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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

NameCHEMBL319279
Molecular formulaC28H27NO5
IUPAC name(1S,2S,3S)-2-[1-amino-1-carboxy-2-(9H-xanthen-9-yl)ethyl]-3-(2-phenylethyl)cyclopropane-1-carboxylic acid
Molecular weight457.526
Hydrogen bond acceptor6
Hydrogen bond donor3
XlogP2.1
SynonymsBDBM50072176
(1S,2S,3S)-2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-3-phenethyl-cyclopropanecarboxylic acid
Inchi KeyBCMKQOREHHIJIN-KOUVAXTNSA-N
Inchi IDInChI=1S/C28H27NO5/c29-28(27(32)33,25-20(24(25)26(30)31)15-14-17-8-2-1-3-9-17)16-21-18-10-4-6-12-22(18)34-23-13-7-5-11-19(21)23/h1-13,20-21,24-25H,14-16,29H2,(H,30,31)(H,32,33)/t20-,24+,25+,28?/m1/s1
PubChem CID10456810
ChEMBLCHEMBL319279
IUPHARN/A
BindingDB50072176
DrugBankN/A

Structure

SDF download

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

Experimental Data

ParameterValueReferenceDatabase source
IC50990.0 nMPMID9873635BindingDB,ChEMBL

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