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

来源：ChEMBL 靶标：Tyrosine-protein kinase JAK3

External ID: CHEMBL5231773

Protocol: N/A

Comment: Journal: Eur J Med Chem
Year: 2020
Volume: 207
First Page: 112836
Last Page: 112836
DOI: 10.1016/j.ejmech.2020.112836

Target ChEMBL ID: CHEMBL2148
ChEMBL Target Name: Tyrosine-protein kinase JAK3
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	=	101	%
Inhibition	=	100	%
Inhibition	=	23	%
Inhibition	=	7	%
Inhibition	=	-4	%
Inhibition	=	21	%
Inhibition	=	70	%
Inhibition	=	99	%
Inhibition	=	94	%
Inhibition	=	97	%
Inhibition	=	40	%
Inhibition	=	15	%
Inhibition	=	98	%
Inhibition	=	-1	%
Inhibition	=	89	%
Inhibition	=	26	%
Inhibition	=	36	%

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

来源：ChEMBL 靶标：Dual specificity mitogen-activated protein kinase kinase 4

External ID: CHEMBL5231772

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: Eur J Med Chem
Year: 2020
Volume: 207
First Page: 112836
Last Page: 112836
DOI: 10.1016/j.ejmech.2020.112836

Target ChEMBL ID: CHEMBL2897
ChEMBL Target Name: Dual specificity mitogen-activated protein kinase kinase 4
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
	Inhibition	=	11	%
	Inhibition	=	24	%
	Inhibition	=	11	%
	Inhibition	=	37	%
	Inhibition	=	50	%
	Inhibition	=	40	%
	Inhibition	=	55	%
	Inhibition	=	26	%
	Inhibition	=	47	%
	Inhibition	=	10	%
	Inhibition	=	94	%
	Inhibition	=	76	%
	Inhibition	=	5	%
	Inhibition	=	44	%
	Inhibition	=	21	%
0.281	IC50	=	281	nM

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

来源：ChEMBL 靶标：Maternal embryonic leucine zipper kinase

External ID: CHEMBL5231774

Protocol: N/A

Comment: Journal: Eur J Med Chem
Year: 2020
Volume: 207
First Page: 112836
Last Page: 112836
DOI: 10.1016/j.ejmech.2020.112836

Target ChEMBL ID: CHEMBL4578
ChEMBL Target Name: Maternal embryonic leucine zipper kinase
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	=	102	%
Inhibition	=	100	%
Inhibition	=	73	%
Inhibition	=	24	%
Inhibition	=	44	%
Inhibition	=	15	%
Inhibition	=	39	%
Inhibition	=	23	%
Inhibition	=	94	%
Inhibition	=	36	%
Inhibition	=	11	%
Inhibition	=	37	%
Inhibition	=	100	%
Inhibition	=	11	%
Inhibition	=	11	%
Inhibition	=	7	%
Inhibition	=	63	%

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

来源：ChEMBL 靶标：Tyrosine-protein kinase BTK

External ID: CHEMBL5231769

Protocol: N/A

Comment: Journal: Eur J Med Chem
Year: 2020
Volume: 207
First Page: 112836
Last Page: 112836
DOI: 10.1016/j.ejmech.2020.112836

Target ChEMBL ID: CHEMBL5251
ChEMBL Target Name: Tyrosine-protein kinase BTK
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	=	101	%
Inhibition	=	78	%
Inhibition	=	54	%
Inhibition	=	24	%
Inhibition	=	38	%
Inhibition	=	18	%
Inhibition	=	32	%
Inhibition	=	81	%
Inhibition	=	29	%
Inhibition	=	81	%
Inhibition	=	60	%
Inhibition	=	39	%
Inhibition	=	99	%
Inhibition	=	5	%
Inhibition	=	94	%
Inhibition	=	16	%
Inhibition	=	16	%

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: CHEMBL5231768

Protocol: N/A

Comment: Journal: Eur J Med Chem
Year: 2020
Volume: 207
First Page: 112836
Last Page: 112836
DOI: 10.1016/j.ejmech.2020.112836

Standard Type	Standard Relation	Standard Value	Standard Units
T1/2	=	0.5	hr
T1/2	=	49.5	hr
T1/2	=	2.4	hr
T1/2	=	2.2	hr
T1/2	=	1.1	hr
T1/2	=	2.2	hr
T1/2	=	0.5	hr
T1/2	>	72	hr
T1/2	=	2.2	hr
T1/2	>	72	hr
T1/2	=	1.5	hr
T1/2	=	2.5	hr
T1/2	=	2.6	hr
T1/2	>	72	hr
T1/2	>	72	hr
T1/2	=	3.9	hr
T1/2	=	2.4	hr

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

来源：ChEMBL 靶标：Ribosomal protein S6 kinase alpha-3

External ID: CHEMBL5231771

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: Eur J Med Chem
Year: 2020
Volume: 207
First Page: 112836
Last Page: 112836
DOI: 10.1016/j.ejmech.2020.112836

Target ChEMBL ID: CHEMBL2345
ChEMBL Target Name: Ribosomal protein S6 kinase alpha 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
	Inhibition	=	36	%
	Inhibition	=	61	%
	Inhibition	=	3	%
	Inhibition	=	25	%
	Inhibition	=	12	%
	Inhibition	=	61	%
	Inhibition	=	14	%
	Inhibition	=	56	%
	Inhibition	=	34	%
	Inhibition	=	51	%
0.399	IC50	=	399	nM
	Inhibition	=	75	%
	Inhibition	=	18	%
	Inhibition	=	55	%
	Inhibition	=	46	%
0.399	IC50	=	399	nM

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

来源：ChEMBL 靶标：Mitogen-activated protein kinase 1

External ID: CHEMBL5231770

Protocol: N/A

Comment: Journal: Eur J Med Chem
Year: 2020
Volume: 207
First Page: 112836
Last Page: 112836
DOI: 10.1016/j.ejmech.2020.112836

Target ChEMBL ID: CHEMBL4040
ChEMBL Target Name: MAP kinase ERK2
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	=	102	%
Inhibition	=	68	%
Inhibition	=	6	%
Inhibition	=	4	%
Inhibition	=	8	%
Inhibition	=	4	%
Inhibition	=	56	%
Inhibition	=	7	%
Inhibition	=	11	%
Inhibition	=	7	%
Inhibition	=	9	%
Inhibition	=	9	%
Inhibition	=	84	%
Inhibition	=	4	%
Inhibition	=	7	%
Inhibition	=	4	%
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: CHEMBL5231765

Protocol: N/A

Comment: Journal: Eur J Med Chem
Year: 2020
Volume: 207
First Page: 112836
Last Page: 112836
DOI: 10.1016/j.ejmech.2020.112836

Standard Type	Standard Relation	Standard Value	Standard Units
K	>	13.86	/hr
K	=	0.022	/hr
K	=	0.063	/hr
K	=	0.007	/hr
K	=	0.004	/hr
K	=	0.001	/hr
K	>	13.86	/hr
K	=	0.165	/hr
K	>	13.86	/hr
K	=	0.12	/hr
K	=	0.116	/hr
K	=	0.002	/hr
K	>	13.86	/hr
K	=	0.001	/hr
K	=	0.007	/hr
K	=	0.175	/hr
K	=	0.005	/hr

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: CHEMBL5231767

Protocol: N/A

Comment: Journal: Eur J Med Chem
Year: 2020
Volume: 207
First Page: 112836
Last Page: 112836
DOI: 10.1016/j.ejmech.2020.112836

Standard Type	Standard Relation	Standard Value	Standard Units
K	=	1.525	/hr
K	=	0.014	/hr
K	=	0.286	/hr
K	=	0.312	/hr
K	=	0.616	/hr
K	=	0.322	/hr
K	=	1.525	/hr
K	=	0.005	/hr
K	=	0.315	/hr
K	=	0.004	/hr
K	=	0.455	/hr
K	=	0.277	/hr
K	=	0.265	/hr
K	=	0.001	/hr
K	=	0.007	/hr
K	=	0.18	/hr
K	=	0.289	/hr

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: CHEMBL5231766

Protocol: N/A

Comment: Journal: Eur J Med Chem
Year: 2020
Volume: 207
First Page: 112836
Last Page: 112836
DOI: 10.1016/j.ejmech.2020.112836

Standard Type	Standard Relation	Standard Value	Standard Units
T1/2	<	0.05	hr
T1/2	=	31.7	hr
T1/2	=	11	hr
T1/2	>	72	hr
T1/2	>	72	hr
T1/2	>	72	hr
T1/2	<	0.05	hr
T1/2	=	4.2	hr
T1/2	<	0.05	hr
T1/2	=	5.8	hr
T1/2	=	6	hr
T1/2	>	72	hr
T1/2	<	0.05	hr
T1/2	>	72	hr
T1/2	>	72	hr
T1/2	=	4	hr
T1/2	<	72	hr

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

来源：ChEMBL 靶标：Tyrosine-protein kinase JAK3

External ID: CHEMBL5231776

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: Eur J Med Chem
Year: 2020
Volume: 207
First Page: 112836
Last Page: 112836
DOI: 10.1016/j.ejmech.2020.112836

Target ChEMBL ID: CHEMBL2148
ChEMBL Target Name: Tyrosine-protein kinase JAK3
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
	Inhibition			%	Active
	Inhibition			%	Active
	Inhibition			%	Active
	Inhibition			%	Active
	Inhibition			%	Active
	Inhibition			%	Active
	Inhibition			%	Active
	Inhibition			%	Active
	Inhibition			%	Active
	Inhibition			%	Active
	Inhibition			%	Active
	Inhibition			%	Active
0.00102	IC50	=	1.02	nM
7.7E-4	IC50	=	0.77	nM
	Inhibition			%	Active
	Inhibition			%	Active
	Inhibition			%	Active
0.0559	IC50	=	55.9	nM

401-95-6 靶点实验数据