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Go to the GPCR, ligand, or experimental data tables.
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GPCR

Name	Histamine H3 receptor
Species	Homo sapiens (Human)
Gene	HRH3
Synonym	HH3R H3R H3 receptor GPCR97 G-protein coupled receptor 97
Disease	Obese insulin-resistant disorders Excessive daytime sleepiness Sleep disorders Schizophrenia Pain Obesity Metabolic disorders Mild to moderate alzheimer disease; Dementia Narcolepsy Neurological disease Eating disorder; Epilepsy; Pain Diabetic neuropathy; Musculoskeletal pain Dementia Alcohol use disorders Allergic rhinitis Alzheimer disease Alzheimer disease; Schizophrenia Anxiety disorder Attention deficit hyperactivity disorder Central nervous system disease Cognitive disorders [ Show all ]
Length	445
Amino acid sequence	MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFVADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTSSAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGGSSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAAGPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSVASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSLAVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFRRAFTKLLCPQKLKIQPHSSLEHCWK
UniProt	Q9Y5N1
Protein Data Bank	N/A
GPCR-HGmod model	Q9Y5N1
3D structure model	This predicted structure model is from GPCR-EXP Q9Y5N1.
BioLiP	N/A
Therapeutic Target Database	T64765
ChEMBL	CHEMBL264
IUPHAR	264
DrugBank	BE0000968

Ligand

Name	(R)-alpha-Methylhistamine
Molecular formula	C6H11N3
IUPAC name	(2R)-1-(1H-imidazol-5-yl)propan-2-amine
Molecular weight	125.175
Hydrogen bond acceptor	2
Hydrogen bond donor	2
XlogP	-0.3
Synonyms	LS-191796 PDSP2_000507 RAMH (R)-alpha-MeHA alpha-methylhistamine, (R)-isomer D04HEZ NCGC00024656-03 R(-)-alpha-METHYLHISTAMINE Tocris-0569 (2R)-1-(1H-imidazol-5-yl)propan-2-amine (R)alpha-Me-histamine 75614-87-8 BDBM22904 CCG-204707 Lopac0_000618 PDSP1_000541 r(-)alpha methylhistamine [3H](R)-alpha-methylhistamine (R)-(-)-alpha-methylhistamine AKOS006343508 CHEMBL268229 NCGC00024656-01 PDSP2_000533 SCHEMBL4155130 4491AJ Alpha-Methylhistamine-R GTPL1236 NCGC00024656-04 R(-)-\|A-Methyl Histamine Dihydrochloride XNQIOISZPFVUFG-RXMQYKEDSA-N (2R)-1-(3H-imidazol-4-yl)propan-2-amine (\|AR)-\|A-Methyl-1H-imidazole-4-ethanamine Dihydrochloride AC1L4GIC BDBM50215536 CHEBI:73337 LS-177199 PDSP1_000542 r-alpha-methylhistamine [3H]-R-alpha-Methylhistamine (R)-2-(3H-Imidazol-4-yl)-1-methyl-ethylamine 1H-Imidazole-4-ethanamine, alpha-methyl-, (alphaR)- Alpha Methylhistamine D03SAM NCGC00024656-02 PDSP2_000539 SCHEMBL73663 (2R)-1-(1H-imidazol-4-yl)propan-2-amine (R)-[3H]alpha-methylhistamine Alpha-Methylhistane-R GTPL1237 PDSP1_000535 R(-)-\|A-Methyl-1H-imidazole-5-ethanamine Dihydrochloride ZINC3872814 (R)-(-)-4-(2-aminopropyl)imidazole AC1Q299Z C6H11N3 [ Show all ]
Inchi Key	XNQIOISZPFVUFG-RXMQYKEDSA-N
Inchi ID	InChI=1S/C6H11N3/c1-5(7)2-6-3-8-4-9-6/h3-5H,2,7H2,1H3,(H,8,9)/t5-/m1/s1
PubChem CID	156615
ChEMBL	CHEMBL268229
IUPHAR	1237, 1236
BindingDB	22904, 50215536
DrugBank	N/A
Structure SDF download
Lipinski's druglikeness	This ligand satisfies Lipinski's rule of five.

Experimental Data

Parameter	Value	Reference	Database source
EC50	0.3162 nM	PMID21044842	ChEMBL
EC50	0.6761 nM	PMID14640553	ChEMBL
EC50	2.8 nM	PMID20384344	BindingDB,ChEMBL
IC50	2.3 nM	PMID23403082	ChEMBL
Inhibition	6.0 %	PMID23403082	ChEMBL
Intrinsic activity	0.95 -	PMID14640553	ChEMBL
Intrinsic activity	1.0 -	PMID21044842	ChEMBL
Kd	0.6 nM	PMID11179434	IUPHAR
Ki	0.15 nM	PMID11179436	BindingDB
Ki	0.55 nM	PMID20384344	BindingDB
Ki	0.55 nM	PMID20384344	ChEMBL
Ki	0.630957 - 3.98107 nM	PMID10869375, PMID11284713, PMID11714875, PMID11090094, PMID12393057, PMID11179434	IUPHAR
Ki	0.7 nM	PMID12954048, PMID11179434	BindingDB,ChEMBL
Ki	0.8 nM	PMID19577344	BindingDB,ChEMBL
Ki	0.88 nM	PMID12723960	ChEMBL
Ki	0.88 nM	PMID12723960	BindingDB
Ki	1.1 nM	PMID23403082	ChEMBL
Ki	1.995 nM	PMID18433114	ChEMBL
Ki	2.1 nM	PMID10869375	BindingDB
Ki	2.7 nM	PMID15139761	BindingDB,ChEMBL
Ki	4.365 nM	PMID14640553	ChEMBL
Ki	6.0 nM	PMID15947036	BindingDB
Ki	6.31 nM	PMID21044842	ChEMBL
Selectivity	55.0 -	PMID14640553	ChEMBL