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481-96-9 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:Solute carrier organic anion transporter family member 1A1
External ID: CHEMBL2076234
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: Am. J. Physiol.
Year: 1996
Volume: 270
Issue: 1
First Page: F326
Last Page: F331
DOI: 10.1152/ajprenal.1996.270.2.f326

Target ChEMBL ID: CHEMBL1781859
ChEMBL Target Name: Solute carrier organic anion transporter family member 1A1
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: H - Homologous protein target assigned
Confidence: Homologous single protein target assigned
PubChem Standard ValueStandard TypeStandard RelationStandard ValueStandard UnitsActivity CommentData Validity Comment
9.8Ki=9800nMinhibitor [Ki=9.8uM]
15.7Ki=15700nMinhibitor [Ki=15.7uM]
1.3Ki=1300nMinhibitor [Ki=1.3uM]
5.4Ki=5400nMinhibitor [Ki=5.4uM]
1.3Ki=1300nMinhibitor [Ki=1.3uM]
200Ki>200000nMinhibitor [Ki>200uM]Outside typical range
1.1Ki=1100nMinhibitor [Ki=1.1uM]
2.4Ki=2400nMinhibitor [Ki=2.4uM]
1.6Ki=1600nMinhibitor [Ki=1.6uM]
76.2Ki=76200nMinhibitor [Ki=76.2uM]
9.7Ki=9700nMinhibitor [Ki=9.7uM]
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Broad substrate specificity ATP-binding cassette transporter ABCG2
External ID: CHEMBL2076814
Protocol: N/A
Comment: Journal: Mol. Pharmacol.
Year: 2003
Volume: 64
Issue: 1
First Page: 610
Last Page: 618
DOI: 10.1124/mol.64.3.610

Target ChEMBL ID: CHEMBL5393
ChEMBL Target Name: ATP-binding cassette sub-family G member 2
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: H - Homologous protein target assigned
Confidence: Homologous single protein target assigned
Standard TypeStandard RelationStandard ValueStandard UnitsActivity Comment
Activity=50%inhibitor [50% of control]
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Solute carrier organic anion transporter family member 2B1
External ID: CHEMBL2077867
Protocol: N/A
Comment: Journal: Pharm. Res.
Year: 2001
Volume: 18
Issue: 1
First Page: 1262
Last Page: 1269
DOI: 10.1023/a:1013077609227

Target ChEMBL ID: CHEMBL1743124
ChEMBL Target Name: Solute carrier organic anion transporter family member 2B1
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: H - Homologous protein target assigned
Confidence: Homologous single protein target assigned
Standard TypeActivity Comment
Activityinhibitor [(at a rough estimate) 30 % of control]
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Cholesterol 24-hydroxylase
External ID: CHEMBL4417815
Protocol: N/A
Comment: Target ChEMBL ID: CHEMBL4523510
ChEMBL Target Name: Cholesterol 24-hydroxylase
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: SureChEMBL Patent Bioactivity Data
Standard TypeStandard RelationStandard ValueStandard Units
Activity=75%
Activity=79%
Activity=8%
Activity=83%
Activity=86%
Activity=70%
Activity=16%
Activity=0%
Activity=9%
Activity=32%
Activity=84%
Activity=60%
Activity=80%
Activity=90%
Activity=31%
Activity=38%
Activity=100%
Activity=89%
Activity=56%
Activity=27%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Sodium/bile acid cotransporter
External ID: CHEMBL2078469
Protocol: N/A
Comment: Journal: Am. J. Physiol.
Year: 1998
Volume: 274
Issue: 1
First Page: G370
Last Page: G375
DOI: 10.1152/ajpgi.1998.274.2.g370

Target ChEMBL ID: CHEMBL4847
ChEMBL Target Name: Bile acid transporter
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: H - Homologous protein target assigned
Confidence: Homologous single protein target assigned
Standard TypeActivity Comment
Activityinhibitor [(at a rough estmate) 5 % of control]
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Broad substrate specificity ATP-binding cassette transporter ABCG2
External ID: CHEMBL2075865
Protocol: N/A
Comment: Journal: Mol. Pharmacol.
Year: 2003
Volume: 64
Issue: 1
First Page: 610
Last Page: 618
DOI: 10.1124/mol.64.3.610

Target ChEMBL ID: CHEMBL5393
ChEMBL Target Name: ATP-binding cassette sub-family G member 2
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: H - Homologous protein target assigned
Confidence: Homologous single protein target assigned
Standard TypeActivity Comment
Activitysubstrate []
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Solute carrier organic anion transporter family member 1A2
External ID: CHEMBL2076569
Protocol: N/A
Comment: Journal: FEBS Lett.
Year: 1998
Volume: 424
Issue: 1
First Page: 173
Last Page: 176
DOI: 10.1016/s0014-5793(98)00168-9

Target ChEMBL ID: CHEMBL1743123
ChEMBL Target Name: Solute carrier organic anion transporter family member 1A2
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: H - Homologous protein target assigned
Confidence: Homologous single protein target assigned
Standard TypeStandard RelationStandard ValueStandard UnitsActivity Comment
Inhibition=92.9%inhibitor [92.9 % inhibition]
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: CHEMBL823714
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 2000
Volume: 43
Issue: 2
First Page: 146
Last Page: 155
DOI: 10.1021/jm990329z

Target ChEMBL ID: CHEMBL335
ChEMBL Target Name: Protein-tyrosine phosphatase 1B
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: H - Homologous protein target assigned
Confidence: Homologous single protein target assigned
Standard TypeActivity Comment
NIno inhibition at 1 mM
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Solute carrier organic anion transporter family member 1B1
External ID: CHEMBL2077598
Protocol: N/A
Comment: Journal: Pharm. Res.
Year: 2001
Volume: 18
Issue: 1
First Page: 1262
Last Page: 1269
DOI: 10.1023/a:1013077609227

Target ChEMBL ID: CHEMBL1697668
ChEMBL Target Name: Solute carrier organic anion transporter family member 1B1
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: H - Homologous protein target assigned
Confidence: Homologous single protein target assigned
Standard TypeActivity Comment
Activityinhibitor [(at a rough estimate) 10 % of control]
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Solute carrier family 22 member 11
External ID: CHEMBL2075410
Protocol: N/A
Comment: Journal: J. Biol. Chem.
Year: 2000
Volume: 275
Issue: 1
First Page: 4507
Last Page: 4512
DOI: 10.1074/jbc.275.6.4507

Target ChEMBL ID: CHEMBL2073677
ChEMBL Target Name: Solute carrier family 22 member 11
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: H - Homologous protein target assigned
Confidence: Homologous single protein target assigned
Standard TypeActivity Comment
Activityinhibitor [(at a rough estimate) 25 % of control]
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.