General Information of the Protein
Protein ID
PT01588
Protein Name
Corticotropin-releasing factor receptor 1
Secondarily
Protein Name
Corticotropin-releasing hormone receptor 1
Gene Name
CRHR1
Secondarily
Gene Name
CRFR
CRFR1
CRHR
Sequence
MGGHPQLRLVKALLLLGLNPVSASLQDQHCESLSLASNISGLQCNASVDLIGTCWPRSPAGQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYSECQEILNEEKKSKVHYHVAVIINYLGHCISLVALLVAFVLFLRLRPGCTHWGDQADGALEVGAPWSGAPFQVRRSIRCLRNIIHWNLISAFILRNATWFVVQLTMSPEVHQSNVGWCRLVTAAYNYFHVTNFFWMFGEGCYLHTAIVLTYSTDRLRKWMFICIGWGVPFPIIVAWAIGKLYYDNEKCWFGKRPGVYTDYIYQGPMILVLLINFIFLFNIVRILMTKLRASTTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDEVSRVVFIYFNSFLESFQGFFVSVFYCFLNSEVRSAIRKRWHRWQDKHSIRARVARAMSIPTSPTRVSFHSIKQSTAV
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Organism
Homo sapiens, Human
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
Primary ID:
P34998

Secondarily ID:
B4DIE9
Q13008
Q4QRJ1
Q9UK64
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Ensembl ID
ENSG00000120088
HGNC ID
HGNC:2357
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: CL000367 , AtT-20
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0478377
 Compound Info 
2-(4-chloro-2,6-dimethoxyphenyl)-4-methoxy-6-methyl-N,N-dipropylpyrimidin-5-amine
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C20H28ClN3O3
  1
1
IC50 = 1 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0486463
 Compound Info 
2-(4-chloro-2,6-dimethoxyphenyl)-4-methoxy-6-methyl-5-(pentan-3-yloxy)pyrimidine
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C19H25ClN2O4
  1
1
IC50 = 7 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0453236
 Compound Info 
1-(2-methoxy-4,6-dimethylphenyl)-3-methyl-N,N-dipropylisoquinolin-4-amine
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C25H32N2O
  2
1
IC50 = 12 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
Ki = 12 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0486464
 Compound Info 
4-methoxy-2-(2-methoxy-4,6-dimethylphenyl)-6-methyl-5-(pentan-3-yloxy)pyrimidine
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C20H28N2O3
  1
1
IC50 = 19 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0471135
 Compound Info 
1-(2,4-bis(2,2-difluoroethyl)-6-methoxyphenyl)-3-methyl-N,N-dipropylisoquinolin-4-amine
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C27H32F4N2O
  1
1
Ki = 22 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000011 , CHO
 Cell Line Info 
Cell Line ID: CL000026 , CHO-K1
 Cell Line Info 
Cell Line ID: CL000583 , COS-M6
 Cell Line Info 
Cell Line ID: CL000025 , HEK-293T
 Cell Line Info 
Cell Line ID: CL000809 , HEK273
 Cell Line Info 
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000065 , HEK293-EBNA
 Cell Line Info 
Cell Line ID: CL000017 , HeLa
 Cell Line Info 
Cell Line ID: CL000016 , IMR-32
 Cell Line Info 
Cell Line ID: CL000041 , LTK-
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0035677
 Compound Info 
Pyrazolo[1,5-a]-1,3,5-triazine, 13-15
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C18H24N6O
  1
1 IC50 = 6.1 nM
CP0311099
 Compound Info 
3,6-dimethyl-4-(pentan-3-yloxy)-2-(2,4,6-trimethylphenoxy)pyridine
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C21H29NO2
  1
1 IC50 = 6.8 nM
CP0324234
 Compound Info 
N-(cyclopropylmethyl)-3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-6-methyl-N-(oxan-4-ylmethyl)pyrazolo[5,1-b][1,3]thiazol-7-amine
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C26H35N3O4S
  1
1 IC50 = 46 nM
CP0227068
 Compound Info 
N-(cyclopropylmethyl)-3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-6-methoxy-N-(2-methoxyethyl)pyrazolo[5,1-b][1,3]thiazol-7-amine
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C23H31N3O5S
  1
1 IC50 = 48 nM
CP0328875
 Compound Info 
US850504, 91
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C26H34FN3O5S
  1
1 IC50 = 61 nM
CP0218317
 Compound Info 
N-(cyclopropylmethyl)-3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-2,6-dimethyl-N-(oxan-4-ylmethyl)pyrazolo[5,1-b][1,3]thiazol-7-amine
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C27H37N3O4S
  1
1 IC50 = 76 nM
CP0113466
 Compound Info 
8-(2,4-dichlorophenyl)-N-(1,3-dimethoxypropan-2-yl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine
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C18H21Cl2N5O2
  2
1 IC50 = 82 nM
2 Ki = 1.7 nM
CP0504853
 Compound Info 
8-(dipropylamino)-3-(2,4,6-trimethylanilino)-1H-quinoxalin-2-one
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C23H30N4O
  2
1 IC50 = 100 nM
2 IC50 = 469 nM
CP0523128
 Compound Info 
3-methyl-5-N,5-N-dipropyl-2-N-(2,4,6-trimethylphenyl)quinoxaline-2,5-diamine
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C24H32N4
  2
1 IC50 = 155 nM
2 IC50 = 563 nM
CP0039659
 Compound Info 
1,3,4,6,8,13-hexahydroxy-10,11-dimethylphenanthro[1,10,9,8-opqra]perylene-7,14-dione
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C30H16O8
  1
1 IC50 = 300 nM
CP0051881
 Compound Info 
(2S,3S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-carboxy-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-carboxy-2-[[(2S,3S)-2-[[(2S)-3-hydroxy-2-[[(2S,3S)-3-methyl-2-[[(2S)-1-[(2S)-1-[2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]acetyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]propanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]butanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]pentanoyl]amino]hexanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-4-carboxybutanoyl]amino]hexanoyl]amino]-4-carboxybutanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-4-oxobutanoyl]amino]-4-oxobutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-carboxypropanoyl]amino]-3-hydroxybutanoyl]amino]-3-methylpentanoic acid
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C202H345N55O64S
  1
1 Ki = 0.8 nM
CP0244594
 Compound Info 
(1-Ethyl-propyl)-[3-(4-methoxy-2-methyl-phenyl)-2,5-dimethyl-pyrazolo[1,5-a]pyrimidin-7-yl]-amine
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C21H28N4O
  1
1 Ki = 1 nM
CP0144716
 Compound Info 
N-(cyclopropylmethyl)-3-(2,4-dichlorophenyl)-2,5-dimethyl-N-propylpyrazolo[1,5-a]pyrimidin-7-amine
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C21H24Cl2N4
  1
1 Ki = 1.3 nM
CP0722686
 Compound Info 
Butyl-[2,5-dimethyl-7-(2,4,6-trimethyl-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-ethyl-amine
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C23H33ClN4
  1
1 Ki = 1.6 nM
CP0042421
 Compound Info 
5-Chloro-N-cyclopropylmethyl-2-methyl-N-propyl-N''-(2,4,6-trichloro-phenyl)-pyrimidine-4,6-diamine
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C18H20Cl4N4
  2
1 Ki = 1.7 nM
2 Ki = 2.7 nM
CP0255382
 Compound Info 
Butyl-[2,5-dimethyl-7-(2,4,6-trimethyl-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-ethyl-amine
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C23H32N4
  1
1 Ki = 2.7 nM
CP0116903
 Compound Info 
3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine
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C22H32N6
  1
1 Ki = 3 nM
CP0789127
 Compound Info 
(2-Chloro-4,6-dimethyl-phenyl)-[1-(2-methoxy-1-methoxymethyl-ethyl)-6-methyl-1H-[1,2,3]triazolo[4,5-c]pyridin-4-yl]-amine; compound with methanesulfonic acid
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C20H28ClN5O5S
  1
1 Ki = 3.3 nM
CP0279533
 Compound Info 
3-(2,4-dimethoxyphenyl)-N-(2-methoxyethyl)-2,5-dimethyl-N-propylpyrazolo[1,5-a]pyrimidin-7-amine
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C22H30N4O3
  1
1 Ki = 3.4 nM
CP0310325
 Compound Info 
3-(2-Bromo-4-isopropyl-phenyl)-7-diethylamino-5-methyl-3H-thiazolo[4,5-d]pyrimidine-2-thione
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C19H23BrN4S2
  1
1 Ki = 4.1 nM
CP0274618
 Compound Info 
9-(2-Bromo-4-isopropyl-phenyl)-6-(butyl-ethyl-amino)-2,7-dimethyl-7,9-dihydro-purin-8-one
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C22H30BrN5O
  1
1 Ki = 5 nM
CP0289537
 Compound Info 
Butyl-[3-(2,4-dichloro-phenyl)-2,5-dimethyl-pyrazolo[1,5-a]pyrimidin-7-yl]-ethyl-amine
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C20H24Cl2N4
  1
1 Ki = 5 nM
CP0275845
 Compound Info 
2-N-(2-bromo-4-propan-2-ylphenyl)-2-N-ethyl-6-methyl-4-N,4-N-dipropylpyrimidine-2,4-diamine
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C22H33BrN4
  1
1 Ki = 9 nM
CP0040853
 Compound Info 
2,5-dimethyl-3-(3-methyl-5-nitropyridin-2-yl)-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine
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C20H26N6O2
  1
1 Ki = 9.1 nM
CP0182111
 Compound Info 
3-(2-Bromo-4-isopropyl-phenyl)-7-diethylamino-5-methyl-3H-thiazolo[4,5-d]pyrimidin-2-one
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C19H23BrN4OS
  1
1 Ki = 9.4 nM
CP0295460
 Compound Info 
3-[5-(dimethylamino)-3-methylpyridin-2-yl]-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine
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C22H32N6
  1
1 Ki = 10 nM
CP0289681
 Compound Info 
3-(5-amino-3-methylpyridin-2-yl)-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine
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C20H28N6
  1
1 Ki = 85 nM
Clinical Information about the Protein
Target 1 ( Corticotropin-releasing factor receptor 1 (CRHR1) )
Target Type Successful Target
Disease 5 Target-related Diseases  5
1 Anxiety disorder [ICD-11: 6B00-6B0Z]
2 Major depressive disorder [ICD-11: 6A70.3]
3 Mood disorder [ICD-11: 6A60-6E23]
4 Irritable bowel syndrome [ICD-11: DD91.0]
5 Depression [ICD-11: 6A70-6A7Z]
Clinical Trial Drug(s) 4 Clinical Trial Drugs  4
1 Pexacerfont
 Drug Info 
Phase 2/3
Anxiety disorder
2 GSK561679
 Drug Info 
Phase 2
Major depressive disorder
3 ONO-2333Ms
 Drug Info 
Phase 2
Anxiety disorder
4 SSR125543
 Drug Info 
Phase 2
Anxiety disorder
Discontinued Drug(s) 4 Discontinued Drugs  4
1 CP-316,311
 Drug Info 
Discontinued in Phase 2
Mood disorder
2 GW876008
 Drug Info 
Discontinued in Phase 2
Irritable bowel syndrome
3 Antalarmin
 Drug Info 
Terminated
Depression
4 DMP-696
 Drug Info 
Terminated
Anxiety disorder
Investigative Drug(s) 3 Investigative Drugs  3
1 BMS-561388
 Drug Info 
Investigative
Anxiety disorder
2 CP154,526
 Drug Info 
Investigative
Depression
3 Des-Arg(9)-[Leu(8)]-BK
 Drug Info 
Investigative
Depression