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

来源：IUPHAR-DB 靶标：mGlu5 receptor (Metabotropic glutamate receptors) [Rattus norvegicus]

External ID: 293_Rat

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)
		8.5	8.5					Allosteric modulator	Negative	12565928
6.4	6.4							Allosteric modulator	Neutral	16155210
6.7	6.7					7.8	7.8	Allosteric modulator	Positive	20923853
				10.4	10.4			Allosteric modulator	Negative	17571866
				7.7	7.7			Allosteric modulator	Negative	12438526
		8.8	8.8					Allosteric modulator	Negative	21849627
5.6	5.6							Antagonist	Antagonist	16078827
7	7			7.2	7.2			Allosteric modulator	Negative	17189691
				5.7	5.7			Agonist	Full agonist	11080213
5.4	5.4			6.5	6.5	7.3	7.3	Allosteric modulator	Positive	22884720
8	8							Allosteric modulator	Negative	16439120
5.9	5.9					7	7	Allosteric modulator	Positive	22884720
						6.9	6.9	Allosteric modulator	Positive	22021324
						7.4	7.4	Allosteric modulator	Positive	22021324
5.7	5.7					6.5	6.5	Allosteric modulator	Positive	23291536
7.8	7.8			7.6	7.6			Allosteric modulator	Negative	20923853
		7.3	7.3					Allosteric modulator	Negative	16040814
				8.1	8.1			Allosteric modulator	Negative	25173999
				5.8	5.8			Agonist	Full agonist	11080213
				7.5	7.5			Agonist	Full agonist	11080213

Standard Type	Standard Relation	Standard Value
LogD	=	2.1
LogD	=	3.5
LogD	=	2
LogD	=	2.25

524924-80-9 靶点实验数据