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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

NameL-AP4
Molecular formulaC4H10NO5P
IUPAC name(2S)-2-amino-4-phosphonobutanoic acid
Molecular weight183.1
Hydrogen bond acceptor6
Hydrogen bond donor4
XlogP-5.5
SynonymsJ-014961
L-2-amino-4-phosphonobutiric acid
NCGC00013365
NSC-30079
[3H]AP4
[ Show all ]
Inchi KeyDDOQBQRIEWHWBT-VKHMYHEASA-N
Inchi IDInChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m0/s1
PubChem CID179394
ChEMBLCHEMBL33567
IUPHAR1410, 1412
BindingDB50007548
DrugBankN/A

Structure

SDF download

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

Experimental Data

ParameterValueReferenceDatabase source
EC50560.0 nMPMID17602546BindingDB,ChEMBL
IC5063.0957 - 100.0 nMPMID10216218IUPHAR
Kd199.526 - 251.189 nMPMID10216218IUPHAR
Ki61.0 nMPMID10893301BindingDB,ChEMBL

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