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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
CHEMBL2096904 Serotonin (5-HT) receptor PROTEIN FAMILY
CHEMBL2111460 Dopamine D2 receptor and serotonin 1a receptor SELECTIVITY GROUP

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
CHEMBL218166 BIFEPRUNOX Serotonin 1a (5-HT1a) receptor partial agonist 3 PubMed
CHEMBL1742408 OSEMOZOTAN Serotonin 1a (5-HT1a) receptor agonist 3 PubMed
CHEMBL2103832 PARDOPRUNOX 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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