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Name | Prostaglandin E2 receptor EP4 subtype |
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Species | Homo sapiens (Human) |
Gene | PTGER4 |
Synonym | Prostanoid EP4 receptor PGE2 receptor EP4 subtype PGE receptor EP4 subtype EP4 receptor EP2 |
Disease | Ulcerative colitis Glaucoma Inflammatory disease Migraine Osteoarthritis [ Show all ] |
Length | 488 |
Amino acid sequence | MSTPGVNSSASLSPDRLNSPVTIPAVMFIFGVVGNLVAIVVLCKSRKEQKETTFYTLVCGLAVTDLLGTLLVSPVTIATYMKGQWPGGQPLCEYSTFILLFFSLSGLSIICAMSVERYLAINHAYFYSHYVDKRLAGLTLFAVYASNVLFCALPNMGLGSSRLQYPDTWCFIDWTTNVTAHAAYSYMYAGFSSFLILATVLCNVLVCGALLRMHRQFMRRTSLGTEQHHAAAAASVASRGHPAASPALPRLSDFRRRRSFRRIAGAEIQMVILLIATSLVVLICSIPLVVRVFVNQLYQPSLEREVSKNPDLQAIRIASVNPILDPWIYILLRKTVLSKAIEKIKCLFCRIGGSRRERSGQHCSDSQRTSSAMSGHSRSFISRELKEISSTSQTLLPDLSLPDLSENGLGGRNLLPGVPGMGLAQEDTTSLRTLRISETSDSSQGQDSESVLLVDEAGGSGRAGPAPKGSSLQVTFPSETLNLSEKCI |
UniProt | P35408 |
Protein Data Bank | 5ywy, 5yhl |
GPCR-HGmod model | P35408 |
3D structure model | This structure is from PDB ID 5ywy. |
BioLiP | BL0434347, BL0434289 |
Therapeutic Target Database | T18876 |
ChEMBL | CHEMBL1836 |
IUPHAR | 343 |
DrugBank | BE0003522 |
Name | Prostaglandin E2 |
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Molecular formula | C20H32O5 |
IUPAC name | (Z)-7-[(1R,2R,3R)-3-hydroxy-2-[(E,3S)-3-hydroxyoct-1-enyl]-5-oxocyclopentyl]hept-5-enoic acid |
Molecular weight | 352.471 |
Hydrogen bond acceptor | 5 |
Hydrogen bond donor | 3 |
XlogP | 2.8 |
Synonyms | Dinoprostone, United States Pharmacopeia (USP) Reference Standard (Z)-7-[(1r,2r,3r)-3-Hydroxy-2-[(E,3s)-3-Hydroxyoct-1-Enyl]-5-Oxo-Cyclopentyl]hept-5-Enoic Acid E2, Prostaglandin 1798-EP2301922A1 HMS1361K12 [ Show all ] |
Inchi Key | XEYBRNLFEZDVAW-ARSRFYASSA-N |
Inchi ID | InChI=1S/C20H32O5/c1-2-3-6-9-15(21)12-13-17-16(18(22)14-19(17)23)10-7-4-5-8-11-20(24)25/h4,7,12-13,15-17,19,21,23H,2-3,5-6,8-11,14H2,1H3,(H,24,25)/b7-4-,13-12+/t15-,16+,17+,19+/m0/s1 |
PubChem CID | 5280360 |
ChEMBL | CHEMBL548 |
IUPHAR | 1883, 1916 |
BindingDB | 35847 |
DrugBank | DB00917 |
Structure | |
Lipinski's druglikeness | This ligand satisfies Lipinski's rule of five. |
Parameter | Value | Reference | Database source |
---|---|---|---|
N/A | N/A | DrugBank | |
Activity | 40.0 % | PMID24279689 | ChEMBL |
EC50 | 3.0 nM | PMID12643927, PMID18039575 | BindingDB,ChEMBL |
EC50 | 7.5 nM | PMID26985320 | BindingDB,ChEMBL |
EC50 | 900.0 nM | PMID19584306 | IUPHAR |
IC50 | 0.45 nM | PMID23466604 | ChEMBL |
IC50 | 0.55 nM | PMID27876250 | ChEMBL |
IC50 | 0.7 nM | PMID12643927 | BindingDB |
IC50 | 0.7 nM | PMID12643927 | ChEMBL |
IC50 | 1.1 nM | PMID23403082 | ChEMBL |
IC50 | 3.8 nM | PMID18983139 | ChEMBL |
IC50 | 5.5 nM | PMID27876250 | BindingDB |
IC50 | 9.9 nM | PMID20218623 | BindingDB,ChEMBL |
Inhibition | 5.0 % | PMID23403082 | ChEMBL |
Kd | 0.3 - 24.0 nM | PMID16604093, PMID10634944, PMID10952683, PMID22480736 | IUPHAR |
Ki | 0.17 nM | PMID23466604 | ChEMBL |
Ki | 0.45 nM | PMID23403082 | ChEMBL |
Ki | 0.79 nM | PMID18039575, PMID17931866, PMID10634944, PMID17531488 | BindingDB,ChEMBL |
Ki | 0.794 - 7.94 nM | PMID16604093, PMID10634944, PMID10462542, PMID10952683, PMID17495127 | IUPHAR |
Ki | 1.9 nM | PMID18983139 | ChEMBL |
Ki | 3.1 nM | PMID24279689 | BindingDB,ChEMBL |
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