2017-89-2 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：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.

EXPID	PREFIX	CONCENTRATION_UNIT	CONCENTRATION	PANELNBR	CELLNBR	PANELNAME	CELLNAME	PANELCODE	M_GIPRCNT	N_GIPRCNT	EXP_COUNT
2106OS49	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	88.231	1	1
2106OS49	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	87.1119	1	1
2106OS49	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	14.4371	1	1
2106OS49	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	89.7113	1	1
2106OS49	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	97.2463	1	1
2106OS49	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	90.0129	1	1
2106OS49	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	85.7031	1	1
2106OS49	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	30.8539	1	1
2106OS49	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	14.2896	1	1
2106OS49	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	85.8526	1	1
2106OS49	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	83.1036	1	1
2106OS49	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	84.2194	1	1
2106OS49	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	89.3237	1	1
2106OS49	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	85.6034	1	1
2106OS49	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	89.6643	1	1
2106OS52	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	91.2503	1	1
2106OS52	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	94.8714	1	1
2106OS52	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	93.7372	1	1
2106OS52	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	112.6132	1	1
2106OS52	S	M	1.0E-5	5	1	Breast Cancer	MCF7	BRE	73.375	1	1

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

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.

EXPID	PREFIX	CONCENTRATION_UNIT	CONCENTRATION	PANELNBR	CELLNBR	PANELNAME	CELLNAME	PANELCODE	M_GIPRCNT	N_GIPRCNT	EXP_COUNT
0809OS51	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	89.6274	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	94.0185	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	77.1805	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	76.1686	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	82.5618	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	88.7561	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	83.5845	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	92.7497	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	70.9555	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	58.7306	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	72.6041	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	90.3839	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	110.2345	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	97.6538	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	93.7697	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	56.4618	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	80.8893	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	79.078	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	-20.3008	1	1
0810OS71	S	M	1.0E-5	6	10	Ovarian Cancer	IGROV1	OVA	72.0949	1	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

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.