General Information of the Protein
Protein ID
PT03374
Protein Name
Estrogen-related receptor gamma
Secondarily
Protein Name
ERR gamma-2
Estrogen receptor-related protein 3
Nuclear receptor subfamily 3 group B member 3
Gene Name
ESRRG
Secondarily
Gene Name
ERR3
ERRG2
KIAA0832
NR3B3
Sequence
MDSVELCLPESFSLHYEEELLCRMSNKDRHIDSSCSSFIKTEPSSPASLTDSVNHHSPGGSSDASGSYSSTMNGHQNGLDSPPLYPSAPILGGSGPVRKLYDDCSSTIVEDPQTKCEYMLNSMPKRLCLVCGDIASGYHYGVASCEACKAFFKRTIQGNIEYSCPATNECEITKRRRKSCQACRFMKCLKVGMLKEGVRLDRVRGGRQKYKRRIDAENSPYLNPQLVQPAKKPYNKIVSHLLVAEPEKIYAMPDPTVPDSDIKALTTLCDLADRELVVIIGWAKHIPGFSTLSLADQMSLLQSAWMEILILGVVYRSLSFEDELVYADDYIMDEDQSKLAGLLDLNNAILQLVKKYKSMKLEKEEFVTLKAIALANSDSMHIEDVEAVQKLQDVLHEALQDYEAGQHMEDPRRAGKMLMTLPLLRQTSTKAVQHFYNIKLEGKVPMHKLFLEMLEAKV
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Organism
Homo sapiens, Human
Protein Classification
Transcription factor
>
Nuclear receptor
>
Nuclear hormone receptor subfamily 3
>
Nuclear hormone receptor subfamily 3 group B
>
Nuclear hormone receptor subfamily 3 group B member 3
Function
Orphan receptor that acts as a transcription activator in the absence of bound ligand. Binds specifically to an estrogen response element and activates reporter genes controlled by estrogen response elements (By similarity). Induces the expression of PERM1 in the skeletal muscle.
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Uniprot ID
Primary ID:
P62508

Secondarily ID:
A8K4I0
A8K6I2
B3KY84
E9PGB7
F8W8J3
O75454
O96021
Q68DA0
Q6P274
Q6PK28
Q6TS38
Q9R1F3
Q9UNJ4
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Ensembl ID
ENSG00000196482
HGNC ID
HGNC:3474
Subcellular Location
Nucleus
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: CL000192 , AD-293
Compound ID Compound Name Compound Formula
CP0164237
4-[(E)-5-hydroxy-2-phenyl-1-[4-(4-propan-2-ylpiperazin-1-yl)phenyl]pent-1-enyl]phenol;dihydrochloride
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C30H38Cl2N2O2
 1
1
IC50 = 6 nM
   TI
   LI
   LO
   TS
CP0096836
(Z)-5-[4-(4-ethylpiperazin-1-yl)phenyl]-5-(4-methylphenyl)-4-phenylpent-4-en-1-ol;dihydrochloride
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C30H38Cl2N2O
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0117254
(Z)-5-(4-methylphenyl)-4-phenyl-5-[4-(4-propan-2-ylpiperazin-1-yl)phenyl]pent-4-en-1-ol;dihydrochloride
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C31H40Cl2N2O
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0344043
(E)-5-(3-bromophenyl)-4-phenyl-5-[4-(4-propan-2-ylpiperazin-1-yl)phenyl]pent-4-en-1-ol;dihydrochloride
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C30H37BrCl2N2O
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0143014
3-[(E)-5-hydroxy-2-phenyl-1-[4-(4-propan-2-ylpiperazin-1-yl)phenyl]pent-1-enyl]phenol;dihydrochloride
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C30H38Cl2N2O2
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0131412
4-[(Z)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-5-fluoro-2-phenylpent-1-enyl]phenol;hydrochloride
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C27H31ClFNO2
 1
1
IC50 = 48 nM
   TI
   LI
   LO
   TS
CP0133940
4-[(Z)-1-[4-[3-(dimethylamino)propoxy]phenyl]-5-hydroxy-2-phenylpent-1-enyl]phenol;hydrochloride
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C28H34ClNO3
 1
1
IC50 = 58 nM
   TI
   LI
   LO
   TS
CP0536297
(E)-5-(4-bromophenyl)-4-phenyl-5-[4-(4-propan-2-ylpiperazin-1-yl)phenyl]pent-4-en-1-ol;dihydrochloride
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C30H37BrCl2N2O
 1
1
IC50 = 64 nM
   TI
   LI
   LO
   TS
CP0060960
(Z)-5-(4-methylphenyl)-4-phenyl-5-(4-piperazin-1-ylphenyl)pent-4-en-1-ol;dihydrochloride
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C28H34Cl2N2O
 1
1
IC50 = 65 nM
   TI
   LI
   LO
   TS
CP0060959
(Z)-5-(4-methylphenyl)-5-[4-(4-methylpiperazin-1-yl)phenyl]-4-phenylpent-4-en-1-ol;dihydrochloride
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C29H36Cl2N2O
 1
1
IC50 = 69 nM
   TI
   LI
   LO
   TS
CP0739308
4-[(Z)-1-[4-(2-dimethylaminoethyloxy)phenyl]-5-hydroxy-2-phenyl-pent-1-enyl]phenol hydrochloride salt
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C27H32ClNO3
 1
1
IC50 = 77 nM
   TI
   LI
   LO
   TS
CP0132048
4-[(Z)-1-[4-[2-(diethylamino)ethoxy]phenyl]-5-hydroxy-2-phenylpent-1-enyl]phenol;hydrochloride
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C29H36ClNO3
 1
1
IC50 = 79 nM
   TI
   LI
   LO
   TS
CP0197679
4-[(Z)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-5,5-difluoro-2-phenylpent-1-enyl]phenol;hydrochloride
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C27H30ClF2NO2
 1
1
IC50 = 111 nM
   TI
   LI
   LO
   TS
CP0316921
4-[(Z)-5-hydroxy-1-[4-[2-(methylamino)ethoxy]phenyl]-2-phenylpent-1-enyl]phenol;hydrochloride
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C26H30ClNO3
 1
1
IC50 = 187 nM
   TI
   LI
   LO
   TS
CP0182080
(Z)-5-[4-[2-(dimethylamino)ethoxy]phenyl]-5-(4-methylphenyl)-4-phenylpent-4-en-1-ol;hydrochloride
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C28H34ClNO2
 1
1
IC50 = 669 nM
   TI
   LI
   LO
   TS
CP0182081
(E)-5-(4-bromophenyl)-5-[4-[2-(dimethylamino)ethoxy]phenyl]-4-phenylpent-4-en-1-ol;hydrochloride
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C27H31BrClNO2
 1
1
IC50 = 719 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0648741
4-Hydroxytamoxifen
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C26H29NO2
 2
1 IC50 = 11 nM
2 IC50 = 13 nM
CP0117254
(Z)-5-(4-methylphenyl)-4-phenyl-5-[4-(4-propan-2-ylpiperazin-1-yl)phenyl]pent-4-en-1-ol;dihydrochloride
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C31H40Cl2N2O
 1
1 IC50 = 17 nM
CP0131412
4-[(Z)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-5-fluoro-2-phenylpent-1-enyl]phenol;hydrochloride
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C27H31ClFNO2
 1
1 IC50 = 20 nM
CP0536297
(E)-5-(4-bromophenyl)-4-phenyl-5-[4-(4-propan-2-ylpiperazin-1-yl)phenyl]pent-4-en-1-ol;dihydrochloride
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C30H37BrCl2N2O
 1
1 IC50 = 21 nM
CP0096836
(Z)-5-[4-(4-ethylpiperazin-1-yl)phenyl]-5-(4-methylphenyl)-4-phenylpent-4-en-1-ol;dihydrochloride
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C30H38Cl2N2O
 1
1 IC50 = 25 nM
CP0060959
(Z)-5-(4-methylphenyl)-5-[4-(4-methylpiperazin-1-yl)phenyl]-4-phenylpent-4-en-1-ol;dihydrochloride
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C29H36Cl2N2O
 1
1 IC50 = 26 nM
CP0060960
(Z)-5-(4-methylphenyl)-4-phenyl-5-(4-piperazin-1-ylphenyl)pent-4-en-1-ol;dihydrochloride
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C28H34Cl2N2O
 1
1 IC50 = 27 nM
CP0344043
(E)-5-(3-bromophenyl)-4-phenyl-5-[4-(4-propan-2-ylpiperazin-1-yl)phenyl]pent-4-en-1-ol;dihydrochloride
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C30H37BrCl2N2O
 1
1 IC50 = 33 nM
CP0143014
3-[(E)-5-hydroxy-2-phenyl-1-[4-(4-propan-2-ylpiperazin-1-yl)phenyl]pent-1-enyl]phenol;dihydrochloride
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C30H38Cl2N2O2
 1
1 IC50 = 35 nM
CP0164237
4-[(E)-5-hydroxy-2-phenyl-1-[4-(4-propan-2-ylpiperazin-1-yl)phenyl]pent-1-enyl]phenol;dihydrochloride
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C30H38Cl2N2O2
 1
1 IC50 = 40 nM
CP0133940
4-[(Z)-1-[4-[3-(dimethylamino)propoxy]phenyl]-5-hydroxy-2-phenylpent-1-enyl]phenol;hydrochloride
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C28H34ClNO3
 1
1 IC50 = 90 nM
CP0739308
4-[(Z)-1-[4-(2-dimethylaminoethyloxy)phenyl]-5-hydroxy-2-phenyl-pent-1-enyl]phenol hydrochloride salt
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C27H32ClNO3
 1
1 IC50 = 110 nM
CP0182081
(E)-5-(4-bromophenyl)-5-[4-[2-(dimethylamino)ethoxy]phenyl]-4-phenylpent-4-en-1-ol;hydrochloride
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C27H31BrClNO2
 1
1 IC50 = 117 nM
CP0132048
4-[(Z)-1-[4-[2-(diethylamino)ethoxy]phenyl]-5-hydroxy-2-phenylpent-1-enyl]phenol;hydrochloride
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C29H36ClNO3
 1
1 IC50 = 180 nM
CP0316921
4-[(Z)-5-hydroxy-1-[4-[2-(methylamino)ethoxy]phenyl]-2-phenylpent-1-enyl]phenol;hydrochloride
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C26H30ClNO3
 1
1 IC50 = 190 nM
CP0182080
(Z)-5-[4-[2-(dimethylamino)ethoxy]phenyl]-5-(4-methylphenyl)-4-phenylpent-4-en-1-ol;hydrochloride
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C28H34ClNO2
 1
1 IC50 = 270 nM
CP0197679
4-[(Z)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-5,5-difluoro-2-phenylpent-1-enyl]phenol;hydrochloride
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C27H30ClF2NO2
 1
1 IC50 = 480 nM
CP0174777
4-Hydroxy-benzoic acid (4-isopropyl-benzylidene)-hydrazide
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C17H18N2O2
 2
1 IC50 = 2000 nM
2 Kd = 5000 nM
Clinical Information about the Protein
Target 1 ( Estrogen-related receptor-gamma (ESRRG) )
Target Type Literature-reported Target
Similar Protein(s) and Bioactivity Statistics
100% Identity
Protein ID Protein Name Protein Organism
PT03765 Estrogen-related receptor gamma Mus musculus, Mouse