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 84

External ID: CHEMBL4343760

Protocol: N/A

Comment: Journal: J Med Chem
Year: 2020
Volume: 63
Issue: 5
First Page: 2391
Last Page: 2410
DOI: 10.1021/acs.jmedchem.9b01339

Target ChEMBL ID: CHEMBL3714079
ChEMBL Target Name: G-protein coupled receptor 84
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	=	-17	%
Emax	=	77	%
Emax	=	82	%
Emax	=	61	%
Emax	=	2	%
Emax	=	92	%
Emax	=	77	%
Emax	=	101	%
Emax	=	125	%
Emax	=	54	%
Emax	=	5	%
Emax	=	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 84

External ID: CHEMBL4343759

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: 2020
Volume: 63
Issue: 5
First Page: 2391
Last Page: 2410
DOI: 10.1021/acs.jmedchem.9b01339

Target ChEMBL ID: CHEMBL3714079
ChEMBL Target Name: G-protein coupled receptor 84
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
1.93	Ki	=	1930	nM
0.108	Ki	=	108	nM
2.64	Ki	=	2640	nM
1.78	Ki	=	1780	nM
19.6	Ki	=	19600	nM
2.17	Ki	=	2170	nM
7.26E-4	Ki	=	0.726	nM
0.00298	Ki	=	2.98	nM
0.091	Ki	=	91	nM
	Inhibition			%	Not Active
14	IC50	=	14000	nM
0.472	Ki	=	472	nM
10	Ki	>	10000	nM
2.19E-4	Ki	=	0.219	nM
6.26E-4	Ki	=	0.626	nM
3.24E-4	Ki	=	0.324	nM
0.00156	Ki	=	1.56	nM
7.0E-4	Ki	=	0.7	nM
46.3	IC50	=	46300	nM
0.11	Ki	=	110	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 84

External ID: CHEMBL4343757

Protocol: N/A

Comment: Journal: J Med Chem
Year: 2020
Volume: 63
Issue: 5
First Page: 2391
Last Page: 2410
DOI: 10.1021/acs.jmedchem.9b01339

Target ChEMBL ID: CHEMBL3714079
ChEMBL Target Name: G-protein coupled receptor 84
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	=	5	%
Inhibition	=	-3	%
Inhibition	=	50	%

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

来源：IUPHAR-DB 靶标：HCA3 receptor (Hydroxycarboxylic acid receptors) [Homo sapiens]

External ID: 313_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)
8.5	8.5	Agonist	Full agonist	19524438
4.7	5.2	Agonist	Full agonist	12522134,15929991,17358052,16389067
6.4	6.4	Agonist	Full agonist	16480258
5	5	Agonist	Full agonist	19237584
7.5	7.5	Agonist	Full agonist	17931863
5.1	5.1	Agonist	Full agonist	19561068
5.6	5.6	Agonist	Full agonist	19237584
5	5	Agonist	Full agonist	19237584
4	6.5	Agonist	Full agonist	12522134
6.7	6.7	Agonist	Full agonist	17358052

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 84

External ID: CHEMBL4343755

Protocol: N/A

Comment: Journal: J Med Chem
Year: 2020
Volume: 63
Issue: 5
First Page: 2391
Last Page: 2410
DOI: 10.1021/acs.jmedchem.9b01339

Target ChEMBL ID: CHEMBL3714079
ChEMBL Target Name: G-protein coupled receptor 84
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	=	27	%
Emax	=	51	%
Emax	=	93	%
Emax	=	63	%
Emax	=	36	%
Emax	=	94	%
Emax	=	91	%
Emax	=	102	%
Emax	=	112	%
Emax	=	97	%
Emax	=	17	%
Emax	=	88	%

617-73-2 靶点实验数据