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GPCR

Name5-hydroxytryptamine receptor 2A
SpeciesRattus norvegicus (Rat)
GeneHtr2a
Synonymserotonin 5HT-2 receptor
5Ht-2
'D' receptor
5-hydroxytryptamine (serotonin) receptor 2A, G protein-coupled
5-HT2A receptor
[ Show all ]
DiseaseN/A for non-human GPCRs
Length471
Amino acid sequenceMEILCEDNISLSSIPNSLMQLGDGPRLYHNDFNSRDANTSEASNWTIDAENRTNLSCEGYLPPTCLSILHLQEKNWSALLTTVVIILTIAGNILVIMAVSLEKKLQNATNYFLMSLAIADMLLGFLVMPVSMLTILYGYRWPLPSKLCAIWIYLDVLFSTASIMHLCAISLDRYVAIQNPIHHSRFNSRTKAFLKIIAVWTISVGISMPIPVFGLQDDSKVFKEGSCLLADDNFVLIGSFVAFFIPLTIMVITYFLTIKSLQKEATLCVSDLSTRAKLASFSFLPQSSLSSEKLFQRSIHREPGSYAGRRTMQSISNEQKACKVLGIVFFLFVVMWCPFFITNIMAVICKESCNENVIGALLNVFVWIGYLSSAVNPLVYTLFNKTYRSAFSRYIQCQYKENRKPLQLILVNTIPALAYKSSQLQVGQKKNSQEDAEQTVDDCSMVTLGKQQSEENCTDNIETVNEKVSCV
UniProtP14842
Protein Data BankN/A
GPCR-HGmod modelN/A
3D structure modelNo available structures or models
BioLiPN/A
Therapeutic Target DatabaseN/A
ChEMBLCHEMBL322
IUPHAR6
DrugBankN/A

Ligand

Nameserotonin
Molecular formulaC10H12N2O
IUPAC name3-(2-aminoethyl)-1H-indol-5-ol
Molecular weight176.219
Hydrogen bond acceptor2
Hydrogen bond donor3
XlogP0.2
SynonymsKBio2_005040
5-Hydroxy-3-(beta-aminoethyl)indole
KBioSS_000452
50-67-9
NCGC00015525-01
[ Show all ]
Inchi KeyQZAYGJVTTNCVMB-UHFFFAOYSA-N
Inchi IDInChI=1S/C10H12N2O/c11-4-3-7-6-12-10-2-1-8(13)5-9(7)10/h1-2,5-6,12-13H,3-4,11H2
PubChem CID5202
ChEMBLCHEMBL39
IUPHAR5
BindingDB10755
DrugBankDB08839

Structure

SDF download

2D structure
Lipinski's druglikenessThis ligand satisfies Lipinski's rule of five.

Experimental Data

ParameterValueReferenceDatabase source
Activity52.0 %PMID23792350ChEMBL
EC5055.8 nMPMID12954071BindingDB,ChEMBL
EC5057.9 nMPMID16392816ChEMBL
EC5058.0 nMPMID16392816BindingDB
EC50351.0 nMPMID12954071BindingDB,ChEMBL
Emax99.0 %PMID16392816ChEMBL
IC500.9 nMPMID12954071BindingDB,ChEMBL
IC500.94 nMPMID16392816ChEMBL
IC500.94 nMPMID16392816BindingDB
IC50600.0 nMPMID23792350ChEMBL
IC502350.0 nMPMID9357534BindingDB,ChEMBL
IC5013000.0 nMPMID23792350ChEMBL
IC5030600.0 nMPMID23792350ChEMBL
Ki0.3 nMPMID12954071BindingDB,ChEMBL
Ki1.99 nMPMID7984267BindingDB
Ki3.0 nMPMID2795135BindingDB
Ki5.75 nMPMID7984267BindingDB
Ki83.0 nMPMID6645787BindingDB
Ki96.0 nMPMID9686407BindingDB
Ki120.22 nMPMID9225287BindingDB
Ki125.89 nMPMID7582481BindingDB
Ki251.18 nMPMID7984267BindingDB
Ki270.0 nMPMID6645787BindingDB
Ki316.228 - 1000.0 nMPMID11040033, PMID11104741, PMID9655845IUPHAR
Ki478.63 nMPMID7984267BindingDB
Ki707.94 nMPMID7984267BindingDB
Ki1258.0 nMPMID19425598, PMID19831400BindingDB,ChEMBL
Ki1258.93 nMPMID10543880ChEMBL
Ki2955.0 nMPMID8510008BindingDB

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