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BioAssay: AID 488935

SAR analysis of small molecule antagonists of the kappa opioid receptor via a luminescent beta-arrestin assay - Set 6

Network: NIH Molecular Libraries Probe Production Centers Network(MLPCN)Grant Number: 1X01DA026208-01 ..more
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 Tested Compounds
 Tested Compounds
All(18)
 
 
Active(12)
 
 
Inactive(6)
 
 
 Tested Substances
 Tested Substances
All(18)
 
 
Active(12)
 
 
Inactive(6)
 
 
AID: 488935
Data Source: Burnham Center for Chemical Genomics (SBCCG-A509-KOR-Antagonist-DryPowder-Assay-6)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2010-10-26
Hold-until Date: 2011-05-01
Modify Date: 2011-05-03

Data Table ( Complete ):           View Active Data    View All Data
Target
BioActive Compounds: 12
Related Experiments
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AIDNameTypeProbeComment
1777uHTS identification of small molecule agonists of the kappa opioid receptor via a luminescent beta-arrestin assayConfirmatory depositor-specified cross reference
1778uHTS identification of small molecule antagonists of the kappa opioid receptor via a luminescent beta-arrestin assayConfirmatory depositor-specified cross reference
1785Summary of small molecule antagonists of the kappa opioid receptorSummary2 depositor-specified cross reference: Summary AID.
1786Summary of small molecule agonists of the kappa opioid receptorSummary2 depositor-specified cross reference: Summary AID.
1966HTS Dose response counterscreen for assays utilizing the enzyme, b-galactosidaseConfirmatory depositor-specified cross reference
2133HTS Image-Based Screen for Selective Agonists of the KOR ReceptorConfirmatory depositor-specified cross reference
2136HTS Image-Based Screen for Selective Antagonists of the KOR ReceptorConfirmatory depositor-specified cross reference
2285SAR analysis of small molecule antagonists of the kappa opioid receptor via a luminescent beta-arrestin assayConfirmatory depositor-specified cross reference
2344HTS Image-Based Screen for Agonists of the MOR ReceptorConfirmatory same project related to Summary assay
2348SAR analysis of Antagonists of the Kappa Opioid Receptor (KOR) using an Image-Based AssayConfirmatory same project related to Summary assay
2352SAR Analysis of Agonists of the MOR Receptor using an Image-Based AssayConfirmatory same project related to Summary assay
2356HTS Image-Based Screen for Antagonists of the DOR ReceptorConfirmatory same project related to Summary assay
2357SAR Analysis of Antagonists of the DOR Receptor using an Image-Based AssayConfirmatory same project related to Summary assay
2359SAR analysis of Agonists of the Kappa Opioid Receptor (KOR) using an Image-Based AssayConfirmatory same project related to Summary assay
2370SAR Analysis of Agonists of the DOR Receptor using an Image-Based AssayConfirmatory same project related to Summary assay
2420SAR Analysis of Antagonists of the MOR Receptor using an Image-Based AssayConfirmatory same project related to Summary assay
2478SAR Analysis of Antagonists of the MOR Receptor using an Image-Based Assay - Set 2Confirmatory same project related to Summary assay
2491SAR analysis of Antagonists of the Kappa Opioid Receptor (KOR) using an Image-Based Assay - Set 2Confirmatory same project related to Summary assay
2492SAR Analysis of Agonists of the MOR Receptor using an Image-Based Assay - Set 2Confirmatory same project related to Summary assay
2493SAR Analysis of Agonists of the DOR Receptor using an Image-Based Assay - Set 2Confirmatory same project related to Summary assay
2495SAR analysis of small molecule antagonists of the kappa opioid receptor via a luminescent beta-arrestin assay - Set 2Confirmatory same project related to Summary assay
2498SAR Analysis of Antagonists of the DOR Receptor using an Image-Based Assay - Set 2Confirmatory same project related to Summary assay
2500SAR analysis of small molecule agonists of the kappa opioid receptor via a luminescent beta-arrestin assay - Set 2Confirmatory same project related to Summary assay
434981SAR analysis of small molecule antagonists of the kappa opioid receptor via a luminescent beta-arrestin assay - Set 3Confirmatory same project related to Summary assay
449737SAR analysis of small molecule agonists of the kappa opioid receptor via a luminescent beta-arrestin assay - Set 3Confirmatory same project related to Summary assay
463105SAR analysis of small molecule antagonists of the kappa opioid receptor via a luminescent beta-arrestin assay - Set 4Confirmatory same project related to Summary assay
488819SAR analysis of Antagonists of the Kappa Opioid Receptor (KOR) using an Image-Based Assay - Set 3Confirmatory same project related to Summary assay
488822SAR Analysis of Agonists of the MOR Receptor using an Image-Based Assay - Set 3Confirmatory same project related to Summary assay
488826SAR analysis of small molecule antagonists of the kappa opioid receptor via a luminescent beta-arrestin assay - Set 5Confirmatory same project related to Summary assay
488831SAR Analysis of Antagonists of the DOR Receptor using an Image-Based Assay - Set 3Confirmatory same project related to Summary assay
488842SAR Analysis of Antagonists of the MOR Receptor using an Image-Based Assay - Set 3Confirmatory same project related to Summary assay
488925SAR analysis of Antagonists of the Kappa Opioid Receptor (KOR) using an Image-Based Assay - Set 4Confirmatory same project related to Summary assay
2284SAR analysis of small molecule agonists of the kappa opioid receptor via a luminescent beta-arrestin assayConfirmatory same project related to Summary assay
2343HTS Image-Based Screen for Agonists of the DOR ReceptorConfirmatory same project related to Summary assay
2344HTS Image-Based Screen for Agonists of the MOR ReceptorConfirmatory same project related to Summary assay
2348SAR analysis of Antagonists of the Kappa Opioid Receptor (KOR) using an Image-Based AssayConfirmatory same project related to Summary assay
2352SAR Analysis of Agonists of the MOR Receptor using an Image-Based AssayConfirmatory same project related to Summary assay
2356HTS Image-Based Screen for Antagonists of the DOR ReceptorConfirmatory same project related to Summary assay
2357SAR Analysis of Antagonists of the DOR Receptor using an Image-Based AssayConfirmatory same project related to Summary assay
2359SAR analysis of Agonists of the Kappa Opioid Receptor (KOR) using an Image-Based AssayConfirmatory same project related to Summary assay
2370SAR Analysis of Agonists of the DOR Receptor using an Image-Based AssayConfirmatory same project related to Summary assay
2420SAR Analysis of Antagonists of the MOR Receptor using an Image-Based AssayConfirmatory same project related to Summary assay
2478SAR Analysis of Antagonists of the MOR Receptor using an Image-Based Assay - Set 2Confirmatory same project related to Summary assay
2491SAR analysis of Antagonists of the Kappa Opioid Receptor (KOR) using an Image-Based Assay - Set 2Confirmatory same project related to Summary assay
2492SAR Analysis of Agonists of the MOR Receptor using an Image-Based Assay - Set 2Confirmatory same project related to Summary assay
2493SAR Analysis of Agonists of the DOR Receptor using an Image-Based Assay - Set 2Confirmatory same project related to Summary assay
2495SAR analysis of small molecule antagonists of the kappa opioid receptor via a luminescent beta-arrestin assay - Set 2Confirmatory same project related to Summary assay
2497SAR analysis of Agonists of the Kappa Opioid Receptor (KOR) using an Image-Based Assay - Set 2Confirmatory same project related to Summary assay
2498SAR Analysis of Antagonists of the DOR Receptor using an Image-Based Assay - Set 2Confirmatory same project related to Summary assay
2500SAR analysis of small molecule agonists of the kappa opioid receptor via a luminescent beta-arrestin assay - Set 2Confirmatory same project related to Summary assay
434981SAR analysis of small molecule antagonists of the kappa opioid receptor via a luminescent beta-arrestin assay - Set 3Confirmatory same project related to Summary assay
449737SAR analysis of small molecule agonists of the kappa opioid receptor via a luminescent beta-arrestin assay - Set 3Confirmatory same project related to Summary assay
463105SAR analysis of small molecule antagonists of the kappa opioid receptor via a luminescent beta-arrestin assay - Set 4Confirmatory same project related to Summary assay
488822SAR Analysis of Agonists of the MOR Receptor using an Image-Based Assay - Set 3Confirmatory same project related to Summary assay
488824SAR Analysis of Agonists of the DOR Receptor using an Image-Based Assay - Set 3Confirmatory same project related to Summary assay
488833SAR analysis of Agonists of the Kappa Opioid Receptor (KOR) using an Image-Based Assay-Set 3Confirmatory same project related to Summary assay
488842SAR Analysis of Antagonists of the MOR Receptor using an Image-Based Assay - Set 3Confirmatory same project related to Summary assay
Description:
Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG)
Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA)
Network: NIH Molecular Libraries Probe Production Centers Network(MLPCN)Grant Number: 1X01DA026208-01
Assay Provider: Dr. Lawrance Barak , Duke University, Durham NC

Drug addiction is a disease originating in the central nervous system that produces compulsive behaviors despite the negative consequences that may result. Major addictive drugs of abuse include components of tobacco, opiates, marijuana, ethanol, cocaine, and derivatives of amphetamines. While the addictive behaviors produced by these substances may be generally similar, the drugs act at different receptor sites in the brain. Recent studies have shown that opioid receptors play a role regulating the addictive behaviors of other receptors that interact with illicit and legal substances of abuse. Opioid receptors are composed of multiple subtypes whose contributions to addictive behaviors are not fully delineated. Moreover, different compounds acting at a single receptor type may produce dissimilar behaviors due to variations in their chemical structures. Thus, both for delineating the biology and signaling ability of each receptor and for developing novel therapies, it would be desirable to identify multiple small molecule ligands that target a given receptor subtype. This entails expanding the chemical space about each of the receptors as variations in receptor conformations due to distinct ligand structures affect receptor signaling behaviors, and consequently physiological responsiveness. Morphine is a prime example of an opioid ligand with distinctive signaling properties.

The specific aim of this project is to identify subtype specific small molecule agonists of the human kappa opioid receptor (KOR). These compounds can be optimized to provide the pharmacological means to precisely control the signaling of their specific target receptor subtype. This work thus provides the addiction field both novel research tools and potential therapeutic scaffolds. This is a luminescence assay based off of a kappa opioid cell line and beta-arrestin technology from DiscoveRx.

This dose response assay is developed and performed to confirm hits originally identified in "uHTS identification of small molecule antagonists of the kappa opioid receptor via a luminescent beta-arrestin assay" (AID 1778) and to study the structure-activity relationship on analogs of the confirmed hits. Compounds are either acquired from commercial sources or synthesized internally.
Protocol
Assay materials:

1) OPRK1 beta-Arrestin (DiscoveRx)
2) Assay Medium: Opti-MEM Medium supplemented with 1% hiFBS, 1X Pen/Strep/Glu, 125 ug/mL Hygromycin (1/2 recommended), 250 ug/mL Geneticin (1/2 recommended)
3) Growth Medium: MEM supplemented with 10% hiFBS, 1X Pen/Strep/Glu, 125 ug/mL Hygromycin (1/2 recommended), 250 ug/mL Geneticin (1/2 recommended)

Day 1
1) Harvest cells using Enzyme-Free Dissociation Buffer (Invitrogen Cat#13151-14). Add 500 cells/well in 5 uL of media to each well of a white, 1536 well plate.
2) Spin cells at 500 rpm for 1 min, then wrap plates in Saran Wrap.
3) Incubate overnight at 37C with 5% CO2.

Day 2
1) Using a Labcyte Echo, DMSO and test compounds are transferred to wells. DMSO only is transferred to columns 1-3 and 46-48(Control wells), while varying volumes of test compounds are transferred to columns 4-45 to achieve the desired test concentrations. Test compound wells in the assay plate are back-filled with DMSO to equalize final assay concentrations.
2) Immediately following Echo transfer, 1.0 uL of assay media is added to columns 1-45 and 1.0 uL of assay media containing 6 uM dynorphin A is added to columns 46-48 for a final assay concentration of 1.0 uM. Centrifuge plates at 500 rpm for 1 min immediately following additions.
3) Incubate for 1hr and 30 minutes.
4) During test incubation, prepare Detection Reagent Solution from DiscoveRx (1 part Galacton Star: 5 parts Emerald II and 19 parts Cell Assay Buffer)
5) Add 2.5ul of detection reagent solution to each well.
6) Incubate at room temperature for 60 min in the dark
7) Read plates in a Perkin Elmer Envision using a luminescence protocol
Comment
Compounds with an IC50 < 10 uM are defined as actives in the dose response confirmation.

To simplify the distinction between the inactives of the primary screen and of the confirmatory screening stage, the Tiered Activity Scoring System was developed and implemented. Its utilization for the assay is described below.

Activity Scoring
Activity scoring rules were devised to take into consideration compound efficacy, its potential interference with the assay and the screening stage that the data was obtained. Details of the Scoring System will be published elsewhere. Briefly, the outline of the scoring system utilized for the assay is as follows:
1) First tier (0-40 range) is reserved for primary screening data and is not applicable to this assay

2) Second tier (41-80 range) is reserved for dose-response confirmation data and is not applicable to this assay

3) Third tier (81-100 range) is reserved for resynthesized true positives and their analogues.

a. Inactive compounds of the confirmatory stage are assigned a score value equal 81.
b. For the remaining compounds the score is linearly correlated with a compound's inhibitory potency and, in addition, provides a measure of the likelihood that the compound is not an artifact based on the available information.
c. The Hill coefficient is taken as a measure of compound behavior in the assay via an additional scaling factor QC:
QC = 2.6*[exp(-0.5*nH^2) - exp(-1.5*nH^2)]
This empirical factor prorates the likelihood of target-specific compound effect vs. its non-specific behavior in the assay. This factor is based on expectation that a compound with a single mode of action that achieved equilibrium in the inhibition assay demonstrates the Hill coefficient value of 1. Compounds deviating from that behavior are penalized proportionally to the degree of their deviation.
d. Summary equation that takes into account the items discussed above is
Score = 82 + 3*(pIC50 - 3)*QC,
where pIC50 is a negative log(10) of the IC50 value expressed in mole/L concentration units. This equation results in the Score values above 50 for compounds that demonstrate high potency and predictable behavior. Compounds that are inactive in the assay or whose concentration-dependent behavior are likely to be an artifact of that assay will generally have lower Score values.
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: Functional
Assay Cell Type: NULL
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1IC50_Mean_QualifierThis qualifier is to be used with the next TID, IC50_Mean. If qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that valueString
2IC50_Mean*IC50 value determined using sigmoidal dose response equationFloatμM
3IC50_Qualifier_1This qualifier is to be used with the next TID, IC50_1. If qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that valueString
4IC50_1IC50 value determined using sigmoidal dose response equationFloatμM
5Std.Err(IC50)_1Standard Error of IC50 valueFloatμM
6nH_1Hill coefficient determined using sigmoidal dose response equationFloat
7Excluded_Points_first_pointFlags to indicate which of the first dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
8% Activity at 20 uM_first_point (20μM**)% Inhibition at a given concentrationFloat%
9% Activity at 10 uM_first_point (10μM**)% Inhibition at a given concentrationFloat%
10% Activity at 5 uM_first_point (5μM**)% Inhibition at a given concentrationFloat%
11% Activity at 2.5 uM_first_point (2.5μM**)% Inhibition at a given concentrationFloat%
12% Activity at 1.25 uM_first_point (1.25μM**)% Inhibition at a given concentrationFloat%
13% Activity at 0.625 uM_first_point (0.625μM**)% Inhibition at a given concentrationFloat%
14% Activity at 0.3125 uM_first_point (0.3125μM**)% Inhibition at a given concentrationFloat%
15% Activity at 0.15625 uM_first_point (0.15625μM**)% Inhibition at a given concentrationFloat%
16% Activity at 0.078125 uM_first_point (0.078125μM**)% Inhibition at a given concentrationFloat%
17% Activity at 0.0390625 uM_first_point (0.0390625μM**)% Inhibition at a given concentrationFloat%
18Excluded_Points_second_pointFlags to indicate which of the second dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
19% Activity at 20 uM_second_point (20μM**)% Inhibition at a given concentrationFloat%
20% Activity at 10 uM_second_point (10μM**)% Inhibition at a given concentrationFloat%
21% Activity at 5 uM_second_point (5μM**)% Inhibition at a given concentrationFloat%
22% Activity at 2.5 uM_second_point (2.5μM**)% Inhibition at a given concentrationFloat%
23% Activity at 1.25 uM_second_point (1.25μM**)% Inhibition at a given concentrationFloat%
24% Activity at 0.625 uM_second_point (0.625μM**)% Inhibition at a given concentrationFloat%
25% Activity at 0.3125 uM_second_point (0.3125μM**)% Inhibition at a given concentrationFloat%
26% Activity at 0.15625 uM_second_point (0.15625μM**)% Inhibition at a given concentrationFloat%
27% Activity at 0.078125 uM_second_point (0.078125μM**)% Inhibition at a given concentrationFloat%
28% Activity at 0.0390625 uM_second_point (0.0390625μM**)% Inhibition at a given concentrationFloat%
29Excluded_Points_third_pointFlags to indicate which of the third dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
30% Activity at 20 uM_third_point (20μM**)% Inhibition at a given concentrationFloat%
31% Activity at 10 uM_third_point (10μM**)% Inhibition at a given concentrationFloat%
32% Activity at 5 uM_third_point (5μM**)% Inhibition at a given concentrationFloat%
33% Activity at 2.5 uM_third_point (2.5μM**)% Inhibition at a given concentrationFloat%
34% Activity at 1.25 uM_third_point (1.25μM**)% Inhibition at a given concentrationFloat%
35% Activity at 0.625 uM_third_point (0.625μM**)% Inhibition at a given concentrationFloat%
36% Activity at 0.3125 uM_third_point (0.3125μM**)% Inhibition at a given concentrationFloat%
37% Activity at 0.15625 uM_third_point (0.15625μM**)% Inhibition at a given concentrationFloat%
38% Activity at 0.078125 uM_third_point (0.078125μM**)% Inhibition at a given concentrationFloat%
39% Activity at 0.0390625 uM_third_point (0.0390625μM**)% Inhibition at a given concentrationFloat%
40IC50_Qualifier_2This qualifier is to be used with the next TID, IC50_2. If qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that valueString
41IC50_2IC50 value determined using sigmoidal dose response equationFloatμM
42Std.Err(IC50)_2Standard Error of IC50 valueFloatμM
43nH_2Hill coefficient determined using sigmoidal dose response equationFloat
44Excluded_Points_fourth_pointFlags to indicate which of the fourth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
45% Activity at 20 uM_fourth_point (20μM**)% Inhibition at a given concentrationFloat%
46% Activity at 10 uM_fourth_point (10μM**)% Inhibition at a given concentrationFloat%
47% Activity at 5 uM_fourth_point (5μM**)% Inhibition at a given concentrationFloat%
48% Activity at 2.5 uM_fourth_point (2.5μM**)% Inhibition at a given concentrationFloat%
49% Activity at 1.25 uM_fourth_point (1.25μM**)% Inhibition at a given concentrationFloat%
50% Activity at 0.625 uM_fourth_point (0.625μM**)% Inhibition at a given concentrationFloat%
51% Activity at 0.3125 uM_fourth_point (0.3125μM**)% Inhibition at a given concentrationFloat%
52% Activity at 0.15625 uM_fourth_point (0.15625μM**)% Inhibition at a given concentrationFloat%
53% Activity at 0.078125 uM_fourth_point (0.078125μM**)% Inhibition at a given concentrationFloat%
54% Activity at 0.0390625 uM_fourth_point (0.0390625μM**)% Inhibition at a given concentrationFloat%
55Excluded_Points_fifth_pointFlags to indicate which of the fifth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
56% Activity at 20 uM_fifth_point (20μM**)% Inhibition at a given concentrationFloat%
57% Activity at 10 uM_fifth_point (10μM**)% Inhibition at a given concentrationFloat%
58% Activity at 5 uM_fifth_point (5μM**)% Inhibition at a given concentrationFloat%
59% Activity at 2.5 uM_fifth_point (2.5μM**)% Inhibition at a given concentrationFloat%
60% Activity at 1.25 uM_fifth_point (1.25μM**)% Inhibition at a given concentrationFloat%
61% Activity at 0.625 uM_fifth_point (0.625μM**)% Inhibition at a given concentrationFloat%
62% Activity at 0.3125 uM_fifth_point (0.3125μM**)% Inhibition at a given concentrationFloat%
63% Activity at 0.15625 uM_fifth_point (0.15625μM**)% Inhibition at a given concentrationFloat%
64% Activity at 0.078125 uM_fifth_point (0.078125μM**)% Inhibition at a given concentrationFloat%
65% Activity at 0.0390625 uM_fifth_point (0.0390625μM**)% Inhibition at a given concentrationFloat%
66Excluded_Points_sixth_pointFlags to indicate which of the sixth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
67% Activity at 20 uM_sixth_point (20μM**)% Inhibition at a given concentrationFloat%
68% Activity at 10 uM_sixth_point (10μM**)% Inhibition at a given concentrationFloat%
69% Activity at 5 uM_sixth_point (5μM**)% Inhibition at a given concentrationFloat%
70% Activity at 2.5 uM_sixth_point (2.5μM**)% Inhibition at a given concentrationFloat%
71% Activity at 1.25 uM_sixth_point (1.25μM**)% Inhibition at a given concentrationFloat%
72% Activity at 0.625 uM_sixth_point (0.625μM**)% Inhibition at a given concentrationFloat%
73% Activity at 0.3125 uM_sixth_point (0.3125μM**)% Inhibition at a given concentrationFloat%
74% Activity at 0.15625 uM_sixth_point (0.15625μM**)% Inhibition at a given concentrationFloat%
75% Activity at 0.078125 uM_sixth_point (0.078125μM**)% Inhibition at a given concentrationFloat%
76% Activity at 0.0390625 uM_sixth_point (0.0390625μM**)% Inhibition at a given concentrationFloat%
77IC50_Qualifier_3This qualifier is to be used with the next TID, IC50_3. If qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that valueString
78IC50_3IC50 value determined using sigmoidal dose response equationFloatμM
79Std.Err(IC50)_3Standard Error of IC50 valueFloatμM
80nH_3Hill coefficient determined using sigmoidal dose response equationFloat
81Excluded_Points_seventh_pointFlags to indicate which of the seventh dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
82% Activity at 20 uM_seventh_point (20μM**)% Inhibition at a given concentrationFloat%
83% Activity at 10 uM_seventh_point (10μM**)% Inhibition at a given concentrationFloat%
84% Activity at 5 uM_seventh_point (5μM**)% Inhibition at a given concentrationFloat%
85% Activity at 2.5 uM_seventh_point (2.5μM**)% Inhibition at a given concentrationFloat%
86% Activity at 1.25 uM_seventh_point (1.25μM**)% Inhibition at a given concentrationFloat%
87% Activity at 0.625 uM_seventh_point (0.625μM**)% Inhibition at a given concentrationFloat%
88% Activity at 0.3125 uM_seventh_point (0.3125μM**)% Inhibition at a given concentrationFloat%
89% Activity at 0.15625 uM_seventh_point (0.15625μM**)% Inhibition at a given concentrationFloat%
90% Activity at 0.078125 uM_seventh_point (0.078125μM**)% Inhibition at a given concentrationFloat%
91% Activity at 0.0390625 uM_seventh_point (0.0390625μM**)% Inhibition at a given concentrationFloat%
92Excluded_Points_eighth_pointFlags to indicate which of the eighth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
93% Activity at 20 uM_eighth_point (20μM**)% Inhibition at a given concentrationFloat%
94% Activity at 10 uM_eighth_point (10μM**)% Inhibition at a given concentrationFloat%
95% Activity at 5 uM_eighth_point (5μM**)% Inhibition at a given concentrationFloat%
96% Activity at 2.5 uM_eighth_point (2.5μM**)% Inhibition at a given concentrationFloat%
97% Activity at 1.25 uM_eighth_point (1.25μM**)% Inhibition at a given concentrationFloat%
98% Activity at 0.625 uM_eighth_point (0.625μM**)% Inhibition at a given concentrationFloat%
99% Activity at 0.3125 uM_eighth_point (0.3125μM**)% Inhibition at a given concentrationFloat%
100% Activity at 0.15625 uM_eighth_point (0.15625μM**)% Inhibition at a given concentrationFloat%
101% Activity at 0.078125 uM_eighth_point (0.078125μM**)% Inhibition at a given concentrationFloat%
102% Activity at 0.0390625 uM_eighth_point (0.0390625μM**)% Inhibition at a given concentrationFloat%
103Excluded_Points_ninth_pointFlags to indicate which of the ninth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
104% Activity at 20 uM_ninth_point (20μM**)% Inhibition at a given concentrationFloat%
105% Activity at 10 uM_ninth_point (10μM**)% Inhibition at a given concentrationFloat%
106% Activity at 5 uM_ninth_point (5μM**)% Inhibition at a given concentrationFloat%
107% Activity at 2.5 uM_ninth_point (2.5μM**)% Inhibition at a given concentrationFloat%
108% Activity at 1.25 uM_ninth_point (1.25μM**)% Inhibition at a given concentrationFloat%
109% Activity at 0.625 uM_ninth_point (0.625μM**)% Inhibition at a given concentrationFloat%
110% Activity at 0.3125 uM_ninth_point (0.3125μM**)% Inhibition at a given concentrationFloat%
111% Activity at 0.15625 uM_ninth_point (0.15625μM**)% Inhibition at a given concentrationFloat%
112% Activity at 0.078125 uM_ninth_point (0.078125μM**)% Inhibition at a given concentrationFloat%
113% Activity at 0.0390625 uM_ninth_point (0.0390625μM**)% Inhibition at a given concentrationFloat%
114IC50_Qualifier_4This qualifier is to be used with the next TID, IC50_4. If qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that valueString
115IC50_4IC50 value determined using sigmoidal dose response equationFloatμM
116Std.Err(IC50)_4Standard Error of IC50 valueFloatμM
117nH_4Hill coefficient determined using sigmoidal dose response equationFloat
118Excluded_Points_tenth_pointFlags to indicate which of the tenth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
119% Activity at 20 uM_tenth_point (20μM**)% Inhibition at a given concentrationFloat%
120% Activity at 10 uM_tenth_point (10μM**)% Inhibition at a given concentrationFloat%
121% Activity at 5 uM_tenth_point (5μM**)% Inhibition at a given concentrationFloat%
122% Activity at 2.5 uM_tenth_point (2.5μM**)% Inhibition at a given concentrationFloat%
123% Activity at 1.25 uM_tenth_point (1.25μM**)% Inhibition at a given concentrationFloat%
124% Activity at 0.625 uM_tenth_point (0.625μM**)% Inhibition at a given concentrationFloat%
125% Activity at 0.3125 uM_tenth_point (0.3125μM**)% Inhibition at a given concentrationFloat%
126% Activity at 0.15625 uM_tenth_point (0.15625μM**)% Inhibition at a given concentrationFloat%
127% Activity at 0.078125 uM_tenth_point (0.078125μM**)% Inhibition at a given concentrationFloat%
128% Activity at 0.0390625 uM_tenth_point (0.0390625μM**)% Inhibition at a given concentrationFloat%
129Excluded_Points_eleventh_pointFlags to indicate which of the eleventh dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
130% Activity at 20 uM_eleventh_point (20μM**)% Inhibition at a given concentrationFloat%
131% Activity at 10 uM_eleventh_point (10μM**)% Inhibition at a given concentrationFloat%
132% Activity at 5 uM_eleventh_point (5μM**)% Inhibition at a given concentrationFloat%
133% Activity at 2.5 uM_eleventh_point (2.5μM**)% Inhibition at a given concentrationFloat%
134% Activity at 1.25 uM_eleventh_point (1.25μM**)% Inhibition at a given concentrationFloat%
135% Activity at 0.625 uM_eleventh_point (0.625μM**)% Inhibition at a given concentrationFloat%
136% Activity at 0.3125 uM_eleventh_point (0.3125μM**)% Inhibition at a given concentrationFloat%
137% Activity at 0.15625 uM_eleventh_point (0.15625μM**)% Inhibition at a given concentrationFloat%
138% Activity at 0.078125 uM_eleventh_point (0.078125μM**)% Inhibition at a given concentrationFloat%
139% Activity at 0.0390625 uM_eleventh_point (0.0390625μM**)% Inhibition at a given concentrationFloat%
140Excluded_Points_twelfth_pointFlags to indicate which of the twelfth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
141% Activity at 20 uM_twelfth_point (20μM**)% Inhibition at a given concentrationFloat%
142% Activity at 10 uM_twelfth_point (10μM**)% Inhibition at a given concentrationFloat%
143% Activity at 5 uM_twelfth_point (5μM**)% Inhibition at a given concentrationFloat%
144% Activity at 2.5 uM_twelfth_point (2.5μM**)% Inhibition at a given concentrationFloat%
145% Activity at 1.25 uM_twelfth_point (1.25μM**)% Inhibition at a given concentrationFloat%
146% Activity at 0.625 uM_twelfth_point (0.625μM**)% Inhibition at a given concentrationFloat%
147% Activity at 0.3125 uM_twelfth_point (0.3125μM**)% Inhibition at a given concentrationFloat%
148% Activity at 0.15625 uM_twelfth_point (0.15625μM**)% Inhibition at a given concentrationFloat%
149% Activity at 0.078125 uM_twelfth_point (0.078125μM**)% Inhibition at a given concentrationFloat%
150% Activity at 0.0390625 uM_twelfth_point (0.0390625μM**)% Inhibition at a given concentrationFloat%

* Activity Concentration. ** Test Concentration.
Additional Information
Grant Number: 1X01DA026208-01

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