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BioAssay: AID 1666

SAR assay for compounds that inhibit PHOSPHO1

Mineralization of cartilage and bone occurs by a series of physicochemical and biochemical processes that together facilitate the deposition of hydroxyapatite (HA) in specific areas of the extracellular matrix (ECM). Experimental evidence has pointed to the presence of HA crystals along collagen fibrils in the ECM and also within the lumen of chondroblast- and osteoblast-derived matrix vesicles more ..
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 Tested Compounds
 Tested Compounds
All(69)
 
 
Active(27)
 
 
Inactive(42)
 
 
 Tested Substances
 Tested Substances
All(71)
 
 
Active(28)
 
 
Inactive(43)
 
 
AID: 1666
Data Source: Burnham Center for Chemical Genomics (BCCG-A185-Phospho1-Absorbance-DryPowder)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2009-04-07
Modify Date: 2011-01-19

Data Table ( Complete ):           Active    All
Target
BioActive Compounds: 27
Depositor Specified Assays
AIDNameTypeComment
1545Summary - Compounds inhibiting phosphomannose isomerase (PMI) via a fluorescence intensity assay.summary
1565uHTS absorbance assay for the identification of compounds that inhibit PHOSPHO1confirmatory
1574Summary assay for the identification of compounds that inhibit PHOSPHO1summary
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 MH084086-01
Assay Provider: Dr. Jose Luis Milan, Sanford-Burnham Medical Research Institute, San Diego CA

Mineralization of cartilage and bone occurs by a series of physicochemical and biochemical processes that together facilitate the deposition of hydroxyapatite (HA) in specific areas of the extracellular matrix (ECM). Experimental evidence has pointed to the presence of HA crystals along collagen fibrils in the ECM and also within the lumen of chondroblast- and osteoblast-derived matrix vesicles (MVs). Dr. Milan's working model is that bone mineralization is first initiated within the lumen of MVs. In a second step, HA crystals grow beyond the confines of the MVs and become exposed to the extracellular milieu where they continue to propagate along collagen fibrils. Recent data have indicated that tissue-nonspecific alkaline phosphatase (TNAP) plays a crucial role in restricting the concentration of extracellular inorganic pyrophosphate (PP), a mineralization inhibitor, to maintain a P/PPi ratio permissive for normal bone mineralization. Using a variety of single and double gene knockout experiments it has been found that mice deficient in TNAP function, i.e., Akp2-/- mice, display osteomalacia due to an arrest in the propagation of HA crystals outside the MVs caused by an increase in extracellular PPi concentrations. Inside the MVs, however, HA crystals are still present in Akp2-/- mice. It is hypothesize that a newly identified soluble phosphatase, PHOSPHO1, with specificity for phosphoethanolamine (PEA) and phosphoserine (PS) present in the MVs, is responsible for increasing the local concentration of Pi inside the MVs to change the P/PPi ratio to favor precipitation of HA seed crystals.

This biochemical assay employs a colorimetric readout based on the enzyme's ability to liberate phosphate from phosphoethanolamine and its reaction with Biomol Green reagent.

This dose response assay is developed and performed to confirm hits originally identified in "uHTS absorbance assay for the identification of compounds that inhibit PHOSPHO1" (AID 1565) and to study the structure-activity relationship on analogs of the confirmed hits. Compounds are either acquired from commercial sources or synthesized internally.
Protocol
Assay materials:
1) POSPHO1 was obtained from the assay provider's laboratory.
2) Assay Buffer: 20mM MES-NaOH pH 6.7, 2mM MgCl2, 0.0125% Tween-20, 0.01% BSA

Procedure
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. 2 uL of compounds in 10% DMSO were transferred into columns 3-22 of Greiner 384-well white small-volume plates (784075). Each curve was performed in duplicate.
2) Columns 1-2 and 23-24 contained 4 uL of NC and PC solutions, respectively.
For the following additions, using the Multidrop sterilizing the tubing with copious amounts of water and 70% EtOH before and after each reagent.
3) Add 9 uL of buffer to columns 1-2.
4) Add 9 uL PHOSPHO1 intermediate solution to columns 3-24.
5) Add 9 uL of PEA intermediate solution to the entire plate (columns 1-24).
6) Spin plate down to maintain an even level of volume.
7) Incubate plate at room temperature for 1 hr (covered).
8) Add 20 uL of Biomol Green to the entire plate (columns 1-24).
9) Spin plate down to maintain an even level of volume.
10) Incubate plate for 30 mins to allow Biomol signal to develop.
11) Read plate on a Perkin Elmer Viewlux at 630nm in absorbance mode
Comment
The compounds were tested in 1 or more concentration ranges.

Range1 0-1 uM
Range2 0-100 uM
Range3 0-10 uM
Range4 0-50 uM
Range5 0-0.5 uM

For all samples in each range that resolved to an IC50 the results were averaged and reported as IC50_Range. Also the IC50 results for all of the ranges were averaged to produce IC50_Mean. Compounds with an IC50_Mean < 1 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 Phospho1 assay is as follows:
1) First tier (0-40 range) is reserved for primary screening data and is not applicable to this assay
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 the Phospho1 inhibition activation assay demonstrates the Hill coefficient value of 1. Compounds deviating from that behavior are penalized proportionally to the degree of their deviation.
d. Summary equation that takes into account the items discussed above is
Score = 82 + 3*(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. 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. If the qualifier is "<", the IC50 result is smaller than that valueString
2IC50_Mean*IC50 value determined using sigmoidal dose response equationFloatμM
3IC50_Qualifier_Range1This qualifier is to be used with the next TID, IC50. 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. If the qualifier is "<", the IC50 result is smaller than that valueString
4IC50_Range1IC50 value determined using sigmoidal dose response equationFloatμM
5Std.Err(IC50)_Range1Standard Error of IC50 valueFloat
6nH_Range1Hill coefficient determined using sigmoidal dose response equationFloat
7Excluded_Points_first_point_Range1Flags to indicate which of the first dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
8% inhibition at 1 uM_first_point_Range1 (1μM**)% inhibition at a given concentrationFloat%
9% inhibition at 0.5 uM_first_point_Range1 (0.5μM**)% inhibition at a given concentrationFloat%
10% inhibition at 0.25 uM_first_point_Range1 (0.25μM**)% inhibition at a given concentrationFloat%
11% inhibition at 0.125 uM_first_point_Range1 (0.125μM**)% inhibition at a given concentrationFloat%
12% inhibition at 0.0625 uM_first_point_Range1 (0.0625μM**)% inhibition at a given concentrationFloat%
13% inhibition at 0.03125 uM_first_point_Range1 (0.03125μM**)% inhibition at a given concentrationFloat%
14% inhibition at 0.015625 uM_first_point_Range1 (0.015625μM**)% inhibition at a given concentrationFloat%
15% inhibition at 0.0078125 uM_first_point_Range1 (0.0078125μM**)% inhibition at a given concentrationFloat%
16% inhibition at 0.00390625 uM_first_point_Range1 (0.00390625μM**)% inhibition at a given concentrationFloat%
17% inhibition at 0.001953125 uM_first_point_Range1 (0.00195312μM**)% 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 (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
19% inhibition at 1 uM_second_point_Range1 (1μM**)% inhibition at a given concentrationFloat%
20% inhibition at 0.5 uM_second_point_Range1 (0.5μM**)% inhibition at a given concentrationFloat%
21% inhibition at 0.25 uM_second_point_Range1 (0.25μM**)% inhibition at a given concentrationFloat%
22% inhibition at 0.125 uM_second_point_Range1 (0.125μM**)% inhibition at a given concentrationFloat%
23% inhibition at 0.0625 uM_second_point_Range1 (0.0625μM**)% inhibition at a given concentrationFloat%
24% inhibition at 0.03125 uM_second_point_Range1 (0.03125μM**)% inhibition at a given concentrationFloat%
25% inhibition at 0.015625 uM_second_point_Range1 (0.015625μM**)% inhibition at a given concentrationFloat%
26% inhibition at 0.0078125 uM_second_point_Range1 (0.0078125μM**)% inhibition at a given concentrationFloat%
27% inhibition at 0.00390625 uM_second_point_Range1 (0.00390625μM**)% inhibition at a given concentrationFloat%
28% inhibition at 0.001953125 uM_second_point_Range1 (0.00195312μM**)% inhibition at a given concentrationFloat%
29Excluded_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
30% inhibition at 1 uM_third_point_Range1 (1μM**)% inhibition at a given concentrationFloat%
31% inhibition at 0.5 uM_third_point_Range1 (0.5μM**)% inhibition at a given concentrationFloat%
32% inhibition at 0.25 uM_third_point_Range1 (0.25μM**)% inhibition at a given concentrationFloat%
33% inhibition at 0.125 uM_third_point_Range1 (0.125μM**)Float%
34% inhibition at 0.0625 uM_third_point_Range1 (0.0625μM**)% inhibition at a given concentrationFloat%
35% inhibition at 0.03125 uM_third_point_Range1 (0.03125μM**)% inhibition at a given concentrationFloat%
36% inhibition at 0.015625 uM_third_point_Range1 (0.015625μM**)% inhibition at a given concentrationFloat%
37% inhibition at 0.0078125 uM_third_point_Range1 (0.0078125μM**)% inhibition at a given concentrationFloat%
38% inhibition at 0.00390625 uM_third_point_Range1 (0.00390625μM**)% inhibition at a given concentrationFloat%
39% inhibition at 0.001953125 uM_third_point_Range1 (0.00195312μM**)% inhibition at a given concentrationFloat%
40Excluded_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
41% inhibition at 1 uM_fourth_point_Range1 (1μM**)% inhibition at a given concentrationFloat%
42% inhibition at 0.5 uM_fourth_point_Range1 (0.5μM**)% inhibition at a given concentrationFloat%
43% inhibition at 0.25 uM_fourth_point_Range1 (0.25μM**)% inhibition at a given concentrationFloat%
44% inhibition at 0.125 uM_fourth_point_Range1 (0.125μM**)% inhibition at a given concentrationFloat%
45% inhibition at 0.0625 uM_fourth_point_Range1 (0.0625μM**)% inhibition at a given concentrationFloat%
46% inhibition at 0.03125 uM_fourth_point_Range1 (0.03125μM**)% inhibition at a given concentrationFloat%
47% inhibition at 0.015625 uM_fourth_point_Range1 (0.015625μM**)% inhibition at a given concentrationFloat%
48% inhibition at 0.0078125 uM_fourth_point_Range1 (0.0078125μM**)% inhibition at a given concentrationFloat%
49% inhibition at 0.00390625 uM_fourth_point_Range1 (0.00390625μM**)% inhibition at a given concentrationFloat%
50% inhibition at 0.001953125 uM_fourth_point_Range1 (0.00195312μM**)% inhibition at a given concentrationFloat%
51IC50_Qualifier_Range2This qualifier is to be used with the next TID, IC50. 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. If the qualifier is "<", the IC50 result is smaller than that valueString
52IC50_Range2IC50 value determined using sigmoidal dose response equationFloat
53Std.Err(IC50)_Range2Standard Error of IC50 valueFloat
54nH_Range2Hill coefficient determined using sigmoidal dose response equationFloat
55Excluded_Points_first_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
56% inhibition at 100 uM_first_point_Range2 (100μM**)% inhibition at a given concentrationFloat%
57% inhibition at 50 uM_first_point_Range2 (50μM**)% inhibition at a given concentrationFloat%
58% inhibition at 25 uM_first_point_Range2 (25μM**)% inhibition at a given concentrationFloat%
59% inhibition at 12.5 uM_first_point_Range2 (12.5μM**)% inhibition at a given concentrationFloat%
60% inhibition at 6.25 uM_first_point_Range2 (6.35μM**)% inhibition at a given concentrationFloat%
61% inhibition at 3.125 uM_first_point_Range2 (3.125μM**)% inhibition at a given concentrationFloat%
62% inhibition at 1.5625 uM_first_point_Range2 (1.5625μM**)% inhibition at a given concentrationFloat%
63% inhibition at 0.78125 uM_first_point_Range2 (0.78125μM**)% inhibition at a given concentrationFloat%
64% inhibition at 0.390625 uM_first_point_Range2 (0.390625μM**)% inhibition at a given concentrationFloat%
65% inhibition at 0.1953125 uM_first_point_Range2 (0.195312μM**)% inhibition at a given concentrationFloat%
66Excluded_Points_second_point_Range2String
67% inhibition at 100 uM_second_point_Range2 (100μM**)Float%
68% inhibition at 50 uM_second_point_Range2 (50μM**)Float%
69% inhibition at 25 uM_second_point_Range2 (25μM**)Float%
70% inhibition at 12.5 uM_second_point_Range2 (12.5μM**)Float%
71% inhibition at 6.25 uM_second_point_Range2 (6.25μM**)Float%
72% inhibition at 3.125 uM_second_point_Range2 (3.125μM**)Float%
73% inhibition at 1.5625 uM_second_point_Range2 (1.5625μM**)Float%
74% inhibition at 0.78125 uM_second_point_Range2 (0.78125μM**)Float%
75% inhibition at 0.390625 uM_second_point_Range2 (0.390625μM**)Float%
76% inhibition at 0.1953125 uM_second_point_Range2 (0.195312μM**)Float%
77Excluded_Points_third_point_Range2String
78% inhibition at 100 uM_third_point_Range2 (100μM**)Float%
79% inhibition at 50 uM_third_point_Range2 (50μM**)Float%
80% inhibition at 25 uM_third_point_Range2 (25μM**)Float%
81% inhibition at 12.5 uM_third_point_Range2 (12.5μM**)Float%
82% inhibition at 6.25 uM_third_point_Range2 (6.25μM**)Float%
83% inhibition at 3.125 uM_third_point_Range2 (3.125μM**)Float%
84% inhibition at 1.5625 uM_third_point_Range2 (1.5625μM**)Float%
85% inhibition at 0.78125 uM_third_point_Range2 (0.78125μM**)Float%
86% inhibition at 0.390625 uM_third_point_Range2 (0.390625μM**)Float%
87% inhibition at 0.1953125 uM_third_point_Range2 (0.195312μM**)Float%
88Excluded_Points_fourth_point_Range2String
89% inhibition at 100 uM_fourth_point_Range2 (100μM**)Float%
90% inhibition at 50 uM_fourth_point_Range2 (50μM**)Float%
91% inhibition at 25 uM_fourth_point_Range2 (25μM**)Float%
92% inhibition at 12.5 uM_fourth_point_Range2 (12.5μM**)Float%
93% inhibition at 6.25 uM_fourth_point_Range2 (6.25μM**)Float%
94% inhibition at 3.125 uM_fourth_point_Range2 (3.125μM**)Float%
95% inhibition at 1.5625 uM_fourth_point_Range2 (1.5625μM**)Float%
96% inhibition at 0.78125 uM_fourth_point_Range2 (0.78125μM**)Float%
97% inhibition at 0.390625 uM_fourth_point_Range2 (0.390625μM**)Float%
98% inhibition at 0.1953125 uM_fourth_point_Range2 (0.193125μM**)Float%
99IC50_Qualifier_Range3String
100IC50_Range3FloatμM
101Std.Err(IC50)_Range3Float
102nH_Range3Float
103Excluded_Points_first_point_Range3String
104% inhibition at 10 uM_first_point_Range3 (10μM**)Float%
105% inhibition at 5 uM_first_point_Range3 (5μM**)Float%
106% inhibition at 2.5 uM_first_point_Range3 (2.5μM**)Float%
107% inhibition at 1.25 uM_first_point_Range3 (1.25μM**)Float%
108% inhibition at 0.625 uM_first_point_Range3 (0.625μM**)Float%
109% inhibition at 0.3125 uM_first_point_Range3 (0.3125μM**)Float%
110% inhibition at 0.15625 uM_first_point_Range3 (0.15625μM**)Float%
111% inhibition at 0.078125 uM_first_point_Range3 (0.078125μM**)Float%
112% inhibition at 0.0390625 uM_first_point_Range3 (0.0390625μM**)Float%
113% inhibition at 0.01953125 uM_first_point_Range3 (0.0195312μM**)Float%
114Excluded_Points_second_point_Range3String
115% inhibition at 10 uM_second_point_Range3 (10μM**)Float%
116% inhibition at 5 uM_second_point_Range3 (5μM**)Float%
117% inhibition at 2.5 uM_second_point_Range3 (2.5μM**)Float%
118% inhibition at 1.25 uM_second_point_Range3 (1.25μM**)Float%
119% inhibition at 0.625 uM_second_point_Range3 (0.625μM**)Float%
120% inhibition at 0.3125 uM_second_point_Range3 (0.3125μM**)Float%
121% inhibition at 0.15625 uM_second_point_Range3 (0.15625μM**)Float%
122% inhibition at 0.078125 uM_second_point_Range3 (0.078125μM**)Float%
123% inhibition at 0.0390625 uM_second_point_Range3 (0.0390625μM**)Float%
124% inhibition at 0.01953125 uM_second_point_Range3 (0.0195312μM**)Float%
125Excluded_Points_third_point_Range3String
126% inhibition at 10 uM_third_point_Range3 (10μM**)Float%
127% inhibition at 5 uM_third_point_Range3 (5μM**)Float%
128% inhibition at 2.5 uM_third_point_Range3 (2.6μM**)Float%
129% inhibition at 1.25 uM_third_point_Range3 (1.25μM**)Float%
130% inhibition at 0.625 uM_third_point_Range3 (0.625μM**)Float%
131% inhibition at 0.3125 uM_third_point_Range3 (0.3125μM**)Float%
132% inhibition at 0.15625 uM_third_point_Range3 (0.15625μM**)Float%
133% inhibition at 0.078125 uM_third_point_Range3 (0.078125μM**)Float%
134% inhibition at 0.0390625 uM_third_point_Range3 (0.0390625μM**)Float%
135% inhibition at 0.01953125 uM_third_point_Range3 (0.0195312μM**)Float%
136Excluded_Points_fourth_point_Range3String
137% inhibition at 10 uM_fourth_point_Range3 (10μM**)Float%
138% inhibition at 5 uM_fourth_point_Range3 (5μM**)Float%
139% inhibition at 2.5 uM_fourth_point_Range3 (2.5μM**)Float%
140% inhibition at 1.25 uM_fourth_point_Range3 (1.25μM**)Float%
141% inhibition at 0.625 uM_fourth_point_Range3 (0.625μM**)Float%
142% inhibition at 0.3125 uM_fourth_point_Range3 (0.3125μM**)Float%
143% inhibition at 0.15625 uM_fourth_point_Range3 (0.15625μM**)Float%
144% inhibition at 0.078125 uM_fourth_point_Range3 (0.078125μM**)Float%
145% inhibition at 0.0390625 uM_fourth_point_Range3 (0.0390625μM**)Float%
146% inhibition at 0.01953125 uM_fourth_point_Range3 (0.0195312μM**)Float%
147IC50_Qualifier_Range4String
148IC50_Range4FloatμM
149Std.Err(IC50)_Range4Float
150nH_Range4Float
151Excluded_Points_first_point_Range4String
152% inhibition at 50 uM_first_point_Range4 (50μM**)Float%
153% inhibition at 25 uM_first_point_Range4 (25μM**)Float%
154% inhibition at 12.5 uM_first_point_Range4 (12.5μM**)Float%
155% inhibition at 6.25 uM_first_point_Range4 (6.25μM**)Float%
156% inhibition at 3.125 uM_first_point_Range4 (3.125μM**)Float%
157% inhibition at 1.5625 uM_first_point_Range4 (1.5625μM**)Float%
158% inhibition at 0.78125 uM_first_point_Range4 (0.78125μM**)Float%
159% inhibition at 0.390625 uM_first_point_Range4 (0.390625μM**)Float%
160% inhibition at 0.1953125 uM_first_point_Range4 (0.195312μM**)Float%
161% inhibition at 0.09765625 uM_first_point_Range4 (0.0976562μM**)Float%
162Excluded_Points_second_point_Range4String
163% inhibition at 50 uM_second_point_Range4 (50μM**)Float%
164% inhibition at 25 uM_second_point_Range4 (25μM**)Float%
165% inhibition at 12.5 uM_second_point_Range4 (12.5μM**)Float%
166% inhibition at 6.25 uM_second_point_Range4 (6.25μM**)Float%
167% inhibition at 3.125 uM_second_point_Range4 (3.125μM**)Float%
168% inhibition at 1.5625 uM_second_point_Range4 (1.5625μM**)Float%
169% inhibition at 0.78125 uM_second_point_Range4 (0.78125μM**)Float%
170% inhibition at 0.390625 uM_second_point_Range4 (0.390625μM**)Float%
171% inhibition at 0.1953125 uM_second_point_Range4 (0.195312μM**)Float%
172% inhibition at 0.09765625 uM_second_point_Range4 (0.0976562μM**)Float%
173IC50_Qualifier_Range5String
174IC50_Range5FloatμM
175Std.Err(IC50)_Range5Float
176nH_Range5Float
177Excluded_Points_first_point_Range5String
178% inhibition at 0.5 uM_first_point_Range5 (0.5μM**)Float%
179% inhibition at 0.25 uM_first_point_Range5 (0.25μM**)Float%
180% inhibition at 0.125 uM_first_point_Range5 (0.125μM**)Float%
181% inhibition at 0.0625 uM_first_point_Range5 (0.0625μM**)Float%
182% inhibition at 0.03125 uM_first_point_Range5 (0.03125μM**)Float%
183% inhibition at 0.015625 uM_first_point_Range5 (0.015625μM**)Float%
184% inhibition at 0.0078125 uM_first_point_Range5 (0.0078125μM**)Float%
185% inhibition at 0.00390625 uM_first_point_Range5 (0.00390625μM**)Float%
186% inhibition at 0.001953125 uM_first_point_Range5 (0.00195312μM**)Float%
187% inhibition at 0.0009765625 uM_first_point_Range5 (0.000976562μM**)Float%
188Excluded_Points_second_point_Range5String
189% inhibition at 0.5 uM_second_point_Range5 (0.5μM**)Float%
190% inhibition at 0.25 uM_second_point_Range5 (0.25μM**)Float%
191% inhibition at 0.125 uM_second_point_Range5 (0.125μM**)Float%
192% inhibition at 0.0625 uM_second_point_Range5 (0.0625μM**)Float%
193% inhibition at 0.03125 uM_second_point_Range5 (0.03125μM**)Float%
194% inhibition at 0.015625 uM_second_point_Range5 (0.015625μM**)Float%
195% inhibition at 0.0078125 uM_second_point_Range5 (0.0078125μM**)Float%
196% inhibition at 0.00390625 uM_second_point_Range5 (0.00390625μM**)Float%
197% inhibition at 0.001953125 uM_second_point_Range5 (0.00195312μM**)Float%
198% inhibition at 0.0009765625 uM_second_point_Range5 (0.000976562μM**)Float%

* Activity Concentration. ** Test Concentration.
Additional Information
Grant Number: R03 MH084086-01

Data Table (Concise)
Classification
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