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BioAssay: AID 1512

Luminescent assay for HTS discovery of chemical inhibitors of placental alkaline phosphatase confirmation

This PLAP dose response assay is developed and performed to confirm hits originally identified in the PLAP Luminescent HTS assay (AID 690) 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(262)
 
 
Active(93)
 
 
Inactive(169)
 
 
 Tested Substances
 Tested Substances
All(274)
 
 
Active(96)
 
 
Inactive(178)
 
 
AID: 1512
Data Source: Burnham Center for Chemical Genomics (BCCG-A128-PLAP-Dry-Powder)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: NIH Molecular Libraries Screening Center Network
BioAssay Version:
Deposit Date: 2009-01-21
Modify Date: 2010-12-29

Data Table ( Complete ):           View Active Data    View All Data
Target
BioActive Compounds: 93
Related Experiments
AIDNameTypeProbeComment
518TNAP luminescent HTS assayConfirmatory depositor-specified cross reference
690Luminescent assay for HTS discovery of chemical inhibitors of placental alkaline phosphataseConfirmatory depositor-specified cross reference
1577Summary luminescent assay for discovery of chemical inhibitors of placental alkaline phosphataseSummary2 depositor-specified cross reference
696Luminescent assay for HTS discovery of chemical activators of placental alkaline phosphataseConfirmatory same project related to Summary assay
1017Luminescent assay for identification of inhibitors of human intestinal alkaline phosphataseConfirmatory same project related to Summary assay
1019Luminescent assay for identification of inhibitors of bovine intestinal alkaline phosphataseScreening same project related to Summary assay
1056SAR analysis of an In Vitro TNAP Dose Response Luminescent 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: MH077602-01
Assay Provider: Dr. Jose Luis Millan, Sanford-Burnham Medical Research Institute, San Diego, CA.

This PLAP dose response assay is developed and performed to confirm hits originally identified in the PLAP Luminescent HTS assay (AID 690) and to study the structure-activity relationship on analogs of the confirmed hits. Compounds are either acquired from commercial sources or synthesized internally.

Alkaline phosphatase (EC 3.1.3.1) (APs) catalyze the hydrolysis of phosphomonoesters, releasing phosphate and alcohol. APs are dimeric enzymes found in most organisms. In human, four isozymes of APs have been identified: three isozymes are tissue-specific and the fourth one is tissue-nonspecific. Placental alkaline phosphatase (PLAP) is highly expressed in primate placental tissue. Its biological function is unknown. Identification of PLAP-specific inhibitors should provide necessary tools for characterization of its biological role.

PLAP screening was developed and performed at the Sanford-Burnham Center for Chemical Genomics (SBCCG) as part of the Molecular Library Screening Center Network (MLSCN). AID 690 was a selectivity screening for tissue nonspecific alkaline phosphatase (TNAP) screened at SBCCG (AID 518). XO1 submission, MH077602-01, Pharmacological inhibitors of tissue-nonspecific alkaline phosphatase (TNAP), Assay Provider Dr. Jose Luis Millan, Sanford-Burnham Medical Research Institute, San Diego, CA.
Protocol
PLAP assay materials:
1) PLAP 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: 250 mM DEA, pH 9.8, 2.5 mM MgCl2, and 0.05 mM ZnCl.
3) PLAP working solution contained a 1/6400 dilution in assay buffer. Solution was prepared fresh prior to use.
4) CDP-star working solution contained 212.5 uM CDP-star in MQ water.
5) TCEP working solution - 5 mM in 10% DMSO.
PLAP 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). Columns 1-2 and 23-24 contained 4 uL of TCEP working solution and 10% DMSO, respectively.
2) 8 uL of PLAP working solution was added to the whole plate using WellMate bulk dispenser (Matrix).
3) 8 uL of CDP-star working solution was added to the whole plate using WellMate bulk dispenser (Matrix).
4) Plates were incubated for 30 mins at room temperature.
5) Luminescence was measured on the Envision plate reader (Perkin Elmer).
6) Data analysis was performed using CBIS software (ChemInnovations, Inc) using sigmoidal dose-response equation through non-linear regression
Comment
The 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 IC50 the results were averaged and reported as IC50_Range. The IC50 results for all of the IC50s were averaged to produce IC50_Mean.
IC50 results are an average of two dose response curves. If for a given range there are 6 sets of curves there will be three IC50 results reported.
Compounds with an IC50_Mean < 100 uM are considered to be active in this assay.
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 PLAP 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 PLAP assay is as follows:
1) First tier (0-40 range) is reserved for primary screening data and is not applicable to this asay.
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. 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 the PLAP 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 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.
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: Functional
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 the qualifier is "=", the IC50 result equals the value in that column; if the qualifier is ">", the IC50 result is greater than that valueString
2IC50_Mean*The mean IC50 for all of the assaysFloatμM
3IC50_Qualifier_1_Range1This qualifier is to be used with the next TID, IC50_1_Range1. If the qualifier is "=", the IC50 result equals the value in that column; if the qualifier is ">", the IC50 result is greater than that value.String
4IC50_1_Range1The first IC50 value for Range1 determined using sigmoidal dose response equationFloatμM
5Std.Err(IC50)_1_Range1Standard Error of the preceeding IC50 valueFloatμM
6nH_1_Range1Hill coefficient determined using sigmoidal dose response equationFloat
7IC50_Qualifier_2_Range1This qualifier is to be used with the next TID, IC50_2_Range1. If the qualifier is "=", the IC50 result equals the value in that column; if the qualifier is ">", the IC50 result is greater than that value.String
8IC50_2_Range1The second IC50 value for Range1 determined using sigmoidal dose response equationFloatμM
9Std.Err(IC50)_2_Range1Standard Error of the preceeding IC50 valueFloatμM
10nH_2_Range1Hill coefficient determined using sigmoidal dose response equationFloat
11IC50_Qualifier_3_Range1This qualifier is to be used with the next TID, IC50_3_Range1. If the qualifier is "=", the IC50 result equals the value in that column; if the qualifier is ">", the IC50 result is greater than that value.String
12IC50_3_Range1The third IC50 value for Range1 determined using sigmoidal dose response equationFloatμM
13Std.Err(IC50)_3_Range1Standard Error of the preceeding IC50 valueFloatμM
14nH_3_Range1Hill coefficient determined using sigmoidal dose response equationFloat
15IC50_Qualifier_1_Range2This qualifier is to be used with the next TID, IC50_1_Range2. If the qualifier is "=", the IC50 result equals the value in that column; if the qualifier is ">", the IC50 result is greater than that value.String
16IC50_1_Range2The first IC50 value for Range2 determined using sigmoidal dose response equationFloatμM
17Std.Err(IC50)_1_Range2Standard Error of the preceeding IC50 valueFloatμM
18nH_1_Range2Hill coefficient determined using sigmoidal dose response equationFloat
19IC50_Qualifier_2_Range2This qualifier is to be used with the next TID, IC50_2_Range2. If the qualifier is "=", the IC50 result equals the value in that column; if the qualifier is ">", the IC50 result is greater than that value.String
20IC50_2_Range2The second IC50 value for Range2 determined using sigmoidal dose response equationFloatμM
21Std.Err(IC50)_2_Range2Standard Error of the preceeding IC50 valueFloatμM
22nH_2_Range2Hill coefficient determined using sigmoidal dose response equationFloat
23IC50_Qualifier_3_Range2This qualifier is to be used with the next TID, IC50_3_Range3. If the qualifier is "=", the IC50 result equals the value in that column; if the qualifier is ">", the IC50 result is greater than that value.String
24IC50_3_Range2The third IC50 value for Range2 determined using sigmoidal dose response equationFloatμM
25Std.Err(IC50)_3_Range2Standard Error of the preceeding IC50 valueFloatμM
26nH_3_Range2Hill coefficient determined using sigmoidal dose response equationFloat
27IC50_Qualifier_1_Range3This qualifier is to be used with the next TID, IC50_1_Range3. If the qualifier is "=", the IC50 result equals the value in that column; if the qualifier is ">", the IC50 result is greater than that value.String
28IC50_1_Range3The first IC50 value for Range2 determined using sigmoidal dose response equationFloatμM
29Std.Err(IC50)_1_Range3Standard Error of the preceeding IC50 valueFloatμM
30nH_1_Range3Hill coefficient determined using sigmoidal dose response equationFloat
31IC50_Qualifier_2_Range3This qualifier is to be used with the next TID, IC50_2_Range3. If the qualifier is "=", the IC50 result equals the value in that column; if the qualifier is ">", the IC50 result is greater than that value.String
32IC50_2_Range3The second IC50 value for Range3 determined using sigmoidal dose response equationFloatμM
33Std.Err(IC50)_2_Range3Standard Error of the preceeding IC50 valueFloatμM
34nH_2_Range3Hill coefficient determined using sigmoidal dose response equationFloat
35Excluded_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
36% inhibition at 100 uM_first_point_Range1 (100μM**)% inhibition at a given concentrationFloat%
37% inhibition at 50 uM_first_point_Range1 (50μM**)% inhibition at a given concentrationFloat%
38% inhibition at 25 uM_first_point_Range1 (25μM**)% inhibition at a given concentrationFloat%
39% inhibition at 12.5 uM_first_point_Range1 (12.5μM**)% inhibition at a given concentrationFloat%
40% inhibition at 6.25 uM_first_point_Range1 (6.25μM**)% inhibition at a given concentrationFloat%
41% inhibition at 3.125 uM_first_point_Range1 (3.125μM**)% inhibition at a given concentrationFloat%
42% inhibition at 1.5625 uM_first_point_Range1 (1.5625μM**)% inhibition at a given concentrationFloat%
43% inhibition at 0.78125 uM_first_point_Range1 (0.78125μM**)% inhibition at a given concentrationFloat%
44% inhibition at 0.390625 uM_first_point_Range1 (0.390625μM**)% inhibition at a given concentrationFloat%
45% inhibition at 0.1953125 uM_first_point_Range1 (0.195312μM**)% inhibition at a given concentrationFloat%
46Excluded_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
47% inhibition at 100 uM_second_point_Range1 (100μM**)% inhibition at a given concentrationFloat%
48% inhibition at 50 uM_second_point_Range1 (50μM**)% inhibition at a given concentrationFloat%
49% inhibition at 25 uM_second_point_Range1 (25μM**)% inhibition at a given concentrationFloat%
50% inhibition at 12.5 uM_second_point_Range1 (12.5μM**)% inhibition at a given concentrationFloat%
51% inhibition at 6.25 uM_second_point_Range1 (6.25μM**)% inhibition at a given concentrationFloat%
52% inhibition at 3.125 uM_second_point_Range1 (3.125μM**)% inhibition at a given concentrationFloat%
53% inhibition at 1.5625 uM_second_point_Range1 (1.5625μM**)% inhibition at a given concentrationFloat%
54% inhibition at 0.78125 uM_second_point_Range1 (0.78125μM**)% inhibition at a given concentrationFloat%
55% inhibition at 0.390625 uM_second_point_Range1 (0.390625μM**)% inhibition at a given concentrationFloat%
56% inhibition at 0.1953125 uM_second_point_Range1 (0.195312μM**)% inhibition at a given concentrationFloat%
57Excluded_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
58% inhibition at 100 uM_third_point_Range1 (100μM**)% inhibition at a given concentrationFloat%
59% inhibition at 50 uM_third_point_Range1 (50μM**)% inhibition at a given concentrationFloat%
60% inhibition at 25 uM_third_point_Range1 (25μM**)% inhibition at a given concentrationFloat%
61% inhibition at 12.5 uM_third_point_Range1 (12.5μM**)% inhibition at a given concentrationFloat%
62% inhibition at 6.25 uM_third_point_Range1 (6.25μM**)% inhibition at a given concentrationFloat%
63% inhibition at 3.125 uM_third_point_Range1 (3.125μM**)% inhibition at a given concentrationFloat%
64% inhibition at 1.5625 uM_third_point_Range1 (1.5625μM**)% inhibition at a given concentrationFloat%
65% inhibition at 0.78125 uM_third_point_Range1 (0.78125μM**)% inhibition at a given concentrationFloat%
66% inhibition at 0.390625 uM_third_point_Range1 (0.390625μM**)% inhibition at a given concentrationFloat%
67% inhibition at 0.1953125 uM_third_point_Range1 (0.195312μM**)% inhibition at a given concentrationFloat%
68Excluded_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
69% inhibition at 100 uM_fourth_point_Range1 (100μM**)% inhibition at a given concentrationFloat%
70% inhibition at 50 uM_fourth_point_Range1 (50μM**)% inhibition at a given concentrationFloat%
71% inhibition at 25 uM_fourth_point_Range1 (25μM**)% inhibition at a given concentrationFloat%
72% inhibition at 12.5 uM_fourth_point_Range1 (12.5μM**)% inhibition at a given concentrationFloat%
73% inhibition at 6.25 uM_fourth_point_Range1 (6.25μM**)% inhibition at a given concentrationFloat%
74% inhibition at 3.125 uM_fourth_point_Range1 (3.125μM**)% inhibition at a given concentrationFloat%
75% inhibition at 1.5625 uM_fourth_point_Range1 (1.5625μM**)% inhibition at a given concentrationFloat%
76% inhibition at 0.78125 uM_fourth_point_Range1 (0.78125μM**)% inhibition at a given concentrationFloat%
77% inhibition at 0.390625 uM_fourth_point_Range1 (0.390625μM**)% inhibition at a given concentrationFloat%
78% inhibition at 0.1953125 uM_fourth_point_Range1 (0.195312μM**)% inhibition at a given concentrationFloat%
79Excluded_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
80% inhibition at 100 uM_fifth_point_Range1 (100μM**)% inhibition at a given concentrationFloat%
81% inhibition at 50 uM_fifth_point_Range1 (50μM**)% inhibition at a given concentrationFloat%
82% inhibition at 25 uM_fifth_point_Range1 (25μM**)% inhibition at a given concentrationFloat%
83% inhibition at 12.5 uM_fifth_point_Range1 (12.5μM**)% inhibition at a given concentrationFloat%
84% inhibition at 6.25 uM_fifth_point_Range1 (6.25μM**)% inhibition at a given concentrationFloat%
85% inhibition at 3.125 uM_fifth_point_Range1 (3.125μM**)% inhibition at a given concentrationFloat%
86% inhibition at 1.5625 uM_fifth_point_Range1 (1.5625μM**)% inhibition at a given concentrationFloat%
87% inhibition at 0.78125 uM_fifth_point_Range1 (0.78125μM**)% inhibition at a given concentrationFloat%
88% inhibition at 0.390625 uM_fifth_point_Range1 (0.390625μM**)% inhibition at a given concentrationFloat%
89% inhibition at 0.1953125 uM_fifth_point_Range1 (0.195312μM**)% inhibition at a given concentrationFloat%
90Excluded_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
91% inhibition at 100 uM_sixth_point_Range1 (100μM**)% inhibition at a given concentrationFloat%
92% inhibition at 50 uM_sixth_point_Range1 (50μM**)% inhibition at a given concentrationFloat%
93% inhibition at 25 uM_sixth_point_Range1 (25μM**)% inhibition at a given concentrationFloat%
94% inhibition at 12.5 uM_sixth_point_Range1 (12.5μM**)% inhibition at a given concentrationFloat%
95% inhibition at 6.25 uM_sixth_point_Range1 (6.25μM**)% inhibition at a given concentrationFloat%
96% inhibition at 3.125 uM_sixth_point_Range1 (3.125μM**)% inhibition at a given concentrationFloat%
97% inhibition at 1.5625 uM_sixth_point_Range1 (1.5625μM**)% inhibition at a given concentrationFloat%
98% inhibition at 0.78125 uM_sixth_point_Range1 (0.78125μM**)% inhibition at a given concentrationFloat%
99% inhibition at 0.390625 uM_sixth_point_Range1 (0.390625μM**)% inhibition at a given concentrationFloat%
100% inhibition at 0.1953125 uM_sixth_point_Range1 (0.195312μM**)% inhibition at a given concentrationFloat%
101IC50_Qualifier_Range2This qualifier is to be used with the next TID, IC50_Range2. If the qualifier is "=", the IC50 result equals the value in that column; if the qualifier is ">", the IC50 result is greater than that value.String
102IC50_Range2IC50 value determined using sigmoidal dose response equationFloatμM
103Std.Err(IC50)_Range2Standard Error of IC50 valueFloat
104nH_Range2Hill coefficient determined using sigmoidal dose response equationFloat
105Excluded_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
106% inhibition at 1 uM_first_point_Range2 (1μM**)% inhibition at a given concentrationFloat%
107% inhibition at 0.5 uM_first_point_Range2 (0.5μM**)% inhibition at a given concentrationFloat%
108% inhibition at 0.25 uM_first_point_Range2 (0.25μM**)% inhibition at a given concentrationFloat%
109% inhibition at 0.125 uM_first_point_Range2 (0.125μM**)% inhibition at a given concentrationFloat%
110% inhibition at 0.0625 uM_first_point_Range2 (0.0625μM**)% inhibition at a given concentrationFloat%
111% inhibition at 0.03125 uM_first_point_Range2 (0.03125μM**)% inhibition at a given concentrationFloat%
112% inhibition at 0.015625 uM_first_point_Range2 (0.015625μM**)% inhibition at a given concentrationFloat%
113% inhibition at 0.0078125 uM_first_point_Range2 (0.0078125μM**)% inhibition at a given concentrationFloat%
114% inhibition at 0.00390625 uM_first_point_Range2 (0.00390625μM**)% inhibition at a given concentrationFloat%
115% inhibition at 0.001953125 uM_first_point_Range2 (0.000195313μM**)% inhibition at a given concentrationFloat%
116Excluded_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
117% inhibition at 1 uM_second_point_Range2 (1μM**)% inhibition at a given concentrationFloat%
118% inhibition at 0.5 uM_second_point_Range2 (0.5μM**)% inhibition at a given concentrationFloat%
119% inhibition at 0.25 uM_second_point_Range2 (0.25μM**)% inhibition at a given concentrationFloat%
120% inhibition at 0.125 uM_second_point_Range2 (0.125μM**)% inhibition at a given concentrationFloat%
121% inhibition at 0.0625 uM_second_point_Range2 (0.0625μM**)% inhibition at a given concentrationFloat%
122% inhibition at 0.03125 uM_second_point_Range2 (0.03125μM**)% inhibition at a given concentrationFloat%
123% inhibition at 0.015625 uM_second_point_Range2 (0.015625μM**)% inhibition at a given concentrationFloat%
124% inhibition at 0.0078125 uM_second_point_Range2 (0.0078125μM**)% inhibition at a given concentrationFloat%
125% inhibition at 0.00390625 uM_second_point_Range2 (0.00390625μM**)% inhibition at a given concentrationFloat%
126% inhibition at 0.001953125 uM_second_point_Range2 (0.00195312μM**)% inhibition at a given concentrationFloat%
127Excluded_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
128% inhibition at 1 uM_third_point_Range2 (1μM**)% inhibition at a given concentrationFloat%
129% inhibition at 0.5 uM_third_point_Range2 (0.5μM**)% inhibition at a given concentrationFloat%
130% inhibition at 0.25 uM_third_point_Range2 (0.25μM**)% inhibition at a given concentrationFloat%
131% inhibition at 0.125 uM_third_point_Range2 (0.125μM**)% inhibition at a given concentrationFloat%
132% inhibition at 0.0625 uM_third_point_Range2 (0.625μM**)% inhibition at a given concentrationFloat%
133% inhibition at 0.03125 uM_third_point_Range2 (0.03125μM**)% inhibition at a given concentrationFloat%
134% inhibition at 0.015625 uM_third_point_Range2 (0.015625μM**)% inhibition at a given concentrationFloat%
135% inhibition at 0.0078125 uM_third_point_Range2 (0.0078125μM**)% inhibition at a given concentrationFloat%
136% inhibition at 0.00390625 uM_third_point_Range2 (0.00390625μM**)% inhibition at a given concentrationFloat%
137% inhibition at 0.001953125 uM_third_point_Range2 (0.00195312μM**)% inhibition at a given concentrationFloat%
138Excluded_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
139% inhibition at 1 uM_fourth_point_Range2 (1μM**)% inhibition at a given concentrationFloat%
140% inhibition at 0.5 uM_fourth_point_Range2 (0.5μM**)% inhibition at a given concentrationFloat%
141% inhibition at 0.25 uM_fourth_point_Range2 (0.25μM**)% inhibition at a given concentrationFloat%
142% inhibition at 0.125 uM_fourth_point_Range2 (0.125μM**)% inhibition at a given concentrationFloat%
143% inhibition at 0.0625 uM_fourth_point_Range2 (0.0625μM**)% inhibition at a given concentrationFloat%
144% inhibition at 0.03125 uM_fourth_point_Range2 (0.03125μM**)% inhibition at a given concentrationFloat%
145% inhibition at 0.015625 uM_fourth_point_Range2 (0.015625μM**)% inhibition at a given concentrationFloat%
146% inhibition at 0.0078125 uM_fourth_point_Range2 (0.0078125μM**)% inhibition at a given concentrationFloat%
147% inhibition at 0.00390625 uM_fourth_point_Range2 (0.00390625μM**)% inhibition at a given concentrationFloat%
148% inhibition at 0.001953125 uM_fourth_point_Range2 (0.00195312μM**)% inhibition at a given concentrationFloat%
149Excluded_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
150% inhibition at 1 uM_fifth_point_Range2 (1μM**)% inhibition at a given concentrationFloat%
151% inhibition at 0.5 uM_fifth_point_Range2 (0.5μM**)% inhibition at a given concentrationFloat%
152% inhibition at 0.25 uM_fifth_point_Range2 (0.25μM**)% inhibition at a given concentrationFloat%
153% inhibition at 0.125 uM_fifth_point_Range2 (0.125μM**)% inhibition at a given concentrationFloat%
154% inhibition at 0.0625 uM_fifth_point_Range2 (0.0625μM**)% inhibition at a given concentrationFloat%
155% inhibition at 0.03125 uM_fifth_point_Range2 (0.03125μM**)% inhibition at a given concentrationFloat%
156% inhibition at 0.015625 uM_fifth_point_Range2 (0.015625μM**)% inhibition at a given concentrationFloat%
157% inhibition at 0.0078125 uM_fifth_point_Range2 (0.0078125μM**)% inhibition at a given concentrationFloat%
158% inhibition at 0.00390625 uM_fifth_point_Range2 (0.00390625μM**)% inhibition at a given concentrationFloat%
159% inhibition at 0.001953125 uM_fifth_point_Range2 (0.00195312μM**)% inhibition at a given concentrationFloat%
160Excluded_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
161% inhibition at 1 uM_sixth_point_Range2 (1μM**)% inhibition at a given concentrationFloat%
162% inhibition at 0.5 uM_sixth_point_Range2 (0.5μM**)% inhibition at a given concentrationFloat%
163% inhibition at 0.25 uM_sixth_point_Range2 (0.25μM**)% inhibition at a given concentrationFloat%
164% inhibition at 0.125 uM_sixth_point_Range2 (0.125μM**)% inhibition at a given concentrationFloat%
165% inhibition at 0.0625 uM_sixth_point_Range2 (0.0625μM**)% inhibition at a given concentrationFloat%
166% inhibition at 0.03125 uM_sixth_point_Range2 (0.03125μM**)% inhibition at a given concentrationFloat%
167% inhibition at 0.015625 uM_sixth_point_Range2 (0.015625μM**)% inhibition at a given concentrationFloat%
168% inhibition at 0.0078125 uM_sixth_point_Range2 (0.0078125μM**)% inhibition at a given concentrationFloat%
169% inhibition at 0.00390625 uM_sixth_point_Range2 (0.00390625μM**)% inhibition at a given concentrationFloat%
170% inhibition at 0.001953125 uM_sixth_point_Range2 (0.00195312μM**)% inhibition at a given concentrationFloat%
171IC50_Qualifier_Range3This qualifier is to be used with the next TID, IC50_Range3. If the qualifier is "=", the IC50 result equals the value in that column; if the qualifier is ">", the IC50 result is greater than that value.String
172IC50_Range3IC50 value determined using sigmoidal dose response equationFloatμM
173Std.Err(IC50)_Range3Standard Error of IC50 valueFloat
174nH_Range3Hill coefficient determined using sigmoidal dose response equationFloat
175Excluded_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
176% inhibition at 10 uM_first_point_Range3 (10μM**)% inhibition at a given concentrationFloat%
177% inhibition at 5 uM_first_point_Range3 (5μM**)% inhibition at a given concentrationFloat%
178% inhibition at 2.5 uM_first_point_Range3 (2.5μM**)% inhibition at a given concentrationFloat%
179% inhibition at 1.25 uM_first_point_Range3 (1.25μM**)% inhibition at a given concentrationFloat%
180% inhibition at 0.625 uM_first_point_Range3 (0.625μM**)% inhibition at a given concentrationFloat%
181% inhibition at 0.3125 uM_first_point_Range3 (0.3125μM**)% inhibition at a given concentrationFloat%
182% inhibition at 0.15625 uM_first_point_Range3 (0.15625μM**)% inhibition at a given concentrationFloat%
183% inhibition at 0.078125 uM_first_point_Range3 (0.078125μM**)% inhibition at a given concentrationFloat%
184% inhibition at 0.0390625 uM_first_point_Range3 (0.0390625μM**)% inhibition at a given concentrationFloat%
185% inhibition at 0.01953125 uM_first_point_Range3 (0.0195312μM**)% inhibition at a given concentrationFloat%
186Excluded_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
187% inhibition at 10 uM_second_point_Range3 (10μM**)% inhibition at a given concentrationFloat%
188% inhibition at 5 uM_second_point_Range3 (5μM**)% inhibition at a given concentrationFloat%
189% inhibition at 2.5 uM_second_point_Range3 (2.5μM**)% inhibition at a given concentrationFloat%
190% inhibition at 1.25 uM_second_point_Range3 (1.25μM**)% inhibition at a given concentrationFloat%
191% inhibition at 0.625 uM_second_point_Range3 (0.625μM**)% inhibition at a given concentrationFloat%
192% inhibition at 0.3125 uM_second_point_Range3 (0.3125μM**)% inhibition at a given concentrationFloat%
193% inhibition at 0.15625 uM_second_point_Range3 (0.15625μM**)% inhibition at a given concentrationFloat%
194% inhibition at 0.078125 uM_second_point_Range3 (0.078125μM**)% inhibition at a given concentrationFloat%
195% inhibition at 0.0390625 uM_second_point_Range3 (0.0390625μM**)% inhibition at a given concentrationFloat%
196% inhibition at 0.01953125 uM_second_point_Range3 (0.0195312μM**)% inhibition at a given concentrationFloat%
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% inhibition at 10 uM_third_point_Range3 (10μM**)% inhibition at a given concentrationFloat%
199% inhibition at 5 uM_third_point_Range3 (5μM**)% inhibition at a given concentrationFloat%
200% inhibition at 2.5 uM_third_point_Range3 (2.5μM**)% inhibition at a given concentrationFloat%
201% inhibition at 1.25 uM_third_point_Range3 (1.25μM**)% inhibition at a given concentrationFloat%
202% inhibition at 0.625 uM_third_point_Range3 (0.625μM**)% inhibition at a given concentrationFloat%
203% inhibition at 0.3125 uM_third_point_Range3 (0.3125μM**)% inhibition at a given concentrationFloat%
204% inhibition at 0.15625 uM_third_point_Range3 (0.15625μM**)% inhibition at a given concentrationFloat%
205% inhibition at 0.078125 uM_third_point_Range3 (0.078125μM**)% inhibition at a given concentrationFloat%
206% inhibition at 0.0390625 uM_third_point_Range3 (0.0390625μM**)% inhibition at a given concentrationFloat%
207% inhibition at 0.01953125 uM_third_point_Range3 (0.0195312μM**)% inhibition 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% inhibition at 10 uM_fourth_point_Range3 (10μM**)% inhibition at a given concentrationFloat%
210% inhibition at 5 uM_fourth_point_Range3 (5μM**)% inhibition at a given concentrationFloat%
211% inhibition at 2.5 uM_fourth_point_Range3 (5μM**)% inhibition at a given concentrationFloat%
212% inhibition at 1.25 uM_fourth_point_Range3 (1.25μM**)% inhibition at a given concentrationFloat%
213% inhibition at 0.625 uM_fourth_point_Range3 (0.625μM**)% inhibition at a given concentrationFloat%
214% inhibition at 0.3125 uM_fourth_point_Range3 (0.3125μM**)% inhibition at a given concentrationFloat%
215% inhibition at 0.15625 uM_fourth_point_Range3 (0.15625μM**)% inhibition at a given concentrationFloat%
216% inhibition at 0.078125 uM_fourth_point_Range3 (0.078125μM**)% inhibition at a given concentrationFloat%
217% inhibition at 0.0390625 uM_fourth_point_Range3 (0.0390625μM**)% inhibition at a given concentrationFloat%
218% inhibition at 0.01953125 uM_fourth_point_Range3 (0.0195312μM**)% inhibition at a given concentrationFloat%

* Activity Concentration. ** Test Concentration.
Additional Information
Grant Number: MH081277-01

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