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BioAssay: AID 588725

Late stage counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): Radioactivity-based biochemical assay to identify modulators of a panel of 48 kinases

Name: Late stage counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): Radioactivity-based biochemical assay to identify modulators of a panel of 48 kinases. ..more
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 Tested Compounds
 Tested Compounds
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Inactive(1)
 
 
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 Tested Substances
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Inactive(1)
 
 
AID: 588725
Data Source: The Scripps Research Institute Molecular Screening Center (KINASE-PROFILING_INH_RADIO_2X%INH MCSRUN SAR)
BioAssay Type: Panel
Depositor Category: NIH Molecular Libraries Probe Production Network
Deposit Date: 2011-10-30
Hold-until Date: 2012-10-27
Modify Date: 2012-10-27

Data Table ( Complete ):           All
Tested Compound:
Depositor Specified Assays
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AIDNameTypeComment
1700Primary cell-based high throughput screening assay to identify inhibitors of kruppel-like factor 5 (KLF5)screeningPrimary screen (KLF5 inhibitors in singlicate)
1825Luminescence-based counterscreen assay for KLF5 inhibitors: cell-based high throughput screening assay to identify cytotoxic compounds using the IEC-6 intestinal epithelial cell line.screeningCounterscreen (Cytotoxic compounds in singlicate)
1834Luminescence-based confirmation cell-based high throughput screening assay to identify inhibitors of kruppel-like factor 5 (KLF5)screeningConfirmation screen (KLF5 inhibitors in triplicate)
1858Summary of probe development efforts to identify inhibitors of kruppel-like factor 5 (KLF5)summarySummary (KLF5 inhibitors)
1905Luminescence-based counterscreen assay for KLF5 inhibitors: cell-based high throughput screening assay to identify cytotoxic compounds using the IEC-6 intestinal epithelial cell line in triplicate.screeningCounterscreen (Cytotoxic compounds in triplicate)
1907Luminescence-based confirmation cell-based assay for cytotoxic compounds using the IEC-6 intestinal epithelial cell line.screeningConfirmation screen (Cytotoxic compounds in triplicate)
1972Luminescence-based dose response cell-based high throughput screening assay for cytotoxic compounds using the IEC-6 intestinal epithelial cell line.confirmatoryDose response (Cytotoxic compounds in triplicate)
1973Luminescence-based dose response cell-based high throughput screening assay for inhibitors of kruppel-like factor 5 (KLF5).confirmatoryDose response (KLF5 inhibitors in triplicate)
1975Luminescence-based counterscreen assay for KLF5 inhibitors: dose response cell-based high throughput screening assay to identify cytotoxic compounds using the IEC-6 intestinal epithelial cell line.confirmatoryDose response counterscreen (Cytotoxic compounds in triplicate)
2749Late stage counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): luminescence-based cell-based dose response assay for cytotoxic compounds using the IEC-6 intestinal epithelial cell lineconfirmatoryLate stage counterscreen dose response (Cytotoxic compounds in triplicate)
2750Late stage results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): luminescence-based cell-based dose response assay for inhibitors of KLF5confirmatoryLate stage dose response (KLF5 inhibitors in triplicate)
434956Late stage counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): luminescence-based cell-based dose response assay for cytotoxic compounds using the IEC-6 intestinal epithelial cell line (Round 1)confirmatoryLate stage dose response counterscreen (Cytotoxic compounds in triplicate)
434957Late stage results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): luminescence-based cell-based dose response assay for inhibitors of KLF5 (Round 1)confirmatoryLate stage dose response (KLF5 inhibitors in triplicate)
485336Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of KLF5 protein levelsconfirmatoryLate stage dose response (KLF5 protein levels inhibitors in triplicate)
485338Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): luminescence-based cell-based dose response assay for cytotoxic compounds using the DLD-1 cell line (Round 1)confirmatoryLate stage dose response counterscreen (Cytotoxicity in triplicate)
588539Late stage assay provider counterscreen results for the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): Cell cycle analysis of the DLD-1 cell lineotherLate stage counterscreen (Cell cycle analysis of the DLD-1 cell line)
588610Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Epidermal Growth Factor Receptor (EGFR) protein levels in DLD1 cellsotherLate stage counterscreen (EGFR protein levels in DLD1 cells inhibitors)
588612Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Phosphorylated Mitogen-Activated Protein Kinase 1 (P-MAPK1; P-ERK1/2) protein levels in DLD1 cellsotherLate stage counterscreen (P-ERK1/2 protein levels in DLD1 cells inhibitors)
588613Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Phosphorylated Epidermal Growth Factor Receptor (EGFR) protein levels in DLD1 cells.otherLate stage counterscreen (P-EGFR protein levels in DLD1 cells inhibitors)
588614Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Mitogen-Activated Protein Kinase 1 (MAPK1; ERK1/2) protein levels in DLD1 cellsotherLate stage counterscreen (ERK1/2 protein levels in DLD1 cells inhibitors)
588615Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of P38 protein levels in DLD1 cellsotherLate stage counterscreen (P38 protein levels in DLD1 cells inhibitors)
588616Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of phospho-P38 protein levels in DLD1 cellsotherLate stage counterscreen (phospho-P38 protein levels in DLD1 cells inhibitors)
588617Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of KLF5 protein levels in DLD1 cellsotherLate stage counterscreen (KLF5 protein levels in DLD1 cells inhibitors)
588618Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Early Growth Response 1 (EGR1) protein levels in DLD1 cellsotherLate stage counterscreen (EGR1 protein levels in DLD1 cells inhibitors)
588640Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of P38 protein levels in HCT116 human colorectal carcinoma cellsotherLate stage counterscreen (P38 protein levels in HCT116 cells inhibitors)
588642Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Mitogen-Activated Protein Kinase 1 (MAPK1; ERK1/2) protein levels in HCT116 human colorectal carcinoma cellsotherLate stage counterscreen (ERK1/2 protein levels in HCT116 cells inhibitors)
588643Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Phosphorylated Mitogen-Activated Protein Kinase 1 (P-MAPK1; P-ERK1/2) protein levels in HCT116 human colorectal carcinoma cellsotherLate stage counterscreen (P-ERK1/2 protein levels in HCT116 cells inhibitors)
588644Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Early Growth Response 1 (EGR1) protein levels in HCT116 human colorectal carcinoma cellsotherLate stage counterscreen (EGR1 protein levels in HCT116 cells inhibitors)
588646Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of phosphorylated P38 protein levels in HCT116 human colorectal carcinoma cellsotherLate stage counterscreen (phospho-P38 protein levels in HCT116 cells inhibitors)
588648Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Epidermal Growth Factor Receptor (EGFR) protein levels in HCT116 human colorectal carcinoma cellsotherLate stage counterscreen (EGFR protein levels in HCT116 cells inhibitors)
588650Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Phosphorylated Epidermal Growth Factor Receptor (EGFR) protein levels in HCT116 human colorectal carcinoma cellsotherLate stage counterscreen (P-EGFR protein levels in HCT116 cells inhibitors)
588652Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of KLF5 protein levels in HCT116 human colorectal carcinoma cellsotherLate stage counterscreen (KLF5 protein levels in HCT116 cells inhibitors)
588653Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Phosphorylated Epidermal Growth Factor Receptor (EGFR) protein levels in HT29 human colorectal carcinoma cellsotherLate stage counterscreen (P-EGFR protein levels in HT29 cells inhibitors)
588654Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Epidermal Growth Factor Receptor (EGFR) protein levels in HT29 human colorectal carcinoma cellsotherLate stage counterscreen (EGFR protein levels in HT29 cells inhibitors)
588655Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Phosphorylated Mitogen-Activated Protein Kinase 1 (P-MAPK1; P-ERK1/2) protein levels in HT29 human colorectal carcinoma cellsotherLate stage counterscreen (P-ERK1/2 protein levels in HT29 cells inhibitors)
588656Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Mitogen-Activated Protein Kinase 1 (MAPK1; ERK1/2) protein levels in HT29 human colorectal carcinoma cellsotherLate stage counterscreen (ERK1/2 protein levels in HT29 cells inhibitors)
588657Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Early Growth Response 1 (EGR1) protein levels in HT29 human colorectal carcinoma cellsotherLate stage counterscreen (EGR1 protein levels in HT29 cells inhibitors)
588658Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of phosphorylated P38 protein levels in HT29 human colorectal carcinoma cellsotherLate stage counterscreen (phospho-P38 protein levels in HT29 cells inhibitors)
588659Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of P38 protein levels in HT29 human colorectal carcinoma cellsotherLate stage counterscreen (P38 protein levels in HT29 cells inhibitors)
588660Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of KLF5 protein levels in HT29 human colorectal carcinoma cellsotherLate stage counterscreen (KLF5 protein levels in HT29 cells inhibitors)
588661Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of KLF5 protein levels in SW620 human colorectal carcinoma cellsotherLate stage counterscreen (KLF5 protein levels in SW620 cells inhibitors)
588662Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of P38 protein levels in SW620 human colorectal carcinoma cellsotherLate stage counterscreen (P38 protein levels in SW620 cells inhibitors)
588663Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of phosphorylated P38 protein levels in SW620 human colorectal carcinoma cellsotherLate stage counterscreen (P-P38 protein levels in SW620 cells inhibitors)
588665Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Early Growth Response 1 (EGR1) protein levels in SW620 human colorectal carcinoma cellsotherLate stage counterscreen (EGR1 protein levels in SW620 cells inhibitors)
588666Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Mitogen-Activated Protein Kinase 1 (MAPK1; ERK1/2) protein levels in SW620 human colorectal carcinoma cellsotherLate stage counterscreen (ERK1/2 protein levels in SW620 cells inhibitors)
588667Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Epidermal Growth Factor Receptor (EGFR) protein levels in SW620 human colorectal carcinoma cellsotherLate stage counterscreen (EGFR protein levels in SW620 cells inhibitors)
588668Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Phosphorylated Mitogen-Activated Protein Kinase 1 (P-MAPK1; P-ERK1/2) protein levels in SW620 human colorectal carcinoma cellsotherLate stage counterscreen (P-ERK1/2 protein levels in SW620 cells inhibitors)
588677Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Phosphorylated Epidermal Growth Factor Receptor (EGFR) protein levels in SW620 human colorectal carcinoma cellsotherLate stage counterscreen (P-EGFR protein levels in SW620 cells inhibitors)
Description:
Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center
Affiliation: The Scripps Research Institute, TSRI
Assay Provider: Vincent Yang, Emory University
Network: Molecular Library Probe Production Centers Network (MLPCN)
Grant Proposal Number: 1-R03-DA026215-01
Grant Proposal PI: Vincent Yang
External Assay ID: KINASE-PROFILING_INH_RADIO_2X%INH MCSRUN SAR

Name: Late stage counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): Radioactivity-based biochemical assay to identify modulators of a panel of 48 kinases.

Description:

Transcription factors are essential regulators of transcription that bind DNA to control both the rate and frequency of gene expression (1). Many diseases of cell homeostasis are associated with aberrant transcription factor activity (2). Colon cancer, in particular, is a disease of uncontrolled proliferation of the epithelial cells that line the intestinal crypts. Krlike factor 5 (KLF5) is a zinc finger-containing transcription factor that binds to GC-rich sequences in promoters of numerous genes (3) including cyclin D1 (4), cyclin B1/Cdc2 (4), and integrin-linked kinase (5). KLF5 is highly expressed in rapidly dividing epithelial cells in intestinal crypts (6). This expression pattern of KLF5, along with studies demonstrating that KLF5 mediates the transforming effects of oncogenic H-Ras (7), and that ectopic expression of KLF5 leads to increased cell proliferation and anchorage-independent growth of cultured intestinal epithelial cells (8, 9), suggest that KLF5 may be involved in colon cancer pathogenesis. Therefore, the identification of selective inhibitors of KLF5 may provide useful tools to elucidate the role of KLF5 as a regulator of cellular proliferation and tumor formation in the intestinal epithelium (10).

References:

1. Ptashne M. Regulation of transcription: from lambda to eukaryotes. Trends Biochem Sci. 2005 Jun;30(6):275-9.
2. Fre S, Vignjevic D, Schoumacher M, Duffy SL, Janssen KP, Robine S, Louvard D. Adv Cancer Res. 2008;100:85-111. Epithelial morphogenesis and intestinal cancer: new insights in signaling mechanisms.
3. Goldstein BG, Chao HH, Yang Y, Yermolina YA, Tobias JW, Katz JP. Am J Physiol Gastrointest Liver Physiol. 2007 Jun;292(6):G1784-92. Overexpression of Kruppel-like factor 5 in esophageal epithelia in vivo leads to increased proliferation in basal but not suprabasal cells.
4. Ghaleb AM, Nandan MO, Chanchevalap S, Dalton WB, Hisamuddin IM, Yang VW. Krlike factors 4 and 5: the yin and yang regulators of cellular proliferation. Cell Res. 2005 Feb;15(2):92-6.
5. Yang Y, Tetreault MP, Yermolina YA, Goldstein BG, Katz JP. Krlike factor 5 controls keratinocyte migration via the integrin-linked kinase. J Biol Chem. 2008 Jul 4;283(27):18812-20.
6. McConnell BB, Ghaleb AM, Nandan MO, Yang VW. The diverse functions of Krlike factors 4 and 5 in epithelial biology and pathobiology. Bioessays. 2007 Jun;29(6):549-57. Erratum in: Bioessays. 2007 Sep;29(9):946.
7. Nandan MO, Yoon HS, Zhao W, Ouko LA, Chanchevalap S, Yang VW. Krlike factor 5 mediates the transforming activity of oncogenic H-Ras. Oncogene. 2004 Apr 22;23(19):3404-13.
8. Chanchevalap S, Nandan MO, Merlin D, Yang VW. FEBS Lett. 2004 Dec 3;578(1-2):99-105. All-trans retinoic acid inhibits proliferation of intestinal epithelial cells by inhibiting expression of the gene encoding Kruppel-like factor 5.
9. Sun R, Chen X, Yang VW. J Biol Chem. 2001 Mar 9;276(10):6897-900. Intestinal-enriched Krlike factor (Krlike factor 5) is a positive regulator of cellular proliferation.
10. Bialkowska A, Crisp M, Bannister T, He Y, Chowdhury S, Schurer S, Chase P, Spicer T, Madoux F, Tian. Identification of Small-Molecule Inhibitors of the Colorectal Cancer Oncogene Kruppel-Like Factor 5 Expression by Ultrahigh-Throughput Screening. Mol Canc Ther. 2011.

Keywords:

Late stage, late stage AID, kinase, profiling, kinase profiling, outsource, RBC, Reaction Biology Corp, radioactivity, radio, radiolabel, panel, ATP, staurosporine, powders, purchased, synthesized, DLD, DLD-1, cells, cytotoxicity, cell viability, cell, cycle, sort, flow cytometry, KLF5, BTEB2, kruppel-like factor 5, cancer, dose response, counterscreen, inhibitor, inhibition, assay provider, Scripps, Scripps Florida, The Scripps Research Institute Molecular Screening Center, SRIMSC, Molecular Libraries Probe Production Centers Network, MLPCN.
Panel Information
Kinases
    Data Table(All)Show more
PID§NameSubstancePanel TargetsDescriptionAdditional Information
ActiveInactive
1AKT11RAC-alpha serine/threonine-protein kinase [Homo sapiens] [gi:62241011]
Taxonomy id: 9606
Gene id: 207
2AKT21RAC-beta serine/threonine-protein kinase isoform 2 [Homo sapiens] [gi:339895853]
Taxonomy id: 9606
Gene id: 208
3AKT31RAC-gamma serine/threonine-protein kinase isoform 2 [Homo sapiens] [gi:332078559]
Taxonomy id: 9606
Gene id: 10000
4Aurora A1aurora kinase A-interacting protein [Homo sapiens] [gi:187829340]
Taxonomy id: 9606
Gene id: 54998
5BRAF1serine/threonine-protein kinase B-raf [Homo sapiens] [gi:33188459]
Taxonomy id: 9606
Gene id: 673
6CDK1/cyclin A1cyclin-dependent kinase 1 isoform 4 [Homo sapiens] [gi:281427278]
cyclin-A2 [Homo sapiens] [gi:4502613]
Taxonomy id: 9606
Gene id: 983
Gene id: 890
7CDK1/cyclin B1cyclin-dependent kinase 1 isoform 4 [Homo sapiens] [gi:281427278]
G2/mitotic-specific cyclin-B1 [Homo sapiens] [gi:14327896]
Taxonomy id: 9606
Gene id: 983
Gene id: 891
8CDK2/cyclin A1cyclin-dependent kinase 2 isoform 1 [Homo sapiens] [gi:16936528]
cyclin-A2 [Homo sapiens] [gi:4502613]
Taxonomy id: 9606
Gene id: 1017
Gene id: 890
9CDK2/cyclin E1cyclin-dependent kinase 2 isoform 1 [Homo sapiens] [gi:16936528]
G1/S-specific cyclin-E1 [Homo sapiens] [gi:17318559]
Taxonomy id: 9606
Gene id: 1017
Gene id: 898
10CDK5/p251cyclin-dependent kinase 5 isoform 2 [Homo sapiens] [gi:256542306]
cyclin-dependent kinase 5 activator 1 [Homo sapiens] [gi:4502737]
Taxonomy id: 9606
Gene id: 1020
Gene id: 8851
11CDK5/p351cyclin-dependent kinase 5 isoform 2 [Homo sapiens] [gi:256542306]
cyclin-dependent kinase 5 activator 1 [Homo sapiens] [gi:4502737]
Taxonomy id: 9606
Gene id: 1020
Gene id: 8851
12EGFR1epidermal growth factor receptor [Homo sapiens] [gi:326467049]
Taxonomy id: 9606
Gene id: 1956
13ERBB21receptor tyrosine-protein kinase erbB-2 isoform b [Homo sapiens] [gi:54792098]
Taxonomy id: 9606
Gene id: 2064
14ERBB41receptor tyrosine-protein kinase erbB-4 isoform JM-a/CVT-2 precursor [Homo sapiens] [gi:110825958]
Taxonomy id: 9606
Gene id: 2066
15ERK11mitogen-activated protein kinase 3 isoform 2 [Homo sapiens] [gi:91718897]
Taxonomy id: 9606
Gene id: 5595
16ERK21mitogen-activated protein kinase 1 [Homo sapiens] [gi:66932916]
Taxonomy id: 9606
Gene id: 5594
17GSK3a1glycogen synthase kinase-3 alpha [Homo sapiens] [gi:49574532]
Taxonomy id: 9606
Gene id: 2931
18GSK3b1glycogen synthase kinase-3 beta isoform 2 [Homo sapiens] [gi:225903437]
Taxonomy id: 9606
Gene id: 2932
19IKKa1inhibitor of nuclear factor kappa-B kinase subunit alpha [Homo sapiens] [gi:62241001]
Taxonomy id: 9606
Gene id: 1147
20IKKb1inhibitor of nuclear factor kappa-B kinase subunit beta isoform 5 [Homo sapiens] [gi:338753358]
Taxonomy id: 9606
Gene id: 3551
21JAK11tyrosine-protein kinase JAK1 [Homo sapiens] [gi:102469034]
Taxonomy id: 9606
Gene id: 3716
22JNK11mitogen-activated protein kinase 8 isoform JNK1 alpha1 [Homo sapiens] [gi:4506095]
Taxonomy id: 9606
Gene id: 5599
23JNK21mitogen-activated protein kinase 9 isoform JNK2 gamma [Homo sapiens] [gi:205277412]
Taxonomy id: 9606
Gene id: 5601
24JNK31mitogen-activated protein kinase 10 isoform 1 [Homo sapiens] [gi:4506081]
Taxonomy id: 9606
Gene id: 5602
25MEK11dual specificity mitogen-activated protein kinase kinase 1 [Homo sapiens] [gi:5579478]
Taxonomy id: 9606
Gene id: 5604
26MEK21dual specificity mitogen-activated protein kinase kinase 2 [Homo sapiens] [gi:13489054]
Taxonomy id: 9606
Gene id: 5605
27MEKK21mitogen-activated protein kinase kinase kinase 2 [Homo sapiens] [gi:85838511]
Taxonomy id: 9606
Gene id: 10746
28MEKK31mitogen-activated protein kinase kinase kinase 3 isoform 2 [Homo sapiens] [gi:42794765]
Taxonomy id: 9606
Gene id: 4215
29MKK61dual specificity mitogen-activated protein kinase kinase 6 [Homo sapiens] [gi:14589900]
Taxonomy id: 9606
Gene id: 5608
30MLK31mitogen-activated protein kinase kinase kinase 11 [Homo sapiens] [gi:4505195]
Taxonomy id: 9606
Gene id: 4296
31P38a1mitogen-activated protein kinase 14 isoform 1 [Homo sapiens] [gi:4503069]
Taxonomy id: 9606
Gene id: 1432
32P38b1mitogen-activated protein kinase 11 [Homo sapiens] [gi:20128774]
Taxonomy id: 9606
Gene id: 5600
33P38d1mitogen-activated protein kinase 13 [Homo sapiens] [gi:4506085]
Taxonomy id: 9606
Gene id: 5603
34P38g1mitogen-activated protein kinase 12 [Homo sapiens] [gi:48255970]
Taxonomy id: 9606
Gene id: 6300
35p70S6K1ribosomal protein S6 kinase beta-1 [Homo sapiens] [gi:4506737]
Taxonomy id: 9606
Gene id: 6198
36p70S6Kb1ribosomal protein S6 kinase beta-2 [Homo sapiens] [gi:55953117]
Taxonomy id: 9606
Gene id: 6199
37PKCa1protein kinase C, alpha protein [synthetic construct] [gi:254071371]
Taxonomy id: 9606
Gene id: 5578
38PKCb11protein kinase C beta type isoform 2 [Homo sapiens] [gi:20127450]
Taxonomy id: 9606
Gene id: 5579
39PKCb21protein kinase C beta type isoform 2 [Homo sapiens] [gi:20127450]
Taxonomy id: 9606
Gene id: 5579
40PKCd1protein kinase C delta type [Homo sapiens] [gi:31377782]
Taxonomy id: 9606
Gene id: 5580
41PKCepsilon1protein kinase C epsilon type [Homo sapiens] [gi:4885563]
Taxonomy id: 9606
Gene id: 5581
42PKCeta1protein kinase C eta type [Homo sapiens] [gi:28557781]
Taxonomy id: 9606
Gene id: 5583
43PKCg1protein kinase C gamma type [Homo sapiens] [gi:13384594]
Taxonomy id: 9606
Gene id: 5582
44PKCiota1protein kinase C iota type [Homo sapiens] [gi:133908623]
Taxonomy id: 9606
Gene id: 5584
45PKCmu1serine/threonine-protein kinase D1 [Homo sapiens] [gi:115529463]
Taxonomy id: 9606
Gene id: 5587
46PKCnu1serine/threonine-protein kinase D3 [Homo sapiens] [gi:5031689]
Taxonomy id: 9606
Gene id: 23683
47PKCtheta1protein kinase C theta type isoform 2 [Homo sapiens] [gi:334848126]
Taxonomy id: 9606
Gene id: 5588
48PKCzeta1protein kinase C zeta type isoform 2 [Homo sapiens] [gi:75709226]
Taxonomy id: 9606
Gene id: 5590

§ Panel component ID.
Protocol
Assay Overview:

The purpose of this biochemical assay is to determine whether a powder sample of compound identified as a possible KLF5 inhibitor probe candidate can inhibit the activity of a panel of 48 available kinases. This in vitro kinase assay was performed by Reaction Biology Corporation (RBC). Each individual kinase activity was measured at a ATP concentration equivalent to its Km value for each kinase, as duplicate in presence of 10 uM of the test compound, and in the presence of an additional 10-point, 3:1 serial dilution of Staurosporine as a positive control to verify IC50 value.

Protocol Summary:

1. Prepare indicated substrate in freshly prepared Base Reaction Buffer.
2. Deliver any required cofactors to the substrate solution above.
3. Deliver indicated kinase into the substrate solution and gently mix.
4. Deliver compounds in DMSO into the kinase reaction mixture.
5. Deliver 33P-ATP (specific activity 500 uCi/ul) into the reaction mixture to initiate the reaction.
6. Incubate kinase reaction for 120 min. at room temperature.

The percent activity of each enzyme (kinase) following treatment with compound was normalized to the activity in the presence of DMSO alone. The individual duplicate reads and average of the duplicates are provided.

PubChem Activity Outcome and Score:

Compounds with an average % activity less than or equal to 80% or greater than or equal to 120% were considered active (in other words, a 20% change from the normalized DMSO value which was set as 100%). Compounds with an average % activity between 80% and 120% were considered inactive.

This compound was inactive against all 48 kinases tested.

List of Reagents:

Base Reaction buffer (20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/ml BSA, 0.1 mM Na3VO4, 2 mM DTT, 1% DMSO)
Additional details can be found at http://www.reactionbiology.com/
Comment
This assay was run by Reaction Biology Corporation. This assay may have been run as two or more separate campaigns, each campaign testing a unique set of compounds. All test compound concentrations reported above and below are nominal; the specific test concentration(s) for a particular compound may vary based upon the actual sample provided.
Categorized Comment
BAO: version: 1.4b1090

BAO: bioassay specification: assay readout content: assay readout method: regular screening

BAO: bioassay specification: assay readout content: content readout type: single readout

BAO: meta target: biological process target: cell proliferation

BAO: assay design: viability reporter: dna content

BAO: detection technology: absorbance

Result Definitions
Show more
TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Outcome [AKT1]Bioassay outcome.1RAC-alpha serine/threonine-protein kinase [Homo sapiens]Outcome
2Enzyme Activity [1] [AKT1] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.1Float%
3Enzyme Activity [2] [AKT1] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.1Float%
4Average Enzyme Activity [AKT1] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.1Float%
5Outcome [AKT2]Bioassay outcome.2RAC-beta serine/threonine-protein kinase isoform 2 [Homo sapiens]Outcome
6Enzyme Activity [1] [AKT2] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.2Float%
7Enzyme Activity [2] [AKT2] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.2Float%
8Average Enzyme Activity [AKT2] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.2Float%
9Outcome [AKT3]Bioassay outcome.3RAC-gamma serine/threonine-protein kinase isoform 2 [Homo sapiens]Outcome
10Enzyme Activity [1] [AKT3] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.3Float%
11Enzyme Activity [2] [AKT3] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.3Float%
12Average Enzyme Activity [AKT3] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.3Float%
13Outcome [Aurora A]Bioassay outcome.4aurora kinase A-interacting protein [Homo sapiens]Outcome
14Enzyme Activity [1] [Aurora A] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.4Float%
15Enzyme Activity [2] [Aurora A] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.4Float%
16Average Enzyme Activity [Aurora A] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.4Float%
17Outcome [BRAF]Bioassay outcome.5serine/threonine-protein kinase B-raf [Homo sapiens]Outcome
18Enzyme Activity [1] [BRAF] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.5Float%
19Enzyme Activity [2] [BRAF] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.5Float%
20Average Enzyme Activity [BRAF] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.5Float%
21Outcome [CDK1/cyclin A]Bioassay outcome.6cyclin-dependent kinase 1 isoform 4 [Homo sapiens]
cyclin-A2 [Homo sapiens]
Outcome
22Enzyme Activity [1] [CDK1/cyclin A] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.6Float%
23Enzyme Activity [2] [CDK1/cyclin A] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.6Float%
24Average Enzyme Activity [CDK1/cyclin A] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.6Float%
25Outcome [CDK1/cyclin B]Bioassay outcome.7cyclin-dependent kinase 1 isoform 4 [Homo sapiens]
G2/mitotic-specific cyclin-B1 [Homo sapiens]
Outcome
26Enzyme Activity [1] [CDK1/cyclin B] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.7Float%
27Enzyme Activity [2] [CDK1/cyclin B] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.7Float%
28Average Enzyme Activity [CDK1/cyclin B] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.7Float%
29Outcome [CDK2/cyclin A]Bioassay outcome.8cyclin-dependent kinase 2 isoform 1 [Homo sapiens]
cyclin-A2 [Homo sapiens]
Outcome
30Enzyme Activity [1] [CDK2/cyclin A] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.8Float%
31Enzyme Activity [2] [CDK2/cyclin A] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.8Float%
32Average Enzyme Activity [CDK2/cyclin A] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.8Float%
33Outcome [CDK2/cyclin E]Bioassay outcome.9cyclin-dependent kinase 2 isoform 1 [Homo sapiens]
G1/S-specific cyclin-E1 [Homo sapiens]
Outcome
34Enzyme Activity [1] [CDK2/cyclin E] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.9Float%
35Enzyme Activity [2] [CDK2/cyclin E] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.9Float%
36Average Enzyme Activity [CDK2/cyclin E] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.9Float%
37Outcome [CDK5/p25]Bioassay outcome.10cyclin-dependent kinase 5 isoform 2 [Homo sapiens]
cyclin-dependent kinase 5 activator 1 [Homo sapiens]
Outcome
38Enzyme Activity [1] [CDK5/p25] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.10Float%
39Enzyme Activity [2] [CDK5/p25] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.10Float%
40Average Enzyme Activity [CDK5/p25] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.10Float%
41Outcome [CDK5/p35]Bioassay outcome.11cyclin-dependent kinase 5 isoform 2 [Homo sapiens]
cyclin-dependent kinase 5 activator 1 [Homo sapiens]
Outcome
42Enzyme Activity [1] [CDK5/p35] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.11Float%
43Enzyme Activity [2] [CDK5/p35] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.11Float%
44Average Enzyme Activity [CDK5/p35] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.11Float%
45Outcome [EGFR]Bioassay outcome.12epidermal growth factor receptor [Homo sapiens]Outcome
46Enzyme Activity [1] [EGFR] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.12Float%
47Enzyme Activity [2] [EGFR] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.12Float%
48Average Enzyme Activity [EGFR] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.12Float%
49Outcome [ERBB2]Bioassay outcome.13receptor tyrosine-protein kinase erbB-2 isoform b [Homo sapiens]Outcome
50Enzyme Activity [1] [ERBB2] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.13Float%
51Enzyme Activity [2] [ERBB2] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.13Float%
52Average Enzyme Activity [ERBB2] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.13Float%
53Outcome [ERBB4]Bioassay outcome.14receptor tyrosine-protein kinase erbB-4 isoform JM-a/CVT-2 precursor [Homo sapiens]Outcome
54Enzyme Activity [1] [ERBB4] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.14Float%
55Enzyme Activity [2] [ERBB4] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.14Float%
56Average Enzyme Activity [ERBB4] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.14Float%
57Outcome [ERK1]Bioassay outcome.15mitogen-activated protein kinase 3 isoform 2 [Homo sapiens]Outcome
58Enzyme Activity [1] [ERK1] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.15Float%
59Enzyme Activity [2] [ERK1] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.15Float%
60Average Enzyme Activity [ERK1] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.15Float%
61Outcome [ERK2]Bioassay outcome.16mitogen-activated protein kinase 1 [Homo sapiens]Outcome
62Enzyme Activity [1] [ERK2] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.16Float%
63Enzyme Activity [2] [ERK2] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.16Float%
64Average Enzyme Activity [ERK2] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.16Float%
65Outcome [GSK3a]Bioassay outcome.17glycogen synthase kinase-3 alpha [Homo sapiens]Outcome
66Enzyme Activity [1] [GSK3a] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.17Float%
67Enzyme Activity [2] [GSK3a] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.17Float%
68Average Enzyme Activity [GSK3a] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.17Float%
69Outcome [GSK3b]Bioassay outcome.18glycogen synthase kinase-3 beta isoform 2 [Homo sapiens]Outcome
70Enzyme Activity [1] [GSK3b] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.18Float%
71Enzyme Activity [2] [GSK3b] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.18Float%
72Average Enzyme Activity [GSK3b] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.18Float%
73Outcome [IKKa]Bioassay outcome.19inhibitor of nuclear factor kappa-B kinase subunit alpha [Homo sapiens]Outcome
74Enzyme Activity [1] [IKKa] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.19Float%
75Enzyme Activity [2] [IKKa] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.19Float%
76Average Enzyme Activity [IKKa] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.19Float%
77Outcome [IKKb]Bioassay outcome.20inhibitor of nuclear factor kappa-B kinase subunit beta isoform 5 [Homo sapiens]Outcome
78Enzyme Activity [1] [IKKb] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.20Float%
79Enzyme Activity [2] [IKKb] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.20Float%
80Average Enzyme Activity [IKKb] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.20Float%
81Outcome [JAK1]Bioassay outcome.21tyrosine-protein kinase JAK1 [Homo sapiens]Outcome
82Enzyme Activity [1] [JAK1] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.21Float%
83Enzyme Activity [2] [JAK1] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.21Float%
84Average Enzyme Activity [JAK1] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.21Float%
85Outcome [JNK1]Bioassay outcome.22mitogen-activated protein kinase 8 isoform JNK1 alpha1 [Homo sapiens]Outcome
86Enzyme Activity [1] [JNK1] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.22Float%
87Enzyme Activity [2] [JNK1] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.22Float%
88Average Enzyme Activity [JNK1] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.22Float%
89Outcome [JNK2]Bioassay outcome.23mitogen-activated protein kinase 9 isoform JNK2 gamma [Homo sapiens]Outcome
90Enzyme Activity [1] [JNK2] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.23Float%
91Enzyme Activity [2] [JNK2] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.23Float%
92Average Enzyme Activity [JNK2] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.23Float%
93Outcome [JNK3]Bioassay outcome.24mitogen-activated protein kinase 10 isoform 1 [Homo sapiens]Outcome
94Enzyme Activity [1] [JNK3] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.24Float%
95Enzyme Activity [2] [JNK3] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.24Float%
96Average Enzyme Activity [JNK3] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.24Float%
97Outcome [MEK1]Bioassay outcome.25dual specificity mitogen-activated protein kinase kinase 1 [Homo sapiens]Outcome
98Enzyme Activity [1] [MEK1] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.25Float%
99Enzyme Activity [2] [MEK1] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.25Float%
100Average Enzyme Activity [MEK1] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.25Float%
101Outcome [MEK2]Bioassay outcome.26dual specificity mitogen-activated protein kinase kinase 2 [Homo sapiens]Outcome
102Enzyme Activity [1] [MEK2] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.26Float%
103Enzyme Activity [2] [MEK2] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.26Float%
104Average Enzyme Activity [MEK2] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.26Float%
105Outcome [MEKK2]Bioassay outcome.27mitogen-activated protein kinase kinase kinase 2 [Homo sapiens]Outcome
106Enzyme Activity [1] [MEKK2] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.27Float%
107Enzyme Activity [2] [MEKK2] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.27Float%
108Average Enzyme Activity [MEKK2] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.27Float%
109Outcome [MEKK3]Bioassay outcome.28mitogen-activated protein kinase kinase kinase 3 isoform 2 [Homo sapiens]Outcome
110Enzyme Activity [1] [MEKK3] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.28Float%
111Enzyme Activity [2] [MEKK3] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.28Float%
112Average Enzyme Activity [MEKK3] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.28Float%
113Outcome [MKK6]Bioassay outcome.29dual specificity mitogen-activated protein kinase kinase 6 [Homo sapiens]Outcome
114Enzyme Activity [1] [MKK6] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.29Float%
115Enzyme Activity [2] [MKK6] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.29Float%
116Average Enzyme Activity [MKK6] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.29Float%
117Outcome [MLK3]Bioassay outcome.30mitogen-activated protein kinase kinase kinase 11 [Homo sapiens]Outcome
118Enzyme Activity [1] [MLK3] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.30Float%
119Enzyme Activity [2] [MLK3] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.30Float%
120Average Enzyme Activity [MLK3] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.30Float%
121Outcome [P38a]Bioassay outcome.31mitogen-activated protein kinase 14 isoform 1 [Homo sapiens]Outcome
122Enzyme Activity [1] [P38a] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.31Float%
123Enzyme Activity [2] [P38a] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.31Float%
124Average Enzyme Activity [P38a] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.31Float%
125Outcome [P38b]Bioassay outcome.32mitogen-activated protein kinase 11 [Homo sapiens]Outcome
126Enzyme Activity [1] [P38b] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.32Float%
127Enzyme Activity [2] [P38b] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.32Float%
128Average Enzyme Activity [P38b] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.32Float%
129Outcome [P38d]Bioassay outcome.33mitogen-activated protein kinase 13 [Homo sapiens]Outcome
130Enzyme Activity [1] [P38d] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.33Float%
131Enzyme Activity [2] [P38d] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.33Float%
132Average Enzyme Activity [P38d] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.33Float%
133Outcome [P38g]Bioassay outcome.34mitogen-activated protein kinase 12 [Homo sapiens]Outcome
134Enzyme Activity [1] [P38g] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.34Float%
135Enzyme Activity [2] [P38g] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.34Float%
136Average Enzyme Activity [P38g] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.34Float%
137Outcome [p70S6K]Bioassay outcome.35ribosomal protein S6 kinase beta-1 [Homo sapiens]Outcome
138Enzyme Activity [1] [p70S6K] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.35Float%
139Enzyme Activity [2] [p70S6K] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.35Float%
140Average Enzyme Activity [p70S6K] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.35Float%
141Outcome [p70S6Kb]Bioassay outcome.36ribosomal protein S6 kinase beta-2 [Homo sapiens]Outcome
142Enzyme Activity [1] [p70S6Kb] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.36Float%
143Enzyme Activity [2] [p70S6Kb] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.36Float%
144Average Enzyme Activity [p70S6Kb] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.36Float%
145Outcome [PKCa]Bioassay outcome.37protein kinase C, alpha protein [synthetic construct]Outcome
146Enzyme Activity [1] [PKCa] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.37Float%
147Enzyme Activity [2] [PKCa] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.37Float%
148Average Enzyme Activity [PKCa] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.37Float%
149Outcome [PKCb1]Bioassay outcome.38protein kinase C beta type isoform 2 [Homo sapiens]Outcome
150Enzyme Activity [1] [PKCb1] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.38Float%
151Enzyme Activity [2] [PKCb1] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.38Float%
152Average Enzyme Activity [PKCb1] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.38Float%
153Outcome [PKCb2]Bioassay outcome.39protein kinase C beta type isoform 2 [Homo sapiens]Outcome
154Enzyme Activity [1] [PKCb2] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.39Float%
155Enzyme Activity [2] [PKCb2] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.39Float%
156Average Enzyme Activity [PKCb2] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.39Float%
157Outcome [PKCd]Bioassay outcome.40protein kinase C delta type [Homo sapiens]Outcome
158Enzyme Activity [1] [PKCd] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.40Float%
159Enzyme Activity [2] [PKCd] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.40Float%
160Average Enzyme Activity [PKCd] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.40Float%
161Outcome [PKCepsilon]Bioassay outcome.41protein kinase C epsilon type [Homo sapiens]Outcome
162Enzyme Activity [1] [PKCepsilon] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.41Float%
163Enzyme Activity [2] [PKCepsilon] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.41Float%
164Average Enzyme Activity [PKCepsilon] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.41Float%
165Outcome [PKCeta]Bioassay outcome.42protein kinase C eta type [Homo sapiens]Outcome
166Enzyme Activity [1] [PKCeta] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.42Float%
167Enzyme Activity [2] [PKCeta] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.42Float%
168Average Enzyme Activity [PKCeta] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.42Float%
169Outcome [PKCg]Bioassay outcome.43protein kinase C gamma type [Homo sapiens]Outcome
170Enzyme Activity [1] [PKCg] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.43Float%
171Enzyme Activity [2] [PKCg] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.43Float%
172Average Enzyme Activity [PKCg] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.43Float%
173Outcome [PKCiota]Bioassay outcome.44protein kinase C iota type [Homo sapiens]Outcome
174Enzyme Activity [1] [PKCiota] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.44Float%
175Enzyme Activity [2] [PKCiota] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.44Float%
176Average Enzyme Activity [PKCiota] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.44Float%
177Outcome [PKCmu]Bioassay outcome.45serine/threonine-protein kinase D1 [Homo sapiens]Outcome
178Enzyme Activity [1] [PKCmu] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.45Float%
179Enzyme Activity [2] [PKCmu] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.45Float%
180Average Enzyme Activity [PKCmu] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.45Float%
181Outcome [PKCnu]Bioassay outcome.46serine/threonine-protein kinase D3 [Homo sapiens]Outcome
182Enzyme Activity [1] [PKCnu] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.46Float%
183Enzyme Activity [2] [PKCnu] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.46Float%
184Average Enzyme Activity [PKCnu] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.46Float%
185Outcome [PKCtheta]Bioassay outcome.47protein kinase C theta type isoform 2 [Homo sapiens]Outcome
186Enzyme Activity [1] [PKCtheta] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.47Float%
187Enzyme Activity [2] [PKCtheta] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.47Float%
188Average Enzyme Activity [PKCtheta] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.47Float%
189Outcome [PKCzeta]Bioassay outcome.48protein kinase C zeta type isoform 2 [Homo sapiens]Outcome
190Enzyme Activity [1] [PKCzeta] (10μM**)First Replicate value of the radioactivity of the indicated kinase activity (%), normalized to DMSO.48Float%
191Enzyme Activity [2] [PKCzeta] (10μM**)Second Replicate value of the radioactivity of the indicated kinase (%),normalized to DMSO.48Float%
192Average Enzyme Activity [PKCzeta] (10μM**)Average value of the radioactivity of the indicated kinase (%),normalized to DMSO.48Float%

** Test Concentration. § Panel component ID.
Additional Information
Grant Number: 1-R03-DA026215-01

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