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60-24-2 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:Carbonic anhydrase 2
External ID: CHEMBL929744
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2008
Volume: 18
Issue: 6
First Page: 1898
Last Page: 1903
DOI: 10.1016/j.bmcl.2008.02.008

Target ChEMBL ID: CHEMBL205
ChEMBL Target Name: Carbonic anhydrase II
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 Units
Activity=73%
Activity=68%
Activity=36%
Activity=68%
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: CHEMBL3241404
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: 2014
Volume: 76
First Page: 132
Last Page: 144
DOI: 10.1016/j.ejmech.2014.02.008
PubChem Standard ValueStandard TypeStandard RelationStandard ValueStandard Units
2.2INH=2.2uM
0.55INH=0.55uM
17Ki=17000nM
1.4INH=1.4uM
0.25INH=0.25uM
1.6IC50=1600nM
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Carbonic anhydrase 9
External ID: CHEMBL929745
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2008
Volume: 18
Issue: 6
First Page: 1898
Last Page: 1903
DOI: 10.1016/j.bmcl.2008.02.008

Target ChEMBL ID: CHEMBL3594
ChEMBL Target Name: Carbonic anhydrase IX
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 Units
Activity=58%
Activity=82%
Activity=84%
Activity=86%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Carbonic anhydrase 9
External ID: CHEMBL929746
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2008
Volume: 18
Issue: 6
First Page: 1898
Last Page: 1903
DOI: 10.1016/j.bmcl.2008.02.008

Target ChEMBL ID: CHEMBL3594
ChEMBL Target Name: Carbonic anhydrase IX
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 Units
Activity=54%
Activity=69%
Activity=86%
Activity=65%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Carbonic anhydrase 9
External ID: CHEMBL929740
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2008
Volume: 18
Issue: 6
First Page: 1898
Last Page: 1903
DOI: 10.1016/j.bmcl.2008.02.008

Target ChEMBL ID: CHEMBL3594
ChEMBL Target Name: Carbonic anhydrase IX
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 Units
Activity=76%
Activity=83%
Activity=91%
Activity=83%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Carbonic anhydrase 2
External ID: CHEMBL929741
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2008
Volume: 18
Issue: 6
First Page: 1898
Last Page: 1903
DOI: 10.1016/j.bmcl.2008.02.008

Target ChEMBL ID: CHEMBL205
ChEMBL Target Name: Carbonic anhydrase II
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 Units
Activity=75%
Activity=70%
Activity=41%
Activity=77%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Carbonic anhydrase 9
External ID: CHEMBL929742
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2008
Volume: 18
Issue: 6
First Page: 1898
Last Page: 1903
DOI: 10.1016/j.bmcl.2008.02.008

Target ChEMBL ID: CHEMBL3594
ChEMBL Target Name: Carbonic anhydrase IX
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 Units
Activity=71%
Activity=83%
Activity=87%
Activity=89%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Carbonic anhydrase 9
External ID: CHEMBL929743
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2008
Volume: 18
Issue: 6
First Page: 1898
Last Page: 1903
DOI: 10.1016/j.bmcl.2008.02.008

Target ChEMBL ID: CHEMBL3594
ChEMBL Target Name: Carbonic anhydrase IX
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 Units
Activity=65%
Activity=77%
Activity=89%
Activity=77%
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 Enzyme Data
Protocol: N/A
Comment: N/A
SpeciesStrainIsPseudotypeVirusAssayMethTargetMutationsIC50ModIC50IC50UnitICOtherPctICOtherPctUnitICOtherConcICOtherConcUnitKiModKiKiUnitKmKmUnitHostAnalogHostAnalogSpeciesRelResFoldChgModRelResFoldChgCommentsReferenceCitationOther Information
3' PROCESSINGIntegrase>100uM18662877EFFICIENT SYNTHESIS AND UTILIZATION OF PHENYL-SUBSTITUTED HETEROAROMATIC CARBOXYLIC ACIDS AS ARYL DIKETO ACID ISOSTERES IN THE DESIGN OF NOVEL HIV-1 INTEGRASE INHIBITORS. Bioorganic & Medical Chemistry Letters 2008, 18(16), 4521-4.
3' PROCESSINGIntegrase>100uM18662877EFFICIENT SYNTHESIS AND UTILIZATION OF PHENYL-SUBSTITUTED HETEROAROMATIC CARBOXYLIC ACIDS AS ARYL DIKETO ACID ISOSTERES IN THE DESIGN OF NOVEL HIV-1 INTEGRASE INHIBITORS. Bioorganic & Medical Chemistry Letters 2008, 18(16), 4521-4.
3' PROCESSINGIntegrase>100uM18662877EFFICIENT SYNTHESIS AND UTILIZATION OF PHENYL-SUBSTITUTED HETEROAROMATIC CARBOXYLIC ACIDS AS ARYL DIKETO ACID ISOSTERES IN THE DESIGN OF NOVEL HIV-1 INTEGRASE INHIBITORS. Bioorganic & Medical Chemistry Letters 2008, 18(16), 4521-4.
STRAND TRANSFERIntegrase>100uM18662877EFFICIENT SYNTHESIS AND UTILIZATION OF PHENYL-SUBSTITUTED HETEROAROMATIC CARBOXYLIC ACIDS AS ARYL DIKETO ACID ISOSTERES IN THE DESIGN OF NOVEL HIV-1 INTEGRASE INHIBITORS. Bioorganic & Medical Chemistry Letters 2008, 18(16), 4521-4.
HIV-1dTTP incorporation assay by liquid scintillationReverse transcriptase6.2uM19442130CHARACTERIZATION OF HIV-1 ENZYME REVERSE TRANSCRIPTASE INHIBITION BY THE COMPOUND 6-CHLORO-1,4-DIHYDRO-4-OXO-1-(BETA-D-RIBOFURANOSYL) QUINOLINE-3-CARBOXYLIC ACID THROUGH KINETIC AND IN SILICO STUDIES. Current HIV Research 2009, 7(3), 327-335.
HIV-1dTTP incorporation assay by liquid scintillationReverse transcriptase5.3uM19442130CHARACTERIZATION OF HIV-1 ENZYME REVERSE TRANSCRIPTASE INHIBITION BY THE COMPOUND 6-CHLORO-1,4-DIHYDRO-4-OXO-1-(BETA-D-RIBOFURANOSYL) QUINOLINE-3-CARBOXYLIC ACID THROUGH KINETIC AND IN SILICO STUDIES. Current HIV Research 2009, 7(3), 327-335.
HIV-1dTTP incorporation assay by liquid scintillationReverse transcriptase5uM19442130CHARACTERIZATION OF HIV-1 ENZYME REVERSE TRANSCRIPTASE INHIBITION BY THE COMPOUND 6-CHLORO-1,4-DIHYDRO-4-OXO-1-(BETA-D-RIBOFURANOSYL) QUINOLINE-3-CARBOXYLIC ACID THROUGH KINETIC AND IN SILICO STUDIES. Current HIV Research 2009, 7(3), 327-335.
HIV-1Nstandard reverse transcriptase assayReverse transcriptase50ug/mLSYNTHESIS AND HIV-1 REVERSE TRANSCRIPTASE INHIBITION ACTIVITY OF 1,4-NAPHTHOQUINONE DERIVATIVES. Chemistry of Natural Compounds 2012, 47(6), 883-887.
STRAND TRANSFERIntegrase>100uM18805696DISCOVERY OF 3-ACETYL-4-HYDROXY-2-PYRANONE DERIVATIVES AND THEIR DIFLUORIDOBORATE COMPLEXES AS A NOVEL CLASS OF HIV-1 INTEGRASE INHIBITORS. Bioorganic & Medical Chemistry 2008, 16(19), 8988-98.
STRAND TRANSFERIntegrase>100uM18805696DISCOVERY OF 3-ACETYL-4-HYDROXY-2-PYRANONE DERIVATIVES AND THEIR DIFLUORIDOBORATE COMPLEXES AS A NOVEL CLASS OF HIV-1 INTEGRASE INHIBITORS. Bioorganic & Medical Chemistry 2008, 16(19), 8988-98.
3'-PROCESSINGIntegrase>100uM18805696DISCOVERY OF 3-ACETYL-4-HYDROXY-2-PYRANONE DERIVATIVES AND THEIR DIFLUORIDOBORATE COMPLEXES AS A NOVEL CLASS OF HIV-1 INTEGRASE INHIBITORS. Bioorganic & Medical Chemistry 2008, 16(19), 8988-98.
HIV-1STRAND TRANSFERIntegrase0.015uM19523819N-(4-FLUOROBENZYL)-3-HYDROXY-9;9-DIMETHYL-4-OXO-6;7;8;9-TETRAHYDRO-4H-PYRAZINO[1;2-A]PYRIMIDINE-2-CARBOXAMIDES A NOVEL CLASS OF POTENT HIV-1 INTEGRASE INHIBITORS. Bioorganic & Medical Chemistry Letters 2009, 19, 4245-9.
HIV-1HPLCProtease5.8uM18543149INHIBITION OF HIV-1 PROTEASE AND RNASE H OF HIV-1 REVERSE TRANSCRIPTASE ACTIVITIES BY LONG CHAIN PHENOLS FROM THE SARCOTESTAS OF GINKGO BILOBA. Planta Medica 2008, 74(5), 532-534.
HIV-1RNASE H OF HIV-1 REVERSE TRANSCRIPTASE ASSAYReverse transcriptase170.3uM18543149INHIBITION OF HIV-1 PROTEASE AND RNASE H OF HIV-1 REVERSE TRANSCRIPTASE ACTIVITIES BY LONG CHAIN PHENOLS FROM THE SARCOTESTAS OF GINKGO BILOBA. Planta Medica 2008, 74(5), 532-534.
HIV-1HPLCProtease10.2uM18543149INHIBITION OF HIV-1 PROTEASE AND RNASE H OF HIV-1 REVERSE TRANSCRIPTASE ACTIVITIES BY LONG CHAIN PHENOLS FROM THE SARCOTESTAS OF GINKGO BILOBA. Planta Medica 2008, 74(5), 532-534.
HIV-1RNASE H OF HIV-1 REVERSE TRANSCRIPTASE ASSAYReverse transcriptase33.7uM18543149INHIBITION OF HIV-1 PROTEASE AND RNASE H OF HIV-1 REVERSE TRANSCRIPTASE ACTIVITIES BY LONG CHAIN PHENOLS FROM THE SARCOTESTAS OF GINKGO BILOBA. Planta Medica 2008, 74(5), 532-534.
HIV-1HPLCProtease24.9uM18543149INHIBITION OF HIV-1 PROTEASE AND RNASE H OF HIV-1 REVERSE TRANSCRIPTASE ACTIVITIES BY LONG CHAIN PHENOLS FROM THE SARCOTESTAS OF GINKGO BILOBA. Planta Medica 2008, 74(5), 532-534.
HIV-13'-processingIntegrase>100uMCOMPOUNDS WITH HIV-1 INTEGRASE INHIBITORY ACTIVITY AND USE THEREOF AS ANTI-HIV/AIDS THERAPEUTICS. . Patent 2009, , .
HIV-1Strand TransferIntegrase>100uMCOMPOUNDS WITH HIV-1 INTEGRASE INHIBITORY ACTIVITY AND USE THEREOF AS ANTI-HIV/AIDS THERAPEUTICS. . Patent 2009, , .
HIV-13'-processingIntegrase>100uMCOMPOUNDS WITH HIV-1 INTEGRASE INHIBITORY ACTIVITY AND USE THEREOF AS ANTI-HIV/AIDS THERAPEUTICS. . Patent 2009, , .
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:BindingDB 靶标:N/A
External ID: BindingDB_998_1
Protocol: N/A
Comment: Compounds with any of Ki, IC50, Kd, or EC50 activity value <= 10uM are labeled as "Active".
If multiple measurements are available for a given compound, it is labeled as "Active" if any of the measurements meet the criterion. Activity values are checked in the order of Ki, IC50, Kd, and EC50. The first entry that meets the above activity threshold is used to determine "Standard Type", "Standard Relation", and "PubChem Standard Value". Otherwise, the first non-empty entry will be used to set those values.
Standard TypePubChem Standard ValueKiTarget Accession(s)LigandTarget
Ki6.46400Q9CYK2BDBM7887Glutaminyl-peptide cyclotransferase
Ki192192000Q9CYK2BDBM7939Glutaminyl-peptide cyclotransferase
Ki4242000Q9CYK2BDBM7968Glutaminyl-peptide cyclotransferase
Ki2929000Q9CYK2BDBM7969Glutaminyl-peptide cyclotransferase
Ki25802580000Q9CYK2BDBM7971Glutaminyl-peptide cyclotransferase
Ki2200022000000Q9CYK2BDBM7972Glutaminyl-peptide cyclotransferase
Ki1930019300000Q9CYK2BDBM7973Glutaminyl-peptide cyclotransferase
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: CHEMBL1937338
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem.
Year: 2012
Volume: 20
Issue: 2
First Page: 1020
Last Page: 1028
DOI: 10.1016/j.bmc.2011.11.049
Standard TypeStandard RelationStandard Value
pKa=8.7
pKa=9.6
pKa=9.2
pKa=8.7
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Endolysin
External ID: CHEMBL2330734
Protocol: N/A
Comment: Journal: J Med Chem
Year: 2013
Volume: 56
Issue: 7
First Page: 2874
Last Page: 2884
DOI: 10.1021/jm301823g

Target ChEMBL ID: CHEMBL5206
ChEMBL Target Name: Lysozyme
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 RelationStandard ValueStandard Units
Delta Tm=1.2degrees C
Delta Tm=0degrees C
Delta Tm=2.9degrees C
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Carbonic anhydrase 2
External ID: CHEMBL929729
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2008
Volume: 18
Issue: 6
First Page: 1898
Last Page: 1903
DOI: 10.1016/j.bmcl.2008.02.008

Target ChEMBL ID: CHEMBL205
ChEMBL Target Name: Carbonic anhydrase II
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 Units
Activity=92%
Activity=94%
Activity=84%
Activity=94%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Carbonic anhydrase 9
External ID: CHEMBL929730
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2008
Volume: 18
Issue: 6
First Page: 1898
Last Page: 1903
DOI: 10.1016/j.bmcl.2008.02.008

Target ChEMBL ID: CHEMBL3594
ChEMBL Target Name: Carbonic anhydrase IX
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 Units
Activity=98%
Activity=99%
Activity=100%
Activity=98%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Carbonic anhydrase 9
External ID: CHEMBL929731
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2008
Volume: 18
Issue: 6
First Page: 1898
Last Page: 1903
DOI: 10.1016/j.bmcl.2008.02.008

Target ChEMBL ID: CHEMBL3594
ChEMBL Target Name: Carbonic anhydrase IX
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 Units
Activity=97%
Activity=98%
Activity=100%
Activity=95%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:DTP/NCI 靶标:N/A
External ID: MCF7_OneDose
Protocol: NCI-60 Human Tumor Cell Lines Screen was performed using the standard one-dose NCI protocol, which is described in more detail at https://dtp.cancer.gov/discovery_development/nci-60/default.htm.

Compounds with GIPRCNT values below 10 were considered active. Activity score was based on GIPRCNT using the following formula:
max(-GIPRCNT/2 + 50, 0)
Score is 0 for GIPRCNT values of 100 or above, 50 for GIPRCNT values of 0, and 100 for GIPRCNT values of -100.
Comment: These data are a subset of the data from the NCI human tumor cell line screen. Compounds are identified by the NCI National Service Center (NSC) number, which is contained in the
PUBCHEM_EXT_DATASOURCE_REGID field. In the NCI cell line identification system, MCF7 is panel number 5, cell number 1. PANELCODE or PANELNAME identify the NCI-60 cell panel. PANELNBR does NOT identify the NCI-60 panel.

EXPID is the NCI internal tracking number for the experiment identifier, and PREFIX = 'S' for the NSCs submitted through the NCI Chemical Agents repository.

Substance concentration unit is indicated in the data table, using the following abbreviations: M = molar (M), u = micrograms/milliliter (microg/mL), V = volumetric fraction.

M_GIPRCNT represents the mean growth percent for that experiment, and N_GIPRCNT indicates the number of values for that NSC within an experiment, while STDEV_GIPRCNT is the standard deviation. Most NSCs are tested once per experiment, resulting in EXP_COUNT = 1.
EXPIDPREFIXCONCENTRATION_UNITCONCENTRATIONPANELNBRCELLNBRPANELNAMECELLNAMEPANELCODEM_GIPRCNTN_GIPRCNTSTDDEV_GIPRCNTEXP_COUNT
2106OS49SM1.0E-551Breast CancerMCF7BRE88.231101
2106OS49SM1.0E-551Breast CancerMCF7BRE87.1119101
2106OS49SM1.0E-551Breast CancerMCF7BRE14.4371101
2106OS49SM1.0E-551Breast CancerMCF7BRE89.7113101
2106OS49SM1.0E-551Breast CancerMCF7BRE97.2463101
2106OS49SM1.0E-551Breast CancerMCF7BRE90.0129101
2106OS49SM1.0E-551Breast CancerMCF7BRE85.7031101
2106OS49SM1.0E-551Breast CancerMCF7BRE30.8539101
2106OS49SM1.0E-551Breast CancerMCF7BRE14.2896101
2106OS49SM1.0E-551Breast CancerMCF7BRE85.8526101
2106OS49SM1.0E-551Breast CancerMCF7BRE83.1036101
2106OS49SM1.0E-551Breast CancerMCF7BRE84.2194101
2106OS49SM1.0E-551Breast CancerMCF7BRE89.3237101
2106OS49SM1.0E-551Breast CancerMCF7BRE85.6034101
2106OS49SM1.0E-551Breast CancerMCF7BRE89.6643101
2106OS52SM1.0E-551Breast CancerMCF7BRE91.2503101
2106OS52SM1.0E-551Breast CancerMCF7BRE94.8714101
2106OS52SM1.0E-551Breast CancerMCF7BRE93.7372101
2106OS52SM1.0E-551Breast CancerMCF7BRE112.6132101
2106OS52SM1.0E-551Breast CancerMCF7BRE73.375101
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Carbonic anhydrase 9
External ID: CHEMBL929736
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2008
Volume: 18
Issue: 6
First Page: 1898
Last Page: 1903
DOI: 10.1016/j.bmcl.2008.02.008

Target ChEMBL ID: CHEMBL3594
ChEMBL Target Name: Carbonic anhydrase IX
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 Units
Activity=93%
Activity=85%
Activity=96%
Activity=94%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Carbonic anhydrase 9
External ID: CHEMBL929737
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2008
Volume: 18
Issue: 6
First Page: 1898
Last Page: 1903
DOI: 10.1016/j.bmcl.2008.02.008

Target ChEMBL ID: CHEMBL3594
ChEMBL Target Name: Carbonic anhydrase IX
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 Units
Activity=85%
Activity=89%
Activity=97%
Activity=87%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:DTP/NCI 靶标:N/A
External ID: IGROV1_OneDose
Protocol: NCI-60 Human Tumor Cell Lines Screen was performed using the standard one-dose NCI protocol, which is described in more detail at https://dtp.cancer.gov/discovery_development/nci-60/default.htm.

Compounds with GIPRCNT values below 10 were considered active. Activity score was based on GIPRCNT using the following formula:
max(-GIPRCNT/2 + 50, 0)
Score is 0 for GIPRCNT values of 100 or above, 50 for GIPRCNT values of 0, and 100 for GIPRCNT values of -100.
Comment: These data are a subset of the data from the NCI human tumor cell line screen. Compounds are identified by the NCI National Service Center (NSC) number, which is contained in the
PUBCHEM_EXT_DATASOURCE_REGID field. In the NCI cell line identification system, IGROV1 is panel number 6, cell number 10. PANELCODE or PANELNAME identify the NCI-60 cell panel. PANELNBR does NOT identify the NCI-60 panel.

EXPID is the NCI internal tracking number for the experiment identifier, and PREFIX = 'S' for the NSCs submitted through the NCI Chemical Agents repository.

Substance concentration unit is indicated in the data table, using the following abbreviations: M = molar (M), u = micrograms/milliliter (microg/mL), V = volumetric fraction.

M_GIPRCNT represents the mean growth percent for that experiment, and N_GIPRCNT indicates the number of values for that NSC within an experiment, while STDEV_GIPRCNT is the standard deviation. Most NSCs are tested once per experiment, resulting in EXP_COUNT = 1.
EXPIDPREFIXCONCENTRATION_UNITCONCENTRATIONPANELNBRCELLNBRPANELNAMECELLNAMEPANELCODEM_GIPRCNTN_GIPRCNTSTDDEV_GIPRCNTEXP_COUNT
0809OS51SM1.0E-5610Ovarian CancerIGROV1OVA89.6274101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA94.0185101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA77.1805101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA76.1686101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA82.5618101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA88.7561101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA83.5845101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA92.7497101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA70.9555101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA58.7306101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA72.6041101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA90.3839101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA110.2345101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA97.6538101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA93.7697101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA56.4618101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA80.8893101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA79.078101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA-20.3008101
0810OS71SM1.0E-5610Ovarian CancerIGROV1OVA72.0949101
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Carbonic anhydrase 2
External ID: CHEMBL929738
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2008
Volume: 18
Issue: 6
First Page: 1898
Last Page: 1903
DOI: 10.1016/j.bmcl.2008.02.008

Target ChEMBL ID: CHEMBL205
ChEMBL Target Name: Carbonic anhydrase II
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 Units
Activity=77%
Activity=72%
Activity=55%
Activity=83%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Carbonic anhydrase 9
External ID: CHEMBL929739
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2008
Volume: 18
Issue: 6
First Page: 1898
Last Page: 1903
DOI: 10.1016/j.bmcl.2008.02.008

Target ChEMBL ID: CHEMBL3594
ChEMBL Target Name: Carbonic anhydrase IX
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 Units
Activity=85%
Activity=83%
Activity=90%
Activity=91%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Carbonic anhydrase 2
External ID: CHEMBL929732
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2008
Volume: 18
Issue: 6
First Page: 1898
Last Page: 1903
DOI: 10.1016/j.bmcl.2008.02.008

Target ChEMBL ID: CHEMBL205
ChEMBL Target Name: Carbonic anhydrase II
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 Units
Activity=85%
Activity=87%
Activity=74%
Activity=90%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Carbonic anhydrase 9
External ID: CHEMBL929733
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2008
Volume: 18
Issue: 6
First Page: 1898
Last Page: 1903
DOI: 10.1016/j.bmcl.2008.02.008

Target ChEMBL ID: CHEMBL3594
ChEMBL Target Name: Carbonic anhydrase IX
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 Units
Activity=97%
Activity=94%
Activity=99%
Activity=96%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Carbonic anhydrase 9
External ID: CHEMBL929734
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2008
Volume: 18
Issue: 6
First Page: 1898
Last Page: 1903
DOI: 10.1016/j.bmcl.2008.02.008

Target ChEMBL ID: CHEMBL3594
ChEMBL Target Name: Carbonic anhydrase IX
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 Units
Activity=94%
Activity=95%
Activity=100%
Activity=92%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Carbonic anhydrase 2
External ID: CHEMBL929735
Protocol: N/A
Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2008
Volume: 18
Issue: 6
First Page: 1898
Last Page: 1903
DOI: 10.1016/j.bmcl.2008.02.008

Target ChEMBL ID: CHEMBL205
ChEMBL Target Name: Carbonic anhydrase II
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 Units
Activity=81%
Activity=80%
Activity=66%
Activity=87%