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Name | Glucagon receptor |
---|---|
Species | Homo sapiens (Human) |
Gene | GCGR |
Synonym | GL-R GGR GR glucagon receptor |
Disease | Diabetes Type 2 diabetes Non-insulin dependent diabetes Obesity; Diabetes Type 1 diabetes [ Show all ] |
Length | 477 |
Amino acid sequence | MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQCQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANLFASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYCWLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDNMGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGVHEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRLGKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF |
UniProt | P47871 |
Protein Data Bank | 5yqz, 5xez, 5ee7, 5xf1 |
GPCR-HGmod model | P47871 |
3D structure model | This structure is from PDB ID 5yqz. |
BioLiP | BL0379634,BL0379635, BL0402227, BL0379636,BL0379637, BL0343437 |
Therapeutic Target Database | T60182, T87875 |
ChEMBL | CHEMBL1985 |
IUPHAR | 251 |
DrugBank | N/A |
Name | GRA EX-25 |
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Molecular formula | C29H36F3N3O5 |
IUPAC name | 3-[[4-[[(4-tert-butylcyclohexyl)-[[4-(trifluoromethoxy)phenyl]carbamoyl]amino]methyl]benzoyl]amino]propanoic acid |
Molecular weight | 563.618 |
Hydrogen bond acceptor | 8 |
Hydrogen bond donor | 3 |
XlogP | 5.8 |
Synonyms | 3-{4-[1-(4-tert-Butyl-cyclohexyl)-3-(4-trifluoromethoxy-phenyl)-ureidomethyl]-benzoylamino}-propionic acid BDBM50202056 LS-193210 AKOS032944977 CHEMBL219244 [ Show all ] |
Inchi Key | BZXMLCVDKDXRQY-UHFFFAOYSA-N |
Inchi ID | InChI=1S/C29H36F3N3O5/c1-28(2,3)21-8-12-23(13-9-21)35(27(39)34-22-10-14-24(15-11-22)40-29(30,31)32)18-19-4-6-20(7-5-19)26(38)33-17-16-25(36)37/h4-7,10-11,14-15,21,23H,8-9,12-13,16-18H2,1-3H3,(H,33,38)(H,34,39)(H,36,37) |
PubChem CID | 16100296 |
ChEMBL | CHEMBL198736 |
IUPHAR | N/A |
BindingDB | 50171817 |
DrugBank | N/A |
Structure | |
Lipinski's druglikeness | This ligand is heavier than 500 daltons. This ligand has a partition coefficient log P greater than 5. |
Parameter | Value | Reference | Database source |
---|---|---|---|
IC50 | 21.0 nM | PMID16102966 | BindingDB,ChEMBL |
IC50 | 23.0 nM | PMID18707090 | BindingDB |
IC50 | 23.4 nM | PMID18707090 | ChEMBL |
IC50 | 144.0 nM | PMID16102966 | BindingDB,ChEMBL |
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