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

来源：IUPHAR-DB 靶标：GnRH1 receptor (Gonadotrophin-releasing hormone receptors) [Homo sapiens]

External ID: 256_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	Type	Action	Reference (PubMed ID)
8.8	8.8					Antagonist	Antagonist	21188095
				7	7	Agonist	Full agonist	17452338
9	9.5					Antagonist	Antagonist	17095587
10	10					Antagonist	Antagonist	9300077
		8.5	8.5			Agonist	Full agonist	6346049
7.9	7.9					Antagonist	Antagonist	9300077
9.6	9.6					Antagonist	Antagonist	9300077
				9.2	9.2	Antagonist	Antagonist	12107234,11551758
9.1	9.1					Antagonist	Antagonist	19006286
				9.2	9.2	Antagonist	Antagonist	19638591
		9.7	9.7			Antagonist	Antagonist	16930559
8.7	9.7	9	10.4			Agonist	Full agonist	26398856
						Agonist	Full agonist
						Agonist	Full agonist
8.3	8.3			5.3	5.3	Allosteric modulator, Antagonist	Antagonist, Negative	18344315
						Agonist	Full agonist
7.8	8.4					Agonist	Full agonist	17095587
		8.2	8.2			Agonist	Full agonist	17254668
9.5	9.5			9	9	Antagonist	Antagonist	1850267,11861490
8.2	8.2			7.8	7.8	Allosteric modulator, Antagonist	Antagonist, Negative	12606616,17176055

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

来源：ChEMBL 靶标：Rattus norvegicus

External ID: CHEMBL711012

Protocol: N/A

Comment: Journal: J. Med. Chem.
Year: 2001
Volume: 44
Issue: 3
First Page: 453
Last Page: 467
DOI: 10.1021/jm0003900

Target ChEMBL ID: CHEMBL376
ChEMBL Target Name: Rattus norvegicus
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular

Standard Type	Standard Relation	Standard Units
Inhibition	=	%

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

来源：ChEMBL 靶标：Gonadotropin-releasing hormone receptor

External ID: CHEMBL684350

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: 3
First Page: 453
Last Page: 467
DOI: 10.1021/jm0003900

Target ChEMBL ID: CHEMBL1855
ChEMBL Target Name: Gonadotropin-releasing hormone receptor
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
0.0068	IC50	=	6.8	nM
0.0108	IC50	=	10.8	nM
0.005	IC50	=	5	nM
0.0108	IC50	=	10.8	nM
0.0033	IC50	=	3.3	nM

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

来源：ChEMBL 靶标：Gonadotropin-releasing hormone receptor

External ID: CHEMBL689133

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: 3
First Page: 453
Last Page: 467
DOI: 10.1021/jm0003900

Target ChEMBL ID: CHEMBL1855
ChEMBL Target Name: Gonadotropin-releasing hormone receptor
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
0.002512	Kd	=	2.512	nM
0.001	Kd	=	1	nM
0.001259	Kd	=	1.259	nM
5.012E-4	Kd	=	0.5012	nM

183552-38-7 靶点实验数据