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Target Report Card

Target Name and Classification

Target ID CHEMBL224
Target Type SINGLE PROTEIN
Preferred Name Serotonin 2a (5-HT2a) receptor
Synonyms 5-HT-2 | 5-HT-2A | 5-hydroxytryptamine receptor 2A | HTR2 | HTR2A | Serotonin receptor 2A
Organism Homo sapiens
Species Group No
Protein Target Classification
  • membrane receptor > family a g protein-coupled receptor > small molecule receptor (family a gpcr) > monoamine receptor > serotonin receptor

Target Components

Component Description Relationship Accession
5-hydroxytryptamine receptor 2A SINGLE PROTEIN P28223

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2096904 Serotonin (5-HT) receptor PROTEIN FAMILY
CHEMBL2111468 Dopamine D2 receptor and serotonin 2a receptor SELECTIVITY GROUP
CHEMBL2096662 Serotonin 2 receptors; 5-HT2a & 5-HT2c SELECTIVITY GROUP
CHEMBL2095200 Serotonin 2 (5-HT2) receptor PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL42 CLOZAPINE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed ISBN PubMed
CHEMBL54 HALOPERIDOL Serotonin 2a (5-HT2a) receptor antagonist 4 ISBN PubMed
CHEMBL479 THIORIDAZINE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed ISBN
CHEMBL71 CHLORPROMAZINE Serotonin 2a (5-HT2a) receptor antagonist 4 ISBN PubMed
CHEMBL85 RISPERIDONE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed FDA
CHEMBL14376 ILOPERIDONE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed
CHEMBL654 MIRTAZAPINE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed
CHEMBL715 OLANZAPINE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed FDA
CHEMBL831 LOXAPINE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed FDA
CHEMBL908 CHLORPROTHIXENE Serotonin 2a (5-HT2a) receptor antagonist 4 PubMed PubMed
CHEMBL1108 DROPERIDOL Serotonin 2a (5-HT2a) receptor antagonist 4 ISBN PubMed
CHEMBL1112 ARIPIPRAZOLE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed
CHEMBL1201 THIOTHIXENE Serotonin 2a (5-HT2a) receptor antagonist 4 PubMed PubMed
CHEMBL1423 PIMOZIDE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed ISBN
CHEMBL1621 PALIPERIDONE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed
CHEMBL1710 TRIFLUOPERAZINE HYDROCHLORIDE Serotonin 2a (5-HT2a) receptor antagonist 4 ISBN
CHEMBL1712 ZIPRASIDONE HYDROCHLORIDE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed
CHEMBL1713 CHLORPROMAZINE HYDROCHLORIDE Serotonin 2a (5-HT2a) receptor antagonist 4 ISBN PubMed
CHEMBL1200419 MOLINDONE HYDROCHLORIDE Serotonin 2a (5-HT2a) receptor antagonist 4 PubMed
CHEMBL1200469 PROMAZINE HYDROCHLORIDE Serotonin 2a (5-HT2a) receptor antagonist 4 ISBN ISBN
CHEMBL1200492 NEFAZODONE HYDROCHLORIDE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed
CHEMBL1200636 CYCLOBENZAPRINE HYDROCHLORIDE Serotonin 2a (5-HT2a) receptor antagonist 4 PubMed PubMed
CHEMBL1200798 TRAZODONE HYDROCHLORIDE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed FDA
CHEMBL1200902 THIOTHIXENE HYDROCHLORIDE Serotonin 2a (5-HT2a) receptor antagonist 4 PubMed PubMed
CHEMBL1200911 QUETIAPINE FUMARATE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed
CHEMBL1200916 THIORIDAZINE HYDROCHLORIDE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed ISBN
CHEMBL1200948 TRIMIPRAMINE MALEATE Serotonin 2a (5-HT2a) receptor antagonist 4 ISBN PubMed
CHEMBL1200986 HALOPERIDOL DECANOATE Serotonin 2a (5-HT2a) receptor antagonist 4 ISBN PubMed
CHEMBL1200997 ZIPRASIDONE MESYLATE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed
CHEMBL1201052 MESORIDAZINE BESYLATE Serotonin 2a (5-HT2a) receptor antagonist 4 PubMed PubMed
CHEMBL1201060 LOXAPINE HYDROCHLORIDE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed FDA
CHEMBL1201155 LOXAPINE SUCCINATE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed FDA
CHEMBL1201732 PALIPERIDONE PALMITATE Serotonin 2a (5-HT2a) receptor antagonist 4 FDA
CHEMBL1201741 OLANZAPINE PAMOATE Serotonin 2a (5-HT2a) receptor antagonist 4 FDA
CHEMBL1615372 LURASIDONE HYDROCHLORIDE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed
CHEMBL2096643 HALOPERIDOL LACTATE Serotonin 2a (5-HT2a) receptor antagonist 4 ISBN PubMed
CHEMBL2105760 BREXPIPRAZOLE Serotonin 2a (5-HT2a) receptor antagonist 4 FDA
CHEMBL2219425 ARIPIPRAZOLE LAUROXIL Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed
CHEMBL2358147 CARPHENAZINE MALEATE Serotonin 2a (5-HT2a) receptor antagonist 4 ISBN PubMed
CHEMBL2448613 PIMAVANSERIN TARTRATE Serotonin 2a (5-HT2a) receptor inverse agonist 4 FDA Other PubMed PubMed
CHEMBL3544974 ASENAPINE MALEATE Serotonin 2a (5-HT2a) receptor antagonist 4 DailyMed
CHEMBL74355 VOLINANSERIN Serotonin 2a (5-HT2a) receptor antagonist 3 PubMed
CHEMBL2107339 ESMIRTAZAPINE MALEATE Serotonin 2a (5-HT2a) receptor antagonist 3 PubMed PubMed
CHEMBL2107754 IFERANSERIN Serotonin 2a (5-HT2a) receptor antagonist 3 Other PubMed
CHEMBL3545044 ITI-007 Serotonin 2a (5-HT2a) receptor antagonist 3 Other PubMed PubMed
CHEMBL598172 NELOTANSERIN Serotonin 2a (5-HT2a) receptor inverse agonist 2 PubMed
CHEMBL1215661 PRUVANSERIN Serotonin 2a (5-HT2a) receptor antagonist 2 PubMed
CHEMBL2104986 TEDATIOXETINE Serotonin 2a (5-HT2a) receptor antagonist 2 Other Other
CHEMBL2104991 VABICASERIN HYDROCHLORIDE Serotonin 2a (5-HT2a) receptor antagonist 2 PubMed
CHEMBL3183740 Trelanserin Serotonin 2a (5-HT2a) receptor antagonist 2 PubMed PubMed
CHEMBL3545102 SB-773812 Serotonin 2a (5-HT2a) receptor antagonist 2 PubMed
CHEMBL1084617 TEMANOGREL Serotonin 2a (5-HT2a) receptor inverse agonist 1 PubMed
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000102468
Ensembl ENSG00000102468
GO Cellular Component GO:0005737 (cytoplasm)
GO:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0005901 (caveola)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0016023 (cytoplasmic, membrane-bounded vesicle)
GO:0030424 (axon)
GO:0030425 (dendrite)
GO:0031410 (cytoplasmic vesicle)
GO:0042995 (cell projection)
GO:0043025 (neuronal cell body)
GO:0043198 (dendritic shaft)
GO:0070852 (cell body fiber)
GO Molecular Function GO:0001618 (virus receptor activity)
GO:0001965 (G-protein alpha-subunit binding)
GO:0004871 (signal transducer activity)
GO:0004930 (G-protein coupled receptor activity)
GO:0004993 (G-protein coupled serotonin receptor activity)
GO:0008144 (drug binding)
GO:0032403 (protein complex binding)
GO:0051378 (serotonin binding)
GO:0071886 (1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding)
GO Biological Process GO:0001659 (temperature homeostasis)
GO:0006874 (cellular calcium ion homeostasis)
GO:0006939 (smooth muscle contraction)
GO:0007165 (signal transduction)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007202 (activation of phospholipase C activity)
GO:0007204 (positive regulation of cytosolic calcium ion concentration)
GO:0007208 (phospholipase C-activating serotonin receptor signaling pathway)
GO:0007210 (serotonin receptor signaling pathway)
GO:0007268 (chemical synaptic transmission)
GO:0007568 (aging)
GO:0007610 (behavior)
GO:0007613 (memory)
GO:0008219 (cell death)
GO:0008284 (positive regulation of cell proliferation)
GO:0010513 (positive regulation of phosphatidylinositol biosynthetic process)
GO:0014059 (regulation of dopamine secretion)
GO:0014065 (phosphatidylinositol 3-kinase signaling)
GO:0014824 (artery smooth muscle contraction)
GO:0014832 (urinary bladder smooth muscle contraction)
GO:0016032 (viral process)
GO:0019233 (sensory perception of pain)
GO:0030431 (sleep)
GO:0033674 (positive regulation of kinase activity)
GO:0042493 (response to drug)
GO:0043267 (negative regulation of potassium ion transport)
GO:0043406 (positive regulation of MAP kinase activity)
GO:0044380 (protein localization to cytoskeleton)
GO:0045600 (positive regulation of fat cell differentiation)
GO:0045821 (positive regulation of glycolytic process)
GO:0045907 (positive regulation of vasoconstriction)
GO:0046718 (viral entry into host cell)
GO:0046883 (regulation of hormone secretion)
GO:0048148 (behavioral response to cocaine)
GO:0050731 (positive regulation of peptidyl-tyrosine phosphorylation)
GO:0050795 (regulation of behavior)
GO:0050965 (detection of temperature stimulus involved in sensory perception of pain)
GO:0050966 (detection of mechanical stimulus involved in sensory perception of pain)
GO:0051209 (release of sequestered calcium ion into cytosol)
GO:0051967 (negative regulation of synaptic transmission, glutamatergic)
GO:0070374 (positive regulation of ERK1 and ERK2 cascade)
Wikipedia 5-HT2A_receptor

Target Cross References - Protein

canSAR P28223
CGD Major depressive disorder, response to citalopram therapy in; Clozapine, response to
Human Protein Atlas ENSG00000102468
Guide to Pharmacology 6
MICAD NBK23366 (5-HT2A serotonin receptors)
Open Targets ENSG00000102468
PharmGKB PA193
Pharos P28223 (Tclin)
Reactome R-HSA-390666 (Serotonin receptors.)
R-HSA-416476 (G alpha (q) signalling events.)
UniProt B2RAC5 B4DZ79 F5GWE8 P28223 Q5T8C0

Target Cross References - Domain

InterPro IPR000276 (GPCR_Rhodpsn.)
IPR000455 (5HT2A_rcpt.)
IPR002231 (5HT_rcpt.)
IPR017452 (GPCR_Rhodpsn_7TM.)
Pfam PF00001 (7tm_1)
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