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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	Pecazine
Molecular formula	C19H22N2S
IUPAC name	10-[(1-methylpiperidin-3-yl)methyl]phenothiazine
Molecular weight	310.459
Hydrogen bond acceptor	3
Hydrogen bond donor	0
XlogP	5.6
Synonyms	BDBM50177661 CHEMBL395110 III-2318 Meprazine Oprea1_067080 Pecazina Probes1_000237 10-(1-Methylpiperidyl-3-methyl)phenothiazine 60-89-9 CBDivE_007551 DSSTox_GSID_46177 MCULE-4399173403 MolPort-001-727-944 Pacatal Pecazine [INN:BAN] SMR004703409 (N-Methyl-3-piperidyl)methylphenothiazine 10-[(1-Methyl-3-piperidyl)methyl]phenothiazine AC1Q7G4S AKOS021820849 CHEBI:135324 EINECS 200-490-8 MEPAZINE NCIOpen2_008134 Pakatal Phenothiazine, 10-((1-methyl-3-piperidyl)methyl)- US9504692, Mepezine 10-(1-Methyl-3-piperidyl)methyl phenothiazine 10H-Phenothiazine, 10-[(1-methyl-3-piperidinyl)methyl]- BRD-A82772293-001-01-6 CTK1A4018 Lacumin Mesapin Oprea1_208564 Pecazina [INN-Spanish] Probes2_000278 10-[(1-Methyl-3-piperidinyl)methyl]-10H-phenothiazine # AB00275848-07 CBHCDHNUZWWAPP-UHFFFAOYSA-N DSSTox_RID_81408 mepasin MPMP Pacatal Base Pecazinum STK386548 1'-{[2-methyl-3-(morpholin-4-ylcarbonyl)-4H-thieno[3,2-b]pyrrol-5-yl]carbonyl}-1,4'-bipiperidine 10-[(1-methylpiperidin-3-yl)methyl]phenothiazine AI3-50131 BAS 01176610 GTPL9782 Mepazine Base Nothiazine Pecatal Phenothiazine, 10-[(1-methyl-3-piperidyl)methyl]- 10-(1-Methyl-piperidin-3-ylmethyl)-10H-phenothiazine 2975-36-2 (mono-hydrochloride) CAS-60-89-9 DSSTox_CID_26177 LS-105610 MLS006011657 P 391 SCHEMBL149976 10-[(1-Methyl-3-piperidyl)-methyl]-phenothiazin AC1L1LQX CCG-108581 DTXSID2046177 Mepazin NCGC00160480-01 Pacatol Pecazinum [INN-Latin] Tox21_111842 10-((1-Methyl-3-piperidyl)methyl)phenothiazine 10H-Phenothiazine, 10-((1-methyl-3-piperidinyl)methyl)- AKOS000280691 [ Show all ]
Inchi Key	CBHCDHNUZWWAPP-UHFFFAOYSA-N
Inchi ID	InChI=1S/C19H22N2S/c1-20-12-6-7-15(13-20)14-21-16-8-2-4-10-18(16)22-19-11-5-3-9-17(19)21/h2-5,8-11,15H,6-7,12-14H2,1H3
PubChem CID	6075
ChEMBL	CHEMBL395110
IUPHAR	N/A
BindingDB	N/A
DrugBank	N/A
Structure SDF download
Lipinski's druglikeness	This ligand has a partition coefficient log P greater than 5.

Experimental Data

Parameter	Value	Reference	Database source
Activity	88.0 %	PMID17407813	ChEMBL

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