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

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

来源：ChEMBL 靶标：G-protein coupled receptor 3

External ID: CHEMBL5366025

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 Lett
Year: 2023
Volume: 94
First Page: 129427
Last Page: 129427
DOI: 10.1016/j.bmcl.2023.129427

Target ChEMBL ID: CHEMBL4523856
ChEMBL Target Name: G-protein coupled receptor 3
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	Activity Comment	Data Validity Comment
5.17	EC50	=	5170	nM
7.6	EC50	=	7600	nM
67	EC50	=	67000	nM
29	EC50	=	29000	nM
40	EC50	=	40000	nM
60	EC50	=	60000	nM
382	EC50	=	382000	nM		Outside typical range
1.31	EC50	=	1310	nM
	EC50				Not Determined
105	EC50	=	105000	nM		Outside typical range
19.3	EC50	=	19300	nM
66	EC50	=	66000	nM
86	EC50	=	86000	nM
0.137	EC50	=	137	nM
0.923	EC50	=	923	nM

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

来源：ChEMBL 靶标：G-protein coupled receptor 3

External ID: CHEMBL5366026

Protocol: N/A

Comment: Journal: Bioorg Med Chem Lett
Year: 2023
Volume: 94
First Page: 129427
Last Page: 129427
DOI: 10.1016/j.bmcl.2023.129427

Target ChEMBL ID: CHEMBL4523856
ChEMBL Target Name: G-protein coupled receptor 3
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
Emax	=	33	%
Emax	=	18	%
Emax	=	63	%
Emax	=	50	%
Emax	=	26	%
Emax	=	69	%
Emax	=	72	%
Emax	=	24	%
Emax	=	60	%
Emax	=	13	%
Emax	=	40	%
Emax	=	24	%

3955-65-5 靶点实验数据