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GPCR

Name	D(2) dopamine receptor
Species	Homo sapiens (Human)
Gene	DRD2
Synonym	dopamine receptor 2 Dopamine D2 receptor D2R D2A and D_2B D2(415) and D₂₍₄₄₄₎ D2 receptor [ Show all ]
Disease	Substance dependence Major depressive disorder Maintain blood pressure in hypotensive states Insomnia Inflammatory disease Inflammatory bowel disease Idiopathic thrombocytopenic purpura Hypertension; Angina pectoris Hypertension Hyperprolactinemia Huntington's disease Glaucoma Gastrointestinal problems Malignant phaeochromocytoma; Benign prostatic hypertrophy; Malignant essential hypertension Migraine headaches Nasal congestion Sexual dysfunction Schizophrenia; Schizoaffective disorders Schizophrenia; Bipolar disorder Schizophrenia Psychotic disorders Psychosis Postpartum haemorrhage Peripheral vasoconstriction; Pulmonary hypertension Parkinson's disease Pain; Inflammatory diseases Ophthalmic disease Non-small cell lung cancer Nausea; Vomiting Fibrosis False perceptions; Bipolar disorder Emesis Chronic obstructive pulmonary disease Cerebrovascular ischaemia Cardiotonic Cardiac failure Bacterial infections Breast cancer Bipolar disorder; Schizophrenia Bipolar disorder Corneal vascularity; Hyperaemia; Itching Asthma; Bronchitis Anxiety disorder Carcinoid syndrome; Acromegaly Advanced stage Parkinson's disease Dermal necrosis Depressive fatigue Alcohol use disorders Allergy Alzheimer disease Hypotension [ Show all ]
Length	443
Amino acid sequence	MDPLNLSWYDDDLERQNWSRPFNGSDGKADRPHYNYYATLLTLLIAVIVFGNVLVCMAVSREKALQTTTNYLIVSLAVADLLVATLVMPWVVYLEVVGEWKFSRIHCDIFVTLDVMMCTASILNLCAISIDRYTAVAMPMLYNTRYSSKRRVTVMISIVWVLSFTISCPLLFGLNNADQNECIIANPAFVVYSSIVSFYVPFIVTLLVYIKIYIVLRRRRKRVNTKRSSRAFRAHLRAPLKGNCTHPEDMKLCTVIMKSNGSFPVNRRRVEAARRAQELEMEMLSSTSPPERTRYSPIPPSHHQLTLPDPSHHGLHSTPDSPAKPEKNGHAKDHPKIAKIFEIQTMPNGKTRTSLKTMSRRKLSQQKEKKATQMLAIVLGVFIICWLPFFITHILNIHCDCNIPPVLYSAFTWLGYVNSAVNPIIYTTFNIEFRKAFLKILHC
UniProt	P14416
Protein Data Bank	6cm4, 6c38
GPCR-HGmod model	P14416
3D structure model	This structure is from PDB ID 6cm4.
BioLiP	BL0408379, BL0403379
Therapeutic Target Database	T67162
ChEMBL	CHEMBL217
IUPHAR	215
DrugBank	BE0000756

Ligand

Name	(A+/-)-Quinpirole dihydrochloride
Molecular formula	C13H21N3
IUPAC name	5-propyl-1,4,4a,6,7,8,8a,9-octahydropyrazolo[3,4-g]quinoline
Molecular weight	219.332
Hydrogen bond acceptor	2
Hydrogen bond donor	1
XlogP	2.3
Synonyms	BDBM81873 NCGC00016954-03 CHEBI:91928 NCGC00024974-03 L000007 SCHEMBL9169887 BRD-A85280935-003-01-7 NCGC00016954-04 5-propyl-1,4,4a,6,7,8,8a,9-octahydropyrazolo[3,4-g]quinoline CHEMBL192481 NCGC00024974-04 AC1L1B2N LY-171555 CAS_55397 NCGC00024974-02 5-Propyl-4,4a,5,6,7,8,8a,9-octahydro-1H-pyrazolo[3,4-g]quinoline CTK6E4814 NSC_55397 [ Show all ]
Inchi Key	FTSUPYGMFAPCFZ-UHFFFAOYSA-N
Inchi ID	InChI=1S/C13H21N3/c1-2-5-16-6-3-4-10-7-12-11(8-13(10)16)9-14-15-12/h9-10,13H,2-8H2,1H3,(H,14,15)
PubChem CID	1257
ChEMBL	N/A
IUPHAR	N/A
BindingDB	81873
DrugBank	N/A
Structure SDF download
Lipinski's druglikeness	This ligand satisfies Lipinski's rule of five.

Experimental Data

Parameter	Value	Reference	Database source
Ki	2.8 nM	PMID7756621	PDSP
Ki	14.0 nM	PMID8097160	PDSP
Ki	600.0 nM	PMID8301582	PDSP
Ki	891.251 nM	PMID12388666	PDSP
Ki	1185.0 nM	PMID9686407	PDSP
Ki	1400.0 nM	PMID7756621	PDSP
Ki	1402.0 nM	PMID1586393	PDSP
Ki	1445.44 nM	PMID12388666	PDSP
Ki	2158.0 nM	PMID12023553	PDSP
Ki	5000.0 nM	PMID8097160	PDSP

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