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

来源：ChEMBL 靶标：Reverse transcriptase/RNaseH

External ID: CHEMBL800644

Protocol: N/A

Comment: Journal: J. Med. Chem.
Year: 1996
Volume: 39
Issue: 26
First Page: 5267
Last Page: 5275
DOI: 10.1021/jm960269m

Target ChEMBL ID: CHEMBL247
ChEMBL Target Name: Human immunodeficiency virus type 1 reverse transcriptase
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 Type	Standard Relation	Standard Value	Standard Units
Inhibition	=	98	%
Inhibition	=	92	%
Inhibition	=	97	%
Inhibition	=	96	%
Inhibition	=	91	%
Inhibition	=	0	%
Inhibition	=	0	%

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: CHEMBL763518

Protocol: N/A

Comment: Journal: J. Med. Chem.
Year: 1996
Volume: 39
Issue: 26
First Page: 5267
Last Page: 5275
DOI: 10.1021/jm960269m

Standard Type	Activity Comment
ED50	Not Determined

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: CHEMBL635112

Protocol: N/A

Comment: Journal: J. Med. Chem.
Year: 1996
Volume: 39
Issue: 26
First Page: 5267
Last Page: 5275
DOI: 10.1021/jm960269m

Standard Type	Standard Relation	Standard Value	Standard Units
T1/2	=	0.18	hr
T1/2	=	0.245	hr
T1/2	=	0.06	hr
T1/2	=	0.3667	hr
T1/2	=	0.1667	hr

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：ChEMBL 靶标：N/A

External ID: CHEMBL844096

Protocol: N/A

Comment: Journal: J. Med. Chem.
Year: 1996
Volume: 39
Issue: 26
First Page: 5267
Last Page: 5275
DOI: 10.1021/jm960269m

Standard Type	Standard Relation	Standard Value
Fold resistance	=	1.3
Fold resistance	=	33.3
Fold resistance	=	20

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: CHEMBL844095

Protocol: N/A

Comment: Journal: J. Med. Chem.
Year: 1996
Volume: 39
Issue: 26
First Page: 5267
Last Page: 5275
DOI: 10.1021/jm960269m

Standard Type	Standard Relation	Standard Value
Fold resistance	=	3.8
Fold resistance	=	16.7
Fold resistance	=	12

179556-87-7 靶点实验数据