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GPCR

NamePlatelet-activating factor receptor
SpeciesHomo sapiens (Human)
GenePTAFR
SynonymPAFr
PAF-R
PAF receptor
AGEPC receptor
DiseaseNerve injury
Ocular allergy
Pain
Unspecified
Psoriasis
[ Show all ]
Length342
Amino acid sequenceMEPHDSSHMDSEFRYTLFPIVYSIIFVLGVIANGYVLWVFARLYPCKKFNEIKIFMVNLTMADMLFLITLPLWIVYYQNQGNWILPKFLCNVAGCLFFINTYCSVAFLGVITYNRFQAVTRPIKTAQANTRKRGISLSLVIWVAIVGAASYFLILDSTNTVPDSAGSGNVTRCFEHYEKGSVPVLIIHIFIVFSFFLVFLIILFCNLVIIRTLLMQPVQQQRNAEVKRRALWMVCTVLAVFIICFVPHHVVQLPWTLAELGFQDSKFHQAINDAHQVTLCLLSTNCVLDPVIYCFLTKKFRKHLTEKFYSMRSSRKCSRATTDTVTEVVVPFNQIPGNSLKN
UniProtP25105
Protein Data Bank5zkq, 5zkp
GPCR-HGmod modelP25105
3D structure modelThis structure is from PDB ID 5zkq.
BioLiPBL0417415, BL0417417,BL0417419, BL0417416,BL0417418, BL0417414
Therapeutic Target DatabaseT87023
ChEMBLCHEMBL250
IUPHAR334
DrugBankBE0005561

Ligand

NameCHEMBL3746457
Molecular formulaC18H15FN4O2
IUPAC name5-(5-fluoropyridin-2-yl)-2-(phenoxymethyl)-6,7-dihydropyrazolo[1,5-a]pyrazin-4-one
Molecular weight338.342
Hydrogen bond acceptor5
Hydrogen bond donor0
XlogP2.2
SynonymsBDBM50134443
CNYVJDHTGDPUBS-UHFFFAOYSA-N
5-(5-fluoropyridin-2-yl)-2-(phenoxymethyl)-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one
SCHEMBL9938477
Inchi KeyCNYVJDHTGDPUBS-UHFFFAOYSA-N
Inchi IDInChI=1S/C18H15FN4O2/c19-13-6-7-17(20-11-13)22-8-9-23-16(18(22)24)10-14(21-23)12-25-15-4-2-1-3-5-15/h1-7,10-11H,8-9,12H2
PubChem CID67974411
ChEMBLCHEMBL3746457
IUPHARN/A
BindingDB50134443
DrugBankN/A

Structure

SDF download

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

Experimental Data

ParameterValueReferenceDatabase source
Inhibition57.0 %PMID26684851ChEMBL

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