Details of the Target

General Information of Target

Target ID LDTP02854
Target Name Thyrotropin receptor (TSHR)
Gene Name TSHR
Gene ID 7253
Synonyms
LGR3; Thyrotropin receptor; Thyroid-stimulating hormone receptor; TSH-R
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MRPADLLQLVLLLDLPRDLGGMGCSSPPCECHQEEDFRVTCKDIQRIPSLPPSTQTLKLI
ETHLRTIPSHAFSNLPNISRIYVSIDVTLQQLESHSFYNLSKVTHIEIRNTRNLTYIDPD
ALKELPLLKFLGIFNTGLKMFPDLTKVYSTDIFFILEITDNPYMTSIPVNAFQGLCNETL
TLKLYNNGFTSVQGYAFNGTKLDAVYLNKNKYLTVIDKDAFGGVYSGPSLLDVSQTSVTA
LPSKGLEHLKELIARNTWTLKKLPLSLSFLHLTRADLSYPSHCCAFKNQKKIRGILESLM
CNESSMQSLRQRKSVNALNSPLHQEYEENLGDSIVGYKEKSKFQDTHNNAHYYVFFEEQE
DEIIGFGQELKNPQEETLQAFDSHYDYTICGDSEDMVCTPKSDEFNPCEDIMGYKFLRIV
VWFVSLLALLGNVFVLLILLTSHYKLNVPRFLMCNLAFADFCMGMYLLLIASVDLYTHSE
YYNHAIDWQTGPGCNTAGFFTVFASELSVYTLTVITLERWYAITFAMRLDRKIRLRHACA
IMVGGWVCCFLLALLPLVGISSYAKVSICLPMDTETPLALAYIVFVLTLNIVAFVIVCCC
YVKIYITVRNPQYNPGDKDTKIAKRMAVLIFTDFICMAPISFYALSAILNKPLITVSNSK
ILLVLFYPLNSCANPFLYAIFTKAFQRDVFILLSKFGICKRQAQAYRGQRVPPKNSTDIQ
VQKVTHDMRQGLHNMEDVYELIENSHLTPKKQGQISEEYMQTVL
Target Type
Successful
Target Bioclass
GPCR
Family
G-protein coupled receptor 1 family, FSH/LSH/TSH subfamily
Subcellular location
Cell membrane
Function
Receptor for the thyroid-stimulating hormone (TSH) or thyrotropin. Also acts as a receptor for the heterodimeric glycoprotein hormone (GPHA2:GPHB5) or thyrostimulin. The activity of this receptor is mediated by G proteins which activate adenylate cyclase. Plays a central role in controlling thyroid cell metabolism.
TTD ID
T60606
Uniprot ID
P16473
DrugMap ID
TT6NYJA
Ensemble ID
ENST00000342443.10
HGNC ID
HGNC:12373
ChEMBL ID
CHEMBL1963

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Acrolein
 Probe Info  		N.A.  LDD0227  [2]
Crotonaldehyde
 Probe Info  		N.A.  LDD0219  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0109  NEM HeLa N.A.  LDD0227  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Synaptotagmin-1 (SYT1) Synaptotagmin family P21579
GPCR
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Adenosine receptor A1 (ADORA1) G-protein coupled receptor 1 family P30542
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein scribble homolog (SCRIB) LAP (LRR and PDZ) protein family Q14160
Mid1-interacting protein 1 (MID1IP1) SPOT14 family Q9NPA3

The Drug(s) Related To This Target

Approved
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Thyrotropin Alfa BiotechDrug DB00024
Thyrotropin . D03EER
Thyrotropin Alfa . D0H4TQ
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Recombinant Tsh Superagonists . D0U2DY

References

1 Labeling Preferences of Diazirines with Protein Biomolecules. J Am Chem Soc. 2021 May 5;143(17):6691-6700. doi: 10.1021/jacs.1c02509. Epub 2021 Apr 20.
Mass spectrometry data entry: PXD025140
2 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.