The P450 gene superfamily is involved in the metabolism and clearance of xenobiotics. This assay used various human CYP P450 isozymes to measure the dealkylation of various pro-luciferin substrates to luciferin. The luciferin is then measured by luminescence after the addition of a luciferase detection reagent. Pro-luciferin substrate concentration in the assay was equal to its KM for its CYP P450 isozyme. Inhibitors and some substrates limit the production of luciferin, and decrease measured luminescence. ..more
Tested Compounds:
Description:
NCGC Assay Overview:
The P450 gene superfamily is involved in the metabolism and clearance of xenobiotics. This assay used various human CYP P450 isozymes to measure the dealkylation of various pro-luciferin substrates to luciferin. The luciferin is then measured by luminescence after the addition of a luciferase detection reagent. Pro-luciferin substrate concentration in the assay was equal to its KM for its CYP P450 isozyme. Inhibitors and some substrates limit the production of luciferin, and decrease measured luminescence.
The P450 gene superfamily is involved in the metabolism and clearance of xenobiotics. This assay used various human CYP P450 isozymes to measure the dealkylation of various pro-luciferin substrates to luciferin. The luciferin is then measured by luminescence after the addition of a luciferase detection reagent. Pro-luciferin substrate concentration in the assay was equal to its KM for its CYP P450 isozyme. Inhibitors and some substrates limit the production of luciferin, and decrease measured luminescence.
Panel Information
cytochrome p450 panel assay - cytochrome p450 panel assay
§ Panel component ID.
| Data Table(All) | Show more |
| PID§ | Name | Substance | Panel Targets | Description | Additional Information | ||
|---|---|---|---|---|---|---|---|
| Active | Inactive | ||||||
| 1 | p450-cyp2c19 | 5913 | 7532 | cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] [gi:4503219] | Taxonomy id: 9606 | ||
| 2 | p450-cyp2d6 | 2771 | 11139 | cytochrome P450, family 2, subfamily D, polypeptide 6 isoform 2 [Homo sapiens] [gi:68509921] | Taxonomy id: 9606 | ||
| 3 | p450-cyp3a4 | 5266 | 7751 | cytochrome P450, family 3, subfamily A, polypeptide 4 [Homo sapiens] [gi:13435386] | Taxonomy id: 9606 | ||
| 4 | p450-cyp1a2 | 6000 | 7256 | cytochrome P450, family 1, subfamily A, polypeptide 2 [Homo sapiens] [gi:73915100] | Taxonomy id: 9606 | ||
| 5 | p450-cyp2c9 | 4119 | 8782 | cytochrome P450, family 2, subfamily C, polypeptide 9 [Homo sapiens] [gi:13699818] | Taxonomy id: 9606 | ||
§ Panel component ID.
Protocol
NCGC Assay Protocol Summary:
1, Reagent, 2 uL, Isozyme and Pro-Luciferin
2, Library compounds, 23 nl, 40 uM to 0.24 nM dilution series
3, Controls, 23 nl, Isozyme specific inhibitor
4, Reagent, 2 uL, NADPH regeneration solution
5, Incubation time, 60 min, Isozyme specific temperature
6, Reagent, 4ul, Detection reagent
7, Incubation time, 20 min, Isozyme specific temperature
8, Detection, 1 sec, ViewLux luminescent read
The luciferase-based P450-GloTM Screening Systems were obtained from Promega (Madison, WI) for CYP 1A2 (V9770), CYP 2C9 (V9790), CYP2 C19 (V9880), CYP 2D6 (V9890), and CYP 3A4 Luciferin-PPXE (V9910) and were adapted for 1,536-well microplates and an automated protocol. The control compounds furafylline for 1A2 (F124), sulfaphenazole for CYP 2C9 (S0758), ketoconazole for CYP 2C19 (K1003), quinidine for 2D6 (Q3625), and ketoconazole for 3A4 (K1003) were purchased from Sigma Aldrich (St. Louis, MO). Recombinant P450 enzymes were obtained from baculovirus constructs expressed in insect cells (BD/Gentest).
Medium-binding white solid Kalypsys plates used. Mixtures kept on ice. 1A2: 10 nM 1A2, 100 uM Luc-ME, 100 mM KPO4; 2C9: 10 nM 2C9, 100 uM Luc-H, 25 mM KPO4; 2C19: 5 nM 2C19, 10 uM Luc-H EGE, 50 mM KPO4; 2D6: 5 nM 2D6, 30 uM Luc-ME EGE, 100 mM KPO4; 3A4: 10 nM, 25 uM Luc-PPXE. All amounts are reflected in their final concentration, working concentration is 2x.
NADPH regeneration solution: 1.3 mM NADP+, 3.3 mM glucose-6-phosphate, 3.3 mM MgCl2, 0.4 U/mL glucose-6-phosphate dehydrogenase for all isozymes, 200 mM KPO4 for 3A4. Mixture prepared at RT but kept on ice during automated run.
RT incubation in auxilliary plate hotel for 1A2, 2D6, and 3A4; 37C for 2C9 and 2C19.
Keywords: P450, CYP1A2, CYP2C19, CYP2C9, CYP2D6, CYP3A4, Luciferase, MLSMR, MLSCN, NIH Roadmap, qHTS, NCGC
1, Reagent, 2 uL, Isozyme and Pro-Luciferin
2, Library compounds, 23 nl, 40 uM to 0.24 nM dilution series
3, Controls, 23 nl, Isozyme specific inhibitor
4, Reagent, 2 uL, NADPH regeneration solution
5, Incubation time, 60 min, Isozyme specific temperature
6, Reagent, 4ul, Detection reagent
7, Incubation time, 20 min, Isozyme specific temperature
8, Detection, 1 sec, ViewLux luminescent read
The luciferase-based P450-GloTM Screening Systems were obtained from Promega (Madison, WI) for CYP 1A2 (V9770), CYP 2C9 (V9790), CYP2 C19 (V9880), CYP 2D6 (V9890), and CYP 3A4 Luciferin-PPXE (V9910) and were adapted for 1,536-well microplates and an automated protocol. The control compounds furafylline for 1A2 (F124), sulfaphenazole for CYP 2C9 (S0758), ketoconazole for CYP 2C19 (K1003), quinidine for 2D6 (Q3625), and ketoconazole for 3A4 (K1003) were purchased from Sigma Aldrich (St. Louis, MO). Recombinant P450 enzymes were obtained from baculovirus constructs expressed in insect cells (BD/Gentest).
Medium-binding white solid Kalypsys plates used. Mixtures kept on ice. 1A2: 10 nM 1A2, 100 uM Luc-ME, 100 mM KPO4; 2C9: 10 nM 2C9, 100 uM Luc-H, 25 mM KPO4; 2C19: 5 nM 2C19, 10 uM Luc-H EGE, 50 mM KPO4; 2D6: 5 nM 2D6, 30 uM Luc-ME EGE, 100 mM KPO4; 3A4: 10 nM, 25 uM Luc-PPXE. All amounts are reflected in their final concentration, working concentration is 2x.
NADPH regeneration solution: 1.3 mM NADP+, 3.3 mM glucose-6-phosphate, 3.3 mM MgCl2, 0.4 U/mL glucose-6-phosphate dehydrogenase for all isozymes, 200 mM KPO4 for 3A4. Mixture prepared at RT but kept on ice during automated run.
RT incubation in auxilliary plate hotel for 1A2, 2D6, and 3A4; 37C for 2C9 and 2C19.
Keywords: P450, CYP1A2, CYP2C19, CYP2C9, CYP2D6, CYP3A4, Luciferase, MLSMR, MLSCN, NIH Roadmap, qHTS, NCGC
Comment
Compounds with AC50 equal or less than 10 uM are considered active.
Result Definitions
| Show more |
| TID | Name | Description | PID§ | Panel Targets | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||||
| 1 | Inhibition Observed | Whether compound inhibited pro-luciferin conversion with any of the five isozymes tested. | String | |||||
| 2 | Approved Drug | Whether compound is active ingredient in a marketed drug. | String | |||||
| 3 | Collection | Originating collection of compound sample. Exploratory is a specialized collection of bioactive compounds. Biodiverse is a diversity-oriented collection of screening | String | |||||
| 4 | Analysis Comment | Annotation/notes on a particular compound's data or its analysis | String | |||||
| 5 | Activity Outcome | p450-cyp2c19 Activity Outcome | 1 | cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] |  | Outcome | ||
| 6 | Activity Score | p450-cyp2c19 Activity Score | 1 | | Integer | |||
| 7 | p450-cyp2c19-Potency | Concentration at which compound exhibits half-maximal efficacy, AC50. Extrapolated AC50s also include the highest efficacy observed and the concentration of compound at which it was observed. | 1 | | Float | μM | ||
| 8 | p450-cyp2c19-Curve_Description | A description of dose-response curve quality. A complete curve has two observed asymptotes; a partial curve may not have attained its second asymptote at the highest concentration tested. High efficacy curves exhibit efficacy greater than 80% of control. Partial efficacies are statistically signficant, but below 80% of control. | 1 | String | ||||
| 9 | p450-cyp2c19-Fit_LogAC50 | The logarithm of the AC50 from a fit of the data to the Hill equation (calculated based on Molar Units). | 1 | | Float | |||
| 10 | p450-cyp2c19-Fit_HillSlope | The Hill slope from a fit of the data to the Hill equation. | 1 | | Float | |||
| 11 | p450-cyp2c19-Fit_R2 | R^2 fit value of the curve. Closer to 1.0 equates to better Hill equation fit. | 1 | | Float | |||
| 12 | p450-cyp2c19-Fit_InfiniteActivity | The asymptotic efficacy from a fit of the data to the Hill equation. | 1 | | Float | % | ||
| 13 | p450-cyp2c19-Fit_ZeroActivity | Efficacy at zero concentration of compound from a fit of the data to the Hill equation. | 1 | | Float | % | ||
| 14 | p450-cyp2c19-Fit_CurveClass | Numerical encoding of curve description for the fitted Hill equation. | 1 | | Float | |||
| 15 | p450-cyp2c19-Excluded_Points | Which dose-response titration points were excluded from analysis based on outlier analysis. Each number represents whether a titration point was (1) or was not (0) excluded, for the titration series going from smallest to highest compound concentrations. | 1 | String | ||||
| 16 | p450-cyp2c19-Max_Response | Maximum activity observed for compound (usually at highest concentration tested). | 1 | String | ||||
| 17 | p450-cyp2c19-Activity at 0.0007 uM (0.0007μM**) | % Activity at given concentration. | 1 | | Float | % | ||
| 18 | p450-cyp2c19-Activity at 0.00160 uM (0.001599μM**) | % Activity at given concentration. | 1 | | Float | % | ||
| 19 | p450-cyp2c19-Activity at 0.00368 uM (0.003679μM**) | % Activity at given concentration. | 1 | | Float | % | ||
| 20 | p450-cyp2c19-Activity at 0.00820 uM (0.0082μM**) | % Activity at given concentration. | 1 | | Float | % | ||
| 21 | p450-cyp2c19-Activity at 0.018 uM (0.018μM**) | % Activity at given concentration. | 1 | | Float | % | ||
| 22 | p450-cyp2c19-Activity at 0.041 uM (0.041μM**) | % Activity at given concentration. | 1 | | Float | % | ||
| 23 | p450-cyp2c19-Activity at 0.091 uM (0.091μM**) | % Activity at given concentration. | 1 | | Float | % | ||
| 24 | p450-cyp2c19-Activity at 0.204 uM (0.204μM**) | % Activity at given concentration. | 1 | | Float | % | ||
| 25 | p450-cyp2c19-Activity at 0.457 uM (0.457μM**) | % Activity at given concentration. | 1 | | Float | % | ||
| 26 | p450-cyp2c19-Activity at 1.022 uM (1.022μM**) | % Activity at given concentration. | 1 | | Float | % | ||
| 27 | p450-cyp2c19-Activity at 2.286 uM (2.286μM**) | % Activity at given concentration. | 1 | | Float | % | ||
| 28 | p450-cyp2c19-Activity at 5.111 uM (5.111μM**) | % Activity at given concentration. | 1 | | Float | % | ||
| 29 | p450-cyp2c19-Activity at 11.43 uM (11.43μM**) | % Activity at given concentration. | 1 | | Float | % | ||
| 30 | p450-cyp2c19-Activity at 25.56 uM (25.56μM**) | % Activity at given concentration. | 1 | | Float | % | ||
| 31 | p450-cyp2c19-Activity at 57.14 uM (57.14μM**) | % Activity at given concentration. | 1 | | Float | % | ||
| 32 | Activity Outcome | p450-cyp2d6 Activity Outcome | 2 | cytochrome P450, family 2, subfamily D, polypeptide 6 isoform 2 [Homo sapiens] | | Outcome | ||
| 33 | Activity Score | p450-cyp2d6 Activity Score | 2 | | Integer | |||
| 34 | p450-cyp2d6-Potency | Concentration at which compound exhibits half-maximal efficacy, AC50. Extrapolated AC50s also include the highest efficacy observed and the concentration of compound at which it was observed. | 2 | | Float | μM | ||
| 35 | p450-cyp2d6-Curve_Description | A description of dose-response curve quality. A complete curve has two observed asymptotes; a partial curve may not have attained its second asymptote at the highest concentration tested. High efficacy curves exhibit efficacy greater than 80% of control. Partial efficacies are statistically signficant, but below 80% of control. | 2 | String | ||||
| 36 | p450-cyp2d6-Fit_LogAC50 | The logarithm of the AC50 from a fit of the data to the Hill equation (calculated based on Molar Units). | 2 | | Float | |||
| 37 | p450-cyp2d6-Fit_HillSlope | The Hill slope from a fit of the data to the Hill equation. | 2 | | Float | |||
| 38 | p450-cyp2d6-Fit_R2 | R^2 fit value of the curve. Closer to 1.0 equates to better Hill equation fit. | 2 | | Float | |||
| 39 | p450-cyp2d6-Fit_InfiniteActivity | The asymptotic efficacy from a fit of the data to the Hill equation. | 2 | | Float | % | ||
| 40 | p450-cyp2d6-Fit_ZeroActivity | Efficacy at zero concentration of compound from a fit of the data to the Hill equation. | 2 | | Float | % | ||
| 41 | p450-cyp2d6-Fit_CurveClass | Numerical encoding of curve description for the fitted Hill equation. | 2 | | Float | |||
| 42 | p450-cyp2d6-Excluded_Points | Which dose-response titration points were excluded from analysis based on outlier analysis. Each number represents whether a titration point was (1) or was not (0) excluded, for the titration series going from smallest to highest compound concentrations. | 2 | String | ||||
| 43 | p450-cyp2d6-Max_Response | Maximum activity observed for compound (usually at highest concentration tested). | 2 | | Float | % | ||
| 44 | p450-cyp2d6-Activity at 0.0007 uM (0.0007μM**) | % Activity at given concentration. | 2 | | Float | % | ||
| 45 | p450-cyp2d6-Activity at 0.00160 uM (0.0016μM**) | % Activity at given concentration. | 2 | | Float | % | ||
| 46 | p450-cyp2d6-Activity at 0.00368 uM (0.00368μM**) | % Activity at given concentration. | 2 | | Float | % | ||
| 47 | p450-cyp2d6-Activity at 0.00820 uM (0.0082μM**) | % Activity at given concentration. | 2 | | Float | % | ||
| 48 | p450-cyp2d6-Activity at 0.018 uM (0.018μM**) | % Activity at given concentration. | 2 | | Float | % | ||
| 49 | p450-cyp2d6-Activity at 0.041 uM | % Activity at given concentration. | 2 | | Float | % | ||
| 50 | p450-cyp2d6-Activity at 0.091 uM (0.091μM**) | % Activity at given concentration. | 2 | | Float | % | ||
| 51 | p450-cyp2d6-Activity at 0.204 uM (0.204μM**) | % Activity at given concentration. | 2 | | Float | % | ||
| 52 | p450-cyp2d6-Activity at 0.457 uM (0.457μM**) | % Activity at given concentration. | 2 | | Float | % | ||
| 53 | p450-cyp2d6-Activity at 1.022 uM (1.022μM**) | % Activity at given concentration. | 2 | | Float | % | ||
| 54 | p450-cyp2d6-Activity at 2.286 uM (2.286μM**) | % Activity at given concentration | 2 | | Float | % | ||
| 55 | p450-cyp2d6-Activity at 5.111 uM (5.111μM**) | % Activity at given concentration. | 2 | | Float | % | ||
| 56 | p450-cyp2d6-Activity at 11.43 uM (11.43μM**) | % Activity at given concentration. | 2 | | Float | % | ||
| 57 | p450-cyp2d6-Activity at 25.56 uM (25.56μM**) | % Activity at given concentration. | 2 | | Float | % | ||
| 58 | p450-cyp2d6-Activity at 57.14 uM (57.14μM**) | % Activity at given concentration. | 2 | | Float | % | ||
| 59 | Activity Outcome | p450-cyp3a4 Activity Outcome | 3 | cytochrome P450, family 3, subfamily A, polypeptide 4 [Homo sapiens] | | Outcome | ||
| 60 | Activity Score | p450-cyp3a4 Activity Score | 3 | | Integer | |||
| 61 | p450-cyp3a4-Potency | Concentration at which compound exhibits half-maximal efficacy, AC50. Extrapolated AC50s also include the highest efficacy observed and the concentration of compound at which it was observed. | 3 | | Float | μM | ||
| 62 | p450-cyp3a4-Curve_Description | A description of dose-response curve quality. A complete curve has two observed asymptotes; a partial curve may not have attained its second asymptote at the highest concentration tested. High efficacy curves exhibit efficacy greater than 80% of control. Partial efficacies are statistically signficant, but below 80% of control. | 3 | String | ||||
| 63 | p450-cyp3a4-Fit_LogAC50 | The logarithm of the AC50 from a fit of the data to the Hill equation (calculated based on Molar Units). | 3 | | Float | |||
| 64 | p450-cyp3a4-Fit_HillSlope | The Hill slope from a fit of the data to the Hill equation. | 3 | | Float | |||
| 65 | p450-cyp3a4-Fit_R2 | R^2 fit value of the curve. Closer to 1.0 equates to better Hill equation fit. | 3 | | Float | |||
| 66 | p450-cyp3a4-Fit_InfiniteActivity | The asymptotic efficacy from a fit of the data to the Hill equation. | 3 | | Float | % | ||
| 67 | p450-cyp3a4-Fit_ZeroActivity | Efficacy at zero concentration of compound from a fit of the data to the Hill equation. | 3 | | Float | % | ||
| 68 | p450-cyp3a4-Fit_CurveClass | Numerical encoding of curve description for the fitted Hill equation. | 3 | | Float | |||
| 69 | p450-cyp3a4-Excluded_Points | Which dose-response titration points were excluded from analysis based on outlier analysis. Each number represents whether a titration point was (1) or was not (0) excluded, for the titration series going from smallest to highest compound concentrations. | 3 | String | ||||
| 70 | p450-cyp3a4-Max_Response | Maximum activity observed for compound (usually at highest concentration tested). | 3 | | Float | % | ||
| 71 | p450-cyp3a4-Activity at 0.0007 uM (0.0007μM**) | % Activity at given concentration. | 3 | | Float | % | ||
| 72 | p450-cyp3a4-Activity at 0.00164 uM (0.00164μM**) | % Activity at given concentration. | 3 | | Float | % | ||
| 73 | p450-cyp3a4-Activity at 0.00366 uM (0.00366μM**) | % Activity at given concentration. | 3 | | Float | % | ||
| 74 | p450-cyp3a4-Activity at 0.00818 uM (0.00818μM**) | % Activity at given concentration. | 3 | | Float | % | ||
| 75 | p450-cyp3a4-Activity at 0.018 uM (0.018μM**) | % Activity at given concentration. | 3 | | Float | % | ||
| 76 | p450-cyp3a4-Activity at 0.041 uM (0.041μM**) | % Activity at given concentration. | 3 | | Float | % | ||
| 77 | p450-cyp3a4-Activity at 0.091 uM (0.091μM**) | % Activity at given concentration. | 3 | | Float | % | ||
| 78 | p450-cyp3a4-Activity at 0.204 uM (0.204μM**) | % Activity at given concentration. | 3 | | Float | % | ||
| 79 | p450-cyp3a4-Activity at 0.457 uM (0.457μM**) | % Activity at given concentration | 3 | | Float | % | ||
| 80 | p450-cyp3a4-Activity at 1.022 uM (1.022μM**) | % Activity at given concentration. | 3 | | Float | % | ||
| 81 | p450-cyp3a4-Activity at 2.286 uM (2.286μM**) | % Activity at given concentration. | 3 | | Float | % | ||
| 82 | p450-cyp3a4-Activity at 5.111 uM (5.111μM**) | % Activity at given concentration. | 3 | | Float | % | ||
| 83 | p450-cyp3a4-Activity at 11.43 uM (11.43μM**) | % Activity at given concentration. | 3 | | Float | % | ||
| 84 | p450-cyp3a4-Activity at 25.56 uM (25.56μM**) | % Activity at given concentration. | 3 | | Float | % | ||
| 85 | p450-cyp3a4-Activity at 57.14 uM (57.14μM**) | % Activity at given concentration | 3 | | Float | % | ||
| 86 | Activity Outcome | p450-cyp1a2 Activity Outcome | 4 | cytochrome P450, family 1, subfamily A, polypeptide 2 [Homo sapiens] | | Outcome | ||
| 87 | Activity Score | p450-cyp1a2 Activity Score | 4 | | Integer | |||
| 88 | p450-cyp1a2-Potency | Concentration at which compound exhibits half-maximal efficacy, AC50. Extrapolated AC50s also include the highest efficacy observed and the concentration of compound at which it was observed. | 4 | | Float | μM | ||
| 89 | p450-cyp1a2-Curve_Description | A description of dose-response curve quality. A complete curve has two observed asymptotes; a partial curve may not have attained its second asymptote at the highest concentration tested. High efficacy curves exhibit efficacy greater than 80% of control. Partial efficacies are statistically signficant, but below 80% of control. | 4 | String | ||||
| 90 | p450-cyp1a2-Fit_LogAC50 | The logarithm of the AC50 from a fit of the data to the Hill equation (calculated based on Molar Units). | 4 | | Float | |||
| 91 | p450-cyp1a2-Fit_HillSlope | The Hill slope from a fit of the data to the Hill equation. | 4 | | Float | |||
| 92 | p450-cyp1a2-Fit_R2 | R^2 fit value of the curve. Closer to 1.0 equates to better Hill equation fit. | 4 | | Float | |||
| 93 | p450-cyp1a2-Fit_InfiniteActivity | The asymptotic efficacy from a fit of the data to the Hill equation. | 4 | | Float | % | ||
| 94 | p450-cyp1a2-Fit_ZeroActivity | Efficacy at zero concentration of compound from a fit of the data to the Hill equation. | 4 | | Float | % | ||
| 95 | p450-cyp1a2-Fit_CurveClass | Numerical encoding of curve description for the fitted Hill equation. | 4 | | Float | |||
| 96 | p450-cyp1a2-Excluded_Points | Which dose-response titration points were excluded from analysis based on outlier analysis. Each number represents whether a titration point was (1) or was not (0) excluded, for the titration series going from smallest to highest compound concentrations. | 4 | String | ||||
| 97 | p450-cyp1a2-Max_Response | Maximum activity observed for compound (usually at highest concentration tested). | 4 | | Float | |||
| 98 | p450-cyp1a2-Activity at 0.0007 uM (0.0007μM**) | % Activity at given concentration. | 4 | | Float | % | ||
| 99 | p450-cyp1a2-Activity at 0.00160 uM (0.0016μM**) | % Activity at given concentration. | 4 | | Float | % | ||
| 100 | p450-cyp1a2-Activity at 0.00368 uM (0.00368μM**) | % Activity at given concentration. | 4 | | Float | % | ||
| 101 | p450-cyp1a2-Activity at 0.00820 uM (0.0082μM**) | % Activity at given concentration. | 4 | | Float | % | ||
| 102 | p450-cyp1a2-Activity at 0.018 uM (0.018μM**) | % Activity at given concentration. | 4 | | Float | % | ||
| 103 | p450-cyp1a2-Activity at 0.041 uM (0.041μM**) | % Activity at given concentration. | 4 | | Float | % | ||
| 104 | p450-cyp1a2-Activity at 0.091 uM (0.091μM**) | % Activity at given concentration. | 4 | | Float | % | ||
| 105 | p450-cyp1a2-Activity at 0.204 uM (0.204μM**) | % Activity at given concentration. | 4 | | Float | % | ||
| 106 | p450-cyp1a2-Activity at 0.457 uM (0.457μM**) | % Activity at given concentration. | 4 | | Float | % | ||
| 107 | p450-cyp1a2-Activity at 1.022 uM (1.022μM**) | % Activity at given concentration. | 4 | | Float | % | ||
| 108 | p450-cyp1a2-Activity at 2.286 uM (2.286μM**) | % Activity at given concentration. | 4 | | Float | % | ||
| 109 | p450-cyp1a2-Activity at 5.111 uM (5.111μM**) | % Activity at given concentration. | 4 | | Float | % | ||
| 110 | p450-cyp1a2-Activity at 11.43 uM (11.43μM**) | % Activity at given concentration. | 4 | | Float | % | ||
| 111 | p450-cyp1a2-Activity at 25.56 uM (25.56μM**) | % Activity at given concentration. | 4 | | Float | % | ||
| 112 | p450-cyp1a2-Activity at 57.14 uM (57.14μM**) | % Activity at given concentration. | 4 | | Float | % | ||
| 113 | Activity Outcome | p450-cyp2c9 Activity Outcome | 5 | cytochrome P450, family 2, subfamily C, polypeptide 9 [Homo sapiens] | | Outcome | ||
| 114 | Activity Score | p450-cyp2c9 Activity Score | 5 | | Integer | |||
| 115 | p450-cyp2c9-Potency | Concentration at which compound exhibits half-maximal efficacy, AC50. Extrapolated AC50s also include the highest efficacy observed and the concentration of compound at which it was observed. | 5 | | Float | μM | ||
| 116 | p450-cyp2c9-Curve_Description | A description of dose-response curve quality. A complete curve has two observed asymptotes; a partial curve may not have attained its second asymptote at the highest concentration tested. High efficacy curves exhibit efficacy greater than 80% of control. Partial efficacies are statistically signficant, but below 80% of control. | 5 | String | ||||
| 117 | p450-cyp2c9-Fit_LogAC50 | The logarithm of the AC50 from a fit of the data to the Hill equation (calculated based on Molar Units). | 5 | | Float | |||
| 118 | p450-cyp2c9-Fit_HillSlope | The Hill slope from a fit of the data to the Hill equation. | 5 | | Float | |||
| 119 | p450-cyp2c9-Fit_R2 | R^2 fit value of the curve. Closer to 1.0 equates to better Hill equation fit. | 5 | | Float | |||
| 120 | p450-cyp2c9-Fit_InfiniteActivity | The asymptotic efficacy from a fit of the data to the Hill equation. | 5 | | Float | % | ||
| 121 | p450-cyp2c9-Fit_ZeroActivity | Efficacy at zero concentration of compound from a fit of the data to the Hill equation. | 5 | | Float | % | ||
| 122 | p450-cyp2c9-Fit_CurveClass | Numerical encoding of curve description for the fitted Hill equation. | 5 | | Float | |||
| 123 | p450-cyp2c9-Excluded_Points | Which dose-response titration points were excluded from analysis based on outlier analysis. Each number represents whether a titration point was (1) or was not (0) excluded, for the titration series going from smallest to highest compound concentrations. | 5 | String | ||||
| 124 | p450-cyp2c9-Max_Response | Maximum activity observed for compound (usually at highest concentration tested). | 5 | | Float | |||
| 125 | p450-cyp2c9-Activity at 0.0007 uM (0.0007μM**) | % Activity at given concentration. | 5 | | Float | % | ||
| 126 | p450-cyp2c9-Activity at 0.00160 uM (0.0016μM**) | % Activity at given concentration. | 5 | | Float | % | ||
| 127 | p450-cyp2c9-Activity at 0.00368 uM (0.00368μM**) | % Activity at given concentration. | 5 | | Float | % | ||
| 128 | p450-cyp2c9-Activity at 0.00820 uM (0.0082μM**) | % Activity at given concentration. | 5 | | Float | % | ||
| 129 | p450-cyp2c9-Activity at 0.018 uM (0.018μM**) | % Activity at given concentration. | 5 | | Float | % | ||
| 130 | p450-cyp2c9-Activity at 0.041 uM (0.041μM**) | % Activity at given concentration. | 5 | | Float | % | ||
| 131 | p450-cyp2c9-Activity at 0.091 uM (0.091μM**) | % Activity at given concentration. | 5 | | Float | % | ||
| 132 | p450-cyp2c9-Activity at 0.204 uM (0.204μM**) | % Activity at given concentration. | 5 | | Float | % | ||
| 133 | p450-cyp2c9-Activity at 0.457 uM (0.457μM**) | % Activity at given concentration. | 5 | | Float | % | ||
| 134 | p450-cyp2c9-Activity at 1.022 uM (1.022μM**) | % Activity at given concentration. | 5 | | Float | % | ||
| 135 | p450-cyp2c9-Activity at 2.286 uM (2.286μM**) | % Activity at given concentration. | 5 | | Float | % | ||
| 136 | p450-cyp2c9-Activity at 5.111 uM (5.111μM**) | % Activity at given concentration. | 5 | | Float | % | ||
| 137 | p450-cyp2c9-Activity at 11.43 uM (11.43μM**) | % Activity at given concentration. | 5 | | Float | % | ||
| 138 | p450-cyp2c9-Activity at 25.56 uM (25.56μM**) | % Activity at given concentration. | 5 | | Float | % | ||
| 139 | p450-cyp2c9-Activity at 57.14 uM (57.14μM**) | % Activity at given concentration. | 5 | | Float | % | ||
| 140 | Compound QC | String |
** Test Concentration. § Panel component ID.
Classification
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