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

来源：20881 靶标：interleukin-1 receptor-like 1 isoform [homo sapiens]

External ID: ST2_IL33_Inhibitors_Primary_Screening_77700

Protocol: High-throughput screening was performed at Indiana University screening facility (Indiana University, Indianapolis, IN).

In summary, a mixture of ST2 and IL-33 was prepared by adding 0.30 microL of 14.1 microM recombinant human ST2-Fc Chimera and 0.30 microL of 55.25 biotinylated recombinant human IL-33 to 1.4 mL of assay buffer. In the HTS, each well of a 384-well Proxi-plate was first blocked by 100 microL of assay buffer for 1 h at room temperature. After removing the blocking buffer, 20 microL of ST2/IL-33 mixture was pipetted into each well and incubated at room temperature for 1 h followed by addition of compounds at 17 microM (0.8 microL) to each well and incubated at room temperature for 1 h. Ten microliters of 60 microg/mL anti-6xHis-conjugated AlphaLISA acceptor beads were added to each well and incubated at room temperature for 1 h before addition of 10 microL of 60 microg/mL of streptavidin-labeled AlphaLISA donor beads for incubation at room temperature for 30 min. Incubation of acceptor and receptor beads was conducted in darkness. The well with 3 nM ST2 alone was used as a negative control, whereas the ST2/IL-33 mixture with a human ST2 antibody added at 0.45 ng/microL was used as the positive control. Plates were read using the Envision Plate Reader. The buffer used in the assay contains 14.37 mL PBS, 30 microL Tween 20, and 600 microL of 5% bovine serum albumin in PBS.

Comment: PubChem active indicates >= 30% inhibition of ST2/IL-33 at 17 uM of the compound. Inconclusive: >=10% and < 30% inhibition.

% Inhibition
98
97
97
97
97
97
96
96
96
96
95
95
94
94
93
92
92
89
88
85

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

来源：ChEMBL 靶标：Bacillus anthracis

External ID: CHEMBL1690567

Protocol: N/A

Comment: Journal: Antimicrob Agents Chemother
Year: 2010
Volume: 54
Issue: 12
First Page: 5329
Last Page: 5336
DOI: 10.1128/aac.01029-10

Target ChEMBL ID: CHEMBL613904
ChEMBL Target Name: Bacillus anthracis
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular

PubChem Standard Value	Standard Type	Standard Relation	Standard Value	Standard Units	Activity Comment	Data Validity Comment
	IC50				Not Active
50	IC50	=	50000	nM
20	IC50	=	20000	nM
	IC50				Not Active
	IC50				Not Active
190	IC50	=	190000	nM		Outside typical range
	IC50				Not Active
	IC50				Not Active
	IC50				Not Active
	IC50				Not Active
1550	IC50	=	1550000	nM		Outside typical range
	IC50				Not Active
320	IC50	=	320000	nM		Outside typical range
890	IC50	=	890000	nM		Outside typical range
	IC50				Not Active
700	IC50	=	700000	nM		Outside typical range
7190	IC50	=	7190000	nM		Outside typical range
350	IC50	=	350000	nM		Outside typical range
	IC50				Not Active
360	IC50	=	360000	nM		Outside typical range

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

来源：ChEMBL 靶标：Bacillus anthracis

External ID: CHEMBL1690568

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: Antimicrob Agents Chemother
Year: 2010
Volume: 54
Issue: 12
First Page: 5329
Last Page: 5336
DOI: 10.1128/aac.01029-10

Target ChEMBL ID: CHEMBL613904
ChEMBL Target Name: Bacillus anthracis
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular

PubChem Standard Value	Standard Type	Standard Relation	Standard Value	Standard Units	Activity Comment	Data Validity Comment
2	IC50	=	2000	nM
1040	IC50	=	1040000	nM		Outside typical range
20	IC50	=	20000	nM
	IC50				Not Active
	IC50				Not Active
	IC50				Not Active
400	IC50	=	400000	nM		Outside typical range
	IC50				Not Active
	IC50				Not Active
200	IC50	=	200000	nM		Outside typical range
	IC50				Not Active
	IC50				Not Active
	IC50				Not Active
190	IC50	=	190000	nM		Outside typical range
	IC50				Not Active
	IC50				Not Active
	IC50				Not Active
	IC50				Not Active
40	IC50	=	40000	nM
	IC50				Not Active

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

来源：ChEMBL 靶标：J774.A1

External ID: CHEMBL1690571

Protocol: N/A

Comment: Journal: Antimicrob. Agents Chemother.
Year: 2010
Volume: 54
Issue: 12
First Page: 5329
Last Page: 5336
DOI: 10.1128/aac.01029-10

Target ChEMBL ID: CHEMBL614040
ChEMBL Target Name: J774.A1
ChEMBL Target Type: CELL-LINE - Target is a specific cell-line
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular

Standard Type	Activity Comment
Activity	Non-toxic
Activity	Non-toxic
Activity	Non-toxic
Activity	Non-toxic
Activity	Non-toxic
Activity	Non-toxic
Activity	Non-toxic
Activity	Non-toxic
Activity	Non-toxic
Activity	Non-toxic
Activity	Non-toxic
Activity	Non-toxic
Activity	Non-toxic
Activity	Non-toxic
Activity	Non-toxic
Activity	Non-toxic
Activity	Non-toxic
Activity	Non-toxic
Activity	Non-toxic
Activity	Non-toxic

2139-60-8 靶点实验数据