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

来源：ChEMBL 靶标：Choline kinase alpha

External ID: CHEMBL3769133

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: J. Med. Chem.
Year: 2016
Volume: 59
Issue: 2
First Page: 671
Last Page: 686
DOI: 10.1021/acs.jmedchem.5b01552

Target ChEMBL ID: CHEMBL3117
ChEMBL Target Name: Choline kinase alpha
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
0.457	IC50	=	457	nM
300	IC50	>	300000	nM
0.165	IC50	=	165	nM
0.255	IC50	=	255	nM
17.2	IC50	=	17200	nM

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

来源：11908 靶标：N/A

External ID: RMI-FANCM-MM2

Protocol: FP HTS. Screening took place at the University of Wisconsin Small Molecule Screening and Synthesis Facility. A master mix of RMI core complex and F-MM2 (30 microL per well) was plated in black 384 shallow well plates (ThermoFisher, Waltham, MA), using a BioTek "MicroFlo Select" reagent dispenser. Compounds were added using a Beckman FX liquid handler; 0.33 microL of 10 mM stock was added for a final compound concentration of 33 microM. MM2 and cMM2 were each added to 4 wells of master mix per plate to a final concentration of 10 muM to serve as controls. Following compound addition, plates were covered, centrifuged briefly, and incubated for 20 minutes at room temperature. FP measurements were taking using a Tecan "Safire 2" microplate reader. Instrument settings were as follows: top read, EX 470, EM 525/20, G-factor 0.89947. A suitable gain was calculated from the first plate of each day. Z' scores for were calculated for each plate; plates with Z' scores <0.5 were rerun prior to analysis.

Comment:

Concentration uM	Data readout
33	55
33	63
33	65
33	63
33	61
33	62
33	61
33	58
33	71
33	61
33	64
33	83
33	158
33	84
33	104
33	60
33	62
33	59
33	58
33	59

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

来源：ChEMBL 靶标：Choline kinase alpha

External ID: CHEMBL3769127

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: J. Med. Chem.
Year: 2016
Volume: 59
Issue: 2
First Page: 671
Last Page: 686
DOI: 10.1021/acs.jmedchem.5b01552

Target ChEMBL ID: CHEMBL3117
ChEMBL Target Name: Choline kinase alpha
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
0.382	Kd	=	382	nM
630	Kd	=	630000	nM
0.211	Kd	=	211	nM
0.259	Kd	=	259	nM
7	Kd	=	7000	nM

Concentration uM	Data readout
33	55
33	63
33	65
33	63
33	61
33	62
33	61
33	58
33	71
33	61
33	64
33	83
33	158
33	84
33	104
33	60
33	62
33	59
33	58
33	59

Concentration uM	Data readout
33	55
33	63
33	65
33	63
33	61
33	62
33	61
33	58
33	71
33	61
33	64
33	83
33	158
33	84
33	104
33	60
33	62
33	59
33	58
33	59

672-41-3 靶点实验数据

Concentration uM	Data readout
33	55
33	63
33	65
33	63
33	61
33	62
33	61
33	58
33	71
33	61
33	64
33	83
33	158
33	84
33	104
33	60
33	62
33	59
33	58
33	59