General Information of the Protein
Protein ID
PT01202
Protein Name
5-hydroxytryptamine receptor 1B
Secondarily
Protein Name
S12
Serotonin 1D beta receptor
Serotonin receptor 1B
Gene Name
HTR1B
Secondarily
Gene Name
HTR1DB
Sequence
MEEPGAQCAPPPPAGSETWVPQANLSSAPSQNCSAKDYIYQDSISLPWKVLLVMLLALITLATTLSNAFVIATVYRTRKLHTPANYLIASLAVTDLLVSILVMPISTMYTVTGRWTLGQVVCDFWLSSDITCCTASILHLCVIALDRYWAITDAVEYSAKRTPKRAAVMIALVWVFSISISLPPFFWRQAKAEEEVSECVVNTDHILYTVYSTVGAFYFPTLLLIALYGRIYVEARSRILKQTPNRTGKRLTRAQLITDSPGSTSSVTSINSRVPDVPSESGSPVYVNQVKVRVSDALLEKKKLMAARERKATKTLGIILGAFIVCWLPFFIISLVMPICKDACWFHLAIFDFFTWLGYLNSLINPIIYTMSNEDFKQAFHKLIRFKCTS
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Monoamine receptor
>
Serotonin receptor
Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. Arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Regulates the release of 5-hydroxytryptamine, dopamine and acetylcholine in the brain, and thereby affects neural activity, nociceptive processing, pain perception, mood and behavior. Besides, plays a role in vasoconstriction of cerebral arteries.
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Uniprot ID
Primary ID:
P28222

Secondarily ID:
Q4VAY7
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Ensembl ID
ENSG00000135312
HGNC ID
HGNC:5287
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000901 , 661W
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0387083
 Compound Info 
(3aS,9bS)-3a-methyl-5-phenyl-2,3,4,9b-tetrahydro-1H-pyrrolo[2,3-c]quinoline
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C18H20N2
  1
1
Ki > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0391120
 Compound Info 
(1S,2R)-1-ethyl-7-methoxy-2-methyl-3,4-dihydro-1H-naphthalen-2-amine
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C14H21NO
  1
1
Ki > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0391121
 Compound Info 
(3S,4S)-4-ethyl-3,6-dimethyl-2,4-dihydrochromen-3-amine
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C13H19NO
  1
1
Ki > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0391154
 Compound Info 
(3aS,9bS)-7,9-dimethoxy-3a-methyl-2,3,4,9b-tetrahydro-1H-chromeno[3,4-b]pyrrole
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C14H19NO3
  1
1
Ki > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0411059
 Compound Info 
(3S,4S)-4-ethyl-3-methyl-1-phenyl-2,4-dihydroquinolin-3-amine
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C18H22N2
  1
1
Ki > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000011 , CHO
 Cell Line Info 
Cell Line ID: CL000026 , CHO-K1
 Cell Line Info 
Cell Line ID: CL000053 , COS-7
 Cell Line Info 
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000017 , HeLa
 Cell Line Info 
Cell Line ID: CL000101 , L-M(TK-)
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0001238
 Compound Info 
14C-5-hydroxy tryptamine creatinine disulfate
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C10H12N2O
  10
1 IC50 = 5 nM
2 IC50 = 6.5 nM
3 IC50 = 12 nM
4 IC50 = 16 nM
5 IC50 = 29 nM
6 Ki = 4 nM
7 Ki = 6.76 nM
8 Ki = 7.1 nM
9 Ki = 14 nM
10 Ki = 18 nM
CP0005653
 Compound Info 
(3-[2-(dimethylamino)ethyl]-1H-indol-5-yl)-N-methylmethanesulfonamide
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C14H21N3O2S
  8
1 IC50 = 27 nM
2 Ki = 7.7 nM
3 Ki = 9.6 nM
4 Ki = 10 nM
5 Ki = 19.1 nM
6 Ki = 23.1 nM
7 Ki = 36 nM
8 Ki = 47.9 nM
CP0079840
 Compound Info 
Benzyl-{(S)-1-[2-(5-[1,2,4]triazol-4-yl-1H-indol-3-yl)-ethyl]-pyrrolidin-3-ylmethyl}-amine
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C24H28N6
  1
1 IC50 = 47 nM
CP0056703
 Compound Info 
(S)-4-(3-{2-[(S)-3-(Benzylamino-methyl)-pyrrolidin-1-yl]-ethyl}-1H-indol-5-ylmethyl)-oxazolidin-2-one
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C26H32N4O2
  1
1 IC50 = 49 nM
CP0115159
 Compound Info 
(S)-4-[3-(2-{(S)-3-[((S)-1-Phenyl-ethylamino)-methyl]-pyrrolidin-1-yl}-ethyl)-1H-indol-5-ylmethyl]-oxazolidin-2-one
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C27H34N4O2
  1
1 IC50 = 50 nM
CP0041353
 Compound Info 
C-(3-{2-[(S)-3-(Benzylamino-methyl)-pyrrolidin-1-yl]-ethyl}-1H-indol-5-yl)-N-methyl-methanesulfonamide
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C24H32N4O2S
  1
1 IC50 = 62 nM
CP0136962
 Compound Info 
3-(3-{4-[2-(3-Fluoro-phenyl)-ethyl]-piperazin-1-yl}-propyl)-5-[1,2,4]triazol-4-yl-1H-indole
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C25H29FN6
  1
1 IC50 = 75 nM
CP0169227
 Compound Info 
C-[3-(2-Dimethylamino-ethyl)-1H-indol-5-yl]-N-[4-({[3-(2-dimethylamino-ethyl)-1H-indol-5-ylmethanesulfonyl]-methyl-amino}-methyl)-benzyl]-N-methyl-methanesulfonamide
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C36H48N6O4S2
  1
1 Ki = 0.64 nM
CP0106415
 Compound Info 
2-(5-(2-(8-(4-methylpiperazin-1-yl)naphthalen-2-yloxy)ethoxy)-1H-indol-3-yl)ethanamine
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C27H32N4O2
  1
1 Ki = 0.76 nM
CP0173138
 Compound Info 
N-[3-[[1-[2-(2-methylquinolin-5-yl)oxyethyl]piperidin-4-yl]methyl]phenyl]methanesulfonamide
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C25H31N3O3S
  1
1 Ki = 1.995 nM
CP0056779
 Compound Info 
1,2-di[8-(4-methylhexahydro-1-pyrazinyl)-2-naphthyloxy]ethane
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C32H38N4O2
  1
1 Ki = 2.1 nM
CP0099897
 Compound Info 
(S)-4-((3-(2-(dimethylamino)ethyl)-1H-indol-5-yl)methyl)oxazolidin-2-one
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C16H21N3O2
  1
1 Ki = 4.2 nM
CP0214664
 Compound Info 
2-(dimethylamino)-N-[3-[[1-[2-(2-methylquinolin-5-yl)oxyethyl]piperidin-4-yl]methyl]phenyl]acetamide
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C28H36N4O2
  1
1 Ki = 6.31 nM
CP0056783
 Compound Info 
2N,2N-dipropyl-8-[6-(3-dipropylamino-1,2,3,4-tetrahydro-5-naphthalenyloxy)hexyloxy]-1,2,3,4-tetrahydro-2-naphthalenamine
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C38H60N2O2
  1
1 Ki = 6.4 nM
CP0152118
 Compound Info 
6-[[1-[2-(2-methylquinolin-5-yl)oxyethyl]piperidin-4-yl]methyl]-4H-1,4-benzoxazin-3-one
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C26H29N3O3
  1
1 Ki = 10 nM
CP0030068
 Compound Info 
N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethanamine
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C15H19N5
  1
1 Ki = 10.1 nM
CP0061753
 Compound Info 
1-NP
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C14H16N2
  1
1 Ki = 10.6 nM
CP0658701
 Compound Info 
1-[2-(2,4-Dimethyl-phenylsulfanyl)-phenyl]-piperazine Hydrochloride
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C18H23ClN2S
  1
1 Ki = 33 nM
CP0079263
 Compound Info 
2-methyl-5-[2-[4-(quinolin-8-ylmethyl)piperazin-1-yl]ethoxy]quinoline
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C26H28N4O
  1
1 Ki = 199.53 nM
CP0078427
 Compound Info 
4-Fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide
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C21H22FN3O
  1
1 Ki = 240 nM
CP0077951
 Compound Info 
1-(2-(4-(6-fluoro-1H-indol-3-yl)-5,6-dihydropyridin-1(2H)-yl)ethyl)-3,4-dihydro-1H-isochromene-6-carboxamide
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C25H26FN3O2
  1
1 Ki = 281 nM
CP0037227
 Compound Info 
7-(dipropylamino)-5,6,7,8-tetrahydronaphthalen-1-ol
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C16H25NO
  1
1 Ki = 559 nM
CP0002071
 Compound Info 
N-[2-(5-methoxy-1H-indol-3-yl)ethyl]-N-prop-2-enylprop-2-en-1-amine
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C17H22N2O
  1
1 Ki = 741.31 nM
CP0045069
 Compound Info 
2-[1-(benzenesulfonyl)-5-methoxyindol-3-yl]-N,N-dimethylethanamine
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C19H22N2O3S
  1
1 Ki = 9210 nM
CP0096286
 Compound Info 
(R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidin-1-ylsulfonyl)phenol
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C18H28N2O3S
  1
1 Ki > 10000 nM
Clinical Information about the Protein
Target 1 ( 5-HT 1B receptor (HTR1B) )
Target Type Successful Target
Disease 7 Target-related Diseases  7
1 Migraine [ICD-11: 8A80]
2 Psychotic disorder [ICD-11: 6A20-6A25]
3 Hyperprolactinaemia [ICD-11: 5A60.1]
4 Attention deficit hyperactivity disorder [ICD-11: 6A05.Z]
5 Pain [ICD-11: MG30-MG3Z]
6 Anxiety disorder [ICD-11: 6B00-6B0Z]
7 Major depressive disorder [ICD-11: 6A70.3]
Approved Drug(s) 6 Approved Drugs  6
1 Eletriptan
 Drug Info 
Approved
Migraine
2 Fluphenazine
 Drug Info 
Approved
Psychotic disorder
3 Frovatriptan
 Drug Info 
Approved
Migraine
4 Metergolin
 Drug Info 
Approved
Hyperprolactinaemia
5 Naratriptan
 Drug Info 
Approved
Migraine
6 Zolmitriptan
 Drug Info 
Approved
Migraine
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Eltoprazine
 Drug Info 
Phase 3
Attention deficit hyperactivity disorder
Discontinued Drug(s) 5 Discontinued Drugs  5
1 Alniditan
 Drug Info 
Discontinued in Phase 3
Migraine
2 Anpirtoline
 Drug Info 
Terminated
Pain
3 AZD-1134
 Drug Info 
Terminated
Anxiety disorder
4 CGS-12066B
 Drug Info 
Terminated
Anxiety disorder
5 GR-127935
 Drug Info 
Terminated
Major depressive disorder
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT06668 5-hydroxytryptamine receptor 1B Gorilla gorilla gorilla, Western lowland gorilla
 Protein Info