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Approval Year

Unknown
149124
Substance Class Protein
Created
by admin
on Tue Apr 01 16:58:36 GMT 2025
Edited
by admin
on Tue Apr 01 16:58:36 GMT 2025
Protein Sub Type
Sequence Type COMPLETE
Record UNII
NQI5D806LC
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
5-HT-2
Preferred Name English
5-HYDROXYTRYPTAMINE RECEPTOR 2A
Common Name English
5-HT2A
Common Name English
HTR2
Common Name English
SEROTONIN RECEPTOR 2A
Common Name English
5-HT2A RECEPTOR
Common Name English
5HT2A
Common Name English
Code System Code Type Description
UNIPROT
P28223
Created by admin on Tue Apr 01 16:58:36 GMT 2025 , Edited by admin on Tue Apr 01 16:58:36 GMT 2025
PRIMARY
FDA UNII
NQI5D806LC
Created by admin on Tue Apr 01 16:58:36 GMT 2025 , Edited by admin on Tue Apr 01 16:58:36 GMT 2025
PRIMARY
PHAROS
P28223
Created by admin on Tue Apr 01 16:58:36 GMT 2025 , Edited by admin on Tue Apr 01 16:58:36 GMT 2025
PRIMARY
From To
1_148 1_227
1_349 1_353
Glycosylation Type HUMAN
Glycosylation Link Type Site
N 1_8
N 1_38
N 1_44
N 1_51
N 1_54
Related Record Type Details
Structure of 1-METHYLPSILOCIN
WEAK AGONIST->TARGET
IC50
Structure of 4,5-DHP-DMT
AGONIST -> TARGET
Moderate selectivity over related serotonin receptors. It has lower 5-HT2 affinity and efficacy than the related compound AL-37350A, but higher lipophilicity.
Ki
Structure of TEMANOGREL
INVERSE AGONIST->TARGET
Structure of PSILOCIN
AGONIST -> TARGET
Structure of CISAPRIDE
AGONIST -> TARGET
Structure of ISOPROSCALINE
AGONIST -> TARGET
Structure of AL-37350A
AGONIST -> TARGET
Structure of ESMIRTAZAPINE
INHIBITOR -> TARGET
Structure of CLOMIPRAMINE
INHIBITOR -> TARGET
Structure of CYANODOTHIEPIN
LIGAND->TARGET
Structure of PALIPERIDONE
INHIBITOR -> TARGET
INHIBITOR
Ki
Structure of LISURIDE
AGONIST -> TARGET
Structure of WAY-161503
AGONIST -> TARGET
Structure of 6-(2-(4-(BENZO(D)ISOTHIAZOL-3-YL)PIPERAZIN-1-YL)ETHYL)-4,4,8-TRIMETHYL-3,4-DIHYDRO-1H-QUINOLIN-2-ONE
INHIBITOR -> TARGET
Structure of FANANSERIN
INHIBITOR -> TARGET
Ki
Structure of CINITAPRIDE
INHIBITOR -> TARGET
Structure of ROLUPERIDONE
INHIBITOR -> TARGET
Structure of LANDIPIRDINE
INHIBITOR -> TARGET
Structure of RUZADOLANE
INHIBITOR -> TARGET
Structure of ILOPERIDONE
INHIBITOR -> TARGET
MAJOR
Ki
Structure of 5-METHOXY-N,N-DIETHYLTRYPTAMINE
AGONIST -> TARGET
EC50
Structure of N-ALLYLNORLYSERGIC ACID N,N-DIETHYLAMIDE
AGONIST -> TARGET
Structure of PIMAVANSERIN
INVERSE AGONIST->TARGET
Structure of O-4310
AGONIST -> TARGET
EC50
Structure of N-METHYLKETANSERIN, (N-METHYL C-11)-
RADIOLIGAND->TARGET
Structure of BETA-D
AGONIST -> TARGET
Structure of PNU-181731
AGONIST -> TARGET
Structure of Norquetiapine
INHIBITOR -> TARGET
Ki
Structure of KETANSERIN H-3
RADIOLIGAND->TARGET
Structure of LUCIGENOL
AGONIST -> TARGET
Structure of RITANSERIN
INHIBITOR -> TARGET
Ki
Structure of TRELANSERIN
INHIBITOR -> TARGET
Structure of 25CN-NBMD
AGONIST -> TARGET
Ki
Structure of SERTINDOLE
INHIBITOR -> TARGET
Structure of ESAMISULPRIDE
INHIBITOR -> TARGET
Structure of MIRTAZAPINE
INHIBITOR -> TARGET
Structure of AL-34662
AGONIST -> TARGET
Designed specifically as a peripherally selective drug, which does not cross the blood–brain barrier. AL-34662 has been shown to be potent and effective in the treatment of symptoms of glaucoma, with minimal side effects.
FLUPENTIXOL
INHIBITOR -> TARGET
Structure of DMBMPP
AGONIST -> TARGET
Structure of SB-773812
INHIBITOR -> TARGET
Structure of ZICRONAPINE
INHIBITOR -> TARGET
Structure of Dimethyltryptamine
AGONIST -> TARGET
all of the tryptamines, including DMT but with the exception of psilocin, were more potent agonists at the 5-HT2A receptor than LSD in the assay that was used in the present study. LSD and psilocin were 5-HT2A receptor partial agonists, with 28% and 16% activation efficacy, respectively, whereas all of the other compounds presented higher 5-HT2A receptor activation efficacies (up to >80% for DiPT and 5-MeO-MiPT). DMT has 40 maximal receptor activation.
EC50
5-HYDROXYTRYPTAMINE RECEPTOR 2A
AGONIST -> TARGET
Ki
Structure of 5-METHOXY-N,N-DIISOPROPYLTRYPTAMINE
AGONIST -> TARGET
Structure of DERAMCICLANE
ANTAGONIST->TARGET
Structure of AL-38022A
AGONIST -> TARGET
Structure of NBOME-MESCALINE
PARTIAL AGONIST->TARGET
Structure of DESIPRAMINE
INHIBITOR -> TARGET
Structure of ALTANSERIN F-18
RADIOLIGAND->TARGET
Structure of GLEMANSERIN
INHIBITOR -> TARGET
Structure of PEROSPIRONE
INHIBITOR -> TARGET
Structure of DOTARIZINE
INHIBITOR -> TARGET
Structure of 5-MEO-AMT
AGONIST -> TARGET
Ki
Structure of CPD-1
AGONIST -> TARGET
Structure of LYSERGIDE
AGONIST -> TARGET
[125I]DOI was the radioligand.
Ki
Structure of CIMBI-36_5 C-11
RADIOLIGAND->TARGET
Structure of OSU-6162
PARTIAL AGONIST->TARGET
Structure of NIAPRAZINE
INHIBITOR -> TARGET
Ki
DOXEPIN
INHIBITOR -> TARGET
Structure of 5-MEO-MPMI
AGONIST -> TARGET
Ki
Structure of IPROCIN
AGONIST -> TARGET
BINDING
Ki
Structure of SETOPERONE F-18
RADIOLIGAND->TARGET
Structure of LORCASERIN
AGONIST->OFF-TARGET
Ki
Structure of Brilaroxazine
PARTIAL AGONIST->TARGET
Structure of 1B-LSD
PARTIAL AGONIST->TARGET
Emax=23%
Structure of MIN-117 FREE BASE
INHIBITOR -> TARGET
Structure of CYPROHEPTADINE
INHIBITOR -> TARGET
Structure of 25CN-NBOME
AGONIST -> TARGET
Structure of 25CN-NBOH
PARTIAL AGONIST->TARGET
BINDING
Ki
Structure of TCB-2
AGONIST -> TARGET
Ki
Structure of Deupsilocin
INHIBITOR -> TARGET
PRECLINICAL
IC50
Structure of 2C-T-7
AGONIST -> TARGET
Structure of PHA-57378 Free Base
AGONIST -> TARGET
Structure of 25TFM-NBOME
PARTIAL AGONIST->TARGET
Structure of ARAMISULPRIDE
INHIBITOR -> TARGET
Structure of CARIPRAZINE
WEAK INHIBITOR->TARGET
Ki
Structure of BUTRIPTYLINE
INHIBITOR -> TARGET
Structure of ALD-52
PARTIAL AGONIST->TARGET
Emax=25%
EC50
Structure of DOI I-125
RADIOLIGAND->TARGET
Kd
Structure of LSD-PIP
AGONIST -> TARGET
Structure of NORCLOZAPINE
INHIBITOR -> TARGET
Ki
Structure of SARPOGRELATE
INHIBITOR -> TARGET
Structure of LIDANSERIN
INHIBITOR -> TARGET
Structure of 1-PROPIONYL-LYSERGIC ACID DIETHYLAMIDE
PARTIAL AGONIST->TARGET
Emax=11%
EC50
Structure of BROLAMFETAMINE
AGONIST -> TARGET
Structure of RISPERIDONE
INHIBITOR -> TARGET
INHIBITOR
Ki
Structure of 5-FLUORO-AMT
AGONIST -> TARGET
Could be an active psychedelic in humans, although it is not known to have been tested in humans and could be dangerous due to its strong inhibition of MAO-A.
Structure of ARIPIPRAZOLE
INHIBITOR -> TARGET
Structure of MBL C-11
RADIOLIGAND->TARGET
Ki
Structure of MESPIPERONE C-11
RADIOLIGAND->TARGET
Ki
Structure of TERGURIDE
PARTIAL AGONIST->TARGET
Structure of NELOTANSERIN
INVERSE AGONIST->TARGET
Was under development for the treatment of insomnia. Development was halted in December 2008 because the substance did not meet the trial's effectiveness endpoints.recently, nelotanserin has been repurposed for the treatment of Lewy body disease.
Structure of MINAPRINE
INHIBITOR -> TARGET
Structure of Mebufotenin
WEAK AGONIST->TARGET
Ki
Structure of CIMBI-36 C-11
RADIOLIGAND->TARGET
Structure of N,N-DIETHYLTRYPTAMINE
WEAK AGONIST->TARGET
Hallucinogenic, 31% of the stimulation of 5-hydroxytryptamine. Stimulation of phosphoinositide hydrolysis.
EC50
Structure of CLOZAPINE
INHIBITOR -> TARGET
IC50
Structure of QUETIAPINE
INHIBITOR -> TARGET
Ki
Structure of NORCISAPRIDE
AGONIST -> TARGET
Structure of LOXAPINE
INHIBITOR -> TARGET
Structure of BLONANSERIN
INHIBITOR -> TARGET
Structure of M-CHLOROPHENYLPIPERAZINE
PARTIAL AGONIST->TARGET
Ki
Structure of 4-MEO-MIPT
AGONIST -> TARGET
Assumed target
Structure of MEPHEDRONE
INHIBITOR -> TARGET
Structure of Dimethyltryptamine
PARTIAL AGONIST->TARGET
Ki
Structure of DOI
DOI
INHIBITOR -> TARGET
BINDING
IC50
Structure of ADATANSERIN
INHIBITOR -> TARGET
Structure of CHLORPROTHIXENE
INHIBITOR -> TARGET
Structure of Olanzapine
INHIBITOR -> TARGET
Structure of LY-2624803
INHIBITOR -> TARGET
Structure of Serotonin
AGONIST -> TARGET
Natural agonist
BINDING
IC50
Structure of 7,N,N-TRIMETHYLTRYPTAMINE
AGONIST -> TARGET
Structure of METHYSERGIDE
INHIBITOR -> TARGET
Structure of 6-FLUORO-DMT
AGONIST -> TARGET
Structure of EPLIVANSERIN
INVERSE AGONIST->TARGET
Experimental drug for the treatment of insomnia.
Structure of 2-BROMOMESCALINE
AGONIST -> TARGET
Structure of Remlifanserin
INHIBITOR -> TARGET
5-HT2A receptor inverse agonists/antagonists
Structure of PIZOTYLINE
INHIBITOR -> TARGET
Structure of DEUTEROALTANSERIN F-18
RADIOLIGAND->TARGET
Structure of ITI-333
INHIBITOR -> TARGET
Structure of 25C-NBOME HYDROCHLORIDE
AGONIST -> TARGET
Structure of BREXPIPRAZOLE
INHIBITOR -> TARGET
Structure of 5-MEO-NBPBRT
INHIBITOR -> TARGET
ANTAGONIST
Structure of BROMPERIDOL
INHIBITOR -> TARGET
Ki
Structure of N-METHYL-N-ALLYLTRYPTAMINE
AGONIST -> TARGET
May be an agonist
Structure of KETANSERIN
INHIBITOR -> TARGET
BINDING
IC50
Structure of R-93274
INHIBITOR -> TARGET
Structure of OCAPERIDONE
INHIBITOR -> TARGET
Structure of LY-367265
INHIBITOR -> TARGET
Ki
Structure of MESCALINE
AGONIST -> TARGET
Ki
Structure of Lumateperone
ANTAGONIST->TARGET
BINDING
Ki
Structure of CIMBI-36
AGONIST -> TARGET
Structure of CHLORPROMAZINE
INHIBITOR -> TARGET
Structure of PYR-T
NON-AGONIST->OFF-TARGET
Pyr-T produces few to no effects in humans, but some behavioral changes were observed in animal tests.
Structure of BELOXEPIN
INHIBITOR -> TARGET
Structure of BUFOTENINE
AGONIST -> TARGET
Structure of MESULERGINE
INHIBITOR -> TARGET
BINDING
IC50
Structure of DOET
PARTIAL AGONIST->TARGET
Structure of 4-HYDROXY-N-METHYL-N-ETHYLTRYPTAMINE
AGONIST -> TARGET
Structure of FLIBANSERIN
INHIBITOR -> TARGET
Structure of LORCASERIN
WEAK AGONIST->OFF TARGET
EC50
Structure of KML-010
INHIBITOR -> TARGET
Structure of ERGOTAMINE
AGONIST -> TARGET
Structure of 2,5-Dimethoxy-4-trifluoromethylamphetamine
AGONIST -> TARGET
Structure of LUBAZODONE
INHIBITOR -> TARGET
Structure of MMDA
AGONIST -> TARGET
Structure of 25I-NB34MD
PARTIAL AGONIST->TARGET
Structure of 25B-NBOH
AGONIST -> TARGET
Structure of Lurasidone
INHIBITOR -> TARGET
cell:CHO; ligand: 3-H-KETASERIN
BINDING
Ki
Structure of DOI
DOI
PARTIAL AGONIST->TARGET
Structure of MT-1207
INHIBITOR -> TARGET
Structure of 1-[(1S,2S)-2-(5-Fluoro-2-propoxyphenyl)cyclopropyl]methanamine
AGONIST -> TARGET
Structure of MESORIDAZINE
INHIBITOR -> TARGET
Structure of ASENAPINE
INHIBITOR -> TARGET
Ki
Structure of VOLINANSERIN C-11
INHIBITOR -> TARGET
Kd
Structure of NORTRIPTYLINE
INHIBITOR -> TARGET
Structure of PNU-22394
PARTIAL AGONIST->TARGET
Structure of TFMFLY
AGONIST -> TARGET
Structure of ACEPROMAZINE
INHIBITOR -> TARGET
Structure of 3-METHOXY-4-METHYLAMPHETAMINE
AGONIST -> TARGET
Structure of 25B-NBF
PARTIAL AGONIST->TARGET
Ki
Structure of PRUVANSERIN
INHIBITOR -> TARGET
Structure of FLUPERLAPINE
INHIBITOR -> TARGET
Ki
Structure of 1-(3-Chlorophenyl)-4-(2-phenylethyl)piperazine
LIGAND->TARGET
Structure of ICI-170809 FREE BASE
INHIBITOR -> TARGET
Structure of ZUCLOPENTHIXOL
INHIBITOR -> TARGET
Structure of 4-HO-DSBT
AGONIST -> TARGET
Retains reasonable potency, with a similar 5-HT2A receptor affinity to MiPT but better selectivity over the 5-HT1A and 5-HT2B subtypes.
Structure of ZIPRASIDONE
INHIBITOR -> TARGET
Structure of ABAPERIDONE
INHIBITOR -> TARGET
Structure of Bretisilocin
AGONIST -> TARGET
Structure of CYCLOBENZAPRINE
INHIBITOR -> TARGET
Structure of Amitriptyline
INHIBITOR -> TARGET
Structure of R-93274 I-123
RADIOLIGAND->TARGET
Structure of IFERANSERIN
INHIBITOR -> TARGET
Structure of VOLINANSERIN
INHIBITOR -> TARGET
Kd

Structural Modifications

Modification Type Location Site Location Type Residue Modified Extent Fragment Name Fragment Approval
AMINO ACID SUBSTITUTION [1_280] DEXFOSFOSERINE VI4F0K069V
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT CHEMICAL
Molecular Formula CHEMICAL
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