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

来源：ChEMBL 靶标：Oxysterols receptor LXR-beta

External ID: CHEMBL5372115

Protocol: N/A

Comment: Journal: J Nat Prod
Year: 2023
Volume: 86
Issue: 8
First Page: 1901
Last Page: 1909
DOI: 10.1021/acs.jnatprod.3c00059

Target ChEMBL ID: CHEMBL3706564
ChEMBL Target Name: Liver X receptor
ChEMBL Target Type: PROTEIN FAMILY - Target is a group of closely related proteins
Relationship Type: D - Direct protein target assigned
Confidence: Multiple direct protein targets may be assigned

Standard Type	Activity Comment
Activity	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：Oxysterols receptor LXR-alpha

External ID: CHEMBL836029

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2005
Volume: 15
Issue: 11
First Page: 2824
Last Page: 2828
DOI: 10.1016/j.bmcl.2005.03.100

Target ChEMBL ID: CHEMBL2808
ChEMBL Target Name: LXR-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

Standard Type	Standard Relation	Standard Value
Activity	=	20
Activity	=	4

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

来源：ChEMBL 靶标：Retinoic acid receptor RXR-alpha

External ID: CHEMBL1219324

Protocol: N/A

Comment: Journal: J. Nat. Prod.
Year: 2010
Volume: 73
Issue: 8
First Page: 1332
Last Page: 1336
DOI: 10.1021/np100120c

Target ChEMBL ID: CHEMBL3084
ChEMBL Target Name: Retinoid X receptor 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

Standard Type	Activity Comment
Activity	Active
Activity	Active
Activity	Active

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

来源：ChEMBL 靶标：Oxysterols receptor LXR-beta

External ID: CHEMBL4040642

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: 2017
Volume: 60
Issue: 15
First Page: 6548
Last Page: 6562
DOI: 10.1021/acs.jmedchem.7b00091

Target ChEMBL ID: CHEMBL4093
ChEMBL Target Name: LXR-beta
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
	EC50				Not Active
7.2	EC50	=	7200	nM

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

来源：ChEMBL 靶标：Oxysterols receptor LXR-alpha

External ID: CHEMBL4040641

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: 2017
Volume: 60
Issue: 15
First Page: 6548
Last Page: 6562
DOI: 10.1021/acs.jmedchem.7b00091

Target ChEMBL ID: CHEMBL2808
ChEMBL Target Name: LXR-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	Activity Comment
	EC50				Not Active
4.11	EC50	=	4110	nM

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

来源：ChEMBL 靶标：Oxysterols receptor LXR-alpha

External ID: CHEMBL832531

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2005
Volume: 15
Issue: 11
First Page: 2824
Last Page: 2828
DOI: 10.1016/j.bmcl.2005.03.100

Target ChEMBL ID: CHEMBL2808
ChEMBL Target Name: LXR-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

Standard Type	Standard Relation	Standard Units
EC50	=	nM

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

来源：ChEMBL 靶标：Oxysterols receptor LXR-beta

External ID: CHEMBL832871

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2005
Volume: 15
Issue: 11
First Page: 2824
Last Page: 2828
DOI: 10.1016/j.bmcl.2005.03.100

Target ChEMBL ID: CHEMBL4093
ChEMBL Target Name: LXR-beta
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 Units
EC50	=	nM

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

来源：ChEMBL 靶标：Oxysterols receptor LXR-beta

External ID: CHEMBL5372100

Protocol: N/A

Comment: Journal: J Nat Prod
Year: 2023
Volume: 86
Issue: 8
First Page: 1901
Last Page: 1909
DOI: 10.1021/acs.jnatprod.3c00059

Target ChEMBL ID: CHEMBL4093
ChEMBL Target Name: LXR-beta
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	=	5.3	%

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

来源：ChEMBL 靶标：Oxysterols receptor LXR-alpha

External ID: CHEMBL5372099

Protocol: N/A

Comment: Journal: J Nat Prod
Year: 2023
Volume: 86
Issue: 8
First Page: 1901
Last Page: 1909
DOI: 10.1021/acs.jnatprod.3c00059

Target ChEMBL ID: CHEMBL2808
ChEMBL Target Name: LXR-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

Standard Type	Standard Relation	Standard Value	Standard Units
Emax	=	6.5	%

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

来源：ChEMBL 靶标：Oxysterols receptor LXR-beta

External ID: CHEMBL835560

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2005
Volume: 15
Issue: 11
First Page: 2824
Last Page: 2828
DOI: 10.1016/j.bmcl.2005.03.100

Target ChEMBL ID: CHEMBL4093
ChEMBL Target Name: LXR-beta
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	=	60	%

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

来源：ChEMBL 靶标：Oxysterols receptor LXR-alpha

External ID: CHEMBL835564

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2005
Volume: 15
Issue: 11
First Page: 2824
Last Page: 2828
DOI: 10.1016/j.bmcl.2005.03.100

Target ChEMBL ID: CHEMBL2808
ChEMBL Target Name: LXR-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

Standard Type	Standard Relation	Standard Value	Standard Units
Inhibition	=	70	%

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: CHEMBL5372092

Protocol: N/A

Comment: Journal: J Nat Prod
Year: 2023
Volume: 86
Issue: 8
First Page: 1901
Last Page: 1909
DOI: 10.1021/acs.jnatprod.3c00059

Standard Type	Activity Comment
Activity	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：Oxysterols receptor LXR-beta

External ID: CHEMBL1007710

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. Nat. Prod.
Year: 2005
Volume: 68
Issue: 8
First Page: 1247
Last Page: 1252
DOI: 10.1021/np050182g

Target ChEMBL ID: CHEMBL4093
ChEMBL Target Name: LXR-beta
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
15	EC50	>	15000	nM
50	EC50	>	50000	nM
50	EC50	>	50000	nM
50	EC50	>	50000	nM
50	EC50	>	50000	nM
	EC50				Not Determined
	EC50				Not Determined
0.003	EC50	<	3	nM
50	EC50	>	50000	nM

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

来源：ChEMBL 靶标：Oxysterols receptor LXR-beta

External ID: CHEMBL1007708

Protocol: N/A

Comment: Journal: J. Nat. Prod.
Year: 2005
Volume: 68
Issue: 8
First Page: 1247
Last Page: 1252
DOI: 10.1021/np050182g

Target ChEMBL ID: CHEMBL4093
ChEMBL Target Name: LXR-beta
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
Activity	=	60	%

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

来源：ChEMBL 靶标：Oxysterols receptor LXR-alpha

External ID: CHEMBL1007709

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. Nat. Prod.
Year: 2005
Volume: 68
Issue: 8
First Page: 1247
Last Page: 1252
DOI: 10.1021/np050182g

Target ChEMBL ID: CHEMBL2808
ChEMBL Target Name: LXR-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	Activity Comment
15	EC50	>	15000	nM
0.21	EC50	=	210	nM
0.18	EC50	=	180	nM
0.39	EC50	=	390	nM
0.03	EC50	=	30	nM
	EC50				Not Determined
0.17	EC50	=	170	nM
0.45	EC50	=	450	nM
0.05	EC50	=	50	nM

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

来源：ChEMBL 靶标：Oxysterols receptor LXR-alpha

External ID: CHEMBL1007706

Protocol: N/A

Comment: Journal: J. Nat. Prod.
Year: 2005
Volume: 68
Issue: 8
First Page: 1247
Last Page: 1252
DOI: 10.1021/np050182g

Target ChEMBL ID: CHEMBL2808
ChEMBL Target Name: LXR-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

Standard Type	Standard Relation	Standard Value	Standard Units
Activity	=	70	%

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

来源：ChEMBL 靶标：Oxysterols receptor LXR-alpha

External ID: CHEMBL4049700

Protocol: N/A

Comment: Journal: Bioorg Med Chem Lett
Year: 2017
Volume: 27
Issue: 5
First Page: 1193
Last Page: 1198
DOI: 10.1016/j.bmcl.2017.01.066

Target ChEMBL ID: CHEMBL2808
ChEMBL Target Name: LXR-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

Standard Type	Activity Comment
Activity	Active

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

来源：ChEMBL 靶标：Nuclear receptor ROR-gamma

External ID: CHEMBL3375302

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: 2014
Volume: 24
Issue: 24
First Page: 5769
Last Page: 5776
DOI: 10.1016/j.bmcl.2014.10.037

Target ChEMBL ID: CHEMBL1741186
ChEMBL Target Name: Nuclear receptor ROR-gamma
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
0.02	EC50	=	20	nM
0.13	IC50	=	130	nM
0.032	IC50	=	32	nM

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

来源：ChEMBL 靶标：Oxysterols receptor LXR-beta

External ID: CHEMBL1008519

Protocol: N/A

Comment: Journal: J. Nat. Prod.
Year: 2005
Volume: 68
Issue: 8
First Page: 1247
Last Page: 1252
DOI: 10.1021/np050182g

Target ChEMBL ID: CHEMBL4093
ChEMBL Target Name: LXR-beta
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	Activity Comment
FC			Not Determined
FC	=	35
FC	=	8
FC			Not Determined
FC			Not Determined
FC			Not Determined
FC			Not Determined
FC	=	85

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

来源：IUPHAR-DB 靶标：Liver X receptor-beta (1H. Liver X receptor-like receptors) [Homo sapiens]

External ID: 601_Human

Protocol: The International Union of Basic and Clinical Pharmacology/British Pharmacological Society (IUPHAR/BPS) Guide to PHARMACOLOGY Database (GtoPdb) uses expert subcommittees to collate peer-reviewed information from the published literature regarding individual protein targets, and describes the pharmacology, genetics, function and anatomy of each target. Its pages provide a richly curated overview of the pharmacology of receptors, ion channels, enzymes and other target types, which can be found by following the external link to the GtoPdb website.

Comment: The data collected focuses on ligands at human receptors. Data are provided at rat or mouse orthologues where there are significant species differences, or where data are not yet available at the human target.

Information on individual experimental protocols can be found in the primary references listed for each ligand.

Affinity data are expressed as pKi [-log(Ki)], pKd [-log(Kd)], pIC50 [-log(IC50)], pEC50 [-log(EC50)], pKB [-log(KB)], pA2 or as a micromolar concentration range. In most cases the original concentration can be found in the primary reference.

pKi_min	pKi_max	pKd_min	pKd_max	pIC50_min	pIC50_max	pEC50_min	pEC50_max	Type	Action	Reference (PubMed ID)
				7.5	7.5			Allosteric modulator	Negative	18800767
5.8	5.8							Agonist	Agonist	16857673
						9	9	Agonist	Agonist	11790770
		8.2	8.2					Agonist	Agonist	12072387
						5.5	7	Agonist	Agonist	23292650,9013544
						5.5	5.5	Agonist	Agonist	9013544
						5.5	5.5	Agonist	Agonist	8878485
						7.5	7.5	Agonist	Agonist	11985463
						6	6	Agonist	Agonist
						7.3	7.3	Agonist	Agonist	11090131
8	8							Agonist	Agonist
				7.5	7.5			Antagonist	Antagonist	20345102

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

来源：ChEMBL 靶标：Oxysterols receptor LXR-alpha

External ID: CHEMBL1008515

Protocol: N/A

Comment: Journal: J. Nat. Prod.
Year: 2005
Volume: 68
Issue: 8
First Page: 1247
Last Page: 1252
DOI: 10.1021/np050182g

Target ChEMBL ID: CHEMBL2808
ChEMBL Target Name: LXR-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

Standard Type	Standard Relation	Standard Value	Activity Comment
FC			Not Determined
FC	=	20
FC	=	4
FC			Not Determined
FC			Not Determined
FC			Not Determined
FC	=	50

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: CHEMBL4040650

Protocol: N/A

Comment: Journal: J Med Chem
Year: 2017
Volume: 60
Issue: 15
First Page: 6548
Last Page: 6562
DOI: 10.1021/acs.jmedchem.7b00091

Standard Type	Activity Comment
Activity	Not Active
Activity	Not Active
Activity	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：N/A

External ID: CHEMBL4040651

Protocol: N/A

Comment: Journal: J Med Chem
Year: 2017
Volume: 60
Issue: 15
First Page: 6548
Last Page: 6562
DOI: 10.1021/acs.jmedchem.7b00091

Standard Type	Activity Comment
Activity	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：N/A

External ID: CHEMBL4040649

Protocol: N/A

Comment: Journal: J Med Chem
Year: 2017
Volume: 60
Issue: 15
First Page: 6548
Last Page: 6562
DOI: 10.1021/acs.jmedchem.7b00091

Standard Type	Activity Comment
Activity	Not Active
Activity	Not Active
Activity	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：N/A

External ID: CHEMBL2423071

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2013
Volume: 21
Issue: 17
First Page: 5297
Last Page: 5309
DOI: 10.1016/j.bmc.2013.06.022

Standard Type	Activity Comment
Activity	Not Active
Activity	Not Active
Activity	Not Active
Activity	Not Active
Activity	Not Active
Activity	Not Active
Activity	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：Oxysterol-binding protein 1

External ID: CHEMBL5320826

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: 2023
Volume: 66
Issue: 6
First Page: 3866
Last Page: 3875
DOI: 10.1021/acs.jmedchem.2c01025

Target ChEMBL ID: CHEMBL4523203
ChEMBL Target Name: Oxysterol-binding protein 1
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
0.12	Ki	=	120	nM
0.068	Ki	=	68	nM
0.13	Ki	=	130	nM
100	Ki	>	100000	nM
50	Ki	>	50000	nM
30	Ki	>	30000	nM
10	Ki	>	10000	nM
100	Ki	>	100000	nM
0.078	Ki	=	78	nM
10	Ki	>	10000	nM
0.12	Ki	=	120	nM
20	Ki	>	20000	nM
50	Ki	>	50000	nM
100	Ki	>	100000	nM

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

来源：ChEMBL 靶标：Oxysterol-binding protein 2

External ID: CHEMBL5320827

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: 2023
Volume: 66
Issue: 6
First Page: 3866
Last Page: 3875
DOI: 10.1021/acs.jmedchem.2c01025

Target ChEMBL ID: CHEMBL5465343
ChEMBL Target Name: Oxysterol-binding protein 2
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
0.32	Ki	=	320	nM
50	Ki	>	50000	nM
30	Ki	>	30000	nM
15	Ki	>	15000	nM
3	Ki	>	3000	nM
0.092	Ki	=	92	nM
20	Ki	>	20000	nM
0.87	Ki	>	870	nM
30	Ki	>	30000	nM
50	Ki	>	50000	nM
100	Ki	>	100000	nM

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: CHEMBL4040658

Protocol: N/A

Comment: Journal: J Med Chem
Year: 2017
Volume: 60
Issue: 15
First Page: 6548
Last Page: 6562
DOI: 10.1021/acs.jmedchem.7b00091

Standard Type	Activity Comment
Activity	Active

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: CHEMBL4040659

Protocol: N/A

Comment: Journal: J Med Chem
Year: 2017
Volume: 60
Issue: 15
First Page: 6548
Last Page: 6562
DOI: 10.1021/acs.jmedchem.7b00091

Standard Type	Activity Comment
Activity	Not Active
Activity	Not Active
Activity	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：N/A

External ID: CHEMBL4040656

Protocol: N/A

Comment: Journal: J Med Chem
Year: 2017
Volume: 60
Issue: 15
First Page: 6548
Last Page: 6562
DOI: 10.1021/acs.jmedchem.7b00091

Standard Type	Activity Comment
Activity	Active
Activity	Active
Activity	Active

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: CHEMBL4040654

Protocol: N/A

Comment: Journal: J Med Chem
Year: 2017
Volume: 60
Issue: 15
First Page: 6548
Last Page: 6562
DOI: 10.1021/acs.jmedchem.7b00091

Standard Type	Activity Comment
Activity	Active
Activity	Not Active
Activity	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：N/A

External ID: CHEMBL4040655

Protocol: N/A

Comment: Journal: J Med Chem
Year: 2017
Volume: 60
Issue: 15
First Page: 6548
Last Page: 6562
DOI: 10.1021/acs.jmedchem.7b00091

Standard Type	Activity Comment
Activity	Not Active
Activity	Not Active
Activity	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：Oxysterols receptor LXR-beta

External ID: CHEMBL5372116

Protocol: N/A

Comment: Journal: J Nat Prod
Year: 2023
Volume: 86
Issue: 8
First Page: 1901
Last Page: 1909
DOI: 10.1021/acs.jnatprod.3c00059

Target ChEMBL ID: CHEMBL3706564
ChEMBL Target Name: Liver X receptor
ChEMBL Target Type: PROTEIN FAMILY - Target is a group of closely related proteins
Relationship Type: D - Direct protein target assigned
Confidence: Multiple direct protein targets may be assigned

Standard Type	Activity Comment
Activity	Active

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: CHEMBL4040652

Protocol: N/A

Comment: Journal: J Med Chem
Year: 2017
Volume: 60
Issue: 15
First Page: 6548
Last Page: 6562
DOI: 10.1021/acs.jmedchem.7b00091

Standard Type	Activity Comment
Activity	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：N/A

External ID: CHEMBL4040653

Protocol: N/A

Comment: Journal: J Med Chem
Year: 2017
Volume: 60
Issue: 15
First Page: 6548
Last Page: 6562
DOI: 10.1021/acs.jmedchem.7b00091

Standard Type	Standard Relation	Standard Value	Activity Comment
Activity			Not Active
Activity			Not Active
Activity			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：Oxysterols receptor LXR-alpha

External ID: CHEMBL710255

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: 2001
Volume: 44
Issue: 6
First Page: 886
Last Page: 897
DOI: 10.1021/jm0004749

Target ChEMBL ID: CHEMBL2808
ChEMBL Target Name: LXR-alpha
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: H - Homologous protein target assigned
Confidence: Homologous single protein target assigned

PubChem Standard Value	Standard Type	Standard Relation	Standard Value	Standard Units
5.9	EC50	=	5900	nM
0.325	EC50	=	325	nM
0.18	EC50	=	180	nM
0.17	EC50	=	170	nM
0.67	EC50	=	670	nM
0.22	EC50	=	220	nM
0.46	EC50	=	460	nM
0.25	EC50	=	250	nM
0.47	EC50	=	470	nM

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

来源：ChEMBL 靶标：NPC1-like intracellular cholesterol transporter 1

External ID: CHEMBL3362444

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2014
Volume: 24
Issue: 15
First Page: 3480
Last Page: 3485
DOI: 10.1016/j.bmcl.2014.05.064

Target ChEMBL ID: CHEMBL2027
ChEMBL Target Name: Niemann-Pick C1-like protein 1
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	Activity Comment
Activity	Not Active
Activity	Not Active
Activity	Not Active
Activity	Not Active
Activity	Not Active
Activity	Not Active
Activity	Not Active
Activity	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：Oxysterols receptor LXR-beta

External ID: CHEMBL830099

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: 2005
Volume: 15
Issue: 11
First Page: 2824
Last Page: 2828
DOI: 10.1016/j.bmcl.2005.03.100

Target ChEMBL ID: CHEMBL4093
ChEMBL Target Name: LXR-beta
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
15	EC50	=	15000	nM
0.003	EC50	<	3	nM
0.002	EC50	=	2	nM
0.001	EC50	=	1	nM

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

来源：ChEMBL 靶标：Oxysterols receptor LXR-alpha

External ID: CHEMBL712591

Protocol: N/A

Comment: Journal: J. Med. Chem.
Year: 2001
Volume: 44
Issue: 6
First Page: 886
Last Page: 897
DOI: 10.1021/jm0004749

Target ChEMBL ID: CHEMBL2808
ChEMBL Target Name: LXR-alpha
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: H - Homologous protein target assigned
Confidence: Homologous single protein target assigned

Standard Type	Standard Relation	Standard Value
RE	<	0.1
RE	=	0.2
RE	=	1.1
RE	=	0.7
RE	=	0.85
RE	=	1
RE	=	1.4
RE	=	1
RE	=	0.35
RE	=	0.85
RE	=	1
RE	=	0.3
RE	=	1
RE	<	0.1

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

来源：IUPHAR-DB 靶标：Liver X receptor-alpha (1H. Liver X receptor-like receptors) [Homo sapiens]

External ID: 602_Human

Protocol: The International Union of Basic and Clinical Pharmacology/British Pharmacological Society (IUPHAR/BPS) Guide to PHARMACOLOGY Database (GtoPdb) uses expert subcommittees to collate peer-reviewed information from the published literature regarding individual protein targets, and describes the pharmacology, genetics, function and anatomy of each target. Its pages provide a richly curated overview of the pharmacology of receptors, ion channels, enzymes and other target types, which can be found by following the external link to the GtoPdb website.

Comment: The data collected focuses on ligands at human receptors. Data are provided at rat or mouse orthologues where there are significant species differences, or where data are not yet available at the human target.

Information on individual experimental protocols can be found in the primary references listed for each ligand.

Affinity data are expressed as pKi [-log(Ki)], pKd [-log(Kd)], pIC50 [-log(IC50)], pEC50 [-log(EC50)], pKB [-log(KB)], pA2 or as a micromolar concentration range. In most cases the original concentration can be found in the primary reference.

pKi_min	pKi_max	pKd_min	pKd_max	pIC50_min	pIC50_max	pEC50_min	pEC50_max	Type	Action	Reference (PubMed ID)
5.5	5.5							Agonist	Agonist	16857673
						9	9	Agonist	Agonist	11790770
8.1	8.1							Agonist	Agonist
				7	7			Antagonist	Antagonist	20345102
		7.9	7.9					Agonist	Agonist	12072387
						5.4	6.5	Agonist	Agonist	9013544,9874807,23292650
						5.4	5.4	Agonist	Agonist	12893846
						5.3	5.3	Agonist	Agonist	8878485
						6.7	6.7	Agonist	Agonist	11985463
						7.3	7.3	Agonist	Agonist	11090131

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

来源：ChEMBL 靶标：Oxysterols receptor LXR-alpha

External ID: CHEMBL830107

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: 2005
Volume: 15
Issue: 11
First Page: 2824
Last Page: 2828
DOI: 10.1016/j.bmcl.2005.03.100

Target ChEMBL ID: CHEMBL2808
ChEMBL Target Name: LXR-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
15	EC50	=	15000	nM
0.001	EC50	=	1	nM
0.32	EC50	=	320	nM
0.002	EC50	=	2	nM

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

来源：IUPHAR-DB 靶标：Farnesoid X receptor (1H. Liver X receptor-like receptors) [Homo sapiens]

External ID: 603_Human

Protocol: The International Union of Basic and Clinical Pharmacology/British Pharmacological Society (IUPHAR/BPS) Guide to PHARMACOLOGY Database (GtoPdb) uses expert subcommittees to collate peer-reviewed information from the published literature regarding individual protein targets, and describes the pharmacology, genetics, function and anatomy of each target. Its pages provide a richly curated overview of the pharmacology of receptors, ion channels, enzymes and other target types, which can be found by following the external link to the GtoPdb website.

Comment: The data collected focuses on ligands at human receptors. Data are provided at rat or mouse orthologues where there are significant species differences, or where data are not yet available at the human target.

Information on individual experimental protocols can be found in the primary references listed for each ligand.

Affinity data are expressed as pKi [-log(Ki)], pKd [-log(Kd)], pIC50 [-log(IC50)], pEC50 [-log(EC50)], pKB [-log(KB)], pA2 or as a micromolar concentration range. In most cases the original concentration can be found in the primary reference.

pEC50_min	pEC50_max	Type	Action	Reference (PubMed ID)
5.5	5.5	Agonist	Agonist	16371446
9.7	9.7	Agonist	Agonist	29148806
6.6	6.6	Agonist	Agonist	12718892
5.3	5.3	Agonist	Agonist	10334993,10360171
7	7	Agonist	Agonist	12166927
7.8	7.8	Agonist	Agonist	10956205

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

来源：BindingDB 靶标：N/A

External ID: BindingDB_2414_1

Protocol: N/A

Comment: Compounds with any of Ki, IC50, Kd, or EC50 activity value <= 10uM are labeled as "Active".
If multiple measurements are available for a given compound, it is labeled as "Active" if any of the measurements meet the criterion. Activity values are checked in the order of Ki, IC50, Kd, and EC50. The first entry that meets the above activity threshold is used to determine "Standard Type", "Standard Relation", and "PubChem Standard Value". Otherwise, the first non-empty entry will be used to set those values.

Standard Type	PubChem Standard Value	EC50	Target Accession(s)	Ligand	Target
EC50	0.47	470	Q13133	BDBM20175	Oxysterols receptor LXR-alpha
EC50	0.325	325	Q13133	BDBM20177	Oxysterols receptor LXR-alpha
EC50	5.9	5900	Q13133	BDBM20178	Oxysterols receptor LXR-alpha
EC50	0.13	130	Q13133	BDBM20180	Oxysterols receptor LXR-alpha
EC50	0.22	220	Q13133	BDBM20181	Oxysterols receptor LXR-alpha
EC50	1.16	1160	Q13133	BDBM20182	Oxysterols receptor LXR-alpha
EC50	0.25	250	Q13133	BDBM20183	Oxysterols receptor LXR-alpha
EC50	0.18	180	Q13133	BDBM20185	Oxysterols receptor LXR-alpha
EC50	0.17	170	Q13133	BDBM20186	Oxysterols receptor LXR-alpha
EC50	3	3000	Q13133	BDBM20190	Oxysterols receptor LXR-alpha

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: CHEMBL2161109

Protocol: N/A

Comment: Journal: ACS Med. Chem. Lett.
Year: 2012
Volume: 3
Issue: 10
First Page: 828
Last Page: 833
DOI: 10.1021/ml300192k

Standard Type	Standard Relation	Standard Value
FC	=	3.6
FC	=	24.1
FC	=	9.8
FC	=	13.4
FC	=	0.6
FC	=	2.3
FC	=	4.9

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: CHEMBL2161108

Protocol: N/A

Comment: Journal: ACS Med. Chem. Lett.
Year: 2012
Volume: 3
Issue: 10
First Page: 828
Last Page: 833
DOI: 10.1021/ml300192k

Standard Type	Standard Relation	Standard Value
FC	=	32.4
FC	=	4.7
FC	=	69.9
FC	=	91.8
FC	=	1.6
FC	=	52.5
FC	=	87.1

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: CHEMBL923906

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.
Year: 2008
Volume: 16
Issue: 8
First Page: 4272
Last Page: 4285
DOI: 10.1016/j.bmc.2008.02.078

PubChem Standard Value	Standard Type	Standard Relation	Standard Value	Standard Units	Data Validity Comment
250	IC50	=	250000	nM	Outside typical range
8	IC50	=	8000	nM
100	IC50	=	100000	nM
24.7	IC50	=	24700	nM
9.9	IC50	=	9900	nM
15	IC50	=	15000	nM

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: CHEMBL933516

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem.
Year: 2008
Volume: 16
Issue: 8
First Page: 4272
Last Page: 4285
DOI: 10.1016/j.bmc.2008.02.078

Standard Type	Activity Comment
Activity	Not Active
Activity	Not Active
Activity	Not Active
Activity	Not Active
Activity	Not Active
Activity	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：Oxysterols receptor LXR-beta

External ID: CHEMBL875568

Protocol: N/A

Comment: Journal: Bioorg. Med. Chem. Lett.
Year: 2005
Volume: 15
Issue: 11
First Page: 2824
Last Page: 2828
DOI: 10.1016/j.bmcl.2005.03.100

Target ChEMBL ID: CHEMBL4093
ChEMBL Target Name: LXR-beta
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
Activity	=	35
Activity	=	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: CHEMBL1219319

Protocol: N/A

Comment: Journal: J. Nat. Prod.
Year: 2010
Volume: 73
Issue: 8
First Page: 1332
Last Page: 1336
DOI: 10.1021/np100120c

Standard Type	Activity Comment
Activity	Dose-dependent effect
Activity	Dose-dependent effect
Activity	Dose-dependent effect

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

来源：ChEMBL 靶标：Nuclear receptor ROR-gamma

External ID: CHEMBL3227243

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: MedChemComm
Year: 2013
Volume: 4
Issue: 5
First Page: 764
Last Page: 776
DOI: 10.1039/C3MD00005B

Target ChEMBL ID: CHEMBL1741186
ChEMBL Target Name: Nuclear receptor ROR-gamma
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
0.02	EC50	=	20	nM
0.02	EC50	=	20	nM

17954-98-2 靶点实验数据