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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	aminothiazole, 22
Molecular formula	C30H26F3N3O5S
IUPAC name	(2R)-3-[[4-[[2,3-dihydro-1H-inden-5-yl-[4-[4-(trifluoromethoxy)phenyl]-1,3-thiazol-2-yl]amino]methyl]benzoyl]amino]-2-hydroxypropanoic acid
Molecular weight	597.609
Hydrogen bond acceptor	11
Hydrogen bond donor	3
XlogP	6.4
Synonyms	BDBM29125 CHEMBL504260 BPAUVSAWZVWRTJ-AREMUKBSSA-N SCHEMBL2647902 2(R)-Hydroxy-3-[4-({indan-5-yl-[4-(4-trifluoromethoxyphenyl)thiazol-2-yl]amino}methyl)benzoylamino]propionic acid
Inchi Key	BPAUVSAWZVWRTJ-AREMUKBSSA-N
Inchi ID	InChI=1S/C30H26F3N3O5S/c31-30(32,33)41-24-12-9-20(10-13-24)25-17-42-29(35-25)36(23-11-8-19-2-1-3-22(19)14-23)16-18-4-6-21(7-5-18)27(38)34-15-26(37)28(39)40/h4-14,17,26,37H,1-3,15-16H2,(H,34,38)(H,39,40)/t26-/m1/s1
PubChem CID	20775791
ChEMBL	CHEMBL504260
IUPHAR	N/A
BindingDB	29125
DrugBank	N/A
Structure SDF download
Lipinski's druglikeness	This ligand has more than 10 hydrogen bond acceptor. This ligand is heavier than 500 daltons. This ligand has a partition coefficient log P greater than 5.

Experimental Data

Parameter	Value	Reference	Database source
IC50	225.0 nM	PMID19385613	BindingDB,ChEMBL

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