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BioAssay: AID 504524

SAR analysis of a small molecule agonists of the APJ receptor via a luminescent beta-arrestin assay - Set 5

Currently there are no small molecule tools to investigate the biological functions of apelin and its receptor. Apelin is the endogenous peptide ligand for the G-protein coupled receptor (GPCR) APJ (angiotensin II receptor-like 1, AGTRL-1 and APLNR). Until the discovery of apelin, APJ was an orphan GPCR. APJ is coupled to Gai, and has been shown in cell culture to inhibit adenylate cyclase. The more ..
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 Tested Compounds
 Tested Compounds
All(31)
 
 
Active(23)
 
 
Inactive(8)
 
 
 Tested Substances
 Tested Substances
All(31)
 
 
Active(23)
 
 
Inactive(8)
 
 
AID: 504524
Data Source: Burnham Center for Chemical Genomics (SBCCG-A615-APJ-Agonist-DryPowder-Assay-5)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2011-03-22
Hold-until Date: 2012-03-21
Modify Date: 2012-03-21

Data Table ( Complete ):           View Active Data    View All Data
Target
BioActive Compounds: 23
Related Experiments
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AIDNameTypeProbeComment
2520uHTS identification of small molecule agonists of the APJ receptor via a luminescent beta-arrestin assayScreening depositor-specified cross reference
2580Summary assay for small molecule agonists of the APJ receptorSummary1 depositor-specified cross reference: Summary AID.
2764Single concentration confirmation of uHTS hits from a small molecule agonists of the APJ receptor via a luminescent beta-arrestin assayScreening same project related to Summary assay
488748Dose Response confirmation of uHTS hits from a small molecule agonists of the APJ receptor via a luminescent beta-arrestin assayConfirmatory same project related to Summary assay
488811SAR analysis of a small molecule agonists of the APJ receptor via a luminescent beta-arrestin assayConfirmatory same project related to Summary assay
488865Dose Response screen for agonists of Angiotensin II Receptor Type 1 to assess selectivity of uHTS small molecule agonists hits of the APJ receptorConfirmatory same project related to Summary assay
488881SAR analysis of small molecule agonists of the Angiotensin II Receptor Type 1 to assess selectivity of uHTS small molecule agonists hits of the APJ receptorConfirmatory same project related to Summary assay
488985SAR analysis of a small molecule agonists of the APJ receptor via a luminescent beta-arrestin assay - Set 2Confirmatory same project related to Summary assay
488986SAR analysis of small molecule agonists of the Angiotensin II Receptor Type 1 to assess selectivity of uHTS small molecule agonists hits of the APJ receptor - Set 2Confirmatory same project related to Summary assay
492982SAR analysis of small molecule agonists of the Angiotensin II Receptor Type 1 to assess selectivity of uHTS small molecule agonists hits of the APJ receptor - Set 3Confirmatory same project related to Summary assay
492985SAR analysis of a small molecule agonists of the APJ receptor via a luminescent beta-arrestin assay - Set 3Confirmatory same project related to Summary assay
493183SAR analysis of a small molecule agonists of the APJ receptor via a luminescent beta-arrestin assay - Set 4Confirmatory same project related to Summary assay
493202SAR analysis of small molecule agonists of the Angiotensin II Receptor Type 1 to assess selectivity of uHTS small molecule agonists hits of the APJ receptor - Set 4Confirmatory same project related to Summary assay
504532SAR analysis of small molecule agonists of the Angiotensin II Receptor Type 1 to assess selectivity of uHTS small molecule agonists hits of the APJ receptor - Set 5Confirmatory 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)
Network: NIH Molecular Libraries Production Centers Network (MLPCN)
Grant Number: 1R21NS059422-01
Assay Provider: Dr. Layton Smith, Sanford-Burnham Medical Research Institute

Currently there are no small molecule tools to investigate the biological functions of apelin and its receptor. Apelin is the endogenous peptide ligand for the G-protein coupled receptor (GPCR) APJ (angiotensin II receptor-like 1, AGTRL-1 and APLNR). Until the discovery of apelin, APJ was an orphan GPCR. APJ is coupled to Gai, and has been shown in cell culture to inhibit adenylate cyclase. The APJ gene encodes a receptor that most closely resembles the angiotensin receptor AT1. However, the APJ receptor does not bind angiotensin II. Underscoring the emerging importance of the apelin/APJ system, recent studies have shown that apelin reduces the extent of atherosclerotic lesions in ApoE-/- mice, and opposes the development of abdominal aortic aneurysms. Additional research has revealed that APJ forms a heterodimer with the Ang II receptor AT1, and that this complex facilitates antagonism of Ang II signaling by apelin. Despite these exciting results, there remains a multitude of unanswered questions regarding the role of apelin and APJ in physiology and pathology.
The project goal is to identify a chemical probe of apelin receptor function that transiently and reversibly activates the receptor. An agonist or potentiator of this receptor would provide a novel research tool to evaluate the role of apelin in cardiovascular and metabolic disease pathology.
In this description we utilize enzyme-fragment complementation to directly measure GPCR activation. Unlike imaging or other second messenger assays, the DiscoveRx b-Arrestin assay allows for a direct measure of GPCR activation by detection of b-Arrestin binding to the APJ receptor. In this system, b-Arrestin is fused to an N-terminal deletion mutant of b-gal (termed the enzyme acceptor of EA) and the GPCR of interest is fused to a smaller (42 amino acids), weakly complementing fragment termed ProLink. In cells that stably express these fusion proteins, ligand stimulation results in the interaction of b-Arrestin and the Prolink-tagged GPCR, forcing the complementation of the two b-gal fragments and resulting in the formation of a functional enzyme that converts substrate to detectable signal.

This dose response assay is developed and performed to confirm hits originally identified in "uHTS identification of small molecule agonists of the APJ receptor via a luminescent beta-arrestin assay" (AID 2520) and to study the structure-activity relationship on analogs of the confirmed hits. Compounds are either acquired from commercial sources or synthesized internally.
Protocol
A. Brief Description of the Assay:
The purpose of this assay is to detect agonists that cause the activation the Angiotensin II receptor-like 1 (Apelin receptor) in the CHO-K1 AGTRL-1 beta-Arrestin Cell Line in 1536-well plate format in uHTS mode.
B. Materials:
Angiotensin II receptor-like 1 (AGTRL-1) Cell Line (DiscoveRx, Cat# 93-0250C2)
F12 nutrient mix HAMs (Invitrogen, Cat# 11765)
Fetal Bovine Serum, heat-inactivated (Hyclone, Cat# SH30396)
100X Penicillin/Streptomycin Solution (Invitrogen, Cat#15140-122)
Hygromycin B (Roche, Cat# 10843555001)
Geneticin (MPBiomedicals, Cat# 1672548)
Trypsin-EDTA 0.25% (Invitrogen, Cat# 25200-056)
Cell Dissociation Buffer (Invitrogen, Cat# 13151)
DPBS (Hyclone, Cat# 30028.02)
T225 TC Flask (Nunc, Cat# 159934)
Cell strainer, 40 um (BD, Cat# 352340)
1536-well, white, solid-bottom, Kalypsys compatible, TC plate (Corning)
Apelin-13 (Sigma-Aldrich, Cat# A6469)
PathHunter Detection Reagents (DiscoveRx, Cat# 93-0001)
Galacton Star
Emerald 11
Cell Assay Buffer
D. Dose Response Procedures:
Day1 -Cell Seeding
1) Plate 1000 cells/well in 4 uL of assay media into columns 1-48 of a 1536-well assay plate, using straight tip dispense on a Kalypsys dispenser.
2) Centrifuge plates at 500 rpm for 1 minute on a Vspin centrifuge. Use Kalypsys metal lids.
3) Incubate overnight at 37 degrees, 100% relative humidity, 5% CO2 for 16-18 hours.
Day2 -Compound Addition
1) Centrifuge compound plates at 500 rpm for 1 minute on a Vspin centrifuge.
2) Using LabCyte Echo, transfer varying volumes from a 2 mM Echo qualified plate containing test compounds into assay plate Col. 5 - 48 to achieve the desired dose response concentrations and range. Backfill with DMSO to equalize final DMSO concentrations in all test wells. Transfer equal volume of DMSO to positive and negative control wells in Columns 1 - 4.
3) Immediately following compound/DMSO transfer via the Echo, using the Kalypsys Dispenser, transfer 2ul/well of Assay media to Col. 3-48 for the negative control and test compound wells.
4) Using the Kalypsys Dispenser, add 2ul/well of 30 nM Apelin-13 in assay media to Col. 1-2 for the positive control .
5) Centrifuge plates at 500 rpm for 1 minute on a Vspin centrifuge.
6) Incubate plates at 25 degrees in the dark for 90 minutes.
7) Following 90 minute incubation, deliver 3.0 uL of Detection Reagent solution to each assay plate (Columns 1 - 48) using a Kalypsys dispenser.
8) Centrifuge plates at 2000 rpm for 3 minute on a Vspin centrifuge.
9) Incubate plates for 60 minutes at 25 degrees in the dark.
10) Read plates using the Viewlux using a luminescence protocol.
E. Recipes:
Growth Media
F12 nutrient mix HAMs supplemented with 10% hi-FBS, 1X Penicillin/Streptomycin; selection reagents: 300ug/ml Hygromycin B, 800ug/ml Geneticin
Assay Media
Same as Growth Media without the selection reagents
Trypsin
Dilute 0.25% Trypsin/EDTA to 0.05% Trypsin/EDTA using DPBS
Positive Control
Growth Media with 30 nM Apelin-13
Detection Reagent
Use the following ratio to prepare the detection reagent:
Galacton Star : Emerald II : Assay Buffer = 1 : 5 : 19
Comment
Compounds with an EC50_Mean < 10 are considered to be active
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 in this assay.
2) Second tier (41-80 range) is reserved for dose-response confirmation data and is not applicable in 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. The score is linearly correlated with a compound 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 this 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*(pEC50 - 3)*QC,
where pEC50 is a negative log(10) of the EC50 value expressed in mole/L concentration units. This equation results in the Score values above 85 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.
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1EC50_Mean_QualifierThis qualifier is to be used with the next TID, EC50_Mean. If the qualifier is ""="", the EC50 result equals the value in that column. If the qualifier is "">"", the EC50 result is greater than that value. If the qualifier is ""<"", the EC50 result is smaller than that valueString
2EC50_Mean*EC50 value determined using a sigmoidal dose response equationFloatμM
3EC50_Qualifier_1_Range1This qualifier is to be used with the next TID, EC50_1. If the qualifier is "=", the EC50 result equals the value in that column. If the qualifier is ">", the EC50 result is greater than that value. If the qualifier is "<", the EC50 result is smaller than that valueString
4EC50_1_Range1EC50 value determined using a sigmoidal dose response equationFloatμM
5Std.Err(EC50)_1_Range1Standard Error of the EC50 valueFloatμM
6nH_1_Range1Hill coefficient determined using sigmoidal dose response equationFloat
7Excluded_Points_first_point_Range1Flags 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 79 uM_first_point_Range1 (79μM**)% activity at the test concentrationFloat%
9% Activity at 39.5 uM_first_point_Range1 (39.5μM**)% activity at the test concentrationFloat%
10% Activity at 19.75 uM_first_point_Range1 (19.75μM**)% activity at the test concentrationFloat%
11% Activity at 9.875 uM_first_point_Range1 (9.875μM**)% activity at the test concentrationFloat%
12% Activity at 4.9375 uM_first_point_Range1 (4.9375μM**)% activity at the test concentrationFloat%
13% Activity at 2.46875 uM_first_point_Range1 (2.46875μM**)% activity at the test concentrationFloat%
14% Activity at 1.234375 uM_first_point_Range1 (1.23438μM**)% activity at the test concentrationFloat%
15% Activity at 0.6171875 uM_first_point_Range1 (0.617188μM**)% activity at the test concentrationFloat%
16% Activity at 0.3085938 uM_first_point_Range1 (0.308594μM**)% activity at the test concentrationFloat%
17% Activity at 0.1542969 uM_first_point_Range1 (0.154297μM**)% activity at the test concentrationFloat%
18Excluded_Points_second_point_Range1Flags 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 79 uM_second_point_Range1 (79μM**)% activity at the test concentrationFloat%
20% Activity at 39.5 uM_second_point_Range1 (39.5μM**)% activity at the test concentrationFloat%
21% Activity at 19.75 uM_second_point_Range1 (19.75μM**)% activity at the test concentrationFloat%
22% Activity at 9.875 uM_second_point_Range1 (9.875μM**)% activity at the test concentrationFloat%
23% Activity at 4.9375 uM_second_point_Range1 (4.9375μM**)% activity at the test concentrationFloat%
24% Activity at 2.46875 uM_second_point_Range1 (2.46875μM**)% activity at the test concentrationFloat%
25% Activity at 1.234375 uM_second_point_Range1 (1.23438μM**)% activity at the test concentrationFloat%
26% Activity at 0.6171875 uM_second_point_Range1 (0.617188μM**)% activity at the test concentrationFloat%
27% Activity at 0.3085938 uM_second_point_Range1 (0.308594μM**)% activity at the test concentrationFloat%
28% Activity at 0.1542969 uM_second_point_Range1 (0.154297μM**)% activity at the test concentrationFloat%
29EC50_Qualifier_2_Range1This qualifier is to be used with the next TID, EC50_2. If the qualifier is "=", the EC50 result equals the value in that column. If the qualifier is ">", the EC50 result is greater than that value. If the qualifier is "<", the EC50 result is smaller than that valueString
30EC50_2_Range1EC50 value determined using a sigmoidal dose response equationFloatμM
31Std.Err(EC50)_2_Range1Standard Error of the EC50 valueFloatμM
32nH_2_Range1Hill coefficient determined using sigmoidal dose response equationFloat
33Excluded_Points_third_point_Range1Flags 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
34% Activity at 79 uM_third_point_Range1 (79μM**)% activity at the test concentrationFloat%
35% Activity at 39.5 uM_third_point_Range1 (39.5μM**)% activity at the test concentrationFloat%
36% Activity at 19.75 uM_third_point_Range1 (19.75μM**)% activity at the test concentrationFloat%
37% Activity at 9.875 uM_third_point_Range1 (9.875μM**)% activity at the test concentrationFloat%
38% Activity at 4.9375 uM_third_point_Range1 (4.9375μM**)% activity at the test concentrationFloat%
39% Activity at 2.46875 uM_third_point_Range1 (2.46875μM**)% activity at the test concentrationFloat%
40% Activity at 1.234375 uM_third_point_Range1 (1.23438μM**)% activity at the test concentrationFloat%
41% Activity at 0.6171875 uM_third_point_Range1 (0.617188μM**)% activity at the test concentrationFloat%
42% Activity at 0.3085938 uM_third_point_Range1 (0.308594μM**)% activity at the test concentrationFloat%
43% Activity at 0.1542969 uM_third_point_Range1 (0.154297μM**)% activity at the test concentrationFloat%
44Excluded_Points_fourth_point_Range1Flags 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 79 uM_fourth_point_Range1 (79μM**)% activity at the test concentrationFloat%
46% Activity at 39.5 uM_fourth_point_Range1 (39.5μM**)% activity at the test concentrationFloat%
47% Activity at 19.75 uM_fourth_point_Range1 (19.75μM**)% activity at the test concentrationFloat%
48% Activity at 9.875 uM_fourth_point_Range1 (9.875μM**)% activity at the test concentrationFloat%
49% Activity at 4.9375 uM_fourth_point_Range1 (4.9375μM**)% activity at the test concentrationFloat%
50% Activity at 2.46875 uM_fourth_point_Range1 (2.46875μM**)% activity at the test concentrationFloat%
51% Activity at 1.234375 uM_fourth_point_Range1 (1.23438μM**)% activity at the test concentrationFloat%
52% Activity at 0.6171875 uM_fourth_point_Range1 (0.617188μM**)% activity at the test concentrationFloat%
53% Activity at 0.3085938 uM_fourth_point_Range1 (0.308594μM**)% activity at the test concentrationFloat%
54% Activity at 0.1542969 uM_fourth_point_Range1 (0.154297μM**)% activity at the test concentrationFloat%
55EC50_Qualifier_3_Range1This qualifier is to be used with the next TID, EC50_3. If the qualifier is "=", the EC50 result equals the value in that column. If the qualifier is ">", the EC50 result is greater than that value. If the qualifier is "<", the EC50 result is smaller than that valueString
56EC50_3_Range1EC50 value determined using a sigmoidal dose response equationFloatμM
57Std.Err(EC50)_3_Range1Standard Error of the EC50 valueFloatμM
58nH_3_Range1Hill coefficient determined using sigmoidal dose response equationFloat
59Excluded_Points_fifth_point_Range1Flags 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
60% Activity at 79 uM_fifth_point_Range1 (79μM**)% activity at the test concentrationFloat%
61% Activity at 39.5 uM_fifth_point_Range1 (39.5μM**)% activity at the test concentrationFloat%
62% Activity at 19.75 uM_fifth_point_Range1 (19.75μM**)% activity at the test concentrationFloat%
63% Activity at 9.875 uM_fifth_point_Range1 (9.875μM**)% activity at the test concentrationFloat%
64% Activity at 4.9375 uM_fifth_point_Range1 (4.9375μM**)% activity at the test concentrationFloat%
65% Activity at 2.46875 uM_fifth_point_Range1 (2.46875μM**)% activity at the test concentrationFloat%
66% Activity at 1.234375 uM_fifth_point_Range1 (1.23438μM**)% activity at the test concentrationFloat%
67% Activity at 0.6171875 uM_fifth_point_Range1 (0.617188μM**)% activity at the test concentrationFloat%
68% Activity at 0.3085938 uM_fifth_point_Range1 (0.308594μM**)% activity at the test concentrationFloat%
69% Activity at 0.1542969 uM_fifth_point_Range1 (0.154297μM**)% activity at the test concentrationFloat%
70Excluded_Points_sixth_point_Range1Flags 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
71% Activity at 79 uM_sixth_point_Range1 (79μM**)% activity at the test concentrationFloat%
72% Activity at 39.5 uM_sixth_point_Range1 (39.5μM**)% activity at the test concentrationFloat%
73% Activity at 19.75 uM_sixth_point_Range1 (19.75μM**)% activity at the test concentrationFloat%
74% Activity at 9.875 uM_sixth_point_Range1 (9.875μM**)% activity at the test concentrationFloat%
75% Activity at 4.9375 uM_sixth_point_Range1 (4.9375μM**)% activity at the test concentrationFloat%
76% Activity at 2.46875 uM_sixth_point_Range1 (2.46875μM**)% activity at the test concentrationFloat%
77% Activity at 1.234375 uM_sixth_point_Range1 (1.23438μM**)% activity at the test concentrationFloat%
78% Activity at 0.6171875 uM_sixth_point_Range1 (0.617188μM**)% activity at the test concentrationFloat%
79% Activity at 0.3085938 uM_sixth_point_Range1 (0.308594μM**)% activity at the test concentrationFloat%
80% Activity at 0.1542969 uM_sixth_point_Range1 (0.154297μM**)% activity at the test concentrationFloat%
81EC50_Qualifier_4_Range1This qualifier is to be used with the next TID, EC50_4. If the qualifier is "=", the EC50 result equals the value in that column. If the qualifier is ">", the EC50 result is greater than that value. If the qualifier is "<", the EC50 result is smaller than that valueString
82EC50_4_Range1EC50 value determined using a sigmoidal dose response equationFloatμM
83Std.Err(EC50)_4_Range1Standard Error of the EC50 valueFloatμM
84nH_4_Range1Hill coefficient determined using sigmoidal dose response equationFloat
85Excluded_Points_seventh_point_Range1Flags 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
86% Activity at 79 uM_seventh_point_Range1 (79μM**)% activity at the test concentrationFloat%
87% Activity at 39.5 uM_seventh_point_Range1 (39.5μM**)% activity at the test concentrationFloat%
88% Activity at 19.75 uM_seventh_point_Range1 (19.75μM**)% activity at the test concentrationFloat%
89% Activity at 9.875 uM_seventh_point_Range1 (9.875μM**)% activity at the test concentrationFloat%
90% Activity at 4.9375 uM_seventh_point_Range1 (4.9375μM**)% activity at the test concentrationFloat%
91% Activity at 2.46875 uM_seventh_point_Range1 (2.46875μM**)% activity at the test concentrationFloat%
92% Activity at 1.234375 uM_seventh_point_Range1 (1.23438μM**)% activity at the test concentrationFloat%
93% Activity at 0.6171875 uM_seventh_point_Range1 (0.617188μM**)% activity at the test concentrationFloat%
94% Activity at 0.3085938 uM_seventh_point_Range1 (0.308594μM**)% activity at the test concentrationFloat%
95% Activity at 0.1542969 uM_seventh_point_Range1 (0.154297μM**)% activity at the test concentrationFloat%
96Excluded_Points_eighth_point_Range1Flags 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
97% Activity at 79 uM_eighth_point_Range1 (79μM**)% activity at the test concentrationFloat%
98% Activity at 39.5 uM_eighth_point_Range1 (39.5μM**)% activity at the test concentrationFloat%
99% Activity at 19.75 uM_eighth_point_Range1 (19.75μM**)% activity at the test concentrationFloat%
100% Activity at 9.875 uM_eighth_point_Range1 (9.875μM**)% activity at the test concentrationFloat%
101% Activity at 4.9375 uM_eighth_point_Range1 (4.9375μM**)% activity at the test concentrationFloat%
102% Activity at 2.46875 uM_eighth_point_Range1 (2.46875μM**)% activity at the test concentrationFloat%
103% Activity at 1.234375 uM_eighth_point_Range1 (1.23438μM**)% activity at the test concentrationFloat%
104% Activity at 0.6171875 uM_eighth_point_Range1 (0.617188μM**)% activity at the test concentrationFloat%
105% Activity at 0.3085938 uM_eighth_point_Range1 (0.308594μM**)% activity at the test concentrationFloat%
106% Activity at 0.1542969 uM_eighth_point_Range1 (0.154297μM**)% activity at the test concentrationFloat%
107EC50_Qualifier_5_Range1This qualifier is to be used with the next TID, EC50_5. If the qualifier is "=", the EC50 result equals the value in that column. If the qualifier is ">", the EC50 result is greater than that value. If the qualifier is "<", the EC50 result is smaller than that valueString
108EC50_5_Range1EC50 value determined using a sigmoidal dose response equationFloatμM
109Std.Err(EC50)_5_Range1Standard Error of the EC50 valueFloatμM
110nH_5_Range1Hill coefficient determined using sigmoidal dose response equationFloat
111Excluded_Points_ninth_point_Range1Flags 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
112% Activity at 79 uM_ninth_point_Range1 (79μM**)% activity at the test concentrationFloat%
113% Activity at 39.5 uM_ninth_point_Range1 (39.5μM**)% activity at the test concentrationFloat%
114% Activity at 19.75 uM_ninth_point_Range1 (19.75μM**)% activity at the test concentrationFloat%
115% Activity at 9.875 uM_ninth_point_Range1 (9.875μM**)% activity at the test concentrationFloat%
116% Activity at 4.9375 uM_ninth_point_Range1 (4.9375μM**)% activity at the test concentrationFloat%
117% Activity at 2.46875 uM_ninth_point_Range1 (2.46875μM**)% activity at the test concentrationFloat%
118% Activity at 1.234375 uM_ninth_point_Range1 (1.23438μM**)% activity at the test concentrationFloat%
119% Activity at 0.6171875 uM_ninth_point_Range1 (0.617188μM**)% activity at the test concentrationFloat%
120% Activity at 0.3085938 uM_ninth_point_Range1 (0.308594μM**)% activity at the test concentrationFloat%
121% Activity at 0.1542969 uM_ninth_point_Range1 (0.154297μM**)% activity at the test concentrationFloat%
122Excluded_Points_tenth_point_Range1Flags 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
123% Activity at 79 uM_tenth_point_Range1 (79μM**)% activity at the test concentrationFloat%
124% Activity at 39.5 uM_tenth_point_Range1 (39.5μM**)% activity at the test concentrationFloat%
125% Activity at 19.75 uM_tenth_point_Range1 (19.75μM**)% activity at the test concentrationFloat%
126% Activity at 9.875 uM_tenth_point_Range1 (9.875μM**)% activity at the test concentrationFloat%
127% Activity at 4.9375 uM_tenth_point_Range1 (4.9375μM**)% activity at the test concentrationFloat%
128% Activity at 2.46875 uM_tenth_point_Range1 (2.46875μM**)% activity at the test concentrationFloat%
129% Activity at 1.234375 uM_tenth_point_Range1 (1.23438μM**)% activity at the test concentrationFloat%
130% Activity at 0.6171875 uM_tenth_point_Range1 (0.617188μM**)% activity at the test concentrationFloat%
131% Activity at 0.3085938 uM_tenth_point_Range1 (0.308594μM**)% activity at the test concentrationFloat%
132% Activity at 0.1542969 uM_tenth_point_Range1 (0.154297μM**)% activity at the test concentrationFloat%
133EC50_Qualifier_6_Range1This qualifier is to be used with the next TID, EC50_6. If the qualifier is "=", the EC50 result equals the value in that column. If the qualifier is ">", the EC50 result is greater than that value. If the qualifier is "<", the EC50 result is smaller than that valueString
134EC50_6_Range1EC50 value determined using a sigmoidal dose response equationFloatμM
135Std.Err(EC50)_6_Range1Standard Error of the EC50 valueFloatμM
136nH_6_Range1Hill coefficient determined using sigmoidal dose response equationFloat
137Excluded_Points_eleventh_point_Range1Flags 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
138% Activity at 79 uM_eleventh_point_Range1 (79μM**)% activity at the test concentrationFloat%
139% Activity at 39.5 uM_eleventh_point_Range1 (39.5μM**)% activity at the test concentrationFloat%
140% Activity at 19.75 uM_eleventh_point_Range1 (19.75μM**)% activity at the test concentrationFloat%
141% Activity at 9.875 uM_eleventh_point_Range1 (9.875μM**)% activity at the test concentrationFloat%
142% Activity at 4.9375 uM_eleventh_point_Range1 (4.9375μM**)% activity at the test concentrationFloat%
143% Activity at 2.46875 uM_eleventh_point_Range1 (2.46875μM**)% activity at the test concentrationFloat%
144% Activity at 1.234375 uM_eleventh_point_Range1 (1.23438μM**)% activity at the test concentrationFloat%
145% Activity at 0.6171875 uM_eleventh_point_Range1 (0.617188μM**)% activity at the test concentrationFloat%
146% Activity at 0.3085938 uM_eleventh_point_Range1 (0.308594μM**)% activity at the test concentrationFloat%
147% Activity at 0.1542969 uM_eleventh_point_Range1 (0.154297μM**)% activity at the test concentrationFloat%
148Excluded_Points_twelfth_point_Range1Flags 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
149% Activity at 79 uM_twelfth_point_Range1 (79μM**)% activity at the test concentrationFloat%
150% Activity at 39.5 uM_twelfth_point_Range1 (39.5μM**)% activity at the test concentrationFloat%
151% Activity at 19.75 uM_twelfth_point_Range1 (19.75μM**)% activity at the test concentrationFloat%
152% Activity at 9.875 uM_twelfth_point_Range1 (9.875μM**)% activity at the test concentrationFloat%
153% Activity at 4.9375 uM_twelfth_point_Range1 (4.9375μM**)% activity at the test concentrationFloat%
154% Activity at 2.46875 uM_twelfth_point_Range1 (2.46875μM**)% activity at the test concentrationFloat%
155% Activity at 1.234375 uM_twelfth_point_Range1 (1.23438μM**)% activity at the test concentrationFloat%
156% Activity at 0.6171875 uM_twelfth_point_Range1 (0.617188μM**)% activity at the test concentrationFloat%
157% Activity at 0.3085938 uM_twelfth_point_Range1 (0.308594μM**)% activity at the test concentrationFloat%
158% Activity at 0.1542969 uM_twelfth_point_Range1 (0.154297μM**)% activity at the test concentrationFloat%

* Activity Concentration. ** Test Concentration.
Additional Information
Grant Number: 1R21NS059422-01

Data Table (Concise)
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