HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16

来源：ChEMBL 靶标：DNA topoisomerase 2-beta

External ID: CHEMBL669723

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: J Med Chem
Year: 1992
Volume: 35
Issue: 5
First Page: 871
Last Page: 877
DOI: 10.1021/jm00083a010

Target ChEMBL ID: CHEMBL2094255
ChEMBL Target Name: DNA topoisomerase II
ChEMBL Target Type: PROTEIN FAMILY - Target is a group of closely related proteins
Relationship Type: D - Direct protein target assigned
Confidence: Multiple direct protein targets may be assigned

PubChem Standard Value	Standard Type	Standard Relation	Standard Value	Standard Units
100	ID50	>	100	uM
100	ID50	=	100	uM
100	ID50	>	100	uM
100	ID50	>	100	uM
50	ID50	=	50	uM

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: CHEMBL840314

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 1997
Volume: 7
Issue: 22
First Page: 2897
Last Page: 2902
DOI: 10.1016/S0960-894X(97)10108-1

Standard Type	Standard Relation	Standard Value
Therapeutic index	=	55556
Therapeutic index	=	10
Therapeutic index	=	55.8
Therapeutic index	=	2.1
Therapeutic index	=	1.8
Therapeutic index	=	2.1
Therapeutic index	=	2
Therapeutic index	=	3.9
Therapeutic index	=	4.4
Therapeutic index	=	3
Therapeutic index	=	12.5
Therapeutic index	=	4
Therapeutic index	=	3.3
Therapeutic index	>	141
Therapeutic index	>	158
Therapeutic index	=	4.1
Therapeutic index	>	166
Therapeutic index	=	0.8
Therapeutic index	>	120

HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16

来源：ChEMBL 靶标：H9

External ID: CHEMBL685387

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: Bioorg. Med. Chem. Lett.
Year: 1997
Volume: 7
Issue: 22
First Page: 2897
Last Page: 2902
DOI: 10.1016/S0960-894X(97)10108-1

Target ChEMBL ID: CHEMBL614806
ChEMBL Target Name: H9
ChEMBL Target Type: CELL-LINE - Target is a specific cell-line
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular

PubChem Standard Value	Standard Type	Standard Relation	Standard Value	Standard Units
1.7	IC50	=	1700	nM
0.07	IC50	=	70	nM
0.8	IC50	=	800	nM
1.7	IC50	=	1700	nM
45	IC50	=	45000	nM
0.32	IC50	=	320	nM
6.6	IC50	=	6600	nM
1.85	IC50	=	1850	nM
9.7	IC50	=	9700	nM
9	IC50	=	9000	nM
1.5	IC50	=	1500	nM
1.8	IC50	=	1800	nM
1.5	IC50	=	1500	nM
0.141	IC50	=	141	nM
0.158	IC50	=	158	nM
29	IC50	=	29000	nM
0.166	IC50	=	166	nM
1.9	IC50	=	1900	nM
8	IC50	=	8000	nM
0.12	IC50	=	120	nM

HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16

来源：ChEMBL 靶标：H9

External ID: CHEMBL683257

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: Bioorg. Med. Chem. Lett.
Year: 1997
Volume: 7
Issue: 22
First Page: 2897
Last Page: 2902
DOI: 10.1016/S0960-894X(97)10108-1

Target ChEMBL ID: CHEMBL614806
ChEMBL Target Name: H9
ChEMBL Target Type: CELL-LINE - Target is a specific cell-line
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular

PubChem Standard Value	Standard Type	Standard Relation	Standard Value	Standard Units
0.8	EC50	=	800	nM
0.45	EC50	=	450	nM
0.8	EC50	=	800	nM
0.16	EC50	=	160	nM
1.7	EC50	=	1700	nM
2.2	EC50	=	2200	nM
0.12	EC50	=	120	nM
0.45	EC50	=	450	nM
0.45	EC50	=	450	nM
0.001	EC50	<	1	nM
7	EC50	=	7000	nM
0.001	EC50	<	1	nM
10	EC50	=	10000	nM
0.001	EC50	<	1	nM
0.03	EC50	=	30	nM

HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16

来源：ChEMBL 靶标：Nucleic Acid

External ID: CHEMBL662925

Protocol: N/A

Comment: Journal: J. Med. Chem.
Year: 1992
Volume: 35
Issue: 5
First Page: 871
Last Page: 877
DOI: 10.1021/jm00083a010

Target ChEMBL ID: CHEMBL345
ChEMBL Target Name: Nucleic Acid
ChEMBL Target Type: NUCLEIC-ACID - Target is DNA, RNA or PNA
Relationship Type: M - Molecular target other than protein assigned
Confidence: Target assigned is molecular non-protein target

Standard Type	Standard Relation	Standard Value	Standard Units
Complex formation	=	213	%
Complex formation	=	323	%
Complex formation	=	8	%
Complex formation	=	125	%
Complex formation	=	75	%
Complex formation	=	52	%
Complex formation	=	108	%
Complex formation	=	127	%
Complex formation	=	100	%

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: CHEMBL705961

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: J. Med. Chem.
Year: 1992
Volume: 35
Issue: 5
First Page: 871
Last Page: 877
DOI: 10.1021/jm00083a010

PubChem Standard Value	Standard Type	Standard Relation	Standard Value	Standard Units
0.84	IC50	=	840	nM
1.5	IC50	=	1500	nM
2.1	IC50	>	2100	nM
0.78	IC50	=	780	nM
0.7	IC50	<	700	nM
2	IC50	=	2000	nM
1.46	IC50	=	1460	nM
1.9	IC50	>	1900	nM

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.

138355-97-2 靶点实验数据