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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	Levosulpiride
Molecular formula	C15H23N3O4S
IUPAC name	N-[[(2S)-1-ethylpyrrolidin-2-yl]methyl]-2-methoxy-5-sulfamoylbenzamide
Molecular weight	341.426
Hydrogen bond acceptor	6
Hydrogen bond donor	2
XlogP	0.6
Synonyms	s2104 CC-29928 SR-01000597436 CTK8B3281 SW197477-2 GTPL958 ZINC57008 J-015181 Levopride (S)-(-)-sulpiride Lopac0_001089 5-(Aminosulfonyl)-N-[[(2S)-1-ethyl-2-pyrrolidinyl]methyl]-2-benzamide N-{[(2S)-1-ethylpyrrolidin-2-yl]methyl}-2-methoxy-5-sulfamoylbenzamide AB00639965_09 NCGC00024853-05 API0003164 PDSP1_001649 Biomol-NT_000030 SC-76846 Sulpid DSSTox_GSID_42583 Tox21_110933 HMS2232P10 KS-5103 (-)-N-(((S)-1-Ethyl-2-pyrrolidinyl)methyl)-5-sulfamoyl-o-anisamide Levosulpiride (INN) (S)-5-Aminosulfonyl-N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxybenzamide MLS000759490 672L073 NCGC00016718-01 AC1LELQ0 NCGC00261774-01 BDBM81774 RV-12309 BRD-K51671335-001-04-9 CAS-23672-07-3 SR-01000076136 CPD000466366 Sulpiride-l EU-0101089 UNII-7MNE9M8287 component BGRJTUBHPOOWDU-NSHDSACASA-N HY-B1059 Levopraid (S)-(-)-5-aminosulfonyl-N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxybenzamide Levosulpiridum (S)-sulpiride N-[((2S)-1-ethylpyrrolidin-2-yl)methyl](6-methoxy-3-sulfamoylphenyl)carboxamid e AB00639965-06 NCGC00024853-03 AKOS015897363 PDSP1_000516 BG0325 S-(-)-Sulpiride SAM001246703 CCG-100847 SR-01000597436-1 D07312 TL8001954 HMS2051A08 JTG7R315LK Levosulpirida (S)-(-)-Sulpiride, >=98% (titration) LP01089 5-(Aminosulfonyl)-N-[[(2S)-1-ethyl-2-pyrrolidinyl]methyl]-2-methoxy-benzamide NC00097 AB1009626 NCGC00024853-06 BCP0726000072 PDSP2_000514 BPBio1_001221 C-20361 SCHEMBL70112 CHEMBL267044 Sulpiride [L-(-)] DSSTox_RID_80052 Tox21_110933_1 HMS3263I20 L-Sulpiride (-)-N-[(1-Ethyl-2-pyrrolidinyl)methyl]-5-sulfamoyl-o-anisamide Levosulpiride (Levogastrol) (S)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-methoxy-5-sulfamoylbenzamide MLS001424014 NCGC00024853-01 AK163543 Nexipride Benzamide, 5-(aminosulfonyl)-N-((1-ethyl-2-pyrrolidinyl)methyl)-2-methoxy-, (S)- (9CI) S 7771 CAS_15676-16-1 SR-01000076136-2 CS-4581 Sulpiride-S GP2472 UNII-JTG7R315LK I0821 Levopraid (TN) (S)-(-)-N-((1-Ethyl-2-pyrrolidinyl)methyl)-5-sulfamoyl-o-anisamide Levosulpride 23672-07-3 N-[[(2S)-1-ethylpyrrolidin-2-yl]methyl]-2-methoxy-5-sulfamoylbenzamide AB00639965-08 NCGC00024853-04 ANW-42196 PDSP1_000620 BGRJTUBHPOOWDU-NSHDSACASA-N S-Sulpiride SBB058180 CHEBI:64119 ST50319539 DSSTox_CID_22583 Tocris-0895 HMS2089E04 K-6442 (-)-5-Aminosulfonyl-N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxybenzamide (S)-(-)-Sulpiride, VETRANAL(TM), analytical standard MFCD00055220 5-HT6 Serotonin Receptor from rat, recombinant, expressed in HEK 293 cells, membrane suspension NCGC00015966-10 AC-6821 NCGC00024853-09 BCP9000853 PDSP2_000616 BRD-K51671335-001-01-5 CAS-15676-16-1 SMR000466366 CL-004 SULPIRIDE,(+) DTXSID0042583 Tox21_501089 HMS3266P14 Levogastrol (-)-Sulpiride Levosulpiride [INN] (S)-N-[(1-Ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-sulfamoylbenzamide MolPort-003-930-513 NCGC00024853-02 AKOS007930553 o-ANISAMIDE, N-((1-ETHYL-2-PYRROLIDINYL)METHYL)-5-SULFAMOYL-, (S)-(-)- Benzamide, N-((1-ethyl-2-pyrrolidinyl)methyl)-2-methoxy-5-sulfamoyl-, S-(-)- S-(-)-N-(1-Ethyl-2-pyrrolidinomethyl)-2-methoxy-5-sulfamoylebenzamide [ Show all ]
Inchi Key	BGRJTUBHPOOWDU-NSHDSACASA-N
Inchi ID	InChI=1S/C15H23N3O4S/c1-3-18-8-4-5-11(18)10-17-15(19)13-9-12(23(16,20)21)6-7-14(13)22-2/h6-7,9,11H,3-5,8,10H2,1-2H3,(H,17,19)(H2,16,20,21)/t11-/m0/s1
PubChem CID	688272
ChEMBL	CHEMBL267044
IUPHAR	958
BindingDB	81774
DrugBank	N/A
Structure SDF download
Lipinski's druglikeness	This ligand satisfies Lipinski's rule of five.

Experimental Data

Parameter	Value	Reference	Database source
IC50	2e-08 nM	PMID3156993	ChEMBL
IC50	128.0 nM	DrugMatrix in vitro pharmacology data	ChEMBL
Ki	5.0 nM	PMID9577836	BindingDB
Ki	10.0 - 520.0 nM	PMID8301582, PMID1354163, PMID8301592	IUPHAR
Ki	31.0 nM	PMID1840645	BindingDB
Ki	43.0 nM	DrugMatrix in vitro pharmacology data	ChEMBL
Ki	46.0 nM	PMID1840645	BindingDB
Ki	51.0 nM	PMID10987445, PMID10206547	BindingDB,ChEMBL
Ki	120.0 nM	PMID10987445, PMID10206547	BindingDB,ChEMBL
Ki	3326.0 nM	PMID9021894	BindingDB

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