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559-68-2 靶点实验数据

HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Rattus norvegicus
External ID: CHEMBL2149252
Protocol: N/A
Comment: Journal: Eur. J. Med. Chem.
Year: 2011
Volume: 46
Issue: 6
First Page: 2243
Last Page: 2251
DOI: 10.1016/j.ejmech.2011.03.005

Target ChEMBL ID: CHEMBL376
ChEMBL Target Name: Rattus norvegicus
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard Units
Activity=14.1mg/dl
Activity=24.45mg/dl
Activity=15.23mg/dl
Activity=26.3mg/dl
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Rattus norvegicus
External ID: CHEMBL2149253
Protocol: N/A
Comment: Journal: Eur. J. Med. Chem.
Year: 2011
Volume: 46
Issue: 6
First Page: 2243
Last Page: 2251
DOI: 10.1016/j.ejmech.2011.03.005

Target ChEMBL ID: CHEMBL376
ChEMBL Target Name: Rattus norvegicus
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard Units
Activity=23.2mg/dl
Activity=25.66mg/dl
Activity=8.77mg/dl
Activity=15.3mg/dl
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Rattus norvegicus
External ID: CHEMBL2149251
Protocol: N/A
Comment: Journal: Eur. J. Med. Chem.
Year: 2011
Volume: 46
Issue: 6
First Page: 2243
Last Page: 2251
DOI: 10.1016/j.ejmech.2011.03.005

Target ChEMBL ID: CHEMBL376
ChEMBL Target Name: Rattus norvegicus
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard Units
Activity=26.92mg/dl
Activity=13.46mg/dl
Activity=1.54mg/dl
Activity=17.3mg/dl
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Tyrosine-protein phosphatase non-receptor type 1
External ID: CHEMBL2149371
Protocol: N/A
Comment: Journal: Eur. J. Med. Chem.
Year: 2011
Volume: 46
Issue: 6
First Page: 2243
Last Page: 2251
DOI: 10.1016/j.ejmech.2011.03.005

Target ChEMBL ID: CHEMBL335
ChEMBL Target Name: Protein-tyrosine phosphatase 1B
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: D - Direct protein target assigned
Confidence: Direct single protein target assigned
Standard TypeStandard UnitsActivity Comment
Inhibition%Active
Inhibition%Active
Inhibition%Active
Inhibition%Active
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Tyrosine-protein phosphatase non-receptor type 1
External ID: CHEMBL2149372
Protocol: N/A
Comment: Compounds with activity <= 10uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Journal: Eur. J. Med. Chem.
Year: 2011
Volume: 46
Issue: 6
First Page: 2243
Last Page: 2251
DOI: 10.1016/j.ejmech.2011.03.005

Target ChEMBL ID: CHEMBL335
ChEMBL Target Name: Protein-tyrosine phosphatase 1B
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: D - Direct protein target assigned
Confidence: Direct single protein target assigned
PubChem Standard ValueStandard TypeStandard RelationStandard ValueStandard UnitsActivity Comment
Inhibition%Dose-dependent effect
9.1IC50=9100nM
Inhibition%Dose-dependent effect
13.2IC50=13200nM
Inhibition%Dose-dependent effect
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Rattus norvegicus
External ID: CHEMBL2149254
Protocol: N/A
Comment: Journal: Eur. J. Med. Chem.
Year: 2011
Volume: 46
Issue: 6
First Page: 2243
Last Page: 2251
DOI: 10.1016/j.ejmech.2011.03.005

Target ChEMBL ID: CHEMBL376
ChEMBL Target Name: Rattus norvegicus
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard Units
Activity=21.92mg/dl
Activity=38.01mg/dl
Activity=39.18mg/dl
Activity=29.2mg/dl
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Human immunodeficiency virus 1
External ID: CHEMBL949642
Protocol: N/A
Comment: Journal: J. Nat. Prod.
Year: 2001
Volume: 64
Issue: 10
First Page: 1278
Last Page: 1281
DOI: 10.1021/np010211x

Target ChEMBL ID: CHEMBL378
ChEMBL Target Name: Human immunodeficiency virus 1
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard UnitsActivity Comment
EC50Not Active
EC50=0.00289ug.mL-1
EC50=0.22ug.mL-1
EC50Not Active
EC50Not Active
EC50Not Active
EC50=2.19ug.mL-1
EC50=2.7ug.mL-1
EC50<0.1ug.mL-1
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:H9
External ID: CHEMBL949641
Protocol: N/A
Comment: Journal: J. Nat. Prod.
Year: 2001
Volume: 64
Issue: 10
First Page: 1278
Last Page: 1281
DOI: 10.1021/np010211x

Target ChEMBL ID: CHEMBL614806
ChEMBL Target Name: H9
ChEMBL Target Type: CELL-LINE - Target is a specific cell-line
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard UnitsData Validity Comment
IC50>100ug.mL-1Outside typical range
IC50=500ug.mL-1Outside typical range
IC50=1.8ug.mL-1
IC50=0.205ug.mL-1
IC50=2.14ug.mL-1
IC50=18.8ug.mL-1
IC50=18.9ug.mL-1
IC50=22.1ug.mL-1
IC50=18.6ug.mL-1
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:NIAID 靶标:N/A
External ID: HIV Cellular Data
Protocol: N/A
Comment: N/A
SpeciesStrainIsPseudotypeVirusAssayMethCellTypeCellType2TargetMutationsEC50ModEC50EC50UnitECOtherPctECOtherPctUnitECOtherConcECOtherConcUnitToxAssayMethToxCellTypeCC50ModCC50CC50UnitTIModTIRelResFoldChgCommentsReferenceCitationOther Information
HIV-1LAIRTHuT TK+HuT 78Reverse transcriptase<1uM100%1uMMTT>10uM>10HuT TK+=HuT 78 CELLS EXPRESSING HSV-1 THYMIDINE KINASE; MEASUREMENT WAS MADE ON DAY10 POSTINFECTION AT 10 TCID509281520USE OF HERPES SIMPLEX VIRUS THYMIDINE KINASE TO IMPROVE THE ANTIVIRAL ACTIVITY OF ZIDOVUDINE. Virology 1997, 235, 398-405.
HIV-1MNRTHuT TK+HuT 78Reverse transcriptase<0.3uM76.74%0.3uMMTT>10uM>33.3HuT TK+=HuT 78 CELLS EXPRESSING HSV-1 THYMIDINE KINASE; MEASUREMENT WAS MADE ON DAY14 POSTINFECTION AT 10 TCID509281520USE OF HERPES SIMPLEX VIRUS THYMIDINE KINASE TO IMPROVE THE ANTIVIRAL ACTIVITY OF ZIDOVUDINE. Virology 1997, 235, 398-405.
HIV-1MNRTHuT TK+HuT 78Reverse transcriptase<0.3uM69%0.3uMMTT>10uM>33.3HuT TK+=HuT 78 CELLS EXPRESSING HSV-1 THYMIDINE KINASE; MEASUREMENT WAS MADE ON DAY14 POSTINFECTION AT 100 TCID509281520USE OF HERPES SIMPLEX VIRUS THYMIDINE KINASE TO IMPROVE THE ANTIVIRAL ACTIVITY OF ZIDOVUDINE. Virology 1997, 235, 398-405.
R5; CLINICAL ISOLATE1(JSL)P24PBMCReverse transcriptaseMDR0.07uM90%1uMMTT>100uM>1428HIV-1(JSL) WAS ISOLATED FROM PATIENTS WHO RECEIVED ANTIRETROVIRAL THERAPY FOR A LONG PERIOD AND WHOSE VIRUS ACQUIRED A NUMBER OF MUTATIONS IN THE RT- AND PR-ENCODING GENES; DETAILS OF MUTATIONS NOT GIVEN15280474SPIRODIKETOPIPERAZINE-BASED CCR5 INHIBITOR WHICH PRESERVES CC-CHEMOKINE/CCR5 INTERACTIONS AND EXERTS POTENT ACTIVITY AGAINST R5 HUMAN IMMUNODEFICIENCY VIRUS TYPE 1 IN VITRO. Journal of Virology 2004, 78(16), 8654-8662.ECOtherConcMod:>
HIV-1NL4-3LUCIFERASE1G5 TReverse transcriptase<1uM99%1uMTRYPAN BLUE>1uM>1ASSAY WAS CONDUCTED ON DAY 3 POST-INFECTION16725040INHIBITION OF HIGHLY PRODUCTIVE HIV-1 INFECTION IN T CELLS, PRIMARY HUMAN MACROPHAGES, MICROGLIA, AND ASTROCYTES BY SARGASSUM FUSIFORME. AIDS Research and Therapy 2006, 3(1), 15 PP.CCOtherPct:6 | CCOtherPctUnit:% | CCOtherConc:1 | CCOtherConcUnit:uM
HIV-1NL4-3LUCIFERASE1G5 TReverse transcriptase<1uM99%1uMTRYPAN BLUE>1uM>1ASSAY WAS CONDUCTED ON DAY 5 POST-INFECTION16725040INHIBITION OF HIGHLY PRODUCTIVE HIV-1 INFECTION IN T CELLS, PRIMARY HUMAN MACROPHAGES, MICROGLIA, AND ASTROCYTES BY SARGASSUM FUSIFORME. AIDS Research and Therapy 2006, 3(1), 15 PP.CCOtherPct:7 | CCOtherPctUnit:% | CCOtherConc:1 | CCOtherConcUnit:uM
HIV-1NL4-3LUCIFERASE1G5 TReverse transcriptase<1uM99%1uMTRYPAN BLUE>1uM>1ASSAY WAS CONDUCTED ON DAY 7 POST-INFECTION16725040INHIBITION OF HIGHLY PRODUCTIVE HIV-1 INFECTION IN T CELLS, PRIMARY HUMAN MACROPHAGES, MICROGLIA, AND ASTROCYTES BY SARGASSUM FUSIFORME. AIDS Research and Therapy 2006, 3(1), 15 PP.CCOtherPct:3 | CCOtherPctUnit:% | CCOtherConc:1 | CCOtherConcUnit:uM
HIV-1LAVRTU1(THF-.alpha. STIM)U1Tumor necrosis factor alpha~30ug/mL70%50ug/mL>50ug/mL>1.66CHRONICALLY HIV-1 INFECTED PROMONOCYTE CELL LINE8327469THALIDOMIDE INHIBITS THE REPLICATION OF HUMAN IMMUNODEFICIENCY VIRUS TYPE 1. Proceedings of the National Academy of Sciences of the United States of America 1993, 90, 5974-5978.CCOtherPct:0 | CCOtherPctUnit:% | CCOtherConc:50 | CCOtherConcUnit:ug/mL
HIV-1BaLP24 (DAY 18)MACROPHAGES(GM-CSF)MacrophageRibonucleotide reductase<10uM75%10uM>1000uM>10MAXIMAL P24 EXPRESSION AT DAY 187973634HYDROXYUREA AS AN INHIBITOR OF HUMAN IMMUNODEFICIENCY VIRUS-TYPE 1 REPLICATION. Science 1994, 266(5186), 801-805.CCOtherPct:0 | CCOtherPctUnit:% | CCOtherConc:1000 | CCOtherConcUnit:uM
HIV-1BaLP24 (DAY 18)MACROPHAGES(GM-CSF)MacrophageRibonucleotide reductase<10uM38%2uM>1000uM>10MAXIMAL P24 EXPRESSION AT DAY 187973634HYDROXYUREA AS AN INHIBITOR OF HUMAN IMMUNODEFICIENCY VIRUS-TYPE 1 REPLICATION. Science 1994, 266(5186), 801-805.CCOtherPct:0 | CCOtherPctUnit:% | CCOtherConc:1000 | CCOtherConcUnit:uM
HIV-1BaLP24 (DAY 18)MACROPHAGES(GM-CSF)MacrophageRibonucleotide reductase<10uM99%50uM>1000uM>10MAXIMAL P24 EXPRESSION AT DAY 187973634HYDROXYUREA AS AN INHIBITOR OF HUMAN IMMUNODEFICIENCY VIRUS-TYPE 1 REPLICATION. Science 1994, 266(5186), 801-805.ECOtherPctMod:> | CCOtherPct:0 | CCOtherPctUnit:% | CCOtherConc:1000 | CCOtherConcUnit:uM
HIV-1IIIBRTHT4(R116; AZT RESISTANT CELLS)HT4Reverse transcriptase~0.01uM70%0.01uM~`1uM~100FLOXURIDINE APPEARS TO POTENTIATE AZT ACTIVITY AND ALSO HAVE SOME ANTI-HIV ACTIVITY IN AZT RESISTANT CELL LINES8827211USE OF FLOXURIDINE TO MODULATE THE ANTIVIRAL ACTIVITY OF ZIDOVUDINE. AIDS Research and Human Retroviruses 1996, 12(11), 965-968.ECOtherPctMod:~ | CCOtherPct:35 | CCOtherPctUnit:% | CCOtherConc:.1 | CCOtherConcUnit:uM
HIV-11.beta.GAL AS A MEASURE OF TAT-MEDIATED TRANSACTIVATIONHeLa H12(HIV-1 LTR-Laz, TAT)HeLaTat:TAR/LTR<0.1uM52%0.1uMTRYPAN BLUE>100uM>1000DRUG AND RECOMBINANT TAT WERE INTRODUCED INTO CELLS THROUGH ELECTROPORATION9561563CURCUMIN AND CURCUMIN DERIVATIVES INHIBIT TAT-MEDIATED TRANSACTIVATION OF TYPE 1 HUMAN IMMUNODEFICIENCY VIRUS LONG TERMINAL REPEAT. Research in Virology 1998, 149(1), 43-52.
HIV-11.beta.GAL AS A MEASURE OF TAT-MEDIATED TRANSACTIVATIONHeLa H12(HIV-1 LTR-Laz, TAT)HeLaTat:TAR/LTR<0.01uM78%0.01uMTRYPAN BLUE>100uM>10000DRUG AND RECOMBINANT TAT WERE INTRODUCED INTO CELLS THROUGH ELECTROPORATION9561563CURCUMIN AND CURCUMIN DERIVATIVES INHIBIT TAT-MEDIATED TRANSACTIVATION OF TYPE 1 HUMAN IMMUNODEFICIENCY VIRUS LONG TERMINAL REPEAT. Research in Virology 1998, 149(1), 43-52.
HIV-1IIIBSYNCYT FORMMOLT-4/H9(HIV-1(IIIB))MOLT-4gp120<1uM95%10uM-10010uM>10CHRONICALLY INFECTED H9 CELLS9343823TRIAZINE DYES INHIBIT HIV-1 ENTRY BY BINDING TO ENVELOPE GLYCOPROTEINS. Microbiology and Immunology 1997, 41(9), 717-724.CCOtherPct:30 | CCOtherPctUnit:% | CCOtherConc:10 | CCOtherConcUnit:uM
HIV-11.beta.GAL AS A MEASURE OF TAT-MEDIATED TRANSACTIVATIONHeLa H12(HIV-1 LTR-Laz, TAT)HeLaTat:TAR/LTR<0.01uM75%0.01uMTRYPAN BLUE>100uM>10000DRUG AND RECOMBINANT TAT WERE INTRODUCED INTO CELLS THROUGH ELECTROPORATION9561563CURCUMIN AND CURCUMIN DERIVATIVES INHIBIT TAT-MEDIATED TRANSACTIVATION OF TYPE 1 HUMAN IMMUNODEFICIENCY VIRUS LONG TERMINAL REPEAT. Research in Virology 1998, 149(1), 43-52.
HIV-11P24MT-4Integrase<0.25uM95%0.25uMMICROSCOPIC EXAMINATION>20uM>80IN THE PRESENCE OF 50% NHS16554152A SERIES OF 5-AMINOSUBSTITUTED 4-FLUOROBENZYL-8-HYDROXY-[1,6]NAPHTHYRIDINE-7-CARBOXAMIDE HIV-1 INTEGRASE INHIBITORS. Bioorganic & Medical Chemistry Letters 2006, 16(11), 2900-2904.ECOtherPctMod:>
HIV-11P24MT-4Integrase<0.103uM95%0.103uMMICROSCOPIC EXAMINATION>20uM>194IN THE PRESENCE OF 10% FBS16554152A SERIES OF 5-AMINOSUBSTITUTED 4-FLUOROBENZYL-8-HYDROXY-[1,6]NAPHTHYRIDINE-7-CARBOXAMIDE HIV-1 INTEGRASE INHIBITORS. Bioorganic & Medical Chemistry Letters 2006, 16(11), 2900-2904.ECOtherPctMod:>
HIV-1NL4-3RTMT-4Reverse transcriptase<1uM100%1uMWST-8>1uM>1MEASUREMENTS WERE MADE ON DAY 4, 6 AND 8 POST INFECTION15371436POLYARGININE INHIBITS GP160 PROCESSING BY FURIN AND SUPPRESSES PRODUCTIVE HUMAN IMMUNODEFICIENCY VIRUS TYPE 1 INFECTION. The Journal of Biological Chemistry 2004, 279(47), 49055-49063.
HIV-1LAIRTHuT 78Reverse transcriptase<1uM57.14%1uMMTT>10uM>10MEASUREMENT WAS MADE ON DAY10 POSTINFECTION AT 10 TCID509281520USE OF HERPES SIMPLEX VIRUS THYMIDINE KINASE TO IMPROVE THE ANTIVIRAL ACTIVITY OF ZIDOVUDINE. Virology 1997, 235, 398-405.
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:N/A
External ID: CHEMBL949643
Protocol: N/A
Comment: Journal: J. Nat. Prod.
Year: 2001
Volume: 64
Issue: 10
First Page: 1278
Last Page: 1281
DOI: 10.1021/np010211x
Standard TypeStandard RelationStandard ValueActivity Comment
Ratio IC50/EC50Not Active
Ratio IC50/EC50=173000
Ratio IC50/EC50=8
Ratio IC50/EC50Not Active
Ratio IC50/EC50Not Active
Ratio IC50/EC50Not Active
Ratio IC50/EC50=8.62
Ratio IC50/EC50=8.17
Ratio IC50/EC50>186