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ChEMBL Statistics
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Target Report Card

Target Name and Classification

Target ID CHEMBL214
Target Type SINGLE PROTEIN
Preferred Name Serotonin 1a (5-HT1a) receptor
Synonyms 5-HT-1A | 5-HT1A | 5-hydroxytryptamine receptor 1A | ADRB2RL1 | ADRBRL1 | G-21 | HTR1A | Serotonin receptor 1A
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 1A SINGLE PROTEIN P08908

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2111460 Dopamine D2 receptor and serotonin 1a receptor SELECTIVITY GROUP
CHEMBL2096904 Serotonin (5-HT) receptor PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1112 ARIPIPRAZOLE Serotonin 1a (5-HT1a) receptor partial agonist 4 DailyMed
CHEMBL1200399 BUSPIRONE HYDROCHLORIDE Serotonin 1a (5-HT1a) receptor partial agonist 4 FDA
CHEMBL1200938 METHYSERGIDE MALEATE Serotonin 1a (5-HT1a) receptor partial agonist 4 ISBN PubMed
CHEMBL1615374 VILAZODONE HYDROCHLORIDE Serotonin 1a (5-HT1a) receptor partial agonist 4 FDA PubMed
CHEMBL2105760 BREXPIPRAZOLE Serotonin 1a (5-HT1a) receptor partial agonist 4 FDA
CHEMBL2107387 VORTIOXETINE HYDROBROMIDE Serotonin 1a (5-HT1a) receptor agonist 4 DailyMed PubMed
CHEMBL2219425 ARIPIPRAZOLE LAUROXIL Serotonin 1a (5-HT1a) receptor partial agonist 4 DailyMed
CHEMBL2311030 ERGOLOID MESYLATES Serotonin 1a (5-HT1a) receptor agonist 4 ISBN PubMed
CHEMBL209821 NALUZOTAN Serotonin 1a (5-HT1a) receptor agonist 3 PubMed
CHEMBL1742408 OSEMOZOTAN Serotonin 1a (5-HT1a) receptor agonist 3 PubMed
CHEMBL2107349 LECOZOTAN HYDROCHLORIDE Serotonin 1a (5-HT1a) receptor antagonist 3 PubMed
CHEMBL2146110 SARIZOTAN HYDROCHLORIDE Serotonin 1a (5-HT1a) receptor agonist 3 PubMed PubMed
CHEMBL45305 BEFIRADOL Serotonin 1a (5-HT1a) receptor agonist 2 PubMed
CHEMBL345237 PICLOZOTAN Serotonin 1a (5-HT1a) receptor agonist 2 PubMed PubMed
CHEMBL1628569 ROBALZOTAN Serotonin 1a (5-HT1a) receptor antagonist 2 PubMed PubMed
CHEMBL1631540 GSK163090 Serotonin 1a (5-HT1a) receptor antagonist 2 PubMed
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000178394
Ensembl ENSG00000178394
GO Cellular Component GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO Molecular Function GO:0004871 (signal transducer activity)
GO:0004930 (G-protein coupled receptor activity)
GO:0004993 (G-protein coupled serotonin receptor activity)
GO:0005515 (protein binding)
GO Biological Process GO:0001662 (behavioral fear response)
GO:0007165 (signal transduction)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007198 (adenylate cyclase-inhibiting serotonin receptor signaling pathway)
GO:0007210 (serotonin receptor signaling pathway)
GO:0007610 (behavior)
GO:0008283 (cell proliferation)
GO:0008284 (positive regulation of cell proliferation)
GO:0014062 (regulation of serotonin secretion)
GO:0035640 (exploration behavior)
GO:0042053 (regulation of dopamine metabolic process)
GO:0042310 (vasoconstriction)
GO:0042428 (serotonin metabolic process)
GO:0046883 (regulation of hormone secretion)
GO:0050795 (regulation of behavior)
Wikipedia 5-HT1A_receptor

Target Cross References - Protein

canSAR P08908
CGD Periodic fever, menstrual cycle dependent
Human Protein Atlas ENSG00000178394
IntAct P08908
Guide to Pharmacology 1
MICAD NBK23137 (5-HT1A receptors)
NBK23250 (5-HT1A serotonin receptors)
NBK23263 (5-HT1A receptors)
NBK23391 (5-HT1A receptors)
Open Targets ENSG00000178394
PharmGKB PA192
Pharos P08908 (Tclin)
Reactome R-HSA-390666 (Serotonin receptors.)
R-HSA-418594 (G alpha (i) signalling events.)
UniProt P08908 Q6LAE7

Target Cross References - Domain

InterPro IPR000276 (GPCR_Rhodpsn.)
IPR000610 (5HT1A_rcpt.)
IPR002231 (5HT_rcpt.)
IPR017452 (GPCR_Rhodpsn_7TM.)
Pfam PF00001 (7tm_1)
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