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BioAssay: AID 2335

SAR analysis of compounds that are cytotoxic to HEK293 revised

The modulation of immune response activity is one of the major goals in the development of novel therapeutics for auto-immune and inflammatory diseases. The innate system resides at the intersection of the pathways of microbial recognition, inflammation, and cell death, thereby offering various therapeutic targets. In this context, NOD1 and NOD2 are of particular interest, since they recognize distinct structures derived from bacterial peptidoglycans and directly activate NF-kB, a central regulator of immune response, inflammation, and apoptosis. ..more
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 Tested Compounds
 Tested Compounds
All(285)
 
 
Active(39)
 
 
Inactive(246)
 
 
 Tested Substances
 Tested Substances
All(304)
 
 
Active(39)
 
 
Inactive(265)
 
 
 Related BioAssays
 Related BioAssays
AID: 2335
Data Source: Burnham Center for Chemical Genomics (BCCG-A282-HEK-293-DryPowder-Assay)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: NIH Molecular Libraries Probe Production Network, Assay Provider
BioAssay Version:
Deposit Date: 2010-02-04
Hold-until Date: 2010-09-02
Modify Date: 2011-01-14

Data Table ( Complete ):           Active    All
BioActive Compounds: 39
Depositor Specified Assays
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AIDNameTypeProbeComment
1566uHTS luminescence assay for the identification of compounds that inhibit NOD2confirmatory
1578uHTS luminescence assay for the identification of compounds that inhibit NOD1confirmatory
1575Summary assay for the identification of compounds that inhibit NOD1summary2 Summary AID.
1579Summary assay for the identification of compounds that inhibit NOD2summary Summary AID.
1848uHTS Fluorescence assay for the identification of cytotoxic compounds among compounds active in NOD2 cell inhibition assayconfirmatory
1849uHTS Fluorescence assay for the identification of cytotoxic compounds among compounds active in NOD1 cell inhibition assayconfirmatory
2001uHTS luminescence assay for the identification of compounds that inhibit NOD2 in MDP treated cellsconfirmatory
2333SAR analysis of compounds that inhibit NOD1 revisedconfirmatory
2466SAR analysis of compounds that inhibit NOD1 - Set 2confirmatory
2469SAR analysis of compounds that are cytotoxic to HEK293 - Set 2confirmatory
2475SAR analysis of compounds that inhibit NOD2 - Set 2confirmatory
2483SAR analysis of inhibitors of TNFa specific NF-kB induction - Set 2confirmatory
2798SAR analysis of compounds that inhibit NOD1 - Set 3confirmatory
2799SAR analysis of compounds that inhibit NOD2 - Set 3confirmatory
2800SAR analysis of compounds that are cytotoxic to HEK293 - Set 3confirmatory
2801SAR analysis of inhibitors of TNFa specific NF-kB induction - Set 3confirmatory
Description:
Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG)
Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA)
Network: NIH Molecular Libraries Probe Production Centers Network (MLPCN)
Grant Number: 1 R03 MH084844-01
Assay Provider: Dr. John C. Reed, Sanford-Burham Medical Research Institute, San Diego CA

The modulation of immune response activity is one of the major goals in the development of novel therapeutics for auto-immune and inflammatory diseases. The innate system resides at the intersection of the pathways of microbial recognition, inflammation, and cell death, thereby offering various therapeutic targets. In this context, NOD1 and NOD2 are of particular interest, since they recognize distinct structures derived from bacterial peptidoglycans and directly activate NF-kB, a central regulator of immune response, inflammation, and apoptosis.

Mutations in the NOD1 and NOD2 genes are associated with a number of human inflammatory disorders, including Crohn's disease (CD), Blau syndrome, early-onset sarcoidosis, and atopic diseases, which characteristically cause constitutive NF-kB activation. Chemical inhibitors of NOD1 and NOD2 would provide powerful research tools for elucidating the roles of these proteins in primary cultured cells from humans and in animal models.

This dose response assay is developed and performed to confirm hits originally identified in "uHTS Fluorescence assay for the identification of cytotoxic compounds among compounds active in NOD1 cell inhibition assay" AID 1849 and "uHTS Fluorescence assay for the identification of cytotoxic compounds" among compounds active in NOD2 cell inhibition assay 1848 and to study the structure-activity relationship on analogs of the confirmed hits. Compounds are either acquired from commercial sources or synthesized internally.

Resazurin detects cell viability by converting from a nonfluorescent dye to the red fluorescent dye resorufin in response to chemical reduction of growth medium resulting from cell growth. Continued cell growth maintains a reduced environment while inhibition of growth maintains an oxidized environment. Reduction related to growth causes the REDOX indicator to change from the oxidized (nonfluorescent, purple color) form to the reduced (fluorescent, red color) form. The fluorescent signal is monitored using 531 nm excitation wavelength and 595 nm emission wavelength.

This assay (AID 2056) could be multiplexed with one or more of the following assays:
1) NOD1, the protocol is described in AID 2072.
2) NOD2, the protocol is described in AID 2054.
3) TNFa, the protocol is described in AID 1980.
Protocol
Protocol:
Assay materials:
1) HEK-293-T NF-kB-Luc cell line obtained from the assay provider's laboratory.
2) gamma-tri-DAP (Ana Spec cat #60774) obtained from assay provider's laboratory.
3) Resazurin (Sigma cat# R7017-5G)

Dose response cytotoxity assay for HEK-293-T NF-kB-Luc cells

(This assay was multiplexed with a NOD1 and NOD2 protocol described in AID 1578 and AID 1566).

Day 1 Procedure

1) Harvest HEK-293-T NFKB-Luc at 100% confluency at 100% confluency
2) Add 1 uL/well NOD assay media with Multidrop
3) Spin down plates at 1000 rpm for 1 min in an Eppendorf 5810 centrifuge.
4) Serial compound dilutions: dispense with Labcyte Echo 550 50 nl total volume 100% DMSO (DPI compounds columns 5-46 & DMSO controls col 1-4, 47-48) to plates from step 2.
5) Add gamma-tri-DAP to cell suspension at 0.75 ug/mL.
6) Seed 13000 cells/well in 4 uL/well to full plate HEK-293-T NFKB-Luc to Corning # 3727 white, 1536, hi-profile, TC-treated plate.
7) Spin down plates @ 500 RPM for 5 min on Eppendorf 5810 centrifuge.
8) Lid Plates. Sandwich 4 plates between 2 lidded 384 plates filled with H2O
9) Wrap plates securely in single layer of Plastic Wrap (Saran Wrap PVDC version).
10) Incubate overnight (14 hours) in 37 oC 5% CO2 incubator

Day 2 Procedure
1) Add 20 nL Resazurin 2.2 mM Resarurin in 50%/50% DMSO/dH20 using HighRes biosolution pintool equipped with V&P Scientific pins.
2) Wrap and incubate plates 1 hr in 37 oC 5% CO2 incubator
3) Top read Fluorescence intensity on Envision. (Bodipy dichroic, 595nM emission, 531nM excitation filter).
Comment
Compounds were tested in 1 or more ranges.

Range1 0-20 uM
Range2 0-5 uM

Compounds are considered active if the IC50_Mean < 20 uM.

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

Activity Scoring
Activity scoring rules were devised to take into consideration compound efficacy, its potential interference with the assay and the screening stage that the data was obtained. Details of the Scoring System will be published elsewhere. Briefly, the outline of the scoring system utilized for the assay is as follows:

1) First tier (0-40 range) is reserved for primary screening data and is not applicable to this assay

2) 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's inhibitory potency and, in addition, provides a measure of the likelihood that the compound is not an artifact based on the available information.
c. The Hill coefficient is taken as a measure of compound behavior in the assay via an additional scaling factor QC:
QC = 2.6*[exp(-0.5*nH^2) - exp(-1.5*nH^2)]
This empirical factor prorates the likelihood of target-specific compound effect vs. its non-specific behavior in the assay. This factor is based on expectation that a compound with a single mode of action that achieved equilibrium in this assay demonstrates the Hill coefficient value of 1. Compounds deviating from that behavior are penalized proportionally to the degree of their deviation.
d. Summary equation that takes into account the items discussed above is
Score = 82 + 3*(pIC50 - 3)*QC,
where pIC50 is a negative log(10) of the IC50 value expressed in mole/L concentration units. This equation results in the Score values above 50 for compounds that demonstrate high potency and predictable behavior. Compounds that are inactive in the assay or whose concentration-dependent behavior are likely to be an artifact of that assay will generally have lower Score values.
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_1_Range1This 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_1_Range1IC50 value determined using sigmoidal dose response equationFloatμM
5Std.Err(IC50)_1_Range1Standard Error of IC50 valueFloatμM
6nH_1_Range1Hill coefficient determined using sigmoidal dose response equationFloatμM
7Excluded_Points_first_point_Range1Flags to indicate which of the first dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
8% Activity at 20 uM_first_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
9% Activity at 10 uM_first_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
10% Activity at 5 uM_first_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
11% Activity at 2.5 uM_first_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
12% Activity at 1.25 uM_first_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
13% Activity at 0.625 uM_first_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
14% Activity at 0.3125 uM_first_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
15% Activity at 0.15625 uM_first_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
16% Activity at 0.078125 uM_first_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
17% Activity at 0.0390625 uM_first_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
18Excluded_Points_second_point_Range1Flags to indicate which of the second dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
19% Activity at 20 uM_second_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
20% Activity at 10 uM_second_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
21% Activity at 5 uM_second_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
22% Activity at 2.5 uM_second_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
23% Activity at 1.25 uM_second_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
24% Activity at 0.625 uM_second_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
25% Activity at 0.3125 uM_second_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
26% Activity at 0.15625 uM_second_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
27% Activity at 0.078125 uM_second_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
28% Activity at 0.0390625 uM_second_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
29IC50_Qualifier_2_Range1This 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
30IC50_2_Range1IC50 value determined using sigmoidal dose response equationFloatμM
31Std.Err(IC50)_2_Range1Standard Error of IC50 valueFloatμM
32nH_2_Range1Hill coefficient determined using sigmoidal dose response equationFloatμM
33Excluded_Points_third_point_Range1Flags to indicate which of the third dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
34% Activity at 20 uM_third_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
35% Activity at 10 uM_third_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
36% Activity at 5 uM_third_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
37% Activity at 2.5 uM_third_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
38% Activity at 1.25 uM_third_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
39% Activity at 0.625 uM_third_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
40% Activity at 0.3125 uM_third_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
41% Activity at 0.15625 uM_third_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
42% Activity at 0.078125 uM_third_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
43% Activity at 0.0390625 uM_third_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
44Excluded_Points_fourth_point_Range1Flags to indicate which of the fourth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
45% Activity at 20 uM_fourth_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
46% Activity at 10 uM_fourth_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
47% Activity at 5 uM_fourth_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
48% Activity at 2.5 uM_fourth_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
49% Activity at 1.25 uM_fourth_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
50% Activity at 0.625 uM_fourth_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
51% Activity at 0.3125 uM_fourth_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
52% Activity at 0.15625 uM_fourth_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
53% Activity at 0.078125 uM_fourth_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
54% Activity at 0.0390625 uM_fourth_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
55IC50_Qualifier_3_Range1This 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
56IC50_3_Range1IC50 value determined using sigmoidal dose response equationFloatμM
57Std.Err(IC50)_3_Range1Standard Error of IC50 valueFloatμM
58nH_3_Range1Hill coefficient determined using sigmoidal dose response equationFloatμM
59Excluded_Points_fifth_point_Range1Flags to indicate which of the fifth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
60% Activity at 20 uM_fifth_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
61% Activity at 10 uM_fifth_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
62% Activity at 5 uM_fifth_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
63% Activity at 2.5 uM_fifth_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
64% Activity at 1.25 uM_fifth_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
65% Activity at 0.625 uM_fifth_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
66% Activity at 0.3125 uM_fifth_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
67% Activity at 0.15625 uM_fifth_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
68% Activity at 0.078125 uM_fifth_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
69% Activity at 0.0390625 uM_fifth_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
70Excluded_Points_sixth_point_Range1Flags to indicate which of the sixth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
71% Activity at 20 uM_sixth_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
72% Activity at 10 uM_sixth_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
73% Activity at 5 uM_sixth_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
74% Activity at 2.5 uM_sixth_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
75% Activity at 1.25 uM_sixth_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
76% Activity at 0.625 uM_sixth_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
77% Activity at 0.3125 uM_sixth_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
78% Activity at 0.15625 uM_sixth_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
79% Activity at 0.078125 uM_sixth_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
80% Activity at 0.0390625 uM_sixth_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
81IC50_Qualifier_4_Range1This 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
82IC50_4_Range1IC50 value determined using sigmoidal dose response equationFloatμM
83Std.Err(IC50)_4_Range1Standard Error of IC50 valueFloatμM
84nH_4_Range1Hill coefficient determined using sigmoidal dose response equationFloatμM
85Excluded_Points_seventh_point_Range1Flags to indicate which of the seventh dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
86% Activity at 20 uM_seventh_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
87% Activity at 10 uM_seventh_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
88% Activity at 5 uM_seventh_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
89% Activity at 2.5 uM_seventh_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
90% Activity at 1.25 uM_seventh_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
91% Activity at 0.625 uM_seventh_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
92% Activity at 0.3125 uM_seventh_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
93% Activity at 0.15625 uM_seventh_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
94% Activity at 0.078125 uM_seventh_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
95% Activity at 0.0390625 uM_seventh_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
96Excluded_Points_eighth_point_Range1Flags to indicate which of the eighth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
97% Activity at 20 uM_eighth_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
98% Activity at 10 uM_eighth_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
99% Activity at 5 uM_eighth_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
100% Activity at 2.5 uM_eighth_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
101% Activity at 1.25 uM_eighth_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
102% Activity at 0.625 uM_eighth_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
103% Activity at 0.3125 uM_eighth_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
104% Activity at 0.15625 uM_eighth_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
105% Activity at 0.078125 uM_eighth_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
106% Activity at 0.0390625 uM_eighth_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
107IC50_Qualifier_5_Range1This 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
108IC50_5_Range1IC50 value determined using sigmoidal dose response equationFloatμM
109Std.Err(IC50)_5_Range1Standard Error of IC50 valueFloatμM
110nH_5_Range1Hill coefficient determined using sigmoidal dose response equationFloatμM
111Excluded_Points_ninth_point_Range1Flags to indicate which of the ninth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
112% Activity at 20 uM_ninth_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
113% Activity at 10 uM_ninth_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
114% Activity at 5 uM_ninth_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
115% Activity at 2.5 uM_ninth_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
116% Activity at 1.25 uM_ninth_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
117% Activity at 0.625 uM_ninth_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
118% Activity at 0.3125 uM_ninth_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
119% Activity at 0.15625 uM_ninth_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
120% Activity at 0.078125 uM_ninth_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
121% Activity at 0.0390625 uM_ninth_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
122Excluded_Points_tenth_point_Range1Flags to indicate which of the tenth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
123% Activity at 20 uM_tenth_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
124% Activity at 10 uM_tenth_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
125% Activity at 5 uM_tenth_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
126% Activity at 2.5 uM_tenth_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
127% Activity at 1.25 uM_tenth_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
128% Activity at 0.625 uM_tenth_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
129% Activity at 0.3125 uM_tenth_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
130% Activity at 0.15625 uM_tenth_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
131% Activity at 0.078125 uM_tenth_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
132% Activity at 0.0390625 uM_tenth_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
133IC50_Qualifier_6_Range1This 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
134IC50_6_Range1IC50 value determined using sigmoidal dose response equationFloatμM
135Std.Err(IC50)_6_Range1Standard Error of IC50 valueFloatμM
136nH_6_Range1Hill coefficient determined using sigmoidal dose response equationFloatμM
137Excluded_Points_eleventh_point_Range1Flags to indicate which of the eleventh dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
138% Activity at 20 uM_eleventh_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
139% Activity at 10 uM_eleventh_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
140% Activity at 5 uM_eleventh_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
141% Activity at 2.5 uM_eleventh_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
142% Activity at 1.25 uM_eleventh_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
143% Activity at 0.625 uM_eleventh_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
144% Activity at 0.3125 uM_eleventh_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
145% Activity at 0.15625 uM_eleventh_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
146% Activity at 0.078125 uM_eleventh_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
147% Activity at 0.0390625 uM_eleventh_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
148Excluded_Points_twelfth_point_Range1Flags to indicate which of the twelfth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
149% Activity at 20 uM_twelfth_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
150% Activity at 10 uM_twelfth_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
151% Activity at 5 uM_twelfth_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
152% Activity at 2.5 uM_twelfth_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
153% Activity at 1.25 uM_twelfth_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
154% Activity at 0.625 uM_twelfth_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
155% Activity at 0.3125 uM_twelfth_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
156% Activity at 0.15625 uM_twelfth_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
157% Activity at 0.078125 uM_twelfth_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
158% Activity at 0.0390625 uM_twelfth_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
159IC50_Qualifier_7_Range1This 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
160IC50_7_Range1IC50 value determined using sigmoidal dose response equationFloatμM
161Std.Err(IC50)_7_Range1Standard Error of IC50 valueFloatμM
162nH_7_Range1Hill coefficient determined using sigmoidal dose response equationFloatμM
163Excluded_Points_thirteenth_point_Range1Flags to indicate which of the thirteenth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
164% Activity at 20 uM_thirteenth_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
165% Activity at 10 uM_thirteenth_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
166% Activity at 5 uM_thirteenth_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
167% Activity at 2.5 uM_thirteenth_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
168% Activity at 1.25 uM_thirteenth_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
169% Activity at 0.625 uM_thirteenth_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
170% Activity at 0.3125 uM_thirteenth_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
171% Activity at 0.15625 uM_thirteenth_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
172% Activity at 0.078125 uM_thirteenth_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
173% Activity at 0.0390625 uM_thirteenth_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
174Excluded_Points_fourteenth_point_Range1Flags to indicate which of the fourteenth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
175% Activity at 20 uM_fourteenth_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
176% Activity at 10 uM_fourteenth_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
177% Activity at 5 uM_fourteenth_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
178% Activity at 2.5 uM_fourteenth_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
179% Activity at 1.25 uM_fourteenth_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
180% Activity at 0.625 uM_fourteenth_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
181% Activity at 0.3125 uM_fourteenth_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
182% Activity at 0.15625 uM_fourteenth_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
183% Activity at 0.078125 uM_fourteenth_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
184% Activity at 0.0390625 uM_fourteenth_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
185Excluded_Points_fifteenth_point_Range1Flags to indicate which of the fifteenth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
186% Activity at 20 uM_fifteenth_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
187% Activity at 10 uM_fifteenth_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
188% Activity at 5 uM_fifteenth_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
189% Activity at 2.5 uM_fifteenth_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
190% Activity at 1.25 uM_fifteenth_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
191% Activity at 0.625 uM_fifteenth_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
192% Activity at 0.3125 uM_fifteenth_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
193% Activity at 0.15625 uM_fifteenth_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
194% Activity at 0.078125 uM_fifteenth_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
195% Activity at 0.0390625 uM_fifteenth_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
196Excluded_Points_sixteenth_point_Range1Flags to indicate which of the sixteenth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
197% Activity at 20 uM_sixteenth_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
198% Activity at 10 uM_sixteenth_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
199% Activity at 5 uM_sixteenth_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
200% Activity at 2.5 uM_sixteenth_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
201% Activity at 1.25 uM_sixteenth_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
202% Activity at 0.625 uM_sixteenth_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
203% Activity at 0.3125 uM_sixteenth_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
204% Activity at 0.15625 uM_sixteenth_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
205% Activity at 0.078125 uM_sixteenth_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
206% Activity at 0.0390625 uM_sixteenth_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
207IC50_Qualifier_8_Range1This 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
208IC50_8_Range1IC50 value determined using sigmoidal dose response equationFloatμM
209Std.Err(IC50)_8_Range1Standard Error of IC50 valueFloatμM
210nH_8_Range1Hill coefficient determined using sigmoidal dose response equationFloatμM
211Excluded_Points_seventeenth_point_Range1Flags to indicate which of the seventeenth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
212% Activity at 20 uM_seventeenth_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
213% Activity at 10 uM_seventeenth_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
214% Activity at 5 uM_seventeenth_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
215% Activity at 2.5 uM_seventeenth_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
216% Activity at 1.25 uM_seventeenth_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
217% Activity at 0.625 uM_seventeenth_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
218% Activity at 0.3125 uM_seventeenth_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
219% Activity at 0.15625 uM_seventeenth_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
220% Activity at 0.078125 uM_seventeenth_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
221% Activity at 0.0390625 uM_seventeenth_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
222Excluded_Points_eighteenth_point_Range1Flags to indicate which of the eighteenth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
223% Activity at 20 uM_eighteenth_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
224% Activity at 10 uM_eighteenth_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
225% Activity at 5 uM_eighteenth_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
226% Activity at 2.5 uM_eighteenth_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
227% Activity at 1.25 uM_eighteenth_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
228% Activity at 0.625 uM_eighteenth_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
229% Activity at 0.3125 uM_eighteenth_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
230% Activity at 0.15625 uM_eighteenth_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
231% Activity at 0.078125 uM_eighteenth_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
232% Activity at 0.0390625 uM_eighteenth_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
233Excluded_Points_nineteenth_point_Range1Flags to indicate which of the nineteenth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
234% Activity at 20 uM_nineteenth_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
235% Activity at 10 uM_nineteenth_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
236% Activity at 5 uM_nineteenth_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
237% Activity at 2.5 uM_nineteenth_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
238% Activity at 1.25 uM_nineteenth_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
239% Activity at 0.625 uM_nineteenth_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
240% Activity at 0.3125 uM_nineteenth_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
241% Activity at 0.15625 uM_nineteenth_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
242% Activity at 0.078125 uM_nineteenth_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
243% Activity at 0.0390625 uM_nineteenth_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
244Excluded_Points_twentieth_point_Range1Flags to indicate which of the twentieth dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.String
245% Activity at 20 uM_twentieth_point_Range1 (20μM**)% Inhibition at a given concentrationFloat%
246% Activity at 10 uM_twentieth_point_Range1 (10μM**)% Inhibition at a given concentrationFloat%
247% Activity at 5 uM_twentieth_point_Range1 (5μM**)% Inhibition at a given concentrationFloat%
248% Activity at 2.5 uM_twentieth_point_Range1 (2.5μM**)% Inhibition at a given concentrationFloat%
249% Activity at 1.25 uM_twentieth_point_Range1 (1.25μM**)% Inhibition at a given concentrationFloat%
250% Activity at 0.625 uM_twentieth_point_Range1 (0.625μM**)% Inhibition at a given concentrationFloat%
251% Activity at 0.3125 uM_twentieth_point_Range1 (0.3125μM**)% Inhibition at a given concentrationFloat%
252% Activity at 0.15625 uM_twentieth_point_Range1 (0.15625μM**)% Inhibition at a given concentrationFloat%
253% Activity at 0.078125 uM_twentieth_point_Range1 (0.078125μM**)% Inhibition at a given concentrationFloat%
254% Activity at 0.0390625 uM_twentieth_point_Range1 (0.0390625μM**)% Inhibition at a given concentrationFloat%
255IC50_Qualifier_1_Range2This 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
256IC50_1_Range2IC50 value determined using sigmoidal dose response equationFloatμM
257Std.Err(IC50)_1_Range2Standard Error of IC50 valueFloatμM
258nH_1_Range2Hill coefficient determined using sigmoidal dose response equationFloatμM
259Excluded_Points_first_point_Range2Flags 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
260% Activity at 5 uM_first_point_Range2 (5μM**)% Inhibition at a given concentrationFloat%
261% Activity at 2.5 uM_first_point_Range2 (2.5μM**)% Inhibition at a given concentrationFloat%
262% Activity at 1.25 uM_first_point_Range2 (1.25μM**)% Inhibition at a given concentrationFloat%
263% Activity at 0.625 uM_first_point_Range2 (0.625μM**)% Inhibition at a given concentrationFloat%
264% Activity at 0.3125 uM_first_point_Range2 (0.3125μM**)% Inhibition at a given concentrationFloat%
265% Activity at 0.15625 uM_first_point_Range2 (0.15625μM**)% Inhibition at a given concentrationFloat%
266% Activity at 0.078125 uM_first_point_Range2 (0.078125μM**)% Inhibition at a given concentrationFloat%
267% Activity at 0.0390625 uM_first_point_Range2 (0.0390625μM**)% Inhibition at a given concentrationFloat%
268% Activity at 0.01953125 uM_first_point_Range2 (0.0195312μM**)% Inhibition at a given concentrationFloat%
269% Activity at 0.009765625 uM_first_point_Range2 (0.00976562μM**)% Inhibition at a given concentrationFloat%
270Excluded_Points_second_point_Range2Flags 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
271% Activity at 5 uM_second_point_Range2 (5μM**)% Inhibition at a given concentrationFloat%
272% Activity at 2.5 uM_second_point_Range2 (2.5μM**)% Inhibition at a given concentrationFloat%
273% Activity at 1.25 uM_second_point_Range2 (1.25μM**)% Inhibition at a given concentrationFloat%
274% Activity at 0.625 uM_second_point_Range2 (0.625μM**)% Inhibition at a given concentrationFloat%
275% Activity at 0.3125 uM_second_point_Range2 (0.3125μM**)% Inhibition at a given concentrationFloat%
276% Activity at 0.15625 uM_second_point_Range2 (0.15625μM**)% Inhibition at a given concentrationFloat%
277% Activity at 0.078125 uM_second_point_Range2 (0.078125μM**)% Inhibition at a given concentrationFloat%
278% Activity at 0.0390625 uM_second_point_Range2 (0.0390625μM**)% Inhibition at a given concentrationFloat%
279% Activity at 0.01953125 uM_second_point_Range2 (0.0195312μM**)% Inhibition at a given concentrationFloat%
280% Activity at 0.009765625 uM_second_point_Range2 (0.00976562μM**)% Inhibition at a given concentrationFloat%
281IC50_Qualifier_2_Range2This 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
282IC50_2_Range2IC50 value determined using sigmoidal dose response equationFloatμM
283Std.Err(IC50)_2_Range2Standard Error of IC50 valueFloatμM
284nH_2_Range2Hill coefficient determined using sigmoidal dose response equationFloatμM
285Excluded_Points_third_point_Range2Flags 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
286% Activity at 5 uM_third_point_Range2 (5μM**)% Inhibition at a given concentrationFloat%
287% Activity at 2.5 uM_third_point_Range2 (2.5μM**)% Inhibition at a given concentrationFloat%
288% Activity at 1.25 uM_third_point_Range2 (1.25μM**)% Inhibition at a given concentrationFloat%
289% Activity at 0.625 uM_third_point_Range2 (0.625μM**)% Inhibition at a given concentrationFloat%
290% Activity at 0.3125 uM_third_point_Range2 (0.3125μM**)% Inhibition at a given concentrationFloat%
291% Activity at 0.15625 uM_third_point_Range2 (0.15625μM**)% Inhibition at a given concentrationFloat%
292% Activity at 0.078125 uM_third_point_Range2 (0.078125μM**)% Inhibition at a given concentrationFloat%
293% Activity at 0.0390625 uM_third_point_Range2 (0.0390625μM**)% Inhibition at a given concentrationFloat%
294% Activity at 0.01953125 uM_third_point_Range2 (0.0195312μM**)% Inhibition at a given concentrationFloat%
295% Activity at 0.009765625 uM_third_point_Range2 (0.00976562μM**)% Inhibition at a given concentrationFloat%
296Excluded_Points_fourth_point_Range2Flags 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
297% Activity at 5 uM_fourth_point_Range2 (5μM**)% Inhibition at a given concentrationFloat%
298% Activity at 2.5 uM_fourth_point_Range2 (2.5μM**)% Inhibition at a given concentrationFloat%
299% Activity at 1.25 uM_fourth_point_Range2 (1.25μM**)% Inhibition at a given concentrationFloat%
300% Activity at 0.625 uM_fourth_point_Range2 (0.625μM**)% Inhibition at a given concentrationFloat%
301% Activity at 0.3125 uM_fourth_point_Range2 (0.3125μM**)% Inhibition at a given concentrationFloat%
302% Activity at 0.15625 uM_fourth_point_Range2 (0.15625μM**)% Inhibition at a given concentrationFloat%
303% Activity at 0.078125 uM_fourth_point_Range2 (0.078125μM**)% Inhibition at a given concentrationFloat%
304% Activity at 0.0390625 uM_fourth_point_Range2 (0.0390625μM**)% Inhibition at a given concentrationFloat%
305% Activity at 0.01953125 uM_fourth_point_Range2 (0.0195312μM**)% Inhibition at a given concentrationFloat%
306% Activity at 0.009765625 uM_fourth_point_Range2 (0.00976562μM**)% Inhibition at a given concentrationFloat%

* Activity Concentration. ** Test Concentration.
Additional Information
Grant Number: 1 R03 MH084844-01

Data Table (Concise)
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