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GLASS

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GPCR

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 Hypoglycemia [ 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

Ligand

Name	L-168,049
Molecular formula	C24H20BrClN2O
IUPAC name	4-[3-(5-bromo-2-propoxyphenyl)-5-(4-chlorophenyl)-1H-pyrrol-2-yl]pyridine
Molecular weight	467.791
Hydrogen bond acceptor	2
Hydrogen bond donor	1
XlogP	6.8
Synonyms	CHEMBL351772 HMS3268L08 NCGC00092367-01 AC1NSKCK DTXSID10415520 ZINC37866152 208188-17-4 BDBM50075775 Glucagon Receptor Antagonist II L168049 4-[3-(5-bromo-2-propoxyphenyl)-5-(4-chlorophenyl)-1H-pyrrol-2-yl]pyridine CHEBI:92326 CTK8E7931 J-012341 RT-013470 191034-25-0 AKOS024457045 Glucagon antagonists (diabetes) L-168049 BN0285 GTPL3505 MolPort-003-983-604 D0M3AR L 168049 SCHEMBL6362882 2-(4-Pyridyl)-5-(4-Chlorophenyl)-3-(5-Bromo-2-Propyloxyphenyl)Pyrrole B7014 Glucagon antagonists (diabetes), Merck & Co L000331 4-[3-(5-Bromo-2-propoxy-phenyl)-5-(4-chloro-phenyl)-1H-pyrrol-2-yl]-pyridine BRD-K18036262-001-01-0 [ Show all ]
Inchi Key	HHBOWXZOLYQFNY-UHFFFAOYSA-N
Inchi ID	InChI=1S/C24H20BrClN2O/c1-2-13-29-23-8-5-18(25)14-20(23)21-15-22(16-3-6-19(26)7-4-16)28-24(21)17-9-11-27-12-10-17/h3-12,14-15,28H,2,13H2,1H3
PubChem CID	5311276
ChEMBL	CHEMBL351772
IUPHAR	3505
BindingDB	50075775
DrugBank	N/A
Structure SDF download
Lipinski's druglikeness	This ligand has a partition coefficient log P greater than 5.

Experimental Data

Parameter	Value	Reference	Database source
IC50	3.7 nM	PMID10085108	IUPHAR
IC50	7.0 nM	PMID10201821	BindingDB,ChEMBL
IC50	170.0 nM	PMID10201821	BindingDB,ChEMBL
IC50	1442.0 nM	N/A	BindingDB
IC50	1442.12 nM	Med Chem Res, (2013) None:None:1	ChEMBL

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