General Information of the Protein
Protein ID
PT02921
Protein Name
Corticotropin-releasing factor receptor 2
Secondarily
Protein Name
Corticotropin-releasing hormone receptor 2
Gene Name
CRHR2
Secondarily
Gene Name
CRF2R
CRH2R
Sequence
MDAALLHSLLEANCSLALAEELLLDGWGPPLDPEGPYSYCNTTLDQIGTCWPRSAAGALVERPCPEYFNGVKYNTTRNAYRECLENGTWASKINYSQCEPILDDKQRKYDLHYRIALVVNYLGHCVSVAALVAAFLLFLALRSIRCLRNVIHWNLITTFILRNVMWFLLQLVDHEVHESNEVWCRCITTIFNYFVVTNFFWMFVEGCYLHTAIVMTYSTERLRKCLFLFIGWCIPFPIIVAWAIGKLYYENEQCWFGKEPGDLVDYIYQGPIILVLLINFVFLFNIVRILMTKLRASTTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDDLSQIMFIYFNSFLQSFQGFFVSVFYCFFNGEVRSAVRKRWHRWQDHHSLRVPMARAMSIPTSPTRISFHSIKQTAAV
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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), UCN (urocortin), UCN2 and UCN3. Has high affinity for 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.
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Uniprot ID
Primary ID:
Q13324

Secondarily ID:
B2R967
B3SXS6
B3SXS7
B3SXS8
B3SXT0
F8WA81
O43461
Q4QRJ4
Q99431
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HGNC ID
HGNC:2358
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
CP0902360
Trans-5-Chloro-N-[4-(3-ethyl-2-oxo-2,3-dihydro-benzoimidazol-1-ylmethyl)-cyclohexyl]-2-methyl-nicotinamide
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C23H27ClN4O2
 1
1
IC50 = 256 nM
   TI
   LI
   LO
   TS
CP0850734
Trans-5-Chloro-N-[4-(3-isobutyl-2-oxo-2,3-dihydro-benzoimidazol-1-ylmethyl)-cyclohexyl]-2-methyl-nicotinamide
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C25H31ClN4O2
 1
1
IC50 = 296 nM
   TI
   LI
   LO
   TS
CP0904714
US8835444, 1.8
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C26H27Cl2F3N4O2
 1
1
IC50 = 727 nM
   TI
   LI
   LO
   TS
CP0871523
Trans-5-chloro-N-[-4-((5'-fluoro-2'-oxospiro[cyclopropane-1,3'-indoline]-1'-yl)methyl)cyclohexyl]-2-methylnicotinamide
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C24H25ClFN3O2
 1
1
IC50 = 811 nM
   TI
   LI
   LO
   TS
CP0862006
Trans-5-Chloro-N-[4-(-6-chloro-3-fluoro-3-methyl-2-oxo-2,3-dihydro-indol-1-ylmethyl)-cyclohexyl]-2-methyl-nicotinamide
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C23H24Cl2FN3O2
 1
1
IC50 = 876 nM
   TI
   LI
   LO
   TS
CP0860100
Trans-5-Chloro-N-[4-(7-chloro-3,3-dimethyl-2-oxo-2,3-dihydro-indol-1-ylmethyl)-cyclohexyl]-2-methyl-nicotinamide
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C24H27Cl2N3O2
 1
1
IC50 = 936 nM
   TI
   LI
   LO
   TS
CP0849230
Trans-2-Chloro-N-[4-(7-methoxy-3,3-dimethyl-2-oxo-2,3-dihydro-indol-1-ylmethyl)-cyclohexyl]-5-trifluoromethyl-benzamide
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C26H28ClF3N2O3
 1
1
IC50 = 1685 nM
   TI
   LI
   LO
   TS
CP0902358
Trans-2-Chloro-N-[4-(3-ethyl-2-oxo-2,3-dihydro-bcnzoimidazol-1-ylmethyl)-cyclohexyl]-5-trifluoromethyl-benzamide
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C24H25ClF3N3O2
 1
1
IC50 = 1948 nM
   TI
   LI
   LO
   TS
CP0431983
US8835444, 5.27
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C21H25ClF3N3O
 1
1
IC50 = 2026 nM
   TI
   LI
   LO
   TS
CP0849229
Trans-2-Chloro-5-trifluoromethyl-N-[4-(3,3,7-trimethyl-2-oxo-2,3-dihydro-indol-1-ylmethyl)-cyclohexyl]-benzamide
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C26H28ClF3N2O2
 1
1
IC50 = 2137 nM
   TI
   LI
   LO
   TS
CP0904389
Trans-5-Chloro-N-[4-(6-methoxy-3,3-dimethyl-2-oxo-2,3-dihydro-indol-1-ylmethyl)-cyclohexyl]-2-methyl-nicotinamide
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C25H30ClN3O3
 1
1
IC50 = 3045 nM
   TI
   LI
   LO
   TS
CP0858046
Trans-5-Chloro-N-[4-(6-chloro-3,3-difluoro-2-oxo-2,3-dihydro-indol-1-ylmethyl)-cyclohexyl]-2-methyl-nicotinamide
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C22H21Cl2F2N3O2
 1
1
IC50 = 3124 nM
   TI
   LI
   LO
   TS
CP0902359
Trans-5-Chloro-2-methyl-N-[4-(3-methyl-2-oxo-2,3-dihydro-benzoimidazol-1-ylmethyl)-cyclohexyl]-nicotinamide
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C22H25ClN4O2
 1
1
IC50 = 3560 nM
   TI
   LI
   LO
   TS
CP0429711
US8835444, 3.6
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C23H26ClN5O
 1
1
IC50 = 3737 nM
   TI
   LI
   LO
   TS
CP0911674
Trans-5-chloro-N-[4-(3,3-dimethyl-2-oxo-2,3-dihydro-indol-1-ylmethyl)-cyclohexyl]-2-methyl nicotinamide
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C24H28ClN3O2
 1
1
IC50 = 3795 nM
   TI
   LI
   LO
   TS
CP0862005
Trans-2-Chloro-N-[4-(6-fluoro-2-oxo-2,3-dihydro-indol-1-ylmethyl)-cyclohexyl]-5-trifluoromethyl-bcnzamide
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C23H21ClF4N2O2
 1
1
IC50 = 3874 nM
   TI
   LI
   LO
   TS
CP0860149
Trans-2-chloro-N-[4-(3,3-dimethyl-2-oxo-2,3-dihydro-pyrrolo[2,3-b]pyridin-1-ylmethyl)-cyclohexyl]-5-trifluoromethyl-benzamide
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C23H25ClFN3O2
 1
1
IC50 = 4587 nM
   TI
   LI
   LO
   TS
CP0911855
Trans-5-Chloro-N-[4-(6-chloro-3,3-dimethyl-2-oxo-2,3-dihydro-indol-1-ylmethyl)-cyclohexyl]-2-methyl-nicotinamide
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C24H27Cl2N3O2
 1
1
IC50 = 4620 nM
   TI
   LI
   LO
   TS
CP0441516
US8835444, 3.3
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C24H26ClFN4O
 1
1
IC50 = 4630 nM
   TI
   LI
   LO
   TS
CP0871599
Trans-5-Chloro-2-methyl-N-[4-(3,3,4-trimethyl-2-oxo-2,3-dihydro-indol-1-ylmethyl)-cyclohexyl]-nicotinamide
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C25H30ClN3O2
 1
1
IC50 = 4810 nM
   TI
   LI
   LO
   TS
CP0416315
US8835444, 5.21
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C19H20Cl2F3N3O2
 1
1
IC50 = 4847 nM
   TI
   LI
   LO
   TS
CP0879022
US8835444, 1.1
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C20H28ClN5O
 1
1
IC50 = 4878 nM
   TI
   LI
   LO
   TS
CP0425467
US8835444, 2.4
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C24H27ClN4O
 1
1
IC50 = 4943 nM
   TI
   LI
   LO
   TS
CP0456085
9-chloro-6-[(1R)-1-(difluoromethoxy)-2,2,2-trifluoroethyl]-1-(2-methoxy-4,6-dimethylpyrimidin-5-yl)-3,4-dihydro-2H-pyrimido[1,2-a]benzimidazole
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C20H19ClF5N5O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0275883
5-[[cyclopropylmethyl(propyl)amino]methyl]-N-(2,4,6-trichlorophenyl)-4-(trifluoromethyl)-1,3-thiazol-2-amine
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C18H19Cl3F3N3S
 1
1 IC50 = 10000 nM
Clinical Information about the Protein
Target 1 ( Corticotropin-releasing factor receptor 2 (CRHR2) )
Target Type Clinical trial Target
Disease 2 Target-related Diseases  2
1 Eating disorder [ICD-11: 6B82]
2 Anxiety disorder [ICD-11: 6B00-6B0Z]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 NBI-34041 Phase 1
Eating disorder
Discontinued Drug(s) 1 Discontinued Drug  1
1 SC-241 Terminated
Anxiety disorder