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_11026_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 Type	PubChem Standard Value	Kd	Target Accession(s)	Ligand	Target
Kd	9	9000	P35968	BDBM8195	Vascular endothelial growth factor receptor 2
Kd	0.016	16	P35968	BDBM15003	Vascular endothelial growth factor receptor 2
Kd	1.4	1400	P35968	BDBM24997	Vascular endothelial growth factor receptor 2
Kd	10	10000	P35968	BDBM25981	Vascular endothelial growth factor receptor 2
Kd	10	10000	P35968	BDBM50099967	Vascular endothelial growth factor receptor 2
Kd	10	10000	P35968	BDBM50105748	Vascular endothelial growth factor receptor 2
Kd	10	10000	P35968	BDBM50105753	Vascular endothelial growth factor receptor 2
Kd	1.4	1400	P35968	BDBM50246060	Vascular endothelial growth factor receptor 2
Kd	10	10000	P35968	BDBM50255997	Vascular endothelial growth factor receptor 2
Kd	10	10000	P35968	BDBM50263167	Vascular endothelial growth factor receptor 2
Kd	10	10000	P35968	BDBM50275550	Vascular endothelial growth factor receptor 2
Kd	10	10000	P35968	BDBM50275614	Vascular endothelial growth factor receptor 2
Kd	10	10000	P35968	BDBM50332592	Vascular endothelial growth factor receptor 2
Kd	1.7	1700	P35968	BDBM50349213	Vascular endothelial growth factor receptor 2
Kd	10	10000	P35968	BDBM50381156	Vascular endothelial growth factor receptor 2
Kd	10	10000	P35968	BDBM50418244	Vascular endothelial growth factor receptor 2
Kd	0.015	15	P35968	BDBM50444212	Vascular endothelial growth factor receptor 2
Kd	0.022	22	P35968	BDBM50462635	Vascular endothelial growth factor receptor 2
Kd	2.3	2300	P35968	BDBM429420	Vascular endothelial growth factor receptor 2
Kd	10	10000	P35968	BDBM586644	Vascular endothelial growth factor receptor 2

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: CHEMBL3988182

Protocol: N/A

Comment: Data Source: GSK Published Kinase Inhibitor Set 2

Standard Type	Standard Relation	Standard Value	Standard Units	Activity Comment
MOTILITY REDUCTION/CYTOTOXICITY	=	0	%	Score 1
MOTILITY REDUCTION/CYTOTOXICITY	=	20	%	Score 1
MOTILITY REDUCTION/CYTOTOXICITY	=	100	%	Score 0
MOTILITY REDUCTION/CYTOTOXICITY	=	60	%	Score 0
MOTILITY REDUCTION/CYTOTOXICITY	=	0	%	Score 1
MOTILITY REDUCTION/CYTOTOXICITY	=	33.4	%	Score 1
MOTILITY REDUCTION/CYTOTOXICITY	=	33.4	%	Score 1
MOTILITY REDUCTION/CYTOTOXICITY	=	0	%	Score 1
MOTILITY REDUCTION/CYTOTOXICITY	=	0	%	Score 1
MOTILITY REDUCTION/CYTOTOXICITY	=	0	%	Score 1
MOTILITY REDUCTION/CYTOTOXICITY	=	0	%	Score 1
MOTILITY REDUCTION/CYTOTOXICITY	=	13.4	%	Score 1
MOTILITY REDUCTION/CYTOTOXICITY	=	0	%	Score 1
MOTILITY REDUCTION/CYTOTOXICITY	=	33.4	%	Score 1
MOTILITY REDUCTION/CYTOTOXICITY	=	0	%	Score 1
MOTILITY REDUCTION/CYTOTOXICITY	=	0	%	Score 1
MOTILITY REDUCTION/CYTOTOXICITY	=	33.4	%	Score 0
MOTILITY REDUCTION/CYTOTOXICITY	=	0	%	Score 1
MOTILITY REDUCTION/CYTOTOXICITY	=	0	%	Score 1
MOTILITY REDUCTION/CYTOTOXICITY	=	20	%	Score 1

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_11027_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 Type	PubChem Standard Value	Kd	Target Accession(s)	Ligand	Target
Kd	4.1	4100	O60674	BDBM50105743	Tyrosine-protein kinase JAK2
Kd	7.8	7800	O60674	BDBM50105753	Tyrosine-protein kinase JAK2
Kd	0.0092	9.2	O60674	BDBM50246060	Tyrosine-protein kinase JAK2
Kd	0.4	400	O60674	BDBM50263167	Tyrosine-protein kinase JAK2
Kd	0.072	72	O60674	BDBM50269948	Tyrosine-protein kinase JAK2
Kd	10	10000	O60674	BDBM50275550	Tyrosine-protein kinase JAK2
Kd	10	10000	O60674	BDBM50275614	Tyrosine-protein kinase JAK2
Kd	10	10000	O60674	BDBM50327046	Tyrosine-protein kinase JAK2
Kd	10	10000	O60674	BDBM50327047	Tyrosine-protein kinase JAK2
Kd	10	10000	O60674	BDBM50327065	Tyrosine-protein kinase JAK2
Kd	10	10000	O60674	BDBM50444208	Tyrosine-protein kinase JAK2
Kd	10	10000	O60674	BDBM429420	Tyrosine-protein kinase JAK2
Kd	10	10000	O60674	BDBM586644	Tyrosine-protein kinase JAK2
Kd	1.2	1200	O60674	BDBM586667	Tyrosine-protein kinase JAK2
Kd	2.8	2800	O60674	BDBM586680	Tyrosine-protein kinase JAK2
Kd	0.0078	7.8	O60674	BDBM586692	Tyrosine-protein kinase JAK2
Kd	0.042	42	O60674	BDBM5844	Tyrosine-protein kinase JAK2
Kd	0.73	730	O60674	BDBM15003	Tyrosine-protein kinase JAK2
Kd	10	10000	O60674	BDBM24997	Tyrosine-protein kinase JAK2
Kd	10	10000	O60674	BDBM25981	Tyrosine-protein kinase JAK2

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.

111908-95-3 靶点实验数据