General Information of the Protein
Protein ID
PT06074
Protein Name
Glucagon receptor
Gene Name
GCGR
Sequence
MPLTQLHCPHLLLLLLVLSCLPEAPSAQVMDFLFEKWKLYSDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPPNTTANISCPWYLPWYHKVQHRLVFKRCGPDGQWVRGPRGQPWRNASQCQLDDEEIEVQKGVAKMYSSQQVMYTVGYSLSLGALLLALVILLGLRKLHCTRNYIHGNLFASFVLKAGSVLVIDWLLKTRYSQKIGDDLSVSVWLSDGAMAGCRVATVIMQYGIIANYCWLLVEGVYLYSLLSLATFSERSFFSLYLGIGWGAPLLFVIPWVVVKCLFENVQCWTSNDNMGFWWILRIPVFLALLINFFIFVHIIHLLVAKLRAHQMHYADYKFRLARSTLTLIPLLGVHEVVFAFVTDEHAQGTLRSTKLFFDLFLSSFQGLLVAVLYCFLNKEVQAELMRRWRQWQEGKALQEERLASSHGSHMAPAGPCHGDPCEKLQLMSAGSSSGTGCVPSMETSLASSLPRLADSPT
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Organism
Mus musculus, Mouse
Protein Classification
Membrane receptor
>
Family B G protein-coupled receptor
>
Peptide receptor (family B GPCR)
>
Glucagon-like receptor
>
Glucagon receptor
Function
G-protein coupled receptor for glucagon that plays a central role in the regulation of blood glucose levels and glucose homeostasis. Regulates the rate of hepatic glucose production by promoting glycogen hydrolysis and gluconeogenesis. Plays an important role in mediating the responses to fasting. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Promotes activation of adenylate cyclase. Besides, plays a role in signaling via a phosphatidylinositol-calcium second messenger system.
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Uniprot ID
Primary ID:
Q61606

Secondarily ID:
Q63960
Q8K0B5
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Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0222548
4-[5-(4-Chloro-phenyl)-3-(2-propoxy-phenyl)-1H-pyrrol-2-yl]-pyridine
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C24H21ClN2O
 2
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
2
IC50 = 700 nM
   TI
   LI
   LO
   TS
CP0039137
4-[3-(5-Bromo-2-propoxy-phenyl)-5-(4-chloro-phenyl)-1H-pyrrol-2-yl]-pyridine
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C24H20BrClN2O
 2
1
IC50 = 37 nM
   TI
   LI
   LO
   TS
2
IC50 = 250 nM
   TI
   LI
   LO
   TS
CP0502906
4-[3-(4-Bromo-2-propoxy-phenyl)-5-(4-chloro-phenyl)-1H-pyrrol-2-yl]-pyridine
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C24H20BrClN2O
 2
1
IC50 = 49 nM
   TI
   LI
   LO
   TS
2
IC50 = 830 nM
   TI
   LI
   LO
   TS
CP0380783
4-[5-(4-Chloro-phenyl)-3-(5-chloro-2-propoxy-phenyl)-1H-pyrrol-2-yl]-pyridine
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C24H20Cl2N2O
 2
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
2
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0063780
4-[5-(4-Chloro-phenyl)-3-isopropyl-1H-pyrrol-2-yl]-pyridine
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C18H17ClN2
 2
1
IC50 = 60 nM
   TI
   LI
   LO
   TS
2
IC50 = 3000 nM
   TI
   LI
   LO
   TS
CP0245884
4-[5-(4-Chloro-phenyl)-3-cyclohexyl-1H-pyrrol-2-yl]-pyridine
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C21H21ClN2
 2
1
IC50 = 60 nM
   TI
   LI
   LO
   TS
2
IC50 > 3000 nM
   TI
   LI
   LO
   TS
CP0376681
4-[3-(2-Butoxy-phenyl)-5-(4-chloro-phenyl)-1H-pyrrol-2-yl]-pyridine
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C25H23ClN2O
 2
1
IC50 = 80 nM
   TI
   LI
   LO
   TS
2
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0120350
3-[[4-[(1S)-1-[3-(3,5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)pyrazol-1-yl]ethyl]benzoyl]amino]propanoic acid
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C32H27Cl2N3O4
 1
1
IC50 = 122 nM
   TI
   LI
   LO
   TS
CP0222546
4-[5-(4-Chloro-phenyl)-3-(2-isobutoxy-phenyl)-1H-pyrrol-2-yl]-pyridine
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C25H23ClN2O
 1
1
IC50 = 150 nM
   TI
   LI
   LO
   TS
CP0096778
4-[5-(4-Chloro-phenyl)-3-(4-fluoro-phenyl)-1H-pyrrol-2-yl]-pyridine
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C21H14ClFN2
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0202930
4-[3,5-Bis-(4-chloro-phenyl)-1H-pyrrol-2-yl]-pyridine
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C21H14Cl2N2
 2
1
IC50 = 220 nM
   TI
   LI
   LO
   TS
2
IC50 = 42000 nM
   TI
   LI
   LO
   TS
CP0112393
4-[4-(4-Fluoro-phenyl)-5-pyridin-4-yl-1H-pyrrol-2-yl]-benzonitrile
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C22H14FN3
 1
1
IC50 = 230 nM
   TI
   LI
   LO
   TS
CP0222549
4-[3-(3-Bromo-phenyl)-5-(4-chloro-phenyl)-1H-pyrrol-2-yl]-pyridine
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C21H14BrClN2
 1
1
IC50 = 230 nM
   TI
   LI
   LO
   TS
CP0310029
4-[5-(4-Chloro-phenyl)-3-(4-methoxy-phenyl)-1H-pyrrol-2-yl]-pyridine
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C22H17ClN2O
 1
1
IC50 = 240 nM
   TI
   LI
   LO
   TS
CP0222547
4-[3-(2-Allyloxy-phenyl)-5-(4-chloro-phenyl)-1H-pyrrol-2-yl]-pyridine
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C24H19ClN2O
 1
1
IC50 = 270 nM
   TI
   LI
   LO
   TS
CP0063255
4-[5-(2,4-Dichloro-phenyl)-3-(4-fluoro-phenyl)-1H-pyrrol-2-yl]-pyridine
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C21H13Cl2FN2
 1
1
IC50 = 340 nM
   TI
   LI
   LO
   TS
CP0147411
4-[5-(4-Chloro-phenyl)-3-(2-hexyloxy-phenyl)-1H-pyrrol-2-yl]-pyridine
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C27H27ClN2O
 1
1
IC50 = 340 nM
   TI
   LI
   LO
   TS
CP0280722
4-[5-(4-Chloro-phenyl)-3-(2-ethoxy-phenyl)-1H-pyrrol-2-yl]-pyridine
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C23H19ClN2O
 1
1
IC50 = 340 nM
   TI
   LI
   LO
   TS
CP0115930
4-[5-(4-Chloro-phenyl)-3-(2-methoxy-phenyl)-1H-pyrrol-2-yl]-pyridine
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C22H17ClN2O
 1
1
IC50 = 400 nM
   TI
   LI
   LO
   TS
CP0222552
4-[3,5-Bis-(4-fluoro-phenyl)-1H-pyrrol-2-yl]-pyridine
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C21H14F2N2
 2
1
IC50 = 430 nM
   TI
   LI
   LO
   TS
2
IC50 = 7000 nM
   TI
   LI
   LO
   TS
CP0384133
2-[5-(4-chlorophenyl)-2-pyridin-4-yl-1H-pyrrol-3-yl]-N-propylaniline
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C24H22ClN3
 2
1
IC50 = 440 nM
   TI
   LI
   LO
   TS
2
IC50 > 3000 nM
   TI
   LI
   LO
   TS
CP0313977
4-[5-(3-Chloro-phenyl)-3-(4-fluoro-phenyl)-1H-pyrrol-2-yl]-pyridine
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C21H14ClFN2
 1
1
IC50 = 460 nM
   TI
   LI
   LO
   TS
CP0091849
5-(4-Chloro-phenyl)-2-pyridin-4-yl-1H-pyrrole-3-carboxylic acid ethyl ester
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C18H15ClN2O2
 2
1
IC50 = 500 nM
   TI
   LI
   LO
   TS
2
IC50 > 3000 nM
   TI
   LI
   LO
   TS
CP0375132
4-[5-(4-Chloro-phenyl)-3-(2,6-dipropoxy-phenyl)-1H-pyrrol-2-yl]-pyridine
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C27H27ClN2O2
 2
1
IC50 = 670 nM
   TI
   LI
   LO
   TS
2
IC50 > 3000 nM
   TI
   LI
   LO
   TS
CP0101836
4-[5-(4-Chloro-phenyl)-1H-pyrrol-2-yl]-pyridine
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C15H11ClN2
 2
1
IC50 = 700 nM
   TI
   LI
   LO
   TS
2
IC50 > 3000 nM
   TI
   LI
   LO
   TS
CP0306397
4-[5-(4-Chloro-phenyl)-3-(2-isopropoxy-phenyl)-1H-pyrrol-2-yl]-pyridine
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C24H21ClN2O
 2
1
IC50 = 700 nM
   TI
   LI
   LO
   TS
2
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0509122
5-(4-Chloro-phenyl)-2-pyridin-4-yl-1H-pyrrole-3-carboxylic acid benzyl ester
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C23H17ClN2O2
 1
1
IC50 = 800 nM
   TI
   LI
   LO
   TS
CP0337062
4-[3-(4-Fluoro-phenyl)-5-phenyl-1H-pyrrol-2-yl]-pyridine
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C21H15FN2
 1
1
IC50 = 2700 nM
   TI
   LI
   LO
   TS
CP0182277
4-[5-Cyclohexyl-3-(4-fluoro-phenyl)-1H-pyrrol-2-yl]-pyridine
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C21H21FN2
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT01725 Glucagon receptor Rattus norvegicus, Rat