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: CHEMBL4258734

Protocol: N/A

Comment: Journal: MedChemComm
Year: 2018
Volume: 9
Issue: 3
First Page: 576
Last Page: 582
DOI: 10.1039/C7MD00629B

Standard Type	Standard Relation	Standard Value
Selectivity ratio	=	1
Selectivity ratio	=	32
Selectivity ratio	=	3
Selectivity ratio	=	1

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: CHEMBL4258733

Protocol: N/A

Comment: Journal: MedChemComm
Year: 2018
Volume: 9
Issue: 3
First Page: 576
Last Page: 582
DOI: 10.1039/C7MD00629B

Standard Type	Standard Relation	Standard Value
Selectivity ratio	=	6
Selectivity ratio	=	3
Selectivity ratio	=	0.2
Selectivity ratio	=	0.6
Selectivity ratio	=	0.4

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

来源：ChEMBL 靶标：Alpha-1D adrenergic receptor

External ID: CHEMBL4258730

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: MedChemComm
Year: 2018
Volume: 9
Issue: 3
First Page: 576
Last Page: 582
DOI: 10.1039/C7MD00629B

Target ChEMBL ID: CHEMBL223
ChEMBL Target Name: Alpha-1d adrenergic receptor
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: D - Direct protein target assigned
Confidence: Direct single protein target assigned

PubChem Standard Value	Standard Type	Standard Relation	Standard Value	Standard Units
	pKb	=	6.78
0.046	Kb	=	46	nM
	pKb	=	7.34
0.0922	Kb	=	92.2	nM
	pKb	=	7.04
0.116	Kb	=	116	nM
	pKb	=	6.94

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

来源：ChEMBL 靶标：Alpha-1B adrenergic receptor

External ID: CHEMBL4258729

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: MedChemComm
Year: 2018
Volume: 9
Issue: 3
First Page: 576
Last Page: 582
DOI: 10.1039/C7MD00629B

Target ChEMBL ID: CHEMBL232
ChEMBL Target Name: Alpha-1b adrenergic receptor
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: D - Direct protein target assigned
Confidence: Direct single protein target assigned

PubChem Standard Value	Standard Type	Standard Relation	Standard Value	Standard Units
	pKb	=	7.22
0.266	Kb	=	266	nM
	pKb	=	6.57
0.154	Kb	=	154	nM
	pKb	=	6.81
0.316	Kb	=	316	nM
	pKb	=	6.5

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: CHEMBL4258732

Protocol: N/A

Comment: Journal: MedChemComm
Year: 2018
Volume: 9
Issue: 3
First Page: 576
Last Page: 582
DOI: 10.1039/C7MD00629B

Standard Type	Standard Relation	Standard Value
Selectivity ratio	=	0.1
Selectivity ratio	=	4
Selectivity ratio	=	0.1
Selectivity ratio	=	1
Selectivity ratio	=	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: CHEMBL4258731

Protocol: N/A

Comment: Journal: MedChemComm
Year: 2018
Volume: 9
Issue: 3
First Page: 576
Last Page: 582
DOI: 10.1039/C7MD00629B

Standard Type	Standard Relation	Standard Value
Selectivity ratio	=	0.02
Selectivity ratio	=	2
Selectivity ratio	=	0.8
Selectivity ratio	=	2
Selectivity ratio	=	5

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

来源：ChEMBL 靶标：NON-PROTEIN TARGET

External ID: CHEMBL2317234

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2013
Volume: 21
Issue: 3
First Page: 779
Last Page: 787
DOI: 10.1016/j.bmc.2012.11.038

Target ChEMBL ID: CHEMBL3879801
ChEMBL Target Name: NON-PROTEIN TARGET
ChEMBL Target Type: NON-MOLECULAR - Target has not been defined at a molecular level, only the non-molecular entity which is affected (e.g., organism, cell line etc)
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular

Standard Type	Standard Relation	Standard Value
FC	=	0.65
FC	=	0.88

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

来源：ChEMBL 靶标：Polyphenol oxidase 2

External ID: CHEMBL2317233

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2013
Volume: 21
Issue: 3
First Page: 779
Last Page: 787
DOI: 10.1016/j.bmc.2012.11.038

Target ChEMBL ID: CHEMBL3318
ChEMBL Target Name: Tyrosinase
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: D - Direct protein target assigned
Confidence: Direct single protein target assigned

Standard Type	Standard Relation	Standard Value	Standard Units
Inhibition	<	3	%
Inhibition	<	3	%

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

来源：ChEMBL 靶标：NON-PROTEIN TARGET

External ID: CHEMBL2317238

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2013
Volume: 21
Issue: 3
First Page: 779
Last Page: 787
DOI: 10.1016/j.bmc.2012.11.038

Target ChEMBL ID: CHEMBL3879801
ChEMBL Target Name: NON-PROTEIN TARGET
ChEMBL Target Type: NON-MOLECULAR - Target has not been defined at a molecular level, only the non-molecular entity which is affected (e.g., organism, cell line etc)
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular

Standard Type	Standard Relation	Standard Value
FC	=	0.74
FC	=	0.72

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

来源：ChEMBL 靶标：NON-PROTEIN TARGET

External ID: CHEMBL2317237

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2013
Volume: 21
Issue: 3
First Page: 779
Last Page: 787
DOI: 10.1016/j.bmc.2012.11.038

Target ChEMBL ID: CHEMBL3879801
ChEMBL Target Name: NON-PROTEIN TARGET
ChEMBL Target Type: NON-MOLECULAR - Target has not been defined at a molecular level, only the non-molecular entity which is affected (e.g., organism, cell line etc)
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular

Standard Type	Standard Relation	Standard Value
FC	=	0.36
FC	=	0.49

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

来源：ChEMBL 靶标：NON-PROTEIN TARGET

External ID: CHEMBL2317236

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2013
Volume: 21
Issue: 3
First Page: 779
Last Page: 787
DOI: 10.1016/j.bmc.2012.11.038

Target ChEMBL ID: CHEMBL3879801
ChEMBL Target Name: NON-PROTEIN TARGET
ChEMBL Target Type: NON-MOLECULAR - Target has not been defined at a molecular level, only the non-molecular entity which is affected (e.g., organism, cell line etc)
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular

Standard Type	Standard Relation	Standard Value
FC	=	1.11
FC	=	1.1

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

来源：ChEMBL 靶标：NON-PROTEIN TARGET

External ID: CHEMBL2317235

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2013
Volume: 21
Issue: 3
First Page: 779
Last Page: 787
DOI: 10.1016/j.bmc.2012.11.038

Target ChEMBL ID: CHEMBL3879801
ChEMBL Target Name: NON-PROTEIN TARGET
ChEMBL Target Type: NON-MOLECULAR - Target has not been defined at a molecular level, only the non-molecular entity which is affected (e.g., organism, cell line etc)
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular

Standard Type	Standard Relation	Standard Value
FC	=	0.71
FC	=	0.96

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

来源：ChEMBL 靶标：Serotonin 2 receptors; 5-HT2a & 5-HT2c

External ID: CHEMBL4258726

Protocol: N/A

Comment: Journal: MedChemComm
Year: 2018
Volume: 9
Issue: 3
First Page: 576
Last Page: 582
DOI: 10.1039/C7MD00629B

Target ChEMBL ID: CHEMBL2096662
ChEMBL Target Name: Serotonin 2 receptors; 5-HT2a & 5-HT2c
ChEMBL Target Type: SELECTIVITY GROUP - Target is a pair of proteins for which the selectivity has been assessed
Relationship Type: D - Direct protein target assigned
Confidence: Multiple direct protein targets may be assigned

Standard Type	Standard Relation	Standard Value
Selectivity ratio	=	60
Selectivity ratio	=	0.6
Selectivity ratio	=	1
Selectivity ratio	=	2
Selectivity ratio	=	0.4

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: CHEMBL4258725

Protocol: N/A

Comment: Journal: MedChemComm
Year: 2018
Volume: 9
Issue: 3
First Page: 576
Last Page: 582
DOI: 10.1039/C7MD00629B

Standard Type	Standard Relation	Standard Value
Selectivity ratio	=	1000
Selectivity ratio	=	0.5
Selectivity ratio	=	8
Selectivity ratio	=	2
Selectivity ratio	=	0.5

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

来源：ChEMBL 靶标：Alpha-1A adrenergic receptor

External ID: CHEMBL4258728

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: MedChemComm
Year: 2018
Volume: 9
Issue: 3
First Page: 576
Last Page: 582
DOI: 10.1039/C7MD00629B

Target ChEMBL ID: CHEMBL229
ChEMBL Target Name: Alpha-1a adrenergic receptor
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: D - Direct protein target assigned
Confidence: Direct single protein target assigned

PubChem Standard Value	Standard Type	Standard Relation	Standard Value	Standard Units
	pKb	=	7.31
0.338	Kb	=	338	nM
	pKb	=	6.38
0.086	Kb	=	86	nM
	pKb	=	6.62
0.0671	Kb	=	67.1	nM
	pKb	=	6.91

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: CHEMBL4258727

Protocol: N/A

Comment: Journal: MedChemComm
Year: 2018
Volume: 9
Issue: 3
First Page: 576
Last Page: 582
DOI: 10.1039/C7MD00629B

Standard Type	Standard Relation	Standard Value
Selectivity ratio	=	20
Selectivity ratio	=	1
Selectivity ratio	=	6
Selectivity ratio	=	1
Selectivity ratio	=	1

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

来源：ChEMBL 靶标：5-hydroxytryptamine receptor 2A

External ID: CHEMBL4258722

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: MedChemComm
Year: 2018
Volume: 9
Issue: 3
First Page: 576
Last Page: 582
DOI: 10.1039/C7MD00629B

Target ChEMBL ID: CHEMBL224
ChEMBL Target Name: Serotonin 2a (5-HT2a) receptor
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: D - Direct protein target assigned
Confidence: Direct single protein target assigned

PubChem Standard Value	Standard Type	Standard Relation	Standard Value	Standard Units
	pKb	=	7.18
0.0108	Kb	=	10.8	nM
	pKb	=	7.88
0.0429	Kb	=	42.9	nM
	pKb	=	7.06
0.0843	Kb	=	84.3	nM
	pKb	=	6.85

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

来源：ChEMBL 靶标：5-hydroxytryptamine receptor 2C

External ID: CHEMBL4258724

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: MedChemComm
Year: 2018
Volume: 9
Issue: 3
First Page: 576
Last Page: 582
DOI: 10.1039/C7MD00629B

Target ChEMBL ID: CHEMBL225
ChEMBL Target Name: Serotonin 2c (5-HT2c) receptor
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: D - Direct protein target assigned
Confidence: Direct single protein target assigned

PubChem Standard Value	Standard Type	Standard Relation	Standard Value	Standard Units
	pKb	=	7.44
0.0151	Kb	=	15.1	nM
	pKb	=	7.82
0.0769	Kb	=	76.9	nM
	pKb	=	7.12
0.0417	Kb	=	41.7	nM
	pKb	=	7.51

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

来源：ChEMBL 靶标：5-hydroxytryptamine receptor 2B

External ID: CHEMBL4258723

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: MedChemComm
Year: 2018
Volume: 9
Issue: 3
First Page: 576
Last Page: 582
DOI: 10.1039/C7MD00629B

Target ChEMBL ID: CHEMBL1833
ChEMBL Target Name: Serotonin 2b (5-HT2b) receptor
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: D - Direct protein target assigned
Confidence: Direct single protein target assigned

PubChem Standard Value	Standard Type	Standard Relation	Standard Value	Standard Units
	pKb	=	7.51
0.084	Kb	=	84	nM
	pKb	=	7.08
0.0927	Kb	=	92.7	nM
	pKb	=	7.03
0.0417	Kb	=	41.7	nM
	pKb	=	7.38

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: CHEMBL2317249

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2013
Volume: 21
Issue: 3
First Page: 779
Last Page: 787
DOI: 10.1016/j.bmc.2012.11.038

Standard Type	Standard Relation	Standard Value	Standard Units	Data Validity Comment
Inhibition	=	-54.2	%	Outside typical range
Inhibition	=	9.4	%
Inhibition	=	12.1	%
Inhibition	=	38.1	%
Inhibition	=	18.3	%
Inhibition	=	-1.5	%
Inhibition	=	34	%
Inhibition	=	32.1	%
Inhibition	=	12.1	%
Inhibition	=	27.3	%
Inhibition	=	37.9	%
Inhibition	=	11.8	%

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: CHEMBL2317248

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2013
Volume: 21
Issue: 3
First Page: 779
Last Page: 787
DOI: 10.1016/j.bmc.2012.11.038

Standard Type	Standard Relation	Standard Value	Standard Units
Inhibition	=	2.8	%
Inhibition	=	16.5	%
Inhibition	=	39.7	%
Inhibition	=	61.5	%
Inhibition	=	40.3	%
Inhibition	=	65.3	%
Inhibition	=	50.4	%
Inhibition	=	72.3	%
Inhibition	=	17.6	%
Inhibition	=	65.9	%
Inhibition	=	70.6	%
Inhibition	=	8	%

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: CHEMBL2317247

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2013
Volume: 21
Issue: 3
First Page: 779
Last Page: 787
DOI: 10.1016/j.bmc.2012.11.038

Standard Type	Standard Relation	Standard Value	Standard Units
Inhibition	=	26.1	%
Inhibition	=	15.9	%
Inhibition	=	36.2	%
Inhibition	=	83.7	%
Inhibition	=	66.4	%
Inhibition	=	80.3	%
Inhibition	=	89.3	%
Inhibition	=	91.9	%
Inhibition	=	90.5	%
Inhibition	=	78.4	%

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

来源：ChEMBL 靶标：NON-PROTEIN TARGET

External ID: CHEMBL2317242

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2013
Volume: 21
Issue: 3
First Page: 779
Last Page: 787
DOI: 10.1016/j.bmc.2012.11.038

Target ChEMBL ID: CHEMBL3879801
ChEMBL Target Name: NON-PROTEIN TARGET
ChEMBL Target Type: NON-MOLECULAR - Target has not been defined at a molecular level, only the non-molecular entity which is affected (e.g., organism, cell line etc)
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular

Standard Type	Standard Relation	Standard Value
FC	=	0.61
FC	=	0.65

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

来源：ChEMBL 靶标：NON-PROTEIN TARGET

External ID: CHEMBL2317241

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2013
Volume: 21
Issue: 3
First Page: 779
Last Page: 787
DOI: 10.1016/j.bmc.2012.11.038

Target ChEMBL ID: CHEMBL3879801
ChEMBL Target Name: NON-PROTEIN TARGET
ChEMBL Target Type: NON-MOLECULAR - Target has not been defined at a molecular level, only the non-molecular entity which is affected (e.g., organism, cell line etc)
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular

Standard Type	Standard Relation	Standard Value
FC	=	0.64
FC	=	0.76

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

来源：ChEMBL 靶标：NON-PROTEIN TARGET

External ID: CHEMBL2317240

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2013
Volume: 21
Issue: 3
First Page: 779
Last Page: 787
DOI: 10.1016/j.bmc.2012.11.038

Target ChEMBL ID: CHEMBL3879801
ChEMBL Target Name: NON-PROTEIN TARGET
ChEMBL Target Type: NON-MOLECULAR - Target has not been defined at a molecular level, only the non-molecular entity which is affected (e.g., organism, cell line etc)
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular

Standard Type	Standard Relation	Standard Value
FC	=	0.38
FC	=	0.53

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

来源：ChEMBL 靶标：NON-PROTEIN TARGET

External ID: CHEMBL2317239

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2013
Volume: 21
Issue: 3
First Page: 779
Last Page: 787
DOI: 10.1016/j.bmc.2012.11.038

Target ChEMBL ID: CHEMBL3879801
ChEMBL Target Name: NON-PROTEIN TARGET
ChEMBL Target Type: NON-MOLECULAR - Target has not been defined at a molecular level, only the non-molecular entity which is affected (e.g., organism, cell line etc)
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular

Standard Type	Standard Relation	Standard Value
FC	=	0.76
FC	=	0.79

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: CHEMBL2317246

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.
Year: 2013
Volume: 21
Issue: 3
First Page: 779
Last Page: 787
DOI: 10.1016/j.bmc.2012.11.038

PubChem Standard Value	Standard Type	Standard Relation	Standard Value	Standard Units
25.6	IC50	=	25600	nM
15.8	IC50	=	15800	nM
62.9	IC50	=	62900	nM
13.3	IC50	=	13300	nM
2	IC50	=	2000	nM
19.3	IC50	=	19300	nM
85	IC50	=	85000	nM
5	IC50	=	5000	nM

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: CHEMBL2317245

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2013
Volume: 21
Issue: 3
First Page: 779
Last Page: 787
DOI: 10.1016/j.bmc.2012.11.038

Standard Type	Standard Relation	Standard Value	Standard Units
Inhibition	=	86	%
Inhibition	=	86	%
Inhibition	=	86	%
Inhibition	=	86	%
Inhibition	=	69	%
Inhibition	=	86	%
Inhibition	=	86	%
Inhibition	=	86	%
Inhibition	=	86	%
Inhibition	=	86	%
Inhibition	=	69	%

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: CHEMBL2317244

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2013
Volume: 21
Issue: 3
First Page: 779
Last Page: 787
DOI: 10.1016/j.bmc.2012.11.038

Standard Type	Standard Relation	Standard Value	Standard Units
Inhibition	=	46	%
Inhibition	=	82	%
Inhibition	=	46	%
Inhibition	=	82	%
Inhibition	=	22.5	%
Inhibition	=	82	%
Inhibition	=	46	%
Inhibition	=	82	%
Inhibition	=	39.7	%
Inhibition	=	82	%
Inhibition	=	77	%

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: CHEMBL2319192

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2013
Volume: 21
Issue: 3
First Page: 779
Last Page: 787
DOI: 10.1016/j.bmc.2012.11.038

Standard Type	Standard Relation	Standard Value	Standard Units	Data Validity Comment
Inhibition	=	-12.6	%	Outside typical range
Inhibition	=	10.6	%
Inhibition	=	7.4	%
Inhibition	=	10.6	%
Inhibition	=	4	%
Inhibition	=	4.8	%
Inhibition	=	7.5	%
Inhibition	=	11.5	%
Inhibition	=	5.8	%
Inhibition	=	-2.6	%
Inhibition	=	15.4	%
Inhibition	=	14.5	%

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: CHEMBL2319191

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2013
Volume: 21
Issue: 3
First Page: 779
Last Page: 787
DOI: 10.1016/j.bmc.2012.11.038

Standard Type	Standard Relation	Standard Value	Standard Units	Data Validity Comment
Inhibition	=	-41.5	%	Outside typical range
Inhibition	=	9.7	%
Inhibition	=	-7.4	%
Inhibition	=	20.4	%
Inhibition	=	16.8	%
Inhibition	=	8.7	%
Inhibition	=	18.2	%
Inhibition	=	16.5	%
Inhibition	=	16.2	%
Inhibition	=	11.1	%
Inhibition	=	19.7	%
Inhibition	=	4.8	%

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

来源：26908 靶标：N/A

External ID: HTS97080

Protocol: 96-well plates were coated with 100 microl of 0.25 mg/ml biotin conjugated-gelatin overnight and then washed twice with PBS. Endothelial cells (3 x 104) were plated in pericyte-conditioned medium and the cells were grown to confluence for 6 days followed by the treatment with compounds for 24 h. On day seven, 6 microg/ml of NeutrAvidin TM, FITC conjugate (FITC-avidin, 60 kDa) (Thermo Fisher Scientific) was added to cells for 3 min. The cells were washed twice with PBS to remove the unbound FITC-avidin. Wells were filled with 100 microl of PBS and bound FITC-avidin fluorescence was measured using plate reader with wavelengths of 492 nm. The fluorescence units of cells treated with compounds were normalized to values of cells treated with vehicle (DMSO) and presented as average with standard deviation.

Comment: Measuring the fluorescence of FITC-avidin that has penetrated the endothelial monolayer and bound to a biotinylated gelatin-coated plate can be used as a surrogate parameter for endothelial permeability. Here we show the average FITC-avidin fluorescence of drug-treated cells as fold of vehicle-treated cells. Compounds causing 0.3-fold or higher fluorescence changes are considered active, while compounds causing changes of less than 0.3-fold are considered inactive.

Average (-fold FITC-avidin fluorescence normalized to DMSO)	Standard Deviation	CHEMICAL NAME
1.4	0.03	Phenserine
0.8	0.04	Felbamate
0.8	0.09	Fusaric acid
1.3	0.01	Flunarizine dihydrochloride
1.2	0.05	cis-(Z)-Flupenthixol dihydrochloride
0.9	0.11	L-Glutamic acid hydrochloride
1	0.19	GW7647
1.2	0.05	Ellipticine
0.7	0.03	Ethosuximide
0.8	0	N-Methyl-beta-carboline-3-carboxamide
1	0.02	Fusidic acid sodium
0.8	0.02	Furosemide
0.8	0.05	5-Fluorouracil
0.8	0.01	5-fluoro-5'-deoxyuridine
0.7	0	Furafylline
0.8	0.04	Ganciclovir
0.9	0.05	NS5806
0.7	0.02	RepSox
1.1	0.04	Nitidine chloride
1.2	0.14	SGC-AAK1-1N

475-83-2 靶点实验数据