassium_Channel_hERG_Percent_InhibitionPercent Inhibition53Float%
106Potassium_Channel_hERG_OutcomeActive/Inactive53Integer
107Prostanoid_EP4_Percent_InhibitionPercent Inhibition54Float%
108Prostanoid_EP4_OutcomeActive/Inactive54Integer
109Purinergic_P2X_Percent_InhibitionPercent Inhibition55Float%
110Purinergic_P2X_OutcomeActive/Inactive55Integer
111Purinergic_P2Y_Percent_InhibitionPercent Inhibition56Float%
112Purinergic_P2Y_OutcomeActive/Inactive56Integer
113Rolipram_Percent_InhibitionPercent Inhibition57Float%
114Rolipram_OutcomeActive/Inactive57Integer
115Serotonin_(5-Hydroxytryptamine)_5-HT1A_Percent_InhibitionPercent Inhibition58Float%
116Serotonin_(5-Hydroxytryptamine)_5-HT1A_OutcomeActive/Inactive58Integer
117Serotonin_(5-Hydroxytryptamine)_5-HT2B_Percent_InhibitionPercent Inhibition59Float%
118Serotonin_(5-Hydroxytryptamine)_5-HT2B_OutcomeActive/Inactive59Integer
119Serotonin_(5-Hydroxytryptamine)_5-HT3_Percent_InhibitionPercent Inhibition60Float%
120Serotonin_(5-Hydroxytryptamine)_5-HT3_OutcomeActive/Inactive60Integer
121Transporter_Serotonin_(5-Hydroxytryptamine)_(SERT)_Percent_InhibitionPercent Inhibition61Float%
122Transporter_Serotonin_(5-Hydroxytryptamine)_(SERT)_OutcomeActive/Inactive61Integer
123Sigma1_Percent_InhibitionPercent Inhibition62Float%
124Sigma1_OutcomeActive/Inactive62Integer
125Sodium _Channel_Site_2_Percent_InhibitionPercent Inhibition63Float%
126Sodium _Channel_Site_2_OutcomeActive/Inactive63Integer
127Androgen_(Testosterone)_AR_Percent_InhibitionPercent Inhibition64Float%
128Androgen_(Testosterone)_AR_OutcomeActive/Inactive64Integer
129Thyroid_Hormone_Percent_InhibitionPercent Inhibition65Float%
130Thyroid_Hormone_OutcomeActive/Inactive65Integer
Additional Information
Grant Number: R03DA028852-01

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