General Information of the Protein
Protein ID
PT04462
Protein Name
Thyrotropin receptor
Secondarily
Protein Name
Thyroid-stimulating hormone receptor
Gene Name
TSHR
Secondarily
Gene Name
LGR3
Sequence
MRPADLLQLVLLLDLPRDLGGMGCSSPPCECHQEEDFRVTCKDIQRIPSLPPSTQTLKLIETHLRTIPSHAFSNLPNISRIYVSIDVTLQQLESHSFYNLSKVTHIEIRNTRNLTYIDPDALKELPLLKFLGIFNTGLKMFPDLTKVYSTDIFFILEITDNPYMTSIPVNAFQGLCNETLTLKLYNNGFTSVQGYAFNGTKLDAVYLNKNKYLTVIDKDAFGGVYSGPSLLDVSQTSVTALPSKGLEHLKELIARNTWTLKKLPLSLSFLHLTRADLSYPSHCCAFKNQKKIRGILESLMCNESSMQSLRQRKSVNALNSPLHQEYEENLGDSIVGYKEKSKFQDTHNNAHYYVFFEEQEDEIIGFGQELKNPQEETLQAFDSHYDYTICGDSEDMVCTPKSDEFNPCEDIMGYKFLRIVVWFVSLLALLGNVFVLLILLTSHYKLNVPRFLMCNLAFADFCMGMYLLLIASVDLYTHSEYYNHAIDWQTGPGCNTAGFFTVFASELSVYTLTVITLERWYAITFAMRLDRKIRLRHACAIMVGGWVCCFLLALLPLVGISSYAKVSICLPMDTETPLALAYIVFVLTLNIVAFVIVCCCYVKIYITVRNPQYNPGDKDTKIAKRMAVLIFTDFICMAPISFYALSAILNKPLITVSNSKILLVLFYPLNSCANPFLYAIFTKAFQRDVFILLSKFGICKRQAQAYRGQRVPPKNSTDIQVQKVTHDMRQGLHNMEDVYELIENSHLTPKKQGQISEEYMQTVL
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Glycohormone receptor
>
Glycohormone receptor
Function
Receptor for the thyroid-stimulating hormone (TSH) or thyrotropin (PubMed:11847099, PubMed:12045258). Also acts as a receptor for the heterodimeric glycoprotein hormone (GPHA2:GPHB5) or thyrostimulin (PubMed:12045258). The activity of this receptor is mediated by G proteins which activate adenylate cyclase (PubMed:11847099). Plays a central role in controlling thyroid cell metabolism (By similarity).
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Uniprot ID
Primary ID:
P16473

Secondarily ID:
A0PJU7
F5GYU5
G3V2A9
Q16503
Q8TB90
Q96GT6
Q9P1V4
Q9ULA3
Q9UPH3
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Ensembl ID
ENSG00000165409
HGNC ID
HGNC:12373
Subcellular Location
Cell membrane
Basolateral 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: CL001022 , HEK293EM
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0447021
 Compound Info 
N-[4-[[5-(3-benzyl-5-hydroxy-4-oxo-1,2-dihydroquinazolin-2-yl)-2-methoxyphenyl]methylsulfanyl]phenyl]acetamide
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C31H29N3O4S
  1
1
EC50 = 18 nM
 Bioactivity Info 
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CP0440713
 Compound Info 
N-[4-[[5-(3-benzyl-4-oxo-1,2-dihydroquinazolin-2-yl)-2-methoxyphenyl]methylsulfanyl]phenyl]acetamide
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C31H29N3O3S
  1
1
EC50 = 80 nM
 Bioactivity Info 
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CP0540179
 Compound Info 
N-[4-[[5-(3-benzyl-5-hydroxy-4-oxo-1,2-dihydroquinazolin-2-yl)-2-methoxyphenyl]methoxy]phenyl]acetamide
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C31H29N3O5
  1
1
EC50 = 90 nM
 Bioactivity Info 
   TI
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CP0440711
 Compound Info 
N-[4-[[5-(3-benzyl-5-fluoro-4-oxo-1,2-dihydroquinazolin-2-yl)-2-methoxyphenyl]methoxy]phenyl]acetamide
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C31H28FN3O4
  1
1
EC50 = 280 nM
 Bioactivity Info 
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CP0514413
 Compound Info 
N-[4-[[5-(3-benzyl-4-oxo-1,2-dihydroquinazolin-2-yl)-2-methoxyphenyl]methoxy]phenyl]acetamide
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C31H29N3O4
  1
1
EC50 = 290 nM
 Bioactivity Info 
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CP0401098
 Compound Info 
N-[4-[[5-(3-benzyl-6-hydroxy-4-oxo-1,2-dihydroquinazolin-2-yl)-2-methoxyphenyl]methoxy]phenyl]acetamide
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C31H29N3O5
  1
1
EC50 = 330 nM
 Bioactivity Info 
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CP0492728
 Compound Info 
N-[4-[[2-methoxy-5-[4-oxo-3-(2-phenylethyl)-1,2-dihydroquinazolin-2-yl]phenyl]methoxy]phenyl]acetamide
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C32H31N3O4
  1
1
EC50 = 430 nM
 Bioactivity Info 
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CP0401097
 Compound Info 
N-[4-[[5-(3-benzyl-5-hydroxy-4-oxoquinazolin-2-yl)-2-methoxyphenyl]methoxy]phenyl]acetamide
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C31H27N3O5
  1
1
EC50 = 550 nM
 Bioactivity Info 
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CP0440712
 Compound Info 
N-[4-[[5-(3-butyl-4-oxo-1,2-dihydroquinazolin-2-yl)-2-methoxyphenyl]methoxy]phenyl]acetamide
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C28H31N3O4
  1
1
EC50 = 830 nM
 Bioactivity Info 
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CP0450927
 Compound Info 
N-[4-[[5-[3-(furan-2-ylmethyl)-4-oxoquinazolin-2-yl]-2-methoxyphenyl]methoxy]phenyl]acetamide
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C29H25N3O5
  1
1
EC50 = 930 nM
 Bioactivity Info 
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CP0415668
 Compound Info 
N-[4-[[5-(3-benzyl-4-oxoquinazolin-2-yl)-2-methoxyphenyl]methoxy]phenyl]acetamide
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C31H27N3O4
  1
1
EC50 = 960 nM
 Bioactivity Info 
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CP0234854
 Compound Info 
MLS001073997
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C29H27N3O5
  1
1
EC50 = 1160 nM
 Bioactivity Info 
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CP0450925
 Compound Info 
N-[4-[[3-(3-benzyl-4-oxo-1,2-dihydroquinazolin-2-yl)phenyl]methoxy]phenyl]acetamide
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C30H27N3O3
  1
1
EC50 = 1860 nM
 Bioactivity Info 
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CP0411072
 Compound Info 
3-benzyl-2-[4-methoxy-3-[(4-methoxyphenoxy)methyl]phenyl]-1,2-dihydroquinazolin-4-one
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C30H28N2O4
  1
1
EC50 = 2160 nM
 Bioactivity Info 
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CP0450926
 Compound Info 
3-benzyl-2-[4-methoxy-3-(phenoxymethyl)phenyl]-1,2-dihydroquinazolin-4-one
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C29H26N2O3
  1
1
EC50 = 2570 nM
 Bioactivity Info 
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CP0450924
 Compound Info 
N-[4-[[2-methoxy-5-[4-oxo-3-(pyridin-4-ylmethyl)-1,2-dihydroquinazolin-2-yl]phenyl]methoxy]phenyl]acetamide
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C30H28N4O4
  1
1
EC50 = 3980 nM
 Bioactivity Info 
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CP0447019
 Compound Info 
N-[3-[[5-(3-benzyl-4-oxo-1,2-dihydroquinazolin-2-yl)-2-methoxyphenyl]methoxy]phenyl]acetamide
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C31H29N3O4
  1
1
EC50 = 4340 nM
 Bioactivity Info 
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CP0348903
 Compound Info 
N-[4-[[5-(3-benzyl-5-methoxy-4-oxo-1,2-dihydroquinazolin-2-yl)-2-methoxyphenyl]methoxy]phenyl]acetamide
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C32H31N3O5
  1
1
EC50 = 4480 nM
 Bioactivity Info 
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CP0401096
 Compound Info 
N-[4-[[2-methoxy-5-(4-oxo-3-phenyl-1,2-dihydroquinazolin-2-yl)phenyl]methoxy]phenyl]acetamide
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C30H27N3O4
  1
1
EC50 = 5090 nM
 Bioactivity Info 
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CP0115536
 Compound Info 
5-amino-N-tert-butyl-4-(3-methoxyphenyl)-2-methylsulfanylthieno[2,3-d]pyrimidine-6-carboxamide
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C19H22N4O2S2
  1
1
EC50 = 6500 nM
 Bioactivity Info 
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0115536
 Compound Info 
5-amino-N-tert-butyl-4-(3-methoxyphenyl)-2-methylsulfanylthieno[2,3-d]pyrimidine-6-carboxamide
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C19H22N4O2S2
  1
1 EC50 = 7700 nM
Clinical Information about the Protein
Target 1 ( Thyrotropin receptor (TSHR) )
Target Type Successful Target