179556-58-2 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：NIAID 靶标：N/A

External ID: HIV Enzyme Data

Protocol: N/A

Comment: N/A

Species	Strain	IsPseudotypeVirus	AssayMeth	Target	IC50Mod	IC50	IC50Unit	Ki	KiUnit	Reference	Citation
			3' PROCESSING	Integrase	>	100	uM			18662877	EFFICIENT 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' PROCESSING	Integrase	>	100	uM			18662877	EFFICIENT 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' PROCESSING	Integrase	>	100	uM			18662877	EFFICIENT 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 TRANSFER	Integrase	>	100	uM			18662877	EFFICIENT 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-1		dTTP incorporation assay by liquid scintillation	Reverse transcriptase				6.2	uM	19442130	CHARACTERIZATION 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-1		dTTP incorporation assay by liquid scintillation	Reverse transcriptase				5.3	uM	19442130	CHARACTERIZATION 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-1		dTTP incorporation assay by liquid scintillation	Reverse transcriptase				5	uM	19442130	CHARACTERIZATION 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-1		N	standard reverse transcriptase assay	Reverse transcriptase		50	ug/mL				SYNTHESIS AND HIV-1 REVERSE TRANSCRIPTASE INHIBITION ACTIVITY OF 1,4-NAPHTHOQUINONE DERIVATIVES. Chemistry of Natural Compounds 2012, 47(6), 883-887.
			STRAND TRANSFER	Integrase	>	100	uM			18805696	DISCOVERY 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 TRANSFER	Integrase	>	100	uM			18805696	DISCOVERY 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'-PROCESSING	Integrase	>	100	uM			18805696	DISCOVERY 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-1		STRAND TRANSFER	Integrase		0.015	uM			19523819	N-(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-1		HPLC	Protease		5.8	uM			18543149	INHIBITION 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-1		RNASE H OF HIV-1 REVERSE TRANSCRIPTASE ASSAY	Reverse transcriptase		170.3	uM			18543149	INHIBITION 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-1		HPLC	Protease		10.2	uM			18543149	INHIBITION 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-1		RNASE H OF HIV-1 REVERSE TRANSCRIPTASE ASSAY	Reverse transcriptase		33.7	uM			18543149	INHIBITION 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-1		HPLC	Protease		24.9	uM			18543149	INHIBITION 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-1		3'-processing	Integrase	>	100	uM				COMPOUNDS WITH HIV-1 INTEGRASE INHIBITORY ACTIVITY AND USE THEREOF AS ANTI-HIV/AIDS THERAPEUTICS. . Patent 2009, , .
	HIV-1		Strand Transfer	Integrase	>	100	uM				COMPOUNDS WITH HIV-1 INTEGRASE INHIBITORY ACTIVITY AND USE THEREOF AS ANTI-HIV/AIDS THERAPEUTICS. . Patent 2009, , .
	HIV-1		3'-processing	Integrase	>	100	uM				COMPOUNDS 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

Species	Strain	AssayMeth	CellType	CellType2	Target	Mutations	EC50Mod	EC50	EC50Unit	ECOtherPct	ECOtherPctUnit	ECOtherConc	ECOtherConcUnit	ToxAssayMeth	CC50Mod	CC50	CC50Unit	TIMod	TI	Comments	Reference	Citation	Other Information
HIV-1	LAI	RT	HuT TK+	HuT 78	Reverse transcriptase		<	1	uM	100	%	1	uM	MTT	>	10	uM	>	10	HuT TK+=HuT 78 CELLS EXPRESSING HSV-1 THYMIDINE KINASE; MEASUREMENT WAS MADE ON DAY10 POSTINFECTION AT 10 TCID50	9281520	USE OF HERPES SIMPLEX VIRUS THYMIDINE KINASE TO IMPROVE THE ANTIVIRAL ACTIVITY OF ZIDOVUDINE. Virology 1997, 235, 398-405.
HIV-1	MN	RT	HuT TK+	HuT 78	Reverse transcriptase		<	0.3	uM	76.74	%	0.3	uM	MTT	>	10	uM	>	33.3	HuT TK+=HuT 78 CELLS EXPRESSING HSV-1 THYMIDINE KINASE; MEASUREMENT WAS MADE ON DAY14 POSTINFECTION AT 10 TCID50	9281520	USE OF HERPES SIMPLEX VIRUS THYMIDINE KINASE TO IMPROVE THE ANTIVIRAL ACTIVITY OF ZIDOVUDINE. Virology 1997, 235, 398-405.
HIV-1	MN	RT	HuT TK+	HuT 78	Reverse transcriptase		<	0.3	uM	69	%	0.3	uM	MTT	>	10	uM	>	33.3	HuT TK+=HuT 78 CELLS EXPRESSING HSV-1 THYMIDINE KINASE; MEASUREMENT WAS MADE ON DAY14 POSTINFECTION AT 100 TCID50	9281520	USE OF HERPES SIMPLEX VIRUS THYMIDINE KINASE TO IMPROVE THE ANTIVIRAL ACTIVITY OF ZIDOVUDINE. Virology 1997, 235, 398-405.
R5; CLINICAL ISOLATE	1(JSL)	P24	PBMC		Reverse transcriptase	MDR		0.07	uM	90	%	1	uM	MTT	>	100	uM	>	1428	HIV-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 GIVEN	15280474	SPIRODIKETOPIPERAZINE-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-1	NL4-3	LUCIFERASE	1G5 T		Reverse transcriptase		<	1	uM	99	%	1	uM	TRYPAN BLUE	>	1	uM	>	1	ASSAY WAS CONDUCTED ON DAY 3 POST-INFECTION	16725040	INHIBITION 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-1	NL4-3	LUCIFERASE	1G5 T		Reverse transcriptase		<	1	uM	99	%	1	uM	TRYPAN BLUE	>	1	uM	>	1	ASSAY WAS CONDUCTED ON DAY 5 POST-INFECTION	16725040	INHIBITION 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-1	NL4-3	LUCIFERASE	1G5 T		Reverse transcriptase		<	1	uM	99	%	1	uM	TRYPAN BLUE	>	1	uM	>	1	ASSAY WAS CONDUCTED ON DAY 7 POST-INFECTION	16725040	INHIBITION 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-1	LAV	RT	U1(THF-.alpha. STIM)	U1	Tumor necrosis factor alpha		~	30	ug/mL	70	%	50	ug/mL		>	50	ug/mL	>	1.66	CHRONICALLY HIV-1 INFECTED PROMONOCYTE CELL LINE	8327469	THALIDOMIDE 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-1	BaL	P24 (DAY 18)	MACROPHAGES(GM-CSF)	Macrophage	Ribonucleotide reductase		<	10	uM	75	%	10	uM		>	1000	uM	>	10	MAXIMAL P24 EXPRESSION AT DAY 18	7973634	HYDROXYUREA AS AN INHIBITOR OF HUMAN IMMUNODEFICIENCY VIRUS-TYPE 1 REPLICATION. Science 1994, 266(5186), 801-805.	CCOtherPct:0 \| CCOtherPctUnit:% \| CCOtherConc:1000 \| CCOtherConcUnit:uM
HIV-1	BaL	P24 (DAY 18)	MACROPHAGES(GM-CSF)	Macrophage	Ribonucleotide reductase		<	10	uM	38	%	2	uM		>	1000	uM	>	10	MAXIMAL P24 EXPRESSION AT DAY 18	7973634	HYDROXYUREA AS AN INHIBITOR OF HUMAN IMMUNODEFICIENCY VIRUS-TYPE 1 REPLICATION. Science 1994, 266(5186), 801-805.	CCOtherPct:0 \| CCOtherPctUnit:% \| CCOtherConc:1000 \| CCOtherConcUnit:uM
HIV-1	BaL	P24 (DAY 18)	MACROPHAGES(GM-CSF)	Macrophage	Ribonucleotide reductase		<	10	uM	99	%	50	uM		>	1000	uM	>	10	MAXIMAL P24 EXPRESSION AT DAY 18	7973634	HYDROXYUREA 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-1	IIIB	RT	HT4(R116; AZT RESISTANT CELLS)	HT4	Reverse transcriptase		~	0.01	uM	70	%	0.01	uM		~`	1	uM	~	100	FLOXURIDINE APPEARS TO POTENTIATE AZT ACTIVITY AND ALSO HAVE SOME ANTI-HIV ACTIVITY IN AZT RESISTANT CELL LINES	8827211	USE 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-1	1	.beta.GAL AS A MEASURE OF TAT-MEDIATED TRANSACTIVATION	HeLa H12(HIV-1 LTR-Laz, TAT)	HeLa	Tat:TAR/LTR		<	0.1	uM	52	%	0.1	uM	TRYPAN BLUE	>	100	uM	>	1000	DRUG AND RECOMBINANT TAT WERE INTRODUCED INTO CELLS THROUGH ELECTROPORATION	9561563	CURCUMIN 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-1	1	.beta.GAL AS A MEASURE OF TAT-MEDIATED TRANSACTIVATION	HeLa H12(HIV-1 LTR-Laz, TAT)	HeLa	Tat:TAR/LTR		<	0.01	uM	78	%	0.01	uM	TRYPAN BLUE	>	100	uM	>	10000	DRUG AND RECOMBINANT TAT WERE INTRODUCED INTO CELLS THROUGH ELECTROPORATION	9561563	CURCUMIN 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-1	IIIB	SYNCYT FORM	MOLT-4/H9(HIV-1(IIIB))	MOLT-4	gp120		<	1	uM	95	%	10	uM		-100	10	uM	>	10	CHRONICALLY INFECTED H9 CELLS	9343823	TRIAZINE 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-1	1	.beta.GAL AS A MEASURE OF TAT-MEDIATED TRANSACTIVATION	HeLa H12(HIV-1 LTR-Laz, TAT)	HeLa	Tat:TAR/LTR		<	0.01	uM	75	%	0.01	uM	TRYPAN BLUE	>	100	uM	>	10000	DRUG AND RECOMBINANT TAT WERE INTRODUCED INTO CELLS THROUGH ELECTROPORATION	9561563	CURCUMIN 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-1	1	P24	MT-4		Integrase		<	0.25	uM	95	%	0.25	uM	MICROSCOPIC EXAMINATION	>	20	uM	>	80	IN THE PRESENCE OF 50% NHS	16554152	A 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-1	1	P24	MT-4		Integrase		<	0.103	uM	95	%	0.103	uM	MICROSCOPIC EXAMINATION	>	20	uM	>	194	IN THE PRESENCE OF 10% FBS	16554152	A 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-1	NL4-3	RT	MT-4		Reverse transcriptase		<	1	uM	100	%	1	uM	WST-8	>	1	uM	>	1	MEASUREMENTS WERE MADE ON DAY 4, 6 AND 8 POST INFECTION	15371436	POLYARGININE 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-1	LAI	RT	HuT 78		Reverse transcriptase		<	1	uM	57.14	%	1	uM	MTT	>	10	uM	>	10	MEASUREMENT WAS MADE ON DAY10 POSTINFECTION AT 10 TCID50	9281520	USE OF HERPES SIMPLEX VIRUS THYMIDINE KINASE TO IMPROVE THE ANTIVIRAL ACTIVITY OF ZIDOVUDINE. Virology 1997, 235, 398-405.