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151-41-7 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:Histone deacetylase 6
External ID: CHEMBL4808149
Protocol: N/A
Comment: Target ChEMBL ID: CHEMBL1865
ChEMBL Target Name: Histone deacetylase 6
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: D - Direct protein target assigned
Confidence: Direct single protein target assigned

Data Source: Fraunhofer Institute HDAC6 screening
Standard TypeStandard RelationStandard ValueStandard Text ValueStandard UnitsData Validity Comment
Inhibition=-13.63%Outside typical range
Inhibition=-37.85%Outside typical range
Inhibition=-31.68%Outside typical range
Inhibition=-40.84%Outside typical range
Inhibition=-33.51%Outside typical range
Inhibition=-11.71%Outside typical range
Inhibition=-12.48%Outside typical range
Inhibition=8.75%
Inhibition=-57.22%Outside typical range
Inhibition=-43.91%Outside typical range
Inhibition=-42.06%Outside typical range
Inhibition=25.26%
Inhibition=31.78%
Inhibition=-63.83%Outside typical range
Inhibition=1.14%
Inhibition=-17.63%Outside typical range
Inhibition=14.49%
Inhibition=3.28%
Inhibition=10.08%
Inhibition=13.93%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Histone deacetylase 6
External ID: CHEMBL4808150
Protocol: N/A
Comment: Target ChEMBL ID: CHEMBL1865
ChEMBL Target Name: Histone deacetylase 6
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: D - Direct protein target assigned
Confidence: Direct single protein target assigned

Data Source: Fraunhofer Institute HDAC6 screening
Standard TypeStandard RelationStandard ValueStandard Text ValueStandard UnitsData Validity Comment
Inhibition=-7.39%
Inhibition=-3.08%
Inhibition=97.8%
Inhibition=-9.09%
Inhibition=47.05%
Inhibition=-5.94%
Inhibition=-0.48%
Inhibition=-2.98%
Inhibition=1.42%
Inhibition=12.25%
Inhibition=-2.13%
Inhibition=-4.43%
Inhibition=4.53%
Inhibition=-5.82%
Inhibition=10.36%
Inhibition=-1.3%
Inhibition=12.9%
Inhibition=-3.37%
Inhibition=3.17%
Inhibition=-0.97%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Severe acute respiratory syndrome coronavirus 2
External ID: CHEMBL4513082
Protocol: N/A
Comment: Target ChEMBL ID: CHEMBL4303835
ChEMBL Target Name: SARS-CoV-2
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular

Data Source: SARS-CoV-2 Screening Data
Standard TypeStandard RelationStandard ValueStandard Units
Inhibition=0.24%
Inhibition=4.58%
Inhibition=-0.3%
Inhibition=-0.3%
Inhibition=-0.04%
Inhibition=-0.04%
Inhibition=-0.08%
Inhibition=-0.08%
Inhibition=-0.08%
Inhibition=-0.08%
Inhibition=0.03%
Inhibition=0%
Inhibition=0.03%
Inhibition=0%
Inhibition=-0.27%
Inhibition=-0.27%
Inhibition=-0.08%
Inhibition=-0.08%
Inhibition=14.41%
Inhibition=0.39%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Severe acute respiratory syndrome coronavirus 2
External ID: CHEMBL4303805
Protocol: N/A
Comment: Target ChEMBL ID: CHEMBL4303835
ChEMBL Target Name: SARS-CoV-2
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular

Data Source: SARS-CoV-2 Screening Data
Standard TypeStandard RelationStandard ValueStandard UnitsData Validity Comment
Inhibition=-11.52%Outside typical range
Inhibition=5.09%
Inhibition=-1.71%
Inhibition=3.69%
Inhibition=22.47%
Inhibition=8.51%
Inhibition=-6.86%
Inhibition=-6.18%
Inhibition=-2.07%
Inhibition=3.91%
Inhibition=-5.9%
Inhibition=-2.45%
Inhibition=-5.55%
Inhibition=6.31%
Inhibition=-1.08%
Inhibition=12.7%
Inhibition=0.37%
Inhibition=8.88%
Inhibition=11.63%
Inhibition=-1.96%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Replicase polyprotein 1ab
External ID: CHEMBL4495582
Protocol: N/A
Comment: Target ChEMBL ID: CHEMBL4523582
ChEMBL Target Name: Replicase polyprotein 1ab
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: D - Direct protein target assigned
Confidence: Direct single protein target assigned

Data Source: SARS-CoV-2 Screening Data
Standard TypeStandard RelationStandard ValueStandard UnitsData Validity Comment
Inhibition=13.77%
Inhibition=2.35%
Inhibition=21.17%
Inhibition=18.36%
Inhibition=5.381%
Inhibition=18.17%
Inhibition=10.15%
Inhibition=29.56%
Inhibition=18.27%
Inhibition=11.42%
Inhibition=15.4%
Inhibition=7.437%
Inhibition=-3.216%
Inhibition=18%
Inhibition=1.021%
Inhibition=16.4%
Inhibition=2.544%
Inhibition=19.11%
Inhibition=26.15%
Inhibition=5.133%
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.