General Information of the Protein
Protein ID
PT02513
Protein Name
Steroid hormone receptor ERR1
Secondarily
Protein Name
Estrogen receptor-like 1
Estrogen-related receptor alpha
Nuclear receptor subfamily 3 group B member 1
Gene Name
ESRRA
Secondarily
Gene Name
ERR1
ESRL1
NR3B1
Sequence
MSSQVVGIEPLYIKAEPASPDSPKGSSETETEPPVALAPGPAPTRCLPGHKEEEDGEGAGPGEQGGGKLVLSSLPKRLCLVCGDVASGYHYGVASCEACKAFFKRTIQGSIEYSCPASNECEITKRRRKACQACRFTKCLRVGMLKEGVRLDRVRGGRQKYKRRPEVDPLPFPGPFPAGPLAVAGGPRKTAAPVNALVSHLLVVEPEKLYAMPDPAGPDGHLPAVATLCDLFDREIVVTISWAKSIPGFSSLSLSDQMSVLQSVWMEVLVLGVAQRSLPLQDELAFAEDLVLDEEGARAAGLGELGAALLQLVRRLQALRLEREEYVLLKALALANSDSVHIEDAEAVEQLREALHEALLEYEAGRAGPGGGAERRRAGRLLLTLPLLRQTAGKVLAHFYGVKLEGKVPMHKLFLEMLEAMMD
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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 1
Function
Binds to an ERR-alpha response element (ERRE) containing a single consensus half-site, 5'-TNAAGGTCA-3'. Can bind to the medium-chain acyl coenzyme A dehydrogenase (MCAD) response element NRRE-1 and may act as an important regulator of MCAD promoter. Binds to the C1 region of the lactoferrin gene promoter. Requires dimerization and the coactivator, PGC-1A, for full activity. The ERRalpha/PGC1alpha complex is a regulator of energy metabolism. Induces the expression of PERM1 in the skeletal muscle.
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Uniprot ID
Primary ID:
P11474

Secondarily ID:
Q14514
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Ensembl ID
ENSG00000173153
HGNC ID
HGNC:3471
Subcellular Location
Nucleus
Cytoplasm
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: CL000044 , CV-1
Compound ID Compound Name Compound Formula
CP0077611
3-[4-(2,4-Bis-trifluoromethyl-benzyloxy)-3-methoxy-phenyl]-2-cyano-N-(5-trifluoromethyl-[1,3,4]thiadiazol-2-yl)-acrylamide
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C23H13F9N4O3S
 1
1
IC50 = 370 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0155947
(7R,8R,9S,13S,14S,17S)-7-[4-[1-(2,3-dihydro-1,4-benzodioxin-3-ylmethyl)triazol-4-yl]butyl]-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol
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C33H41N3O4
 1
1 IC50 = 24.4 nM
CP0654308
4-[4-(2,4-Dioxothiazolidin-5-ylidenemethyl)-2-methoxyphenoxy]-3-trifluoromethylbenzonitrile
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C19H11F3N2O4S
 1
1 IC50 = 33 nM
CP0077611
3-[4-(2,4-Bis-trifluoromethyl-benzyloxy)-3-methoxy-phenyl]-2-cyano-N-(5-trifluoromethyl-[1,3,4]thiadiazol-2-yl)-acrylamide
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C23H13F9N4O3S
 2
1 IC50 = 61.33 nM
2 IC50 = 370 nM
CP0067467
3-[4-[4-[(7R,8R,9S,13S,14S,17S)-3,17-dihydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-7-yl]butyl]triazol-1-yl]-7-hydroxychromen-2-one
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C33H37N3O5
 1
1 IC50 = 116 nM
CP0142465
(7R,8R,9S,13S,14S,17S)-13-methyl-7-[6-[4-(1,2-oxazol-5-yl)phenyl]hex-5-ynyl]-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol
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C33H37NO3
 1
1 IC50 = 481.8 nM
CP0067468
tert-butyl 4-[4-[6-[(7R,8R,9S,13S,14S,17S)-3,17-dihydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-7-yl]hex-1-ynyl]phenyl]piperazine-1-carboxylate
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C39H52N2O4
 1
1 IC50 = 567.4 nM
Clinical Information about the Protein
Target 1 ( Estrogen-related receptor-alpha (ESRRA) )
Target Type Successful Target
Disease 2 Target-related Diseases  2
1 Arthritis [ICD-11: FA20]
2 Schizophrenia [ICD-11: 6A20]
Approved Drug(s) 2 Approved Drugs  2
1 Rimexolone Approved
Arthritis
2 Pregnenolone Phase 4
Schizophrenia