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BioAssay: AID 488963

SAR analysis of Antagonists of XIAP-Bir3 domain of IAP-family anti-apoptotic proteins - Set 2

This dose response assay is developed and performed as a counter screen to compounds in the Chemical Antagonists of IAP-family anti-apoptotic proteins confirmation (AID 1449) and to study the structure-activity relationship on analogs of the confirmed hits. Compounds are either acquired from commercial sources or synthesized internally. This assay was performed in the assay providers' laboratory. ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Inactive(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Inactive(1)
 
 
AID: 488963
Data Source: Burnham Center for Chemical Genomics (SBCCG-A507-XIAP-Bir3-Assay-dry powder-2)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: NIH Molecular Libraries Probe Production Network
Deposit Date: 2010-10-28

Data Table ( Complete ):           All
Target
Tested Compound:
Depositor Specified Assays
AIDNameTypeProbeComment
1018Chemical Antagonists IAP-family anti-apoptotic proteinsconfirmatory
1449Chemical Antagonists of IAP-family anti-apoptotic proteins confirmationconfirmatory
1513Counter Screen using XIAP-Bir3 for Chemical Antagonists of Bir1/2 domains of IAP-family anti-apoptotic proteinsconfirmatory
1514Counter Screen using XIAP-Bir3 of the Chemical Antagonists of IAP-family anti-apoptotic proteins confirmation assayconfirmatory
1638Summary of Chemical Antagonists IAP-family anti-apoptotic proteinssummary3
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 Production Centers Network(MLPCN)Grant Proposal Number: MH081277-01
Assay Provider: John C. Reed, Sanford-Burnham Medical Research Institute San Diego, CA

This dose response assay is developed and performed as a counter screen to compounds in the Chemical Antagonists of IAP-family anti-apoptotic proteins confirmation (AID 1449) and to study the structure-activity relationship on analogs of the confirmed hits. Compounds are either acquired from commercial sources or synthesized internally. This assay was performed in the assay providers' laboratory.

Apoptosis plays an essential role in many aspects of normal development and physiology, becoming dysregulated in myriad diseases characterized by insufficient or excessive cell death. Caspases are intracellular proteases that are suppressed by Inhibitor of Apoptosis Proteins (IAPs), a family of evolutionarily conserved anti-apoptotic proteins. Proteins released from mitochondria (SMAC and HtrA2) can competitively displace IAPs from the Caspases, thus helping to drive apoptosis. It has been shown that only a few residues at the N-terminus of activated SMAC protein (4'mer) are sufficient to affect the release of IAPs from Caspases. Thus, it is plausible to identify chemical compounds that mimic the effect of SMAC in antagonizing IAPs by causing them to release Caspases. Non-peptidyl chemical inhibitors would have advantages over SMAC peptides, in terms of cell permeability, stability, and in vivo pharmacology. Thus, the goal of this project is to generate small-molecule chemical probe compounds that mimic the effects of SMAC peptides, inhibiting the function of IAPs.

Basis of the assay is disruption of fluorescence polarization resulting from binding of a XIAP-BIR3 (bacoloviral IAP repeat, "Bir3") domain protein derived from two of the three conserved caspase binding "BIR" domains of XIAP to a rhodamine tagged 7-mer N-terminal SMAC peptide.
Protocol
BIR3 assay materials:
1) Bir3 protein was provided by Prof. John C. Reed (Sanford-Burnham Medical Research Institute, San Diego, CA) and SMAC-rhodamine peptide (AVPIAQK-rhodamine) was provided by Richard Houghten (Torrey Pines Institute for Molecular Studies, San Diego, CA).
2) Assay buffer: 33.35 Hepes @ pH 7.5, 1.33 mM TCEP, 0.00667 % Tween 20, 0.265 uM BIR3 and 0.0267 uM SMAC-rhodamine.

BIR3 protocol:
1) 15 ul of assay buffer was added to a greiner bio-one black 384 well plate (number 784076-25) in columns 9 through 12.
2) Five ul of compounds were added to the plate in columns 9 through 12 with a 16 point curve generated by 2 fold dilutions of each compound. Final compound concentration in the assay ranged from 100 uM to 0.00612 uM via two fold dilutions starting with 400 uM maximum concentration.
3) Positive controls without protein were in column 19. Negative controls with protein were in column 18.
4) Final concentrations of the components were 25 mM Hepes @ pH 7.5/ 1 mm TCEP/0.005% Tween 20/20 nM rhodamine-SMAC/0.2 uM BIR3. Compound was diluted in water starting at 400 uM and diluted serially by a factor of 2. Final concentrations of compounds were one fourth the concentration of the initial compound curve.
5) Plates were then centrifuged at 1000 rpm for 1 minute before reading on an LJL Analyst using an excitation filter of 530 nm with emission at 580 nm and a dichroic mirror at 565 nm.
6) Resultant data was fit to a nonlinear curve in Prism and IC50 values and Hill coefficients were determined. BIR3 assays often had a Hill coefficient greater than 1.
Comment
Compounds with an IC50 < 100 uM are considered "active."

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 Bir1/2 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 Bir1/2 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'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 XIAP 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 90 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
1IC50_Mean_QualifierThis qualifier is to be used with the next TID, IC50_Mean. If qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that valueString
2IC50_Mean*IC50 value determined using sigmoidal dose response equationFloatμM
3IC50_Qualifier_1This qualifier is to be used with the next TID, IC50_1. If qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that valueString
4IC50_1IC50 value determined using sigmoidal dose response equationFloatμM
5Std.Err(IC50)_1Standard Error of IC50 valueFloatμM
6nH_1Hill coefficient determined using sigmoidal dose response equationFloat
7Excluded_Points_first_pointFlags to indicate which of the first dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
8FP at 100 uM_first_point (100μM**)Fluorescence Polarization at a given concentrationFloatmP
9FP at 50 uM_first_point (50μM**)Fluorescence Polarization at a given concentrationFloatmP
10FP at 25 uM_first_point (25μM**)Fluorescence Polarization at a given concentrationFloatmP
11FP at 12.5 uM_first_point (12.5μM**)Fluorescence Polarization at a given concentrationFloatmP
12FP at 6.25 uM_first_point (6.25μM**)Fluorescence Polarization at a given concentrationFloatmP
13FP at 3.125 uM_first_point (3.125μM**)Fluorescence Polarization at a given concentrationFloatmP
14FP at 1.5625 uM_first_point (1.5625μM**)Fluorescence Polarization at a given concentrationFloatmP
15FP at 0.78125 uM_first_point (0.78125μM**)Fluorescence Polarization at a given concentrationFloatmP
16FP at 0.390625 uM_first_point (0.390625μM**)Fluorescence Polarization at a given concentrationFloatmP
17FP at 0.1953125 uM_first_point (0.195312μM**)Fluorescence Polarization at a given concentrationFloatmP
18FP at 0.097656 uM_first_point (0.097656μM**)Fluorescence Polarization at a given concentrationFloatmP
19FP at 0.048828 uM_first_point (0.048828μM**)Fluorescence Polarization at a given concentrationFloatmP
20FP at 0.24414 uM_first_point (0.24414μM**)Fluorescence Polarization at a given concentrationFloatmP
21FP at 0.12207 uM_first_point (0.12207μM**)Fluorescence Polarization at a given concentrationFloatmP
22FP at 0.006104 uM_first_point (0.006104μM**)Fluorescence Polarization at a given concentrationFloatmP
23IC50_Qualifier_2This qualifier is to be used with the next TID, IC50_2. If qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that valueString
24IC50_2IC50 value determined using sigmoidal dose response equationFloatμM
25Std.Err(IC50)_2Standard Error of IC50 valueFloatμM
26nH_2Hill coefficient determined using sigmoidal dose response equationFloat
27Excluded_Points_second_pointFlags to indicate which of the second dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
28FP at 100 uM_second_point (100μM**)Fluorescence Polarization at a given concentrationFloatmP
29FP at 50 uM_second_point (50μM**)Fluorescence Polarization at a given concentrationFloatmP
30FP at 25 uM_second_point (25μM**)Fluorescence Polarization at a given concentrationFloatmP
31FP at 12.5 uM_second_point (12.5μM**)Fluorescence Polarization at a given concentrationFloatmP
32FP at 6.25 uM_second_point (6.25μM**)Fluorescence Polarization at a given concentrationFloatmP
33FP at 3.125 uM_second_point (3.125μM**)Fluorescence Polarization at a given concentrationFloatmP
34FP at 1.5625 uM_second_point (1.5625μM**)Fluorescence Polarization at a given concentrationFloatmP
35FP at 0.78125 uM_second_point (0.78125μM**)Fluorescence Polarization at a given concentrationFloatmP
36FP at 0.390625 uM_second_point (0.390625μM**)Fluorescence Polarization at a given concentrationFloatmP
37FP at 0.1953125 uM_second_point (0.195312μM**)Fluorescence Polarization at a given concentrationFloatmP
38FP at 0.097656 uM_second_point (0.097656μM**)Fluorescence Polarization at a given concentrationFloatmP
39FP at 0.048828 uM_second_point (0.048828μM**)Fluorescence Polarization at a given concentrationFloatmP
40FP at 0.24414 uM_second_point (0.24414μM**)Fluorescence Polarization at a given concentrationFloatmP
41FP at 0.12207 uM_second_point (0.12207μM**)Fluorescence Polarization at a given concentrationFloatmP
42FP at 0.006104 uM_second_point (0.006104μM**)Fluorescence Polarization at a given concentrationFloatmP
43IC50_Qualifier_3This qualifier is to be used with the next TID, IC50_3. If qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that valueString
44IC50_3IC50 value determined using sigmoidal dose response equationFloatμM
45Std.Err(IC50)_3Standard Error of IC50 valueFloatμM
46nH_3Hill coefficient determined using sigmoidal dose response equationFloat
47Excluded_Points_third_pointFlags to indicate which of the third dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
48FP at 100 uM_third_point (100μM**)Fluorescence Polarization at a given concentrationFloatmP
49FP at 50 uM_third_point (50μM**)Fluorescence Polarization at a given concentrationFloatmP
50FP at 25 uM_third_point (25μM**)Fluorescence Polarization at a given concentrationFloatmP
51FP at 12.5 uM_third_point (12.5μM**)Fluorescence Polarization at a given concentrationFloatmP
52FP at 6.25 uM_third_point (6.25μM**)Fluorescence Polarization at a given concentrationFloatmP
53FP at 3.125 uM_third_point (3.125μM**)Fluorescence Polarization at a given concentrationFloatmP
54FP at 1.5625 uM_third_point (1.5625μM**)Fluorescence Polarization at a given concentrationFloatmP
55FP at 0.78125 uM_third_point (0.78125μM**)Fluorescence Polarization at a given concentrationFloatmP
56FP at 0.390625 uM_third_point (0.390625μM**)Fluorescence Polarization at a given concentrationFloatmP
57FP at 0.1953125 uM_third_point (0.195312μM**)Fluorescence Polarization at a given concentrationFloatmP
58FP at 0.097656 uM_third_point (0.097656μM**)Fluorescence Polarization at a given concentrationFloatmP
59FP at 0.048828 uM_third_point (0.048828μM**)Fluorescence Polarization at a given concentrationFloatmP
60FP at 0.24414 uM_third_point (0.24414μM**)Fluorescence Polarization at a given concentrationFloatmP
61FP at 0.12207 uM_third_point (0.12207μM**)Fluorescence Polarization at a given concentrationFloatmP
62FP at 0.006104 uM_third_point (0.006104μM**)Fluorescence Polarization at a given concentrationFloatmP
63IC50_Qualifier_4This qualifier is to be used with the next TID, IC50_4. If qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that valueString
64IC50_4IC50 value determined using sigmoidal dose response equationFloatμM
65Std.Err(IC50)_4Standard Error of IC50 valueFloatμM
66nH_4Hill coefficient determined using sigmoidal dose response equationFloat
67Excluded_Points_fourth_pointFlags to indicate which of the fourth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
68FP at 100 uM_fourth_point (100μM**)Fluorescence Polarization at a given concentrationFloatmP
69FP at 50 uM_fourth_point (50μM**)Fluorescence Polarization at a given concentrationFloatmP
70FP at 25 uM_fourth_point (25μM**)Fluorescence Polarization at a given concentrationFloatmP
71FP at 12.5 uM_fourth_point (12.5μM**)Fluorescence Polarization at a given concentrationFloatmP
72FP at 6.25 uM_fourth_point (6.25μM**)Fluorescence Polarization at a given concentrationFloatmP
73FP at 3.125 uM_fourth_point (3.125μM**)Fluorescence Polarization at a given concentrationFloatmP
74FP at 1.5625 uM_fourth_point (1.5625μM**)Fluorescence Polarization at a given concentrationFloatmP
75FP at 0.78125 uM_fourth_point (0.78125μM**)Fluorescence Polarization at a given concentrationFloatmP
76FP at 0.390625 uM_fourth_point (0.390625μM**)Fluorescence Polarization at a given concentrationFloatmP
77FP at 0.1953125 uM_fourth_point (0.195312μM**)Fluorescence Polarization at a given concentrationFloatmP
78FP at 0.097656 uM_fourth_point (0.097656μM**)Fluorescence Polarization at a given concentrationFloatmP
79FP at 0.048828 uM_fourth_point (0.048828μM**)Fluorescence Polarization at a given concentrationFloatmP
80FP at 0.24414 uM_fourth_point (0.24414μM**)Fluorescence Polarization at a given concentrationFloatmP
81FP at 0.12207 uM_fourth_point (0.12207μM**)Fluorescence Polarization at a given concentrationFloatmP
82FP at 0.006104 uM_fourth_point (0.006104μM**)Fluorescence Polarization at a given concentrationFloatmP
83IC50_Qualifier_5This qualifier is to be used with the next TID, IC50_5. If qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that valueString
84IC50_5IC50 value determined using sigmoidal dose response equationFloatμM
85Std.Err(IC50)_5Standard Error of IC50 valueFloatμM
86nH_5Hill coefficient determined using sigmoidal dose response equationFloat
87Excluded_Points_fifth_pointFlags to indicate which of the fifth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
88FP at 100 uM_fifth_point (100μM**)Fluorescence Polarization at a given concentrationFloatmP
89FP at 50 uM_fifth_point (50μM**)Fluorescence Polarization at a given concentrationFloatmP
90FP at 25 uM_fifth_point (25μM**)Fluorescence Polarization at a given concentrationFloatmP
91FP at 12.5 uM_fifth_point (12.5μM**)Fluorescence Polarization at a given concentrationFloatmP
92FP at 6.25 uM_fifth_point (6.25μM**)Fluorescence Polarization at a given concentrationFloatmP
93FP at 3.125 uM_fifth_point (3.125μM**)Fluorescence Polarization at a given concentrationFloatmP
94FP at 1.5625 uM_fifth_point (1.5625μM**)Fluorescence Polarization at a given concentrationFloatmP
95FP at 0.78125 uM_fifth_point (0.78125μM**)Fluorescence Polarization at a given concentrationFloatmP
96FP at 0.390625 uM_fifth_point (0.390625μM**)Fluorescence Polarization at a given concentrationFloatmP
97FP at 0.1953125 uM_fifth_point (0.195312μM**)Fluorescence Polarization at a given concentrationFloatmP
98FP at 0.097656 uM_fifth_point (0.097656μM**)Fluorescence Polarization at a given concentrationFloatmP
99FP at 0.048828 uM_fifth_point (0.048828μM**)Fluorescence Polarization at a given concentrationFloatmP
100FP at 0.24414 uM_fifth_point (0.24414μM**)Fluorescence Polarization at a given concentrationFloatmP
101FP at 0.12207 uM_fifth_point (0.12207μM**)Fluorescence Polarization at a given concentrationFloatmP
102FP at 0.006104 uM_fifth_point (0.006104μM**)Fluorescence Polarization at a given concentrationFloatmP
103IC50_Qualifier_6This qualifier is to be used with the next TID, IC50_6. If qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that valueString
104IC50_6IC50 value determined using sigmoidal dose response equationFloatμM
105Std.Err(IC50)_6Standard Error of IC50 valueFloatμM
106nH_6Hill coefficient determined using sigmoidal dose response equationFloat
107Excluded_Points_sixth_pointFlags to indicate which of the sixth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
108FP at 100 uM_sixth_point (100μM**)Fluorescence Polarization at a given concentrationFloatmP
109FP at 50 uM_sixth_point (50μM**)Fluorescence Polarization at a given concentrationFloatmP
110FP at 25 uM_sixth_point (25μM**)Fluorescence Polarization at a given concentrationFloatmP
111FP at 12.5 uM_sixth_point (12.5μM**)Fluorescence Polarization at a given concentrationFloatmP
112FP at 6.25 uM_sixth_point (6.25μM**)Fluorescence Polarization at a given concentrationFloatmP
113FP at 3.125 uM_sixth_point (3.125μM**)Fluorescence Polarization at a given concentrationFloatmP
114FP at 1.5625 uM_sixth_point (1.5625μM**)Fluorescence Polarization at a given concentrationFloatmP
115FP at 0.78125 uM_sixth_point (0.78125μM**)Fluorescence Polarization at a given concentrationFloatmP
116FP at 0.390625 uM_sixth_point (0.390625μM**)Fluorescence Polarization at a given concentrationFloatmP
117FP at 0.1953125 uM_sixth_point (0.195312μM**)Fluorescence Polarization at a given concentrationFloatmP
118FP at 0.097656 uM_sixth_point (0.097656μM**)Fluorescence Polarization at a given concentrationFloatmP
119FP at 0.048828 uM_sixth_point (0.048828μM**)Fluorescence Polarization at a given concentrationFloatmP
120FP at 0.24414 uM_sixth_point (0.24414μM**)Fluorescence Polarization at a given concentrationFloatmP
121FP at 0.12207 uM_sixth_point (0.12207μM**)Fluorescence Polarization at a given concentrationFloatmP
122FP at 0.006104 uM_sixth_point (0.006104μM**)Fluorescence Polarization at a given concentrationFloatmP
123IC50_Qualifier_7This qualifier is to be used with the next TID, IC50_7. If qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that valueString
124IC50_7IC50 value determined using sigmoidal dose response equationFloatμM
125Std.Err(IC50)_7Standard Error of IC50 valueFloatμM
126nH_7Hill coefficient determined using sigmoidal dose response equationFloat
127Excluded_Points_seventh_pointFlags to indicate which of the seventh dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
128FP at 100 uM_seventh_point (100μM**)Fluorescence Polarization at a given concentrationFloatmP
129FP at 50 uM_seventh_point (50μM**)Fluorescence Polarization at a given concentrationFloatmP
130FP at 25 uM_seventh_point (25μM**)Fluorescence Polarization at a given concentrationFloatmP
131FP at 12.5 uM_seventh_point (12.5μM**)Fluorescence Polarization at a given concentrationFloatmP
132FP at 6.25 uM_seventh_point (6.25μM**)Fluorescence Polarization at a given concentrationFloatmP
133FP at 3.125 uM_seventh_point (3.125μM**)Fluorescence Polarization at a given concentrationFloatmP
134FP at 1.5625 uM_seventh_point (1.5625μM**)Fluorescence Polarization at a given concentrationFloatmP
135FP at 0.78125 uM_seventh_point (0.78125μM**)Fluorescence Polarization at a given concentrationFloatmP
136FP at 0.390625 uM_seventh_point (0.390625μM**)Fluorescence Polarization at a given concentrationFloatmP
137FP at 0.1953125 uM_seventh_point (0.195312μM**)Fluorescence Polarization at a given concentrationFloatmP
138FP at 0.097656 uM_seventh_point (0.097656μM**)Fluorescence Polarization at a given concentrationFloatmP
139FP at 0.048828 uM_seventh_point (0.048828μM**)Fluorescence Polarization at a given concentrationFloatmP
140FP at 0.24414 uM_seventh_point (0.24414μM**)Fluorescence Polarization at a given concentrationFloatmP
141FP at 0.12207 uM_seventh_point (0.12207μM**)Fluorescence Polarization at a given concentrationFloatmP
142FP at 0.006104 uM_seventh_point (0.006104μM**)Fluorescence Polarization at a given concentrationFloatmP
143IC50_Qualifier_8This qualifier is to be used with the next TID, IC50_8. If qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that valueString
144IC50_8IC50 value determined using sigmoidal dose response equationFloatμM
145Std.Err(IC50)_8Standard Error of IC50 valueFloatμM
146nH_8Hill coefficient determined using sigmoidal dose response equationFloat
147Excluded_Points_eigth_pointFlags to indicate which of the eigth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
148FP at 100 uM_eigth_point (100μM**)Fluorescence Polarization at a given concentrationFloatmP
149FP at 50 uM_eigth_point (50μM**)Fluorescence Polarization at a given concentrationFloatmP
150FP at 25 uM_eigth_point (25μM**)Fluorescence Polarization at a given concentrationFloatmP
151FP at 12.5 uM_eigth_point (12.5μM**)Fluorescence Polarization at a given concentrationFloatmP
152FP at 6.25 uM_eigth_point (6.25μM**)Fluorescence Polarization at a given concentrationFloatmP
153FP at 3.125 uM_eigth_point (3.125μM**)Fluorescence Polarization at a given concentrationFloatmP
154FP at 1.5625 uM_eigth_point (1.5625μM**)Fluorescence Polarization at a given concentrationFloatmP
155FP at 0.78125 uM_eigth_point (0.78125μM**)Fluorescence Polarization at a given concentrationFloatmP
156FP at 0.390625 uM_eigth_point (0.390625μM**)Fluorescence Polarization at a given concentrationFloatmP
157FP at 0.1953125 uM_eigth_point (0.195312μM**)Fluorescence Polarization at a given concentrationFloatmP
158FP at 0.097656 uM_eight_point (0.097656μM**)Fluorescence Polarization at a given concentrationFloatmP
159FP at 0.048828 uM_eight_point (0.048828μM**)Fluorescence Polarization at a given concentrationFloatmP
160FP at 0.24414 uM_eight_point (0.24414μM**)Fluorescence Polarization at a given concentrationFloatmP
161FP at 0.12207 uM_eight_point (0.12207μM**)Fluorescence Polarization at a given concentrationFloatmP
162FP at 0.006104 uM_eight_point (0.006104μM**)Fluorescence Polarization at a given concentrationFloatmP

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

Data Table (Concise)
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