General Information of the Protein
Protein ID
PT03947
Protein Name
Corticotropin-releasing factor receptor 1
Secondarily
Protein Name
Corticotropin-releasing hormone receptor 1
Gene Name
CRHR1
Secondarily
Gene Name
Crhr
Sequence
MGRRPQLRLVKALLLLGLNPVSTSLQDQRCENLSLTSNVSGLQCNASVDLIGTCWPRSPAGQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYSECQEILNEEKKSKVHYHVAVIINYLGHCISLVALLVAFVLFLRLRSIRCLRNIIHWNLISAFILRNATWFVVQLTVSPEVHQSNVAWCRLVTAAYNYFHVTNFFWMFGEGCYLHTAIVLTYSTDRLRKWMFVCIGWGVPFPIIVAWAIGKLHYDNEKCWFGKRPGVYTDYIYQGPMILVLLINFIFLFNIVRILMTKLRASTTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDEVSRVVFIYFNSFLESFQGFFVSVFYCFLNSEVRSAIRKRWRRWQDKHSIRARVARAMSIPTSPTRVSFHSIKQSTAV
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Organism
Rattus norvegicus, Rat
Protein Classification
Membrane receptor
>
Family B G protein-coupled receptor
>
Peptide receptor (family B GPCR)
>
Corticotropin releasing factor receptor
>
Corticotropin releasing factor receptor
Function
G-protein coupled receptor for CRH (corticotropin-releasing factor) and UCN (urocortin). Has high affinity for CRH and UCN. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and down-stream effectors, such as adenylate cyclase. Promotes the activation of adenylate cyclase, leading to increased intracellular cAMP levels. Inhibits the activity of the calcium channel CACNA1H. Required for normal embryonic development of the adrenal gland and for normal hormonal responses to stress. Plays a role in the response to anxiogenic stimuli.
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Uniprot ID
P35353
Ensembl ID
ENSG00000120088
Subcellular Location
Cell membrane
Endosome
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: CL000026 , CHO-K1
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0393082
 Compound Info 
2-[6-(difluoromethoxy)-4-methylpyridin-3-yl]-3,7-dimethyl-5-pentan-3-ylpyrrolo[2,1-f][1,2,4]triazin-4-one
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C20H24F2N4O2
  2
1
EC50 = 2.6 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 8.4 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0397857
 Compound Info 
10-(2-chloro-4-methoxyphenyl)-11-methyl-N-pentan-3-yl-1,8,12-triazatricyclo[7.3.0.03,7]dodeca-2,7,9,11-tetraen-2-amine
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C22H27ClN4O
  1
1
EC50 = 40 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0503328
 Compound Info 
5-N-(2-chloro-4-methoxyphenyl)-6-methyl-7-N,7-N-dipropylpyrazolo[1,5-a]pyrimidine-5,7-diamine
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C20H26ClN5O
  1
1
EC50 = 81 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000016 , IMR-32
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0231706
 Compound Info 
(R)-1-(1-cyclopropyl-2-methoxyethyl)-5-(6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino)-3-methyl-1,2,4-triazin-6(1H)-one
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C18H23F2N5O3
  1
1 IC50 = 1.1 nM
CP0105492
 Compound Info 
(S)-1-(1-cyclopropyl-2-methoxyethyl)-5-(6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino)-3-methyl-1,2,4-triazin-6(1H)-one
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C18H23F2N5O3
  1
1 IC50 = 6.5 nM
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT02597 Corticotropin-releasing factor receptor 1 Mus musculus, Mouse
 Protein Info