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GPCR

NameMetabotropic glutamate receptor 4
SpeciesHomo sapiens (Human)
GeneGRM4
SynonymmGluR4
mGlu4 receptor
GPRC1D
glutamate receptor
DiseaseAnxiety disorder
Neurological disease
Length912
Amino acid sequenceMPGKRGLGWWWARLPLCLLLSLYGPWMPSSLGKPKGHPHMNSIRIDGDITLGGLFPVHGRGSEGKPCGELKKEKGIHRLEAMLFALDRINNDPDLLPNITLGARILDTCSRDTHALEQSLTFVQALIEKDGTEVRCGSGGPPIITKPERVVGVIGASGSSVSIMVANILRLFKIPQISYASTAPDLSDNSRYDFFSRVVPSDTYQAQAMVDIVRALKWNYVSTVASEGSYGESGVEAFIQKSREDGGVCIAQSVKIPREPKAGEFDKIIRRLLETSNARAVIIFANEDDIRRVLEAARRANQTGHFFWMGSDSWGSKIAPVLHLEEVAEGAVTILPKRMSVRGFDRYFSSRTLDNNRRNIWFAEFWEDNFHCKLSRHALKKGSHVKKCTNRERIGQDSAYEQEGKVQFVIDAVYAMGHALHAMHRDLCPGRVGLCPRMDPVDGTQLLKYIRNVNFSGIAGNPVTFNENGDAPGRYDIYQYQLRNDSAEYKVIGSWTDHLHLRIERMHWPGSGQQLPRSICSLPCQPGERKKTVKGMPCCWHCEPCTGYQYQVDRYTCKTCPYDMRPTENRTGCRPIPIIKLEWGSPWAVLPLFLAVVGIAATLFVVITFVRYNDTPIVKASGRELSYVLLAGIFLCYATTFLMIAEPDLGTCSLRRIFLGLGMSISYAALLTKTNRIYRIFEQGKRSVSAPRFISPASQLAITFSLISLQLLGICVWFVVDPSHSVVDFQDQRTLDPRFARGVLKCDISDLSLICLLGYSMLLMVTCTVYAIKTRGVPETFNEAKPIGFTMYTTCIVWLAFIPIFFGTSQSADKLYIQTTTLTVSVSLSASVSLGMLYMPKVYIILFHPEQNVPKRKRSLKAVVTAATMSNKFTQKGNFRPNGEAKSELCENLEAPALATKQTYVTYTNHAI
UniProtQ14833
Protein Data BankN/A
GPCR-HGmod modelN/A
3D structure modelNo available structures or models
BioLiPN/A
Therapeutic Target DatabaseT99402
ChEMBLCHEMBL2736
IUPHAR292
DrugBankBE0000833

Ligand

NameCHEMBL3747116
Molecular formulaC19H16FN3O2
IUPAC name5-(4-fluorophenyl)-2-phenylmethoxy-6,7-dihydropyrazolo[1,5-a]pyrazin-4-one
Molecular weight337.354
Hydrogen bond acceptor4
Hydrogen bond donor0
XlogP3.2
SynonymsBDBM50134466
PVXQBLCMLZKSAX-UHFFFAOYSA-N
2-(benzyloxy)-5-(4-fluorophenyl)-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one
SCHEMBL16270155
Inchi KeyPVXQBLCMLZKSAX-UHFFFAOYSA-N
Inchi IDInChI=1S/C19H16FN3O2/c20-15-6-8-16(9-7-15)22-10-11-23-17(19(22)24)12-18(21-23)25-13-14-4-2-1-3-5-14/h1-9,12H,10-11,13H2
PubChem CID72714783
ChEMBLCHEMBL3747116
IUPHARN/A
BindingDB50134466
DrugBankN/A

Structure

SDF download

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

Experimental Data

ParameterValueReferenceDatabase source
EC50<10000.0 nMPMID26684851BindingDB,ChEMBL

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