General Information of the Protein
Protein ID
PT01019
Protein Name
5-hydroxytryptamine receptor 2B
Secondarily
Protein Name
Serotonin receptor 2B
Gene Name
HTR2B
Sequence
MALSYRVSELQSTIPEHILQSTFVHVISSNWSGLQTESIPEEMKQIVEEQGNKLHWAALLILMVIIPTIGGNTLVILAVSLEKKLQYATNYFLMSLAVADLLVGLFVMPIALLTIMFEAMWPLPLVLCPAWLFLDVLFSTASIMHLCAISVDRYIAIKKPIQANQYNSRATAFIKITVVWLISIGIAIPVPIKGIETDVDNPNNITCVLTKERFGDFMLFGSLAAFFTPLAIMIVTYFLTIHALQKKAYLVKNKPPQRLTWLTVSTVFQRDETPCSSPEKVAMLDGSRKDKALPNSGDETLMRRTSTIGKKSVQTISNEQRASKVLGIVFFLFLLMWCPFFITNITLVLCDSCNQTTLQMLLEIFVWIGYVSSGVNPLVYTLFNKTFRDAFGRYITCNYRATKSVKTLRKRSSKIYFRNPMAENSKFFKKHGIRNGINPAMYQSPMRLRSSTIQSSSIILLDTLLLTENEGDKTEEQVSYV
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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) (PubMed:8143856, PubMed:7926008, PubMed:8078486, PubMed:8882600, PubMed:18703043, PubMed:23519210). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances (PubMed:8143856, PubMed:7926008, PubMed:8078486, PubMed:12970106, PubMed:18703043, PubMed:23519210, PubMed:23519215, PubMed:24357322, PubMed:28129538). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors (PubMed:8143856, PubMed:8078486, PubMed:8882600, PubMed:23519215, PubMed:28129538). Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways (PubMed:23519215, PubMed:28129538). Signaling activates a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and down-stream signaling cascades and promotes the release of Ca(2+) ions from intracellular stores (PubMed:8143856, PubMed:8078486, PubMed:8882600, PubMed:18703043, PubMed:23519215, PubMed:28129538). Plays a role in the regulation of dopamine and 5-hydroxytryptamine release, 5-hydroxytryptamine uptake and in the regulation of extracellular dopamine and 5-hydroxytryptamine levels, and thereby affects neural activity. May play a role in the perception of pain (By similarity). Plays a role in the regulation of behavior, including impulsive behavior (PubMed:21179162). Required for normal proliferation of embryonic cardiac myocytes and normal heart development. Protects cardiomyocytes against apoptosis. Plays a role in the adaptation of pulmonary arteries to chronic hypoxia. Plays a role in vasoconstriction. Required for normal osteoblast function and proliferation, and for maintaining normal bone density. Required for normal proliferation of the interstitial cells of Cajal in the intestine (By similarity).
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Uniprot ID
Primary ID:
P41595

Secondarily ID:
B2R9D5
Q53TI1
Q62221
Q6P523
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Ensembl ID
ENSG00000135914
HGNC ID
HGNC:5294
Subcellular Location
Cell membrane
Synapse
Synaptosome
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
Compound ID Compound Name Compound Formula
CP0426384
(3aS,9bS)-6-bromo-3a-methyl-2,3,4,9b-tetrahydro-1H-chromeno[3,4-b]pyrrole
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C12H14BrNO
 1
1
Ki = 19.95 nM
   TI
   LI
   LO
   TS
CP0426382
(3aS,9bS)-3a,7,9-trimethyl-2,3,4,9b-tetrahydro-1H-chromeno[3,4-b]pyrrole
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C14H19NO
 1
1
Ki = 79.43 nM
   TI
   LI
   LO
   TS
CP0391127
(3aS,9bS)-3a-methyl-7-phenylmethoxy-2,3,4,9b-tetrahydro-1H-chromeno[3,4-b]pyrrole
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C19H21NO2
 1
1
Ki = 125.89 nM
   TI
   LI
   LO
   TS
CP0437998
(3S,4S)-4-ethyl-3-methyl-6-phenyl-2,4-dihydrochromen-3-amine
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C18H21NO
 1
1
Ki = 125.89 nM
   TI
   LI
   LO
   TS
CP0391120
(1S,2R)-1-ethyl-7-methoxy-2-methyl-3,4-dihydro-1H-naphthalen-2-amine
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C14H21NO
 1
1
Ki = 144.54 nM
   TI
   LI
   LO
   TS
CP0426383
(3aS,9bS)-3a-methyl-6-phenyl-2,3,4,9b-tetrahydro-1H-chromeno[3,4-b]pyrrole
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C18H19NO
 1
1
Ki = 158.49 nM
   TI
   LI
   LO
   TS
CP0391121
(3S,4S)-4-ethyl-3,6-dimethyl-2,4-dihydrochromen-3-amine
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C13H19NO
 1
1
Ki = 177.83 nM
   TI
   LI
   LO
   TS
CP0391130
(3aS,9bS)-3,3a-dimethyl-5-phenyl-1,2,4,9b-tetrahydropyrrolo[2,3-c]quinoline
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C19H22N2
 1
1
Ki = 199.53 nM
   TI
   LI
   LO
   TS
CP0391154
(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 = 251.19 nM
   TI
   LI
   LO
   TS
CP0421273
(3S,4S)-4-ethyl-6-methoxy-3-methyl-2,4-dihydrochromen-3-amine
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C13H19NO2
 1
1
Ki = 251.19 nM
   TI
   LI
   LO
   TS
CP0426378
(3aS,9bS)-3,3a-dimethyl-6-phenyl-1,2,4,9b-tetrahydrochromeno[3,4-b]pyrrole
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C19H21NO
 1
1
Ki = 251.19 nM
   TI
   LI
   LO
   TS
CP0426385
(3aS,9bS)-3a-methyl-8-phenyl-2,3,4,9b-tetrahydro-1H-chromeno[3,4-b]pyrrole
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C18H19NO
 1
1
Ki = 251.19 nM
   TI
   LI
   LO
   TS
CP0426405
(3aS,9bS)-3a,8-dimethyl-5-(4-methylphenyl)-2,3,4,9b-tetrahydro-1H-pyrrolo[2,3-c]quinoline
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C20H24N2
 1
1
Ki = 316.23 nM
   TI
   LI
   LO
   TS
CP0432125
(3aS,9bS)-8-bromo-5-(4-bromophenyl)-3a-methyl-2,3,4,9b-tetrahydro-1H-pyrrolo[2,3-c]quinoline
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C18H18Br2N2
 1
1
Ki = 316.23 nM
   TI
   LI
   LO
   TS
CP0387083
(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 = 501.19 nM
   TI
   LI
   LO
   TS
CP0391128
1-[(3aS,9bS)-3a-methyl-6-phenyl-1,2,4,9b-tetrahydrochromeno[3,4-b]pyrrol-3-yl]ethanone
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C20H21NO2
 1
1
Ki = 501.19 nM
   TI
   LI
   LO
   TS
CP0426380
(3aS,9bS)-8-methoxy-3a-methyl-2,3,4,9b-tetrahydro-1H-chromeno[3,4-b]pyrrole
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C13H17NO2
 1
1
Ki = 630.96 nM
   TI
   LI
   LO
   TS
CP0411059
(3S,4S)-4-ethyl-3-methyl-1-phenyl-2,4-dihydroquinolin-3-amine
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C18H22N2
 1
1
Ki = 794.33 nM
   TI
   LI
   LO
   TS
CP0426381
(3aS,9bS)-3,3a-dimethyl-1,2,4,9b-tetrahydrochromeno[3,4-b]pyrrol-7-ol
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C13H17NO2
 1
1
Ki = 1000 nM
   TI
   LI
   LO
   TS
CP0416007
(3S,4S)-3-amino-4-ethyl-3-methyl-2,4-dihydrochromen-7-ol
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C12H17NO2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0432102
1-[(3aS,9bS)-3a-methyl-5-phenyl-1,2,4,9b-tetrahydropyrrolo[2,3-c]quinolin-3-yl]ethanone
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C20H22N2O
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0432122
1-[(3aS,9bS)-7-hydroxy-3a-methyl-1,2,4,9b-tetrahydrochromeno[3,4-b]pyrrol-3-yl]ethanone
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C14H17NO3
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0455607
(3aS,9bS)-3a-methyl-2,3,4,9b-tetrahydro-1H-chromeno[3,4-b]pyrrol-7-ol
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C12H15NO2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0025667
2-[4-(4-Methyl-benzyl)-piperazin-1-yl]-1-(2-methyl-2,3-dihydro-indol-1-yl)-ethanone
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C18H19ClN4
 1
1 EC50 = 20 nM
CP0055945
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine
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C11H16INO2
 4
1 IC50 = 3.2 nM
2 IC50 = 4 nM
3 Ki = 2 nM
4 Ki = 42.7 nM
CP0129858
(9S)-2-benzyl-N,9-dimethyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepin-4-amine
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C17H22N4
 1
1 IC50 = 67 nM
CP0128654
2-[difluoro(phenyl)methyl]-N-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepin-4-amine
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C16H18F2N4
 1
1 IC50 = 110 nM
CP0216239
3-(benzenesulfonyl)-N,5,7-trimethylpyrazolo[1,5-a]pyrimidin-2-amine
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C15H16N4O2S
 1
1 IC50 = 5130 nM
CP0116615
4-(4-fluoronaphthalen-1-yl)-6-isopropylpyrimidin-2-amine
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C17H16FN3
 1
1 Ki = 0.3 nM
CP0071447
(1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine
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C11H14ClN
 4
1 Ki = 1.3 nM
2 Ki = 174 nM
3 Ki = 189 nM
4 Ki = 220 nM
CP0042927
7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-3,4-dihydroquinolin-2(1H)-one
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C23H27Cl2N3O2
 2
1 Ki = 1.4 nM
2 Ki = 5.6 nM
CP0125833
4-N-(3-iodophenyl)-1,3,5-triazaspiro[5.5]undeca-1,4-diene-2,4-diamine
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C14H18IN5
 1
1 Ki = 1.7 nM
CP0161466
(4R,10aR)-7-Chloro-4,6-dimethyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indole
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C13H17ClN2
 1
1 Ki = 3.2 nM
CP0145471
5-((4-(6-chlorothieno[2,3-d]pyrimidin-4-ylamino)piperidin-1-yl)methyl)-2-fluorobenzonitrile
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C19H17ClFN5S
 1
1 Ki = 3.4 nM
CP0193993
(S)-1-(6-chloro-5-fluoro-1H-indol-1-yl)propan-2-amine
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C11H12ClFN2
 1
1 Ki = 5.1 nM
CP0105671
4-N-(3-bromophenyl)-1,3,5-triazaspiro[5.5]undeca-1,4-diene-2,4-diamine
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C14H18BrN5
 2
1 Ki = 5.8 nM
2 Ki = 6.2 nM
CP0354430
4-N-(3-chlorophenyl)-1,3,5-triazaspiro[5.5]undeca-1,4-diene-2,4-diamine
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C14H18ClN5
 1
1 Ki = 6.3 nM
CP0090283
ethyl 3-[(2-amino-1,3,5-triazaspiro[5.5]undeca-1,4-dien-4-yl)amino]benzoate
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C17H23N5O2
 1
1 Ki = 7.2 nM
CP0099665
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine
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C12H16N2O
 1
1 Ki = 7.8 nM
CP0001238
14C-5-hydroxy tryptamine creatinine disulfate
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C10H12N2O
 3
1 Ki = 12 nM
2 Ki = 13 nM
3 Ki = 13.49 nM
CP0172895
(S)-1-(1H-pyrrolo[2,3-f]quinolin-1-yl)propan-2-amine
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C14H15N3
 1
1 Ki = 12 nM
CP0057346
3-(2-aminopropyl)-1H-indol-5-ol
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C11H14N2O
 1
1 Ki = 13 nM
CP0139865
ethyl (1S,2R,3S,4R,5S)-4-[2-chloro-6-(dicyclopropylmethylamino)purin-9-yl]-2,3-dihydroxybicyclo[3.1.0]hexane-1-carboxylate
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C21H26ClN5O4
 1
1 Ki = 15 nM
CP0700641
trans-[2-(2-Chloro-4-fluorophenyl)cyclopropyl]methylamine Hydrochloride
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C10H12Cl2FN
 1
1 Ki = 16 nM
CP0700642
(+)-(S,S)-trans-[2-(2-Bromophenyl)cyclopropyl]methylamine Hydrochloride
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C10H13BrClN
 1
1 Ki = 16 nM
CP0057042
(R)-1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine
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C11H16INO2
 1
1 Ki = 18 nM
CP0216157
(S)-1-(5-chloro-1H-pyrrolo[2,3-f]quinolin-1-yl)propan-2-amine
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C14H14ClN3
 1
1 Ki = 18 nM
CP0074886
(4R,10aS)-7-Chloro-4,6-dimethyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indole
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C13H17ClN2
 1
1 Ki = 19 nM
CP0533258
4-N-(3-methylphenyl)-1,3,5-triazaspiro[5.5]undeca-1,4-diene-2,4-diamine
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C15H21N5
 1
1 Ki = 19.8 nM
CP0018076
5-Methyl-3,5-dihydro-2H-pyrrolo[2,3-f]indole-1-carboxylic acid pyridin-3-ylamide
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C17H16N4O
 1
1 Ki = 20 nM
CP0090282
2-N-(3-bromophenyl)-4,4-dimethyl-1H-1,3,5-triazine-2,6-diamine
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C11H14BrN5
 1
1 Ki = 20.5 nM
CP0784795
trans-[2-(2-Bromophenyl)cyclopropyl]methylamine Hydrochloride
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C10H13BrClN
 1
1 Ki = 22 nM
CP0155461
(1S,2R,3S,4R,5S)-4-[2-chloro-6-(dicyclopropylmethylamino)purin-9-yl]-2,3-dihydroxy-N-methylbicyclo[3.1.0]hexane-1-carboxamide
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C20H25ClN6O3
 1
1 Ki = 23 nM
CP0066194
N-[2-(1,3-benzodioxol-5-yl)ethyl]-N-[2-(3,4-dimethoxyphenyl)ethyl]-3-phenylpropan-1-amine
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C28H33NO4
 1
1 Ki = 26 nM
CP0105673
3-[(2-amino-1,3,5-triazaspiro[5.5]undeca-1,4-dien-4-yl)amino]-N-ethylbenzamide
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C17H24N6O
 1
1 Ki = 27.5 nM
CP0046618
1-(3-chlorophenyl)piperazine
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C10H13ClN2
 1
1 Ki = 32 nM
CP0049639
3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol
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C13H18N2O
 1
1 Ki = 38 nM
CP0090284
ethyl 3-[[4-(dimethylamino)-1,3,5-triazaspiro[5.5]undeca-1,4-dien-2-yl]amino]benzoate
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C19H27N5O2
 1
1 Ki = 38.5 nM
CP0102634
4-N-(3-fluorophenyl)-1,3,5-triazaspiro[5.5]undeca-1,4-diene-2,4-diamine
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C14H18FN5
 1
1 Ki = 53.3 nM
CP0647970
trans-[2-(3-Methylphenyl)cyclopropyl]methylamine Hydrochloride
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C11H16ClN
 1
1 Ki = 85 nM
CP0700640
trans-[2-(4-Fluorophenyl)cyclopropyl]methylamine Hydrochloride
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C10H13ClFN
 1
1 Ki = 89 nM
CP0034920
(S)-1-(1H-pyrrolo[3,2-h]quinolin-1-yl)propan-2-amine
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C14H15N3
 1
1 Ki = 115 nM
CP0172896
(S)-N-(naphthalen-2-ylmethyl)-1-(1H-pyrrolo[2,3-f]quinolin-1-yl)propan-2-amine
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C25H23N3
 1
1 Ki = 136 nM
CP0104535
(S)-N-(benzo[d][1,3]dioxol-5-ylmethyl)-1-(1H-pyrrolo[2,3-f]quinolin-1-yl)propan-2-amine
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C22H21N3O2
 1
1 Ki = 138 nM
CP0398905
4-N-phenyl-1,3,5-triazaspiro[5.5]undeca-1,4-diene-2,4-diamine
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C14H19N5
 1
1 Ki = 151.3 nM
CP0034922
(S)-1-(1H-pyrrolo[3,2-h]isoquinolin-1-yl)propan-2-amine
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C14H15N3
 1
1 Ki = 210 nM
CP0034918
(S)-N-(2-chlorobenzyl)-1-(1H-pyrrolo[2,3-f]quinolin-1-yl)propan-2-amine
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C21H20ClN3
 1
1 Ki = 380 nM
CP0034925
(S)-N-(1-(1H-pyrrolo[2,3-f]quinolin-1-yl)propan-2-yl)prop-2-en-1-amine
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C17H19N3
 1
1 Ki = 455 nM
CP0072415
2-[(4R,5S)-4-(hydroxymethyl)-5-methyl-4,5-dihydro-1,3-thiazol-2-yl]phenol
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C11H13NO2S
 1
1 Ki = 505 nM
CP0216287
(S)-N-benzyl-1-(1H-pyrrolo[2,3-f]quinolin-1-yl)propan-2-amine
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C21H21N3
 1
1 Ki = 515 nM
CP0255556
(S)-N-(cyclohexylmethyl)-1-(1H-pyrrolo[2,3-f]quinolin-1-yl)propan-2-amine
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C21H27N3
 1
1 Ki = 624 nM
CP0169100
(1R,2R,3S,4R,5S)-4-[2-chloro-6-(dicyclopropylmethylamino)purin-9-yl]bicyclo[3.1.0]hexane-2,3-diol
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C18H22ClN5O2
 1
1 Ki = 641 nM
CP0272372
(2-methyl-benzyl)-((S)-1-methyl-2-pyrrolo[2,3-f]quinolin-1-yl-ethyl)-amine
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C22H23N3
 1
1 Ki = 739 nM
CP0034919
(S)-1-(1H-pyrrolo[2,3-f]isoquinolin-1-yl)propan-2-amine
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C14H15N3
 1
1 Ki = 778 nM
CP0034921
(S)-N-(2-methoxybenzyl)-1-(1H-pyrrolo[2,3-f]quinolin-1-yl)propan-2-amine
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C22H23N3O
 1
1 Ki = 883 nM
CP0543598
N-[2-(4-ethyl-6-oxo-1H-pyrimidin-2-yl)-5-methylpyrazol-3-yl]-3-methylbenzamide
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C18H19N5O2
 1
1 Ki = 900 nM
CP0199375
2-(2-hydroxyphenyl)-1,3-thiazole-4-carboxamide
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C10H8N2O2S
 1
1 Ki = 1031 nM
CP0018686
(2S,3S,4R,5R)-3,4-Dihydroxy-5-[6-(3-iodo-benzylamino)-purin-9-yl]-tetrahydro-furan-2-carboxylic acid methylamide
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C18H19IN6O4
 1
1 Ki = 1080 nM
CP0083349
2-(2-hydroxyphenyl)-4,5-dihydro-1,3-thiazole-4-carboxamide
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C10H10N2O2S
 1
1 Ki = 1260 nM
CP0569784
N-[2-(4-ethyl-6-oxo-1H-pyrimidin-2-yl)-5-methylpyrazol-3-yl]-2-fluorobenzamide
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C17H16FN5O2
 1
1 Ki = 1300 nM
CP0110114
2-[(4R)-4-(hydroxymethyl)-4,5-dihydro-1,3-thiazol-2-yl]phenol
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C10H11NO2S
 1
1 Ki = 1360 nM
CP0054731
5-hydroxy-2-(2-phenylethyl)chromen-4-one
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C17H14O3
 1
1 Ki = 2454.71 nM
CP0085828
(2S,4S)-2-[(4R,5S)-2-(2-hydroxyphenyl)-5-methyl-4,5-dihydro-1,3-thiazol-4-yl]-3,4-dimethyl-1,3-thiazolidine-4-carboxylic acid
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C16H20N2O3S2
 1
1 Ki = 3922 nM
CP0083075
(2R,4S)-2-[(4R,5S)-2-(2-hydroxyphenyl)-5-methyl-4,5-dihydro-1,3-thiazol-4-yl]-3,4-dimethyl-1,3-thiazolidine-4-carboxylic acid
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C16H20N2O3S2
 1
1 Ki = 4695 nM
CP0096286
(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 2B receptor (HTR2B) )
Target Type Successful Target
Disease 7 Target-related Diseases  7
1 Hyperprolactinaemia [ICD-11: 5A60.1]
2 Depression [ICD-11: 6A70-6A7Z]
3 Psychotic disorder [ICD-11: 6A20-6A25]
4 Pulmonary arterial hypertension [ICD-11: BB01.0]
5 Coronary artery disease [ICD-11: BA80]
6 Anxiety disorder [ICD-11: 6B00-6B0Z]
7 Migraine [ICD-11: 8A80]
Approved Drug(s) 3 Approved Drugs  3
1 Metergolin Approved
Hyperprolactinaemia
2 Minaprine Approved
Depression
3 Triflupromazine Approved
Psychotic disorder
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 PRX-08066 Phase 2
Pulmonary arterial hypertension
2 Vabicaserin Phase 2
Psychotic disorder
Discontinued Drug(s) 3 Discontinued Drugs  3
1 FENDILINE Withdrawn from market
Coronary artery disease
2 Ritanserin Discontinued in Phase 3
Anxiety disorder
3 MT-500 Discontinued in Phase 1
Migraine