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

来源：ChEMBL 靶标：Fatty acid-binding protein, adipocyte

External ID: CHEMBL3830761

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2016
Volume: 24
Issue: 18
First Page: 4310
Last Page: 4317
DOI: 10.1016/j.bmc.2016.07.022

Target ChEMBL ID: CHEMBL2083
ChEMBL Target Name: Fatty acid binding protein adipocyte
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	Data Validity Comment
Inhibition	=	82.1	%
Inhibition	=	27.9	%
Inhibition	=	-50.8	%	Outside typical range
Inhibition	=	4.9	%
Inhibition	=	-3.2	%
Inhibition	=	-3.6	%
Inhibition	=	-16.6	%	Outside typical range
Inhibition	=	-0.2	%
Inhibition	=	17.1	%
Inhibition	=	-31.7	%	Outside typical range
Inhibition	=	20.3	%
Inhibition	=	13	%
Inhibition	=	2.1	%
Inhibition	=	95.1	%
Inhibition	=	-7.7	%

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

来源：ChEMBL 靶标：Fatty acid-binding protein, adipocyte

External ID: CHEMBL3830763

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2016
Volume: 24
Issue: 18
First Page: 4310
Last Page: 4317
DOI: 10.1016/j.bmc.2016.07.022

Target ChEMBL ID: CHEMBL2083
ChEMBL Target Name: Fatty acid binding protein adipocyte
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
Delta Tm	=	3.3	degrees C
Delta Tm	=	1.1	degrees C
Delta Tm	=	10.6	degrees C
Delta Tm	=	2.8	degrees C
Delta Tm	=	-9.1	degrees C
Delta Tm	=	1	degrees C
Delta Tm	=	0	degrees C
Delta Tm	=	-0.1	degrees C
Delta Tm	=	3.1	degrees C
Delta Tm	=	-0.6	degrees C
Delta Tm	=	0	degrees C
Delta Tm	=	0.8	degrees C
Delta Tm	=	1.2	degrees C
Delta Tm	=	2	degrees C
Delta Tm	=	0.5	degrees C
Delta Tm	=	8.5	degrees C
Delta Tm	=	-0.1	degrees C

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

来源：Center for Chemical Genomics, University of Michigan 靶标：

External ID: MScreen:TargetID_600

Protocol: C-terminally 6xHis tagged CDK2/Cyclin A complex and N-terminally Flag tagged CDC25B C473S (372-566) were expressed and purified. Proteins were incubated together at a final concentration of 125 nM each for 1 hr prior to incubation with compound for 1 hr, followed by addition of anti-6xHis europium cryptate donor beads (Cisbio) and anti-Flag XL-665 acceptor beads (Cisbio) at a final dilution of 1:350 for 1 hr. 20mM potassium fluoride was added 10 minute prior to plate reading. Assay reagents were dispensed using a multidrop liquid dispenser (Thermo Scientific) onto uncoated, black, low-volume, 384-well plates (Corning). Assay plates were quantified using an Envision plate reader (Perkin-Elmer) with excitation of the europium crytate donor at 337 nm wavelength and emission of the donor at 620 nm and emission of the XL-665 acceptor at 665 nm in 18 uL volumes. Assays were performed in a buffer containing 50 mM Tris (pH 7.5), 50 mM NaCl, 10mM MgCl2, 1mM TCEP, with addition of and 1mM ATP, 0.05% BSA, and 0.05% Tween-20 immediately prior to the start of the assay.

Comment: The activity outcome is based on a Z-score (number of standard deviations from the negative control mean) of 3 or higher on at least 50% times that the sample was screened.
For instance, if the sample was screened in n=4 runs, it would be considered active only if it had a Z-score of 3 or above in at least 2 runs.

This screen was funded by NIH grant number: R01CA181185

Z_SCORE
0.28
-0.54
-0.02
0.22
0.37
-0.81
-0.26
-0.14
-0.61
-0.44
0.29
0.22
-0.12
-0.13
0.95
-0.29
-0.37
0.17
-0.64
-0.78

369403-62-3 靶点实验数据