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BioAssay: AID 1655

Counter screen SAR assay for PMM2 inhibitors via a fluorescence intensity assay

Congenital Disorders of Glycosylation (CDGs) are rare genetic disorders in the synthesis of N-linked glycan chains. Mutations in PMM2, encoding phosphomannomutase 2 (PMM2, Man-6-P-> Man-1-P) cause the most common form, CDG-Ia. Patients have a host of problems including hypotonia, variable psychomotor retardation, seizures, peripheral neuropathy, cardiomyopathy, and protein losing enteropathy. more ..
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 Tested Compounds
 Tested Compounds
All(175)
 
 
Active(49)
 
 
Inactive(127)
 
 
 Tested Substances
 Tested Substances
All(178)
 
 
Active(51)
 
 
Inactive(127)
 
 
AID: 1655
Data Source: Burnham Center for Chemical Genomics (BCCG-A180-PMM2-Fluorescence-Assay)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2009-04-03
Modify Date: 2011-01-19

Data Table ( Complete ):           View Active Data    View All Data
Target
BioActive Compounds: 49
Related Experiments
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AIDNameTypeProbeComment
1545Summary - Compounds inhibiting phosphomannose isomerase (PMI) via a fluorescence intensity assay.Summary2 depositor-specified cross reference
1574Summary assay for the identification of compounds that inhibit PHOSPHO1Summary1 depositor-specified cross reference
1020Counter Screen for Glucose-6-Phosphate Dehydrogenase-based Primary AssayScreening same project related to Summary assay
1209HTS identification of compounds inhibiting phosphomannose isomerase (PMI) via a fluorescence intensity assay.Confirmatory same project related to Summary assay
1217uHTS Identification of Diaphorase Inhibitors and Chemcical Oxidizers: Counter Screen for Diaphorase-based Primary AssaysScreening same project related to Summary assay
1220HTS identification of compounds inhibiting phosphomannose isomerase (PMI) via a fluorescence intensity assay using a high concentration of mannose 6-phosphateConfirmatory same project related to Summary assay
1535Confirmation of compounds inhibiting phosphomannose isomerase (PMI) via a fluorescence intensity assay.Confirmatory same project related to Summary assay
1536Confirmation of compounds inhibiting phosphomannose isomerase (PMI) via a fluorescence intensity assay using a high concentration of mannose 6-phosphate.Confirmatory same project related to Summary assay
1553Screening for Phosphomannose Isomerase inhibitors in cellular based assay using Hela cells.Other same project related to Summary assay
1620Toxicity Screening of PMI Inhibitors in Hela cellsOther same project related to Summary assay
1666SAR assay for compounds that inhibit PHOSPHO1Confirmatory same project related to Summary assay
1056SAR analysis of an In Vitro TNAP Dose Response Luminescent AssayConfirmatory same project related to Summary assay
1535Confirmation of compounds inhibiting phosphomannose isomerase (PMI) via a fluorescence intensity assay.Confirmatory same project related to Summary assay
1565uHTS absorbance assay for the identification of compounds that inhibit PHOSPHO1Confirmatory same project related to Summary assay
1666SAR assay for compounds that inhibit PHOSPHO1Confirmatory same project related to Summary assay
Description:
Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG)
Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA)
Network: NIH Molecular Probe Production Centers Network (MLPCN)
Grant Number: R03 MH082386-01
Assay Provider: Dr. Hudson H. Freeze, Sanford-Burnham Medical Research Institute, San Diego, CA

Congenital Disorders of Glycosylation (CDGs) are rare genetic disorders in the synthesis of N-linked glycan chains. Mutations in PMM2, encoding phosphomannomutase 2 (PMM2, Man-6-P-> Man-1-P) cause the most common form, CDG-Ia. Patients have a host of problems including hypotonia, variable psychomotor retardation, seizures, peripheral neuropathy, cardiomyopathy, and protein losing enteropathy. There is no therapy for this disorder. A current approach to ameliorate the physiological conditions associated with CDG-Ia is to provide high influx of mannose for patience. We previously developed a HTS assay through the MLSCN to identify inhibitors of phosphomannose isomerase (PMI) (Fructose-6-P->Mannose-6-P) (AID 1545) to identify inhibitors of PMI that would allow directing the administered mannose into the glycosylation pathway rather than shunting it to glycolysis via the PMI link. Here we describe the PMM2 assay that we use for counter screening purposes in PMI and other projects and to study the structure-activity relationship on analogs of the confirmed hits. Compounds are either acquired from commercial sources or synthesized internally.

REFERENCES:
1) Freeze, H. H. (2006) Genetic defects in the human glycome, Nat Rev Genet 7, 537-551.

2) DeRossi, C., Bode, L., Eklund, E. A., Zhang, F., Davis, J. A., Westphal, V., Wang, L., Borowsky, A. D.,
and Freeze, H. H. (2006) Ablation of mouse phosphomannose isomerase (Mpi) causes mannose 6-phosphate accumulation, toxicity, and embryonic lethality, J Biol Chem 281, 5916-5927.

3) Coman D, Klingberg S, Morris D, McGill J, Mercer H.(2005) Congenital disorder of glycosylation type Ia in a 6-year-old girl with a mild intellectual phenotype: two novel PMM2 mutations, J Inherit Metab Dis. 2005;28(6):1189-90

4) Vuillaumier-Barrot S, Hetet G, Barnier A, Dupre T, Cuer M, de Lonlay P, Cormier-Daire V, Durand G, Grandchamp B, Seta N.(2000) Identification of four novel PMM2 mutations in congenital disorders of glycosylation (CDG) Ia French patients, J Med Genet. 2000 Aug;37(8):579-80.

5) Pirard M, Matthijs G, Heykants L, Schollen E, Grunewald S, Jaeken J, van Schaftingen E (1999) Effect of mutations found in carbohydrate-deficient glycoprotein syndrome type IA on the activity of phosphomannomutase 2, FEBS Lett. 1999 Jun 11;452(3):319-22.
Protocol
PMM assay materials:
1) Human PMM2 protein was provided by Dr. Hudson Freeze (Sanford-Burnham Medical Research Institute, San Diego, CA).
2) Substrate working solution: 50 mM HEPES, pH 7.4, 0.166 mM Mannose-1-phosphate, 0.411 U/ml Diaphorase, 0.056 mM Resazurin.
3) Enzyme working solution: 50 mM HEPES, pH 7.4, 1.11 mM NADP+, 10.0 mM MgCl2, 0.011% Tween 20, 5.0 ug/ml phosphoglucose isomerase, 3.33 ug/ml PMI, 2.0 ug/ml G6PDH, and 1.67 ug/ml PMM2, and 0.11 mM alpha-D-Glucose 1,6-bisphosphate.
PMM2 Dose-response confirmation protocol:
1) 9 uL of Substrate working solution was added to columns 3-24 of a Greiner 384-well black plate (cat # 784076) using a Multidrop Combi liquid dispenser (Thermo)
2) 9 ul of Substrate working solution without mannose-1-p was added to columns 1 and 2 (positive control)
3) 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 50 mM HEPES, pH 7.4 to 10% final DMSO concentration.
4) 2 uL compounds in 10% DMSO were transferred into columns 3-22. Columns 1-2 and 23-24 contained 4 uL of 10% DMSO.
5) 9 uL of Enzyme working solution was added to the whole plate using a Multidrop Combi liquid dispenser
6) Plates were incubated at room temperature for 20 min.
7) The plates were read on an Analyst plate reader (Molecular Devices), Ex544, Em590.
8) Data analysis was performed using CBIS software (ChemInnovations, Inc).
Comment
The compounds were tested in 1 or more concentration ranges.
Range1 0-100 uM
Range2 0-1 uM
For all samples in each range that resolved to an IC50 the results were averaged and reported as IC50_Range. The IC50 results for all of the IC50s were averaged to produce IC50_Mean.
Compounds with an IC50_Mean < 100 uM are considered to be active in this assay.
To simplify the distinction between the inactives of the primary screen and of the confirmatory screening stage, the Tiered Activity Scoring System was developed and implemented. Its utilization for the 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 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 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 PMM 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 pEC50 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.
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: Binding
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1IC50_Mean_QualifierThis qualifier is to be used with the next TID, IC50_Mean. If the qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that value.String
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 value.String
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 100 uM_first_point_Range1 (100μM**)% inhibition at a given concentrationFloat%
9% inhibition at 50 uM_first_point_Range1 (50μM**)% inhibition at a given concentrationFloat%
10% inhibition at 25 uM_first_point_Range1 (25μM**)% inhibition at a given concentrationFloat%
11% inhibition at 12.5 uM_first_point_Range1 (12.5μM**)% inhibition at a given concentrationFloat%
12% inhibition at 6.25 uM_first_point_Range1 (6.25μM**)% inhibition at a given concentrationFloat%
13% inhibition at 3.125 uM_first_point_Range1 (3.125μM**)% inhibition at a given concentrationFloat%
14% inhibition at 1.5625 uM_first_point_Range1 (1.5625μM**)% inhibition at a given concentrationFloat%
15% inhibition at 0.78125 uM_first_point_Range1 (0.78125μM**)% inhibition at a given concentrationFloat%
16% inhibition at 0.390625 uM_first_point_Range1 (0.390625μM**)% inhibition at a given concentrationFloat%
17% inhibition at 0.1953125 uM_first_point_Range1 (0.195312μM**)% 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 100 uM_second_point_Range1 (100μM**)% inhibition at a given concentrationFloat%
20% inhibition at 50 uM_second_point_Range1 (50μM**)% inhibition at a given concentrationFloat%
21% inhibition at 25 uM_second_point_Range1 (25μM**)% inhibition at a given concentrationFloat%
22% inhibition at 12.5 uM_second_point_Range1 (12.5μM**)% inhibition at a given concentrationFloat%
23% inhibition at 6.25 uM_second_point_Range1 (6.25μM**)% inhibition at a given concentrationFloat%
24% inhibition at 3.125 uM_second_point_Range1 (3.125μM**)% inhibition at a given concentrationFloat%
25% inhibition at 1.5625 uM_second_point_Range1 (1.5625μM**)% inhibition at a given concentrationFloat%
26% inhibition at 0.78125 uM_second_point_Range1 (0.78125μM**)% inhibition at a given concentrationFloat%
27% inhibition at 0.390625 uM_second_point_Range1 (0.390625μM**)% inhibition at a given concentrationFloat%
28% inhibition at 0.1953125 uM_second_point_Range1 (0.195312μM**)% 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 100 uM_third_point_Range1 (100μM**)% inhibition at a given concentrationFloat%
31% inhibition at 50 uM_third_point_Range1 (50μM**)% inhibition at a given concentrationFloat%
32% inhibition at 25 uM_third_point_Range1 (25μM**)% inhibition at a given concentrationFloat%
33% inhibition at 12.5 uM_third_point_Range1 (12.5μM**)% inhibition at a given concentrationFloat%
34% inhibition at 6.25 uM_third_point_Range1 (6.25μM**)% inhibition at a given concentrationFloat%
35% inhibition at 3.125 uM_third_point_Range1 (3.125μM**)% inhibition at a given concentrationFloat%
36% inhibition at 1.5625 uM_third_point_Range1 (1.5625μM**)% inhibition at a given concentrationFloat%
37% inhibition at 0.78125 uM_third_point_Range1 (0.78125μM**)% inhibition at a given concentrationFloat%
38% inhibition at 0.390625 uM_third_point_Range1 (0.390625μM**)% inhibition at a given concentrationFloat%
39% inhibition at 0.1953125 uM_third_point_Range1 (0.195312μM**)% 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 100 uM_fourth_point_Range1 (100μM**)% inhibition at a given concentrationFloat%
42% inhibition at 50 uM_fourth_point_Range1 (50μM**)% inhibition at a given concentrationFloat%
43% inhibition at 25 uM_fourth_point_Range1 (25μM**)% inhibition at a given concentrationFloat%
44% inhibition at 12.5 uM_fourth_point_Range1 (12.5μM**)% inhibition at a given concentrationFloat%
45% inhibition at 6.25 uM_fourth_point_Range1 (6.25μM**)% inhibition at a given concentrationFloat%
46% inhibition at 3.125 uM_fourth_point_Range1 (3.125μM**)% inhibition at a given concentrationFloat%
47% inhibition at 1.5625 uM_fourth_point_Range1 (1.5625μM**)% inhibition at a given concentrationFloat%
48% inhibition at 0.78125 uM_fourth_point_Range1 (0.78125μM**)% inhibition at a given concentrationFloat%
49% inhibition at 0.390625 uM_fourth_point_Range1 (0.390625μM**)% inhibition at a given concentrationFloat%
50% inhibition at 0.1953125 uM_fourth_point_Range1 (0.195312μM**)% inhibition at a given concentrationFloat%
51Excluded_Points_fifth_point_Range1Flags to indicate which of the fifth dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
52% inhibition at 100 uM_fifth_point_Range1 (100μM**)% inhibition at a given concentrationFloat%
53% inhibition at 50 uM_fifth_point_Range1 (50μM**)% inhibition at a given concentrationFloat%
54% inhibition at 25 uM_fifth_point_Range1 (25μM**)% inhibition at a given concentrationFloat%
55% inhibition at 12.5 uM_fifth_point_Range1 (12.5μM**)% inhibition at a given concentrationFloat%
56% inhibition at 6.25 uM_fifth_point_Range1 (6.25μM**)% inhibition at a given concentrationFloat%
57% inhibition at 3.125 uM_fifth_point_Range1 (3.125μM**)% inhibition at a given concentrationFloat%
58% inhibition at 1.5625 uM_fifth_point_Range1 (1.5625μM**)% inhibition at a given concentrationFloat%
59% inhibition at 0.78125 uM_fifth_point_Range1 (0.78125μM**)% inhibition at a given concentrationFloat%
60% inhibition at 0.390625 uM_fifth_point_Range1 (0.390625μM**)% inhibition at a given concentrationFloat%
61% inhibition at 0.1953125 uM_fifth_point_Range1 (0.195312μM**)% inhibition at a given concentrationFloat%
62Excluded_Points_sixth_point_Range1Flags to indicate which of the sixth dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
63% inhibition at 100 uM_sixth_point_Range1 (100μM**)% inhibition at a given concentrationFloat%
64% inhibition at 50 uM_sixth_point_Range1 (50μM**)% inhibition at a given concentrationFloat%
65% inhibition at 25 uM_sixth_point_Range1 (25μM**)% inhibition at a given concentrationFloat%
66% inhibition at 12.5 uM_sixth_point_Range1 (12.5μM**)% inhibition at a given concentrationFloat%
67% inhibition at 6.25 uM_sixth_point_Range1 (6.25μM**)% inhibition at a given concentrationFloat%
68% inhibition at 3.125 uM_sixth_point_Range1 (3.125μM**)% inhibition at a given concentrationFloat%
69% inhibition at 1.5625 uM_sixth_point_Range1 (1.5625μM**)% inhibition at a given concentrationFloat%
70% inhibition at 0.78125 uM_sixth_point_Range1 (0.78125μM**)% inhibition at a given concentrationFloat%
71% inhibition at 0.390625 uM_sixth_point_Range1 (0.390625μM**)% inhibition at a given concentrationFloat%
72% inhibition at 0.1953125 uM_sixth_point_Range1 (0.195312μM**)% inhibition at a given concentrationFloat%
73IC50_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 value.String
74IC50_Range2IC50 value determined using sigmoidal dose response equationFloatμM
75Std.Err(IC50)_Range2Standard Error of IC50 valueFloat
76nH_Range2Hill coefficient determined using sigmoidal dose response equationFloat
77Excluded_Points_first_point_Range2Flags to indicate which of the first dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
78% inhibition at 1 uM_first_point_Range2 (1μM**)% inhibition at a given concentrationFloat%
79% inhibition at 0.5 uM_first_point_Range2 (0.5μM**)% inhibition at a given concentrationFloat%
80% inhibition at 0.25 uM_first_point_Range2 (0.25μM**)% inhibition at a given concentrationFloat%
81% inhibition at 0.125 uM_first_point_Range2 (0.125μM**)% inhibition at a given concentrationFloat%
82% inhibition at 0.0625 uM_first_point_Range2 (0.0625μM**)% inhibition at a given concentrationFloat%
83% inhibition at 0.03125 uM_first_point_Range2 (0.03125μM**)% inhibition at a given concentrationFloat%
84% inhibition at 0.015625 uM_first_point_Range2 (0.015625μM**)% inhibition at a given concentrationFloat%
85% inhibition at 0.0078125 uM_first_point_Range2 (0.0078125μM**)% inhibition at a given concentrationFloat%
86% inhibition at 0.00390625 uM_first_point_Range2 (0.00390625μM**)% inhibition at a given concentrationFloat%
87% inhibition at 0.001953125 uM_first_point_Range2 (0.00195312μM**)% inhibition at a given concentrationFloat%
88Excluded_Points_second_point_Range2Flags to indicate which of the second dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
89% inhibition at 1 uM_second_point_Range2 (1μM**)% inhibition at a given concentrationFloat%
90% inhibition at 0.5 uM_second_point_Range2 (0.5μM**)% inhibition at a given concentrationFloat%
91% inhibition at 0.25 uM_second_point_Range2 (0.25μM**)% inhibition at a given concentrationFloat%
92% inhibition at 0.125 uM_second_point_Range2 (0.125μM**)% inhibition at a given concentrationFloat%
93% inhibition at 0.0625 uM_second_point_Range2 (0.0625μM**)% inhibition at a given concentrationFloat%
94% inhibition at 0.03125 uM_second_point_Range2 (0.03425μM**)% inhibition at a given concentrationFloat%
95% inhibition at 0.015625 uM_second_point_Range2 (0.015625μM**)% inhibition at a given concentrationFloat%
96% inhibition at 0.0078125 uM_second_point_Range2 (0.0078125μM**)% inhibition at a given concentrationFloat%
97% inhibition at 0.00390625 uM_second_point_Range2 (0.00390625μM**)% inhibition at a given concentrationFloat%
98% inhibition at 0.001953125 uM_second_point_Range2 (0.00195312μM**)% inhibition at a given concentrationFloat%
99Excluded_Points_third_point_Range2Flags to indicate which of the third dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
100% inhibition at 1 uM_third_point_Range2 (0.1μM**)% inhibition at a given concentrationFloat%
101% inhibition at 0.5 uM_third_point_Range2 (0.5μM**)% inhibition at a given concentrationFloat%
102% inhibition at 0.25 uM_third_point_Range2 (0.25μM**)% inhibition at a given concentrationFloat%
103% inhibition at 0.125 uM_third_point_Range2 (0.125μM**)% inhibition at a given concentrationFloat%
104% inhibition at 0.0625 uM_third_point_Range2 (0.0625μM**)% inhibition at a given concentrationFloat%
105% inhibition at 0.03125 uM_third_point_Range2 (0.03125μM**)% inhibition at a given concentrationFloat%
106% inhibition at 0.015625 uM_third_point_Range2 (0.015625μM**)% inhibition at a given concentrationFloat%
107% inhibition at 0.0078125 uM_third_point_Range2 (0.0078125μM**)% inhibition at a given concentrationFloat%
108% inhibition at 0.00390625 uM_third_point_Range2 (0.00390625μM**)% inhibition at a given concentrationFloat%
109% inhibition at 0.001953125 uM_third_point_Range2 (0.00195312μM**)% inhibition at a given concentrationFloat%
110Excluded_Points_fourth_point_Range2Flags to indicate which of the fourth dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
111% inhibition at 1 uM_fourth_point_Range2 (1μM**)% inhibition at a given concentrationFloat%
112% inhibition at 0.5 uM_fourth_point_Range2 (0.5μM**)% inhibition at a given concentrationFloat%
113% inhibition at 0.25 uM_fourth_point_Range2 (0.25μM**)% inhibition at a given concentrationFloat%
114% inhibition at 0.125 uM_fourth_point_Range2 (0.125μM**)% inhibition at a given concentrationFloat%
115% inhibition at 0.0625 uM_fourth_point_Range2 (0.0625μM**)% inhibition at a given concentrationFloat%
116% inhibition at 0.03125 uM_fourth_point_Range2 (0.03125μM**)% inhibition at a given concentrationFloat%
117% inhibition at 0.015625 uM_fourth_point_Range2 (0.015625μM**)% inhibition at a given concentrationFloat%
118% inhibition at 0.0078125 uM_fourth_point_Range2 (0.0078125μM**)% inhibition at a given concentrationFloat%
119% inhibition at 0.00390625 uM_fourth_point_Range2 (0.00390625μM**)% inhibition at a given concentrationFloat%
120% inhibition at 0.001953125 uM_fourth_point_Range2 (0.00195312μM**)% inhibition at a given concentrationFloat%
121Excluded_Points_fifth_point_Range2Flags to indicate which of the fifth dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
122% inhibition at 1 uM_fifth_point_Range2 (1μM**)% inhibition at a given concentrationFloat%
123% inhibition at 0.5 uM_fifth_point_Range2 (0.5μM**)% inhibition at a given concentrationFloat%
124% inhibition at 0.25 uM_fifth_point_Range2 (0.25μM**)% inhibition at a given concentrationFloat%
125% inhibition at 0.125 uM_fifth_point_Range2 (0.125μM**)% inhibition at a given concentrationFloat%
126% inhibition at 0.0625 uM_fifth_point_Range2 (0.0625μM**)% inhibition at a given concentrationFloat%
127% inhibition at 0.03125 uM_fifth_point_Range2 (0.03125μM**)% inhibition at a given concentrationFloat%
128% inhibition at 0.015625 uM_fifth_point_Range2 (0.015625μM**)% inhibition at a given concentrationFloat%
129% inhibition at 0.0078125 uM_fifth_point_Range2 (0.0078125μM**)% inhibition at a given concentrationFloat%
130% inhibition at 0.00390625 uM_fifth_point_Range2 (0.00390625μM**)% inhibition at a given concentrationFloat%
131% inhibition at 0.001953125 uM_fifth_point_Range2 (0.00195312μM**)% inhibition at a given concentrationFloat%
132Excluded_Points_sixth_point_Range2Flags to indicate which of the sixth dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
133% inhibition at 1 uM_sixth_point_Range2 (1μM**)% inhibition at a given concentrationFloat%
134% inhibition at 0.5 uM_sixth_point_Range2 (0.5μM**)% inhibition at a given concentrationFloat%
135% inhibition at 0.25 uM_sixth_point_Range2 (0.25μM**)% inhibition at a given concentrationFloat%
136% inhibition at 0.125 uM_sixth_point_Range2 (0.125μM**)% inhibition at a given concentrationFloat%
137% inhibition at 0.0625 uM_sixth_point_Range2 (0.0625μM**)% inhibition at a given concentrationFloat%
138% inhibition at 0.03125 uM_sixth_point_Range2 (0.03125μM**)% inhibition at a given concentrationFloat%
139% inhibition at 0.015625 uM_sixth_point_Range2 (0.015625μM**)% inhibition at a given concentrationFloat%
140% inhibition at 0.0078125 uM_sixth_point_Range2 (0.0078125μM**)% inhibition at a given concentrationFloat%
141% inhibition at 0.00390625 uM_sixth_point_Range2 (0.00390625μM**)% inhibition at a given concentrationFloat%
142% inhibition at 0.001953125 uM_sixth_point_Range2 (0.00195312μM**)% inhibition at a given concentrationFloat%
143Excluded_Points_seventh_point_Range2Flags to indicate which of the seventh dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
144% inhibition at 1 uM_seventh_point_Range2 (1μM**)% inhibition at a given concentrationFloat%
145% inhibition at 0.5 uM_seventh_point_Range2 (0.5μM**)% inhibition at a given concentrationFloat%
146% inhibition at 0.25 uM_seventh_point_Range2 (0.25μM**)% inhibition at a given concentrationFloat%
147% inhibition at 0.125 uM_seventh_point_Range2 (0.125μM**)% inhibition at a given concentrationFloat%
148% inhibition at 0.0625 uM_seventh_point_Range2 (0.0625μM**)% inhibition at a given concentrationFloat%
149% inhibition at 0.03125 uM_seventh_point_Range2 (0.03125μM**)% inhibition at a given concentrationFloat%
150% inhibition at 0.015625 uM_seventh_point_Range2 (0.015625μM**)% inhibition at a given concentrationFloat%
151% inhibition at 0.0078125 uM_seventh_point_Range2 (0.0078125μM**)% inhibition at a given concentrationFloat%
152% inhibition at 0.00390625 uM_seventh_point_Range2 (0.00390625μM**)% inhibition at a given concentrationFloat%
153% inhibition at 0.001953125 uM_seventh_point_Range2 (0.00195312μM**)% inhibition at a given concentrationFloat%
154Excluded_Points_eighth_point_Range2Flags to indicate which of the eighth dose-response points were excluded from analysis. (1) means the titration point was (1) excluded and (0) means the point was not excluded, for the titration series going from low to high compound concentrations.String
155% inhibition at 1 uM_eighth_point_Range2 (1μM**)% inhibition at a given concentrationFloat%
156% inhibition at 0.5 uM_eighth_point_Range2 (0.5μM**)% inhibition at a given concentrationFloat%
157% inhibition at 0.25 uM_eighth_point_Range2 (0.25μM**)% inhibition at a given concentrationFloat%
158% inhibition at 0.125 uM_eighth_point_Range2 (0.125μM**)% inhibition at a given concentrationFloat%
159% inhibition at 0.0625 uM_eighth_point_Range2 (0.0625μM**)% inhibition at a given concentrationFloat%
160% inhibition at 0.03125 uM_eighth_point_Range2 (0.03125μM**)% inhibition at a given concentrationFloat%
161% inhibition at 0.015625 uM_eighth_point_Range2 (0.015625μM**)% inhibition at a given concentrationFloat%
162% inhibition at 0.0078125 uM_eighth_point_Range2 (0.0078125μM**)% inhibition at a given concentrationFloat%
163% inhibition at 0.00390625 uM_eighth_point_Range2 (0.00390625μM**)% inhibition at a given concentrationFloat%
164% inhibition at 0.001953125 uM_eighth_point_Range2 (0.00195312μM**)% inhibition at a given concentrationFloat%

* Activity Concentration. ** Test Concentration.
Additional Information
Grant Number: R03 MH082386-01

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