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BioAssay: AID 1659

SAR assay for compounds activating TNAP in the presence of 100 mM DEA performed in a luminescence assay

This TNAP dose response assay is developed and performed to confirm hits originally identified in the TNAP luminescent HTS assay (AID 1001) and to study the structure-activity relationship on analogs of the confirmed hits. Compounds are either acquired from commercial sources or synthesized internally. ..more
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 Tested Compounds
 Tested Compounds
All(109)
 
 
Active(95)
 
 
Inactive(17)
 
 
 Tested Substances
 Tested Substances
All(122)
 
 
Active(105)
 
 
Inactive(17)
 
 
AID: 1659
Data Source: Burnham Center for Chemical Genomics (BCCG-A182-TNAP-Acceptor-DryPowder-Assay)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: NIH Molecular Libraries Screening Center Network
BioAssay Version:
Deposit Date: 2009-04-03
Modify Date: 2010-12-30

Data Table ( Complete ):           View Active Data    View All Data
Target
BioActive Compounds: 95
Related Experiments
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AIDNameTypeProbeComment
518TNAP luminescent HTS assayConfirmatory depositor-specified cross reference
813HTS identification of compounds activating TNAP at intermediate concentration of phosphate acceptor detected in luminescent assayScreening depositor-specified cross reference
1001uHTS identification of compounds activating TNAP in the absence of phosphate acceptor performed in luminescent assayConfirmatory depositor-specified cross reference
1056SAR analysis of an In Vitro TNAP Dose Response Luminescent AssayConfirmatory depositor-specified cross reference
1450SAR assay for compounds activating TNAP in the absence of phosphate acceptor performed in a luminescent assayConfirmatory depositor-specified cross reference
1548Summary assay for compounds activating TNAP performed in a luminescent assaySummary2 depositor-specified cross reference
1941SAR assay for compounds inhibiting TNAP in the absence of phosphate acceptor performed in a luminescent assayConfirmatory depositor-specified cross reference
1136uHTS identification of compounds activating TNAP at a high concentration of phosphate acceptor detected in a luminescent assayScreening same project related to Summary assay
1227GAPDH Dose Response Colorimetric AssayConfirmatory 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 Screening Centers Network (MLSCN)
Grant Proposal Number: 1R03 MH082385-01

This TNAP dose response assay is developed and performed to confirm hits originally identified in the TNAP luminescent HTS assay (AID 1001) and to study the structure-activity relationship on analogs of the confirmed hits. Compounds are either acquired from commercial sources or synthesized internally.

Alkaline phosphatases (EC 3.1.3.1) (APs) catalyze the hydrolysis of phosphomonoesters, releasing phosphate and alcohol. APs are dimeric enzymes found in the most organisms. In human, four isozymes of APs have been identified. Three isozymes are tissue-specific and the fourth one is tissue-non specific, named TNAP. TNAP deficiency is associated with defective bone mineralization in the form of rickets and osteomalacia. Therefore, there is therapeutic potential of modulating TNAP activity.

The goal of this HTS is to identify novel and specific activators of TNAP. The only known to date class of alkaline phosphatases activators are amino-containing alcohols, such as diethanolamine (DEA), that act as phosphoacceptor substrate and exhibit its effect in high-mM concentration range. Compounds with a similar mode of action are expected to demonstrate diminished stimulating potential if tested in the presence of DEA. Therefore, for detection of compounds with diverse mode of action, the HTS assay was optimized and HTS campaigns were performed in the presence and in the absence of DEA. The current AID reports a set of the data from screening in the presence of DEA.

TNAP luminescent assay was developed and performed at the Sanford-Burnham Center for Chemical Genomics (SBCCG), part of the Molecular Library Screening Center Network (MLSCN). RO3 submission, MH082385-01: Activators of the Pyrophosphatase Activity of Alkaline Phosphatase. Assay Providers: Drs. Jose Luis Millan and Eduard Sergienko, Sanford-Burnham Medical Research Institute, San Diego, CA.
Protocol
TNAP assay materials:
1) TNAP protein was provided by Dr. Jose Luis Millan (Sanford-Burnham Medical Research Institute, San Diego, CA). The CDP-star was obtained from New England Biolabs.
2) Assay Buffer: 100 mM CAPS, pH 9.8, 2 mM MgCl2, and 0.04 mM ZnCl2 (for Primary screen, no phosphate acceptor).
3) Assay Buffer: 250 mM DEA, pH 9.8, 2.5 mM MgCl2, and 0.05 mM ZnCl2 (for dose-response assays)
4) TNAP working solution contained a 1/400 dilution in assay buffer.
5) CDP-star working solution contained 200 uM CDP-star in MQ water.
6) Negative Control (NC) solution - 5 mM levamisole.
7) Positive Control (PC) solution - 10% DMSO.
TNAP dose-response confirmation screening protocol:
1) Dose-response curves contained 10 concentrations of compounds obtained using 2-fold serial dilution. Compounds were serially diluted in 100% DMSO, and then diluted with water to 10% final DMSO concentration. 4 uL compounds in 10% DMSO were transferred into columns 3-22 of Greiner 384-well white small-volume plates (784075). Each curve was performed in duplicate.
2) Columns 1-2 and 23-24 contained 4 uL of NC and PC solutions, respectively.
3) 8 uL of TNAP working solution was added to the whole plate using WellMate bulk dispenser (Matrix).
4) 8 uL of CDP-star working solution was added to the whole plate using WellMate bulk dispenser (Matrix).
5) Plates were incubated for 30 mins at room temperature.
6) Luminescence was measured on the Envision plate reader (Perkin Elmer).
7) Data analysis was performed using CBIS software (ChemInnovations, Inc) using sigmoidal dose-response equation through non-linear regression
Comment
Compounds were tested in 1 or more concentration ranges.
Range1 0-100 uM
Range2 0-1 uM
Range3 0-10 uM
For all samples in each range that resolved to an EC50 the results were averaged and reported as EC50_Range. The EC50 results for all of the EC50s were averaged to produce EC50_Mean.
EC50 results are an average of two dose response curves. If for a given range there are 6 sets of curves there will be three EC50 results reported.
TNAP activation was calculated using the following formula:
Activation Factor (AF) = (Signal_Well - Mean_NC)/(Mean_PC - Mean_NC),
where Signal_Well corresponds to luminescence signal in the well with a compound, Mean_NC and Mean_PC correspond to mean values of corresponding controls in the plate.
Compounds that are tested in dose-response and determined to have an EC50 < 100 uM are marked as "active."
The EC50 and Max_value were calculated from fitting the AF vs [compound] curve according to the following equation:
AF = ((Max_Value*[compound]^nH)/EC50^nH + [compound]^nH) + 1
To simplify the distinction between the inactives of the primary screen (see AID 1001) and of the confirmatory screening stage, the Tiered Activity Scoring System was developed and implemented. Its utilization for the TNAP 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 TNAP assay is as follows:
1) First tier (0-40 range) is reserved for primary screening data and is not applicable to this assay
2) In this assay we tested resynthesized analogs, therefore, the second tier (41-80 range) that is reserved for dose-response confirmation data is not applicable.
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's activatory 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 TNAP activation 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. Compounds with a qualifier of < or > are calculated the Score based on their numerical part.
e. The Score of 100 was assigned to any compounds whose Score was calculated to be >100.
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: Binding
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. If the qualifier is "=", the EC50 result equals to the value in that column;if 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 mean value determined using sigmoidal dose response equationFloatμM
3EC50_Qualifier_1_Range1This qualifier is to be used with the next TID, EC50_1_Range1. 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.String
4EC50_1_Range1The first EC50 value for Range1 determined using sigmoidal dose response equationFloatμM
5Std.Err(EC50)_1_Range1Standard Error of the preceeding EC50 valueFloatμM
6nH_1_Range1Hill coefficient determined using sigmoidal dose response equationFloat
7Max_Value_1_Range1The AF value asymptotically approached by the dose response curve at saturating compound concentrationsFloat
8Excluded_Points_first_point_Range1Flags to indicate which of the first dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
9% Efficacy at 100 uM_first_point_Range1 (100μM**)% Efficacy at a given concentrationFloat%
10% Efficacy at 50 uM_first_point_Range1 (50μM**)% Efficacy at a given concentrationFloat%
11% Efficacy at 25 uM_first_point_Range1 (25μM**)% Efficacy at a given concentrationFloat%
12% Efficacy at 12.5 uM_first_point_Range1 (12.5μM**)% Efficacy at a given concentrationFloat%
13% Efficacy at 6.25 uM_first_point_Range1 (6.25μM**)% Efficacy at a given concentrationFloat%
14% Efficacy at 3.125 uM_first_point_Range1 (3.125μM**)% Efficacy at a given concentrationFloat%
15% Efficacy at 1.5625 uM_first_point_Range1 (1.5625μM**)% Efficacy at a given concentrationFloat%
16% Efficacy at 0.78125 uM_first_point_Range1 (0.78125μM**)% Efficacy at a given concentrationFloat%
17% Efficacy at 0.390625 uM_first_point_Range1 (0.390625μM**)% Efficacy at a given concentrationFloat%
18% Efficacy at 0.1953125 uM_first_point_Range1 (0.195312μM**)% Efficacy at a given concentrationFloat%
19Excluded_Points_second_point_Range1Flags to indicate which of the second dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
20% Efficacy at 100 uM_second_point_Range1 (100μM**)% Efficacy at a given concentrationFloat%
21% Efficacy at 50 uM_second_point_Range1 (50μM**)% Efficacy at a given concentrationFloat%
22% Efficacy at 25 uM_second_point_Range1 (25μM**)% Efficacy at a given concentrationFloat%
23% Efficacy at 12.5 uM_second_point_Range1 (12.5μM**)% Efficacy at a given concentrationFloat%
24% Efficacy at 6.25 uM_second_point_Range1 (6.25μM**)% Efficacy at a given concentrationFloat%
25% Efficacy at 3.125 uM_second_point_Range1 (3.125μM**)% Efficacy at a given concentrationFloat%
26% Efficacy at 1.5625 uM_second_point_Range1 (1.5625μM**)% Efficacy at a given concentrationFloat%
27% Efficacy at 0.78125 uM_second_point_Range1 (0.78125μM**)% Efficacy at a given concentrationFloat%
28% Efficacy at 0.390625 uM_second_point_Range1 (0.390625μM**)% Efficacy at a given concentrationFloat%
29% Efficacy at 0.1953125 uM_second_point_Range1 (0.195312μM**)% Efficacy at a given concentrationFloat%
30EC50_Qualifier_2_Range1This qualifier is to be used with the next TID, EC50_2_Range1. 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.String
31EC50_2_Range1The second EC50 value for Range1 determined using sigmoidal dose response equationFloatμM
32Std.Err(EC50)_2_Range1Standard Error of the preceeding EC50 valueFloatμM
33nH_2_Range1Hill coefficient determined using sigmoidal dose response equationFloat
34Max_Value_2_Range1The AF value asymptotically approached by the dose response curve at saturating compound concentrationsFloat
35Excluded_Points_third_point_Range1Flags to indicate which of the third dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
36% Efficacy at 100 uM_third_point_Range1 (100μM**)% Efficacy at a given concentrationFloat%
37% Efficacy at 50 uM_third_point_Range1 (50μM**)% Efficacy at a given concentrationFloat%
38% Efficacy at 25 uM_third_point_Range1 (25μM**)% Efficacy at a given concentrationFloat%
39% Efficacy at 12.5 uM_third_point_Range1 (12.5μM**)% Efficacy at a given concentrationFloat%
40% Efficacy at 6.25 uM_third_point_Range1 (6.25μM**)% Efficacy at a given concentrationFloat%
41% Efficacy at 3.125 uM_third_point_Range1 (3.125μM**)% Efficacy at a given concentrationFloat%
42% Efficacy at 1.5625 uM_third_point_Range1 (1.5625μM**)% Efficacy at a given concentrationFloat%
43% Efficacy at 0.78125 uM_third_point_Range1 (0.78125μM**)% Efficacy at a given concentrationFloat%
44% Efficacy at 0.390625 uM_third_point_Range1 (0.390625μM**)% Efficacy at a given concentrationFloat%
45% Efficacy at 0.1953125 uM_third_point_Range1 (0.195312μM**)% Efficacy at a given concentrationFloat%
46Excluded_Points_fourth_point_Range1Flags to indicate which of the fourth dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
47% Efficacy at 100 uM_fourth_point_Range1 (100μM**)% Efficacy at a given concentrationFloat%
48% Efficacy at 50 uM_fourth_point_Range1 (50μM**)% Efficacy at a given concentrationFloat%
49% Efficacy at 25 uM_fourth_point_Range1 (25μM**)% Efficacy at a given concentrationFloat%
50% Efficacy at 12.5 uM_fourth_point_Range1 (12.5μM**)% Efficacy at a given concentrationFloat%
51% Efficacy at 6.25 uM_fourth_point_Range1 (6.25μM**)% Efficacy at a given concentrationFloat%
52% Efficacy at 3.125 uM_fourth_point_Range1 (3.125μM**)% Efficacy at a given concentrationFloat%
53% Efficacy at 1.5625 uM_fourth_point_Range1 (1.5625μM**)% Efficacy at a given concentrationFloat%
54% Efficacy at 0.78125 uM_fourth_point_Range1 (0.78125μM**)% Efficacy at a given concentrationFloat%
55% Efficacy at 0.390625 uM_fourth_point_Range1 (0.390625μM**)% Efficacy at a given concentrationFloat%
56% Efficacy at 0.1953125 uM_fourth_point_Range1 (0.195312μM**)% Efficacy at a given concentrationFloat%
57EC50_Qualifier_3_Range1This qualifier is to be used with the next TID, EC50_3_Range1. 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.String
58EC50_3_Range1The third EC50 value for Range1 determined using sigmoidal dose response equationFloatμM
59Std.Err(EC50)_3_Range1Standard Error of the preceeding EC50 valueFloatμM
60nH_3_Range1Hill coefficient determined using sigmoidal dose response equationFloat
61Max_Value_3_Range1The AF value asymptotically approached by the dose response curve at saturating compound concentrationsFloat
62Excluded_Points_fifth_point_Range1Flags to indicate which of the fifth dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
63% Efficacy at 100 uM_fifth_point_Range1 (100μM**)% Efficacy at a given concentrationFloat%
64% Efficacy at 50 uM_fifth_point_Range1 (50μM**)% Efficacy at a given concentrationFloat%
65% Efficacy at 25 uM_fifth_point_Range1 (25μM**)% Efficacy at a given concentrationFloat%
66% Efficacy at 12.5 uM_fifth_point_Range1 (12.5μM**)% Efficacy at a given concentrationFloat%
67% Efficacy at 6.25 uM_fifth_point_Range1 (6.25μM**)% Efficacy at a given concentrationFloat%
68% Efficacy at 3.125 uM_fifth_point_Range1 (3.125μM**)% Efficacy at a given concentrationFloat%
69% Efficacy at 1.5625 uM_fifth_point_Range1 (1.5625μM**)% Efficacy at a given concentrationFloat%
70% Efficacy at 0.78125 uM_fifth_point_Range1 (0.78125μM**)% Efficacy at a given concentrationFloat%
71% Efficacy at 0.390625 uM_fifth_point_Range1 (0.390625μM**)% Efficacy at a given concentrationFloat%
72% Efficacy at 0.1953125 uM_fifth_point_Range1 (0.195312μM**)% Efficacy at a given concentrationFloat%
73Excluded_Points_sixth_point_Range1Flags to indicate which of the sixth dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
74% Efficacy at 100 uM_sixth_point_Range1 (100μM**)% Efficacy at a given concentrationFloat%
75% Efficacy at 50 uM_sixth_point_Range1 (50μM**)% Efficacy at a given concentrationFloat%
76% Efficacy at 25 uM_sixth_point_Range1 (25μM**)% Efficacy at a given concentrationFloat%
77% Efficacy at 12.5 uM_sixth_point_Range1 (12.5μM**)% Efficacy at a given concentrationFloat%
78% Efficacy at 6.25 uM_sixth_point_Range1 (6.25μM**)% Efficacy at a given concentrationFloat%
79% Efficacy at 3.125 uM_sixth_point_Range1 (3.125μM**)% Efficacy at a given concentrationFloat%
80% Efficacy at 1.5625 uM_sixth_point_Range1 (1.5625μM**)% Efficacy at a given concentrationFloat%
81% Efficacy at 0.78125 uM_sixth_point_Range1 (0.78125μM**)% Efficacy at a given concentrationFloat%
82% Efficacy at 0.390625 uM_sixth_point_Range1 (0.390625μM**)% Efficacy at a given concentrationFloat%
83% Efficacy at 0.1953125 uM_sixth_point_Range1 (0.195312μM**)% Efficacy at a given concentrationFloat%
84EC50_Qualifier_1_Range2This qualifier is to be used with the next TID, EC50_1_Range2. 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.String
85EC50_1_Range2The first EC50 value for Range2 determined using sigmoidal dose response equationFloat%
86Std.Err(EC50)_1_Range2Standard Error of the preceeding EC50 valueFloatμM
87nH_1_Range2Hill coefficient determined using sigmoidal dose response equationFloat
88Max_Value_1_Range2The AF value asymptotically approached by the dose response curve at saturating compound concentrationsFloat
89Excluded_Points_first_point_Range2Flags to indicate which of the first dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
90% Efficacy at 1 uM_first_point_Range2 (1μM**)% Efficacy at a given concentrationFloat%
91% Efficacy at 0.5 uM_first_point_Range2 (0.5μM**)% Efficacy at a given concentrationFloat%
92% Efficacy at 0.25 uM_first_point_Range2 (0.25μM**)% Efficacy at a given concentrationFloat%
93% Efficacy at 0.125 uM_first_point_Range2 (0.125μM**)% Efficacy at a given concentrationFloat%
94% Efficacy at 0.0625 uM_first_point_Range2 (0.0625μM**)% Efficacy at a given concentrationFloat%
95% Efficacy at 0.03125 uM_first_point_Range2 (0.03125μM**)% Efficacy at a given concentrationFloat%
96% Efficacy at 0.015625 uM_first_point_Range2 (0.015625μM**)% Efficacy at a given concentrationFloat%
97% Efficacy at 0.0078125 uM_first_point_Range2 (0.0078125μM**)% Efficacy at a given concentrationFloat%
98% Efficacy at 0.00390625 uM_first_point_Range2 (0.00390625μM**)% Efficacy at a given concentrationFloat%
99% Efficacy at 0.001953125 uM_first_point_Range2 (0.00195312μM**)% Efficacy at a given concentrationFloat%
100Excluded_Points_second_point_Range2Flags to indicate which of the second dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
101% Efficacy at 1 uM_second_point_Range2 (1μM**)% Efficacy at a given concentrationFloat%
102% Efficacy at 0.5 uM_second_point_Range2 (0.5μM**)% Efficacy at a given concentrationFloat%
103% Efficacy at 0.25 uM_second_point_Range2 (0.25μM**)% Efficacy at a given concentrationFloat%
104% Efficacy at 0.125 uM_second_point_Range2 (0.125μM**)% Efficacy at a given concentrationFloat%
105% Efficacy at 0.0625 uM_second_point_Range2 (0.0625μM**)% Efficacy at a given concentrationFloat%
106% Efficacy at 0.03125 uM_second_point_Range2 (0.03125μM**)% Efficacy at a given concentrationFloat%
107% Efficacy at 0.015625 uM_second_point_Range2 (0.015625μM**)% Efficacy at a given concentrationFloat%
108% Efficacy at 0.0078125 uM_second_point_Range2 (0.0078125μM**)% Efficacy at a given concentrationFloat%
109% Efficacy at 0.00390625 uM_second_point_Range2 (0.00390625μM**)% Efficacy at a given concentrationFloat%
110% Efficacy at 0.001953125 uM_second_point_Range2 (0.00195312μM**)% Efficacy at a given concentrationFloat%
111EC50_Qualifier_2_Range2This qualifier is to be used with the next TID, EC50_2_Range2. 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.String
112EC50_2_Range2The second EC50 value for Range2 determined using sigmoidal dose response equationFloat%
113Std.Err(EC50)_2_Range2Standard Error of the preceeding EC50 valueFloat%
114nH_2_Range2Hill coefficient determined using sigmoidal dose response equationFloat
115Max_Value_2_Range2The AF value asymptotically approached by the dose response curve at saturating compound concentrationsFloat
116Excluded_Points_third_point_Range2Flags to indicate which of the third dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
117% Efficacy at 1 uM_third_point_Range2 (1μM**)% Efficacy at a given concentrationFloat%
118% Efficacy at 0.5 uM_third_point_Range2 (0.5μM**)% Efficacy at a given concentrationFloat%
119% Efficacy at 0.25 uM_third_point_Range2 (0.25μM**)% Efficacy at a given concentrationFloat%
120% Efficacy at 0.125 uM_third_point_Range2 (0.125μM**)% Efficacy at a given concentrationFloat%
121% Efficacy at 0.0625 uM_third_point_Range2 (0.0625μM**)% Efficacy at a given concentrationFloat%
122% Efficacy at 0.03125 uM_third_point_Range2 (0.03125μM**)% Efficacy at a given concentrationFloat%
123% Efficacy at 0.015625 uM_third_point_Range2 (0.015625μM**)% Efficacy at a given concentrationFloat%
124% Efficacy at 0.0078125 uM_third_point_Range2 (0.0078125μM**)% Efficacy at a given concentrationFloat%
125% Efficacy at 0.00390625 uM_third_point_Range2 (0.00390625μM**)% Efficacy at a given concentrationFloat%
126% Efficacy at 0.001953125 uM_third_point_Range2 (0.00195312μM**)% Efficacy at a given concentrationFloat%
127Excluded_Points_fourth_point_Range2Flags to indicate which of the fourth dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
128% Efficacy at 1 uM_fourth_point_Range2 (1μM**)% Efficacy at a given concentrationFloat%
129% Efficacy at 0.5 uM_fourth_point_Range2 (0.5μM**)% Efficacy at a given concentrationFloat%
130% Efficacy at 0.25 uM_fourth_point_Range2 (0.25μM**)% Efficacy at a given concentrationFloat%
131% Efficacy at 0.125 uM_fourth_point_Range2 (0.125μM**)% Efficacy at a given concentrationFloat%
132% Efficacy at 0.0625 uM_fourth_point_Range2 (0.0625μM**)% Efficacy at a given concentrationFloat%
133% Efficacy at 0.03125 uM_fourth_point_Range2 (0.03125μM**)% Efficacy at a given concentrationFloat%
134% Efficacy at 0.015625 uM_fourth_point_Range2 (0.015625μM**)% Efficacy at a given concentrationFloat%
135% Efficacy at 0.0078125 uM_fourth_point_Range2 (0.0078125μM**)% Efficacy at a given concentration% Efficacy at a given concentrationFloat%
136% Efficacy at 0.00390625 uM_fourth_point_Range2 (0.00390625μM**)Float%
137% Efficacy at 0.001953125 uM_fourth_point_Range2 (0.00195312μM**)% Efficacy at a given concentrationFloat%
138EC50_Qualifier_3_Range2This qualifier is to be used with the next TID, EC50_3_Range2. 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.String
139EC50_3_Range2The third EC50 value for Range2 determined using sigmoidal dose response equationFloatμM
140Std.Err(EC50)_3_Range2Standard Error of the preceeding EC50 valueFloatμM
141nH_3_Range2Hill coefficient determined using sigmoidal dose response equationFloat
142Max_Value_3_Range2The AF value asymptotically approached by the dose response curve at saturating compound concentrationsFloat
143Excluded_Points_fifth_point_Range2Flags to indicate which of the fifth dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
144% Efficacy at 1 uM_fifth_point_Range2 (1μM**)% Efficacy at a given concentrationFloat%
145% Efficacy at 0.5 uM_fifth_point_Range2 (0.5μM**)% Efficacy at a given concentrationFloat%
146% Efficacy at 0.25 uM_fifth_point_Range2 (0.25μM**)% Efficacy at a given concentrationFloat%
147% Efficacy at 0.125 uM_fifth_point_Range2 (0.125μM**)% Efficacy at a given concentrationFloat%
148% Efficacy at 0.0625 uM_fifth_point_Range2 (0.0625μM**)% Efficacy at a given concentrationFloat%
149% Efficacy at 0.03125 uM_fifth_point_Range2 (0.03125μM**)% Efficacy at a given concentrationFloat%
150% Efficacy at 0.015625 uM_fifth_point_Range2 (0.015625μM**)% Efficacy at a given concentrationFloat%
151% Efficacy at 0.0078125 uM_fifth_point_Range2 (0.0078125μM**)% Efficacy at a given concentrationFloat%
152% Efficacy at 0.00390625 uM_fifth_point_Range2 (0.00390625μM**)% Efficacy at a given concentrationFloat%
153% Efficacy at 0.001953125 uM_fifth_point_Range2 (0.00195312μM**)% Efficacy at a given concentrationFloat%
154Excluded_Points_sixth_point_Range2Flags to indicate which of the sixth dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
155% Efficacy at 1 uM_sixth_point_Range2 (1μM**)% Efficacy at a given concentrationFloat%
156% Efficacy at 0.5 uM_sixth_point_Range2 (0.5μM**)% Efficacy at a given concentrationFloat%
157% Efficacy at 0.25 uM_sixth_point_Range2 (0.25μM**)% Efficacy at a given concentrationFloat%
158% Efficacy at 0.125 uM_sixth_point_Range2 (0.125μM**)% Efficacy at a given concentrationFloat%
159% Efficacy at 0.0625 uM_sixth_point_Range2 (0.0625μM**)% Efficacy at a given concentrationFloat%
160% Efficacy at 0.03125 uM_sixth_point_Range2 (0.03125μM**)% Efficacy at a given concentrationFloat%
161% Efficacy at 0.015625 uM_sixth_point_Range2 (0.015625μM**)% Efficacy at a given concentrationFloat%
162% Efficacy at 0.0078125 uM_sixth_point_Range2 (0.0078125μM**)% Efficacy at a given concentrationFloat%
163% Efficacy at 0.00390625 uM_sixth_point_Range2 (0.00390625μM**)% Efficacy at a given concentrationFloat%
164% Efficacy at 0.001953125 uM_sixth_point_Range2 (0.00195312μM**)% Efficacy at a given concentrationFloat%
165EC50_Qualifier_1_Range3This qualifier is to be used with the next TID, EC50_1_Range3. 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.String
166EC50_1_Range3The first EC50 value for Range3 determined using sigmoidal dose response equationFloatμM
167Std.Err(EC50)_1_Range3Standard Error of the preceeding EC50 valueFloatμM
168nH_1_Range3Hill coefficient determined using sigmoidal dose response equationFloat
169Max_Value_1_Range3The AF value asymptotically approached by the dose response curve at saturating compound concentrationsFloat
170Excluded_Points_first_point_Range3Flags to indicate which of the first dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
171% Efficacy at 10 uM_first_point_Range3 (10μM**)% Efficacy at a given concentrationFloat%
172% Efficacy at 5 uM_first_point_Range3 (5μM**)% Efficacy at a given concentrationFloat%
173% Efficacy at 2.5 uM_first_point_Range3 (2.5μM**)% Efficacy at a given concentrationFloat%
174% Efficacy at 1.25 uM_first_point_Range3 (1.25μM**)% Efficacy at a given concentrationFloat%
175% Efficacy at 0.625 uM_first_point_Range3 (0.625μM**)% Efficacy at a given concentrationFloat%
176% Efficacy at 0.3125 uM_first_point_Range3 (0.3125μM**)% Efficacy at a given concentrationFloat%
177% Efficacy at 0.15625 uM_first_point_Range3 (0.15625μM**)% Efficacy at a given concentrationFloat%
178% Efficacy at 0.078125 uM_first_point_Range3 (0.078125μM**)% Efficacy at a given concentrationFloat%
179% Efficacy at 0.0390625 uM_first_point_Range3 (0.0390625μM**)% Efficacy at a given concentrationFloat%
180% Efficacy at 0.01953125 uM_first_point_Range3 (0.0195312μM**)% Efficacy at a given concentrationFloat%
181Excluded_Points_second_point_Range3Flags to indicate which of the second dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
182% Efficacy at 10 uM_second_point_Range3 (10μM**)% Efficacy at a given concentrationFloat%
183% Efficacy at 5 uM_second_point_Range3 (5μM**)% Efficacy at a given concentrationFloat%
184% Efficacy at 2.5 uM_second_point_Range3 (2.5μM**)% Efficacy at a given concentrationFloat%
185% Efficacy at 1.25 uM_second_point_Range3 (1.25μM**)% Efficacy at a given concentrationFloat%
186% Efficacy at 0.625 uM_second_point_Range3 (0.625μM**)% Efficacy at a given concentrationFloat%
187% Efficacy at 0.3125 uM_second_point_Range3 (0.3125μM**)% Efficacy at a given concentrationFloat%
188% Efficacy at 0.15625 uM_second_point_Range3 (0.15625μM**)% Efficacy at a given concentrationFloat%
189% Efficacy at 0.078125 uM_second_point_Range3 (0.078125μM**)% Efficacy at a given concentrationFloat%
190% Efficacy at 0.0390625 uM_second_point_Range3 (0.0390625μM**)% Efficacy at a given concentrationFloat%
191% Efficacy at 0.01953125 uM_second_point_Range3 (0.0195312μM**)% Efficacy at a given concentrationFloat%
192EC50_Qualifier_2_Range3This qualifier is to be used with the next TID, EC50_2_Range3. 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.String
193EC50_2_Range3The second EC50 value for Range2 determined using sigmoidal dose response equationFloatμM
194Std.Err(EC50)_2_Range3Standard Error of the preceeding EC50 valueFloat
195nH_2_Range3Hill coefficient determined using sigmoidal dose response equationFloat
196Max_Value_2_Range3The AF value asymptotically approached by the dose response curve at saturating compound concentrationsFloat
197Excluded_Points_third_point_Range3Flags to indicate which of the third dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
198% Efficacy at 10 uM_third_point_Range3 (10μM**)% Efficacy at a given concentrationFloat%
199% Efficacy at 5 uM_third_point_Range3 (5μM**)% Efficacy at a given concentrationFloat%
200% Efficacy at 2.5 uM_third_point_Range3 (2.5μM**)% Efficacy at a given concentrationFloat%
201% Efficacy at 1.25 uM_third_point_Range3 (1.25μM**)% Efficacy at a given concentrationFloat%
202% Efficacy at 0.625 uM_third_point_Range3 (0.625μM**)% Efficacy at a given concentrationFloat%
203% Efficacy at 0.3125 uM_third_point_Range3 (0.3125μM**)% Efficacy at a given concentrationFloat%
204% Efficacy at 0.15625 uM_third_point_Range3 (0.15625μM**)% Efficacy at a given concentrationFloat%
205% Efficacy at 0.078125 uM_third_point_Range3 (0.078125μM**)% Efficacy at a given concentrationFloat%
206% Efficacy at 0.0390625 uM_third_point_Range3 (0.0390625μM**)% Efficacy at a given concentrationFloat%
207% Efficacy at 0.01953125 uM_third_point_Range3 (0.0195312μM**)% Efficacy at a given concentrationFloat%
208Excluded_Points_fourth_point_Range3Flags to indicate which of the fourth dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
209% Efficacy at 10 uM_fourth_point_Range3 (10μM**)% Efficacy at a given concentrationFloat%
210% Efficacy at 5 uM_fourth_point_Range3 (5μM**)% Efficacy at a given concentrationFloat%
211% Efficacy at 2.5 uM_fourth_point_Range3 (2.5μM**)% Efficacy at a given concentrationFloat%
212% Efficacy at 1.25 uM_fourth_point_Range3 (1.25μM**)% Efficacy at a given concentrationFloat%
213% Efficacy at 0.625 uM_fourth_point_Range3 (0.625μM**)% Efficacy at a given concentrationFloat%
214% Efficacy at 0.3125 uM_fourth_point_Range3 (0.3125μM**)% Efficacy at a given concentrationFloat%
215% Efficacy at 0.15625 uM_fourth_point_Range3 (0.15625μM**)% Efficacy at a given concentrationFloat%
216% Efficacy at 0.078125 uM_fourth_point_Range3 (0.078125μM**)% Efficacy at a given concentrationFloat%
217% Efficacy at 0.0390625 uM_fourth_point_Range3 (0.0390625μM**)% Efficacy at a given concentrationFloat%
218% Efficacy at 0.01953125 uM_fourth_point_Range3 (0.0195312μM**)% Efficacy at a given concentrationFloat%

* Activity Concentration. ** Test Concentration.
Additional Information
Grant Number: 1R03 MH082385-01

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