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GPCR

NameMetabotropic glutamate receptor 8
SpeciesHomo sapiens (Human)
GeneGRM8
SynonymmGluR8b
mGluR8
mGlu8 receptor
Gprc1h
glutamate receptor
[ Show all ]
DiseaseN/A
Length908
Amino acid sequenceMVCEGKRSASCPCFFLLTAKFYWILTMMQRTHSQEYAHSIRVDGDIILGGLFPVHAKGERGVPCGELKKEKGIHRLEAMLYAIDQINKDPDLLSNITLGVRILDTCSRDTYALEQSLTFVQALIEKDASDVKCANGDPPIFTKPDKISGVIGAAASSVSIMVANILRLFKIPQISYASTAPELSDNTRYDFFSRVVPPDSYQAQAMVDIVTALGWNYVSTLASEGNYGESGVEAFTQISREIGGVCIAQSQKIPREPRPGEFEKIIKRLLETPNARAVIMFANEDDIRRILEAAKKLNQSGHFLWIGSDSWGSKIAPVYQQEEIAEGAVTILPKRASIDGFDRYFRSRTLANNRRNVWFAEFWEENFGCKLGSHGKRNSHIKKCTGLERIARDSSYEQEGKVQFVIDAVYSMAYALHNMHKDLCPGYIGLCPRMSTIDGKELLGYIRAVNFNGSAGTPVTFNENGDAPGRYDIFQYQITNKSTEYKVIGHWTNQLHLKVEDMQWAHREHTHPASVCSLPCKPGERKKTVKGVPCCWHCERCEGYNYQVDELSCELCPLDQRPNMNRTGCQLIPIIKLEWHSPWAVVPVFVAILGIIATTFVIVTFVRYNDTPIVRASGRELSYVLLTGIFLCYSITFLMIAAPDTIICSFRRVFLGLGMCFSYAALLTKTNRIHRIFEQGKKSVTAPKFISPASQLVITFSLISVQLLGVFVWFVVDPPHIIIDYGEQRTLDPEKARGVLKCDISDLSLICSLGYSILLMVTCTVYAIKTRGVPETFNEAKPIGFTMYTTCIIWLAFIPIFFGTAQSAEKMYIQTTTLTVSMSLSASVSLGMLYMPKVYIIIFHPEQNVQKRKRSFKAVVTAATMQSKLIQKGNDRPNGEVKSELCESLETNTSSTKTTYISYSNHSI
UniProtO00222
Protein Data Bank6bsz, 6bt5, 6e5v
GPCR-HGmod modelN/A
3D structure modelThis structure is from PDB ID 6bsz.
BioLiPBL0432251,BL0432252, BL0403876,BL0403877, BL0403874,BL0403875
Therapeutic Target DatabaseN/A
ChEMBLCHEMBL3228
IUPHAR296
DrugBankBE0000835

Ligand

NameCHEMBL2426616
Molecular formulaC14H14N2O2S
IUPAC name5-methyl-2-(phenoxymethyl)-6,7-dihydro-[1,3]thiazolo[5,4-c]pyridin-4-one
Molecular weight274.338
Hydrogen bond acceptor4
Hydrogen bond donor0
XlogP2.3
Synonyms5-Methyl-2-(phenoxymethyl)-6,7-dihydrothiazolo[5,4-c]pyridine-4(5H)-one
ZINC72315235
BDBM50440185
SCHEMBL2011730
Inchi KeyAOOAPFRKSGWOER-UHFFFAOYSA-N
Inchi IDInChI=1S/C14H14N2O2S/c1-16-8-7-11-13(14(16)17)19-12(15-11)9-18-10-5-3-2-4-6-10/h2-6H,7-9H2,1H3
PubChem CID67246999
ChEMBLCHEMBL2426616
IUPHARN/A
BindingDB50440185
DrugBankN/A

Structure

SDF download

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

Experimental Data

ParameterValueReferenceDatabase source
EC50<10000.0 nMPMID23947773BindingDB,ChEMBL

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