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GPCR

NameMetabotropic glutamate receptor 2
SpeciesHomo sapiens (Human)
GeneGRM2
SynonymmGluR2
mGlu2 receptor
metabotropic glutamate receptor 2
GPRC1B
glutamate receptor
DiseaseCentral nervous system disease
Anxiety disorder
Bipolar disorder
Major depressive disorder
Mood disorder
[ Show all ]
Length872
Amino acid sequenceMGSLLALLALLLLWGAVAEGPAKKVLTLEGDLVLGGLFPVHQKGGPAEDCGPVNEHRGIQRLEAMLFALDRINRDPHLLPGVRLGAHILDSCSKDTHALEQALDFVRASLSRGADGSRHICPDGSYATHGDAPTAITGVIGGSYSDVSIQVANLLRLFQIPQISYASTSAKLSDKSRYDYFARTVPPDFFQAKAMAEILRFFNWTYVSTVASEGDYGETGIEAFELEARARNICVATSEKVGRAMSRAAFEGVVRALLQKPSARVAVLFTRSEDARELLAASQRLNASFTWVASDGWGALESVVAGSEGAAEGAITIELASYPISDFASYFQSLDPWNNSRNPWFREFWEQRFRCSFRQRDCAAHSLRAVPFEQESKIMFVVNAVYAMAHALHNMHRALCPNTTRLCDAMRPVNGRRLYKDFVLNVKFDAPFRPADTHNEVRFDRFGDGIGRYNIFTYLRAGSGRYRYQKVGYWAEGLTLDTSLIPWASPSAGPLPASRCSEPCLQNEVKSVQPGEVCCWLCIPCQPYEYRLDEFTCADCGLGYWPNASLTGCFELPQEYIRWGDAWAVGPVTIACLGALATLFVLGVFVRHNATPVVKASGRELCYILLGGVFLCYCMTFIFIAKPSTAVCTLRRLGLGTAFSVCYSALLTKTNRIARIFGGAREGAQRPRFISPASQVAICLALISGQLLIVVAWLVVEAPGTGKETAPERREVVTLRCNHRDASMLGSLAYNVLLIALCTLYAFKTRKCPENFNEAKFIGFTMYTTCIIWLAFLPIFYVTSSDYRVQTTTMCVSVSLSGSVVLGCLFAPKLHIILFQPQKNVVSHRAPTSRFGSAAARASSSLGQGSGSQFVPTVCNGREVVDSTTSSL
UniProtQ14416
Protein Data Bank5cnj, 5kzn, 5kzq, 5cni, 4xas, 4xaq
GPCR-HGmod modelN/A
3D structure modelThis structure is from PDB ID 5cnj.
BioLiPBL0365442, BL0324559,BL0324560, BL0324557,BL0324558, BL0306697,BL0306698, BL0306695,BL0306696, BL0365443
Therapeutic Target DatabaseT62820
ChEMBLCHEMBL5137
IUPHAR290
DrugBankN/A

Ligand

NameCHEMBL3885379
Molecular formulaC21H19ClF3N3O
IUPAC name7-[[(1S,2S)-2-(4-chlorophenyl)cyclopropyl]methoxy]-3-(cyclopropylmethyl)-8-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine
Molecular weight421.848
Hydrogen bond acceptor6
Hydrogen bond donor0
XlogP6.2
SynonymsBDBM50209103
SCHEMBL16591448
Inchi KeyLETPPZNSGLCXSE-GDBMZVCRSA-N
Inchi IDInChI=1S/C21H19ClF3N3O/c22-15-5-3-13(4-6-15)16-10-14(16)11-29-17-7-8-28-18(9-12-1-2-12)26-27-20(28)19(17)21(23,24)25/h3-8,12,14,16H,1-2,9-11H2/t14-,16-/m1/s1
PubChem CID117972250
ChEMBLCHEMBL3885379
IUPHARN/A
BindingDB50209103
DrugBankN/A

Structure

SDF download

2D structure
Lipinski's druglikenessThis ligand has a partition coefficient log P greater than 5.

Experimental Data

ParameterValueReferenceDatabase source
EC501.4 nMPMID27914948BindingDB,ChEMBL
EC50530.0 nMPMID27914948BindingDB,ChEMBL
Emax85.0 %PMID27914948ChEMBL
Emax99.0 %PMID27914948ChEMBL
FC<18.0 -PMID27914948ChEMBL
Ki1.0 nMPMID27914948BindingDB
Ki1.0 nMPMID27914948ChEMBL

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