General Information of Target

Target ID LDTP15820
Target Name Trace amine-associated receptor 1 (TAAR1)
Gene Name TAAR1
Gene ID 134864
Synonyms
TA1; TAR1; TRAR1; Trace amine-associated receptor 1; TaR-1; Trace amine receptor 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MVNNFSQAEAVELCYKNVNESCIKTPYSPGPRSILYAVLGFGAVLAAFGNLLVMIAILHF
KQLHTPTNFLIASLACADFLVGVTVMPFSTVRSVESCWYFGDSYCKFHTCFDTSFCFASL
FHLCCISVDRYIAVTDPLTYPTKFTVSVSGICIVLSWFFSVTYSFSIFYTGANEEGIEEL
VVALTCVGGCQAPLNQNWVLLCFLLFFIPNVAMVFIYSKIFLVAKHQARKIESTASQAQS
SSESYKERVAKRERKAAKTLGIAMAAFLVSWLPYLVDAVIDAYMNFITPPYVYEILVWCV
YYNSAMNPLIYAFFYQWFGKAIKLIVSGKVLRTDSSTTNLFSEEVETD
Target Type
Successful
Target Bioclass
GPCR
Family
G-protein coupled receptor 1 family
Subcellular location
Cell membrane
Function
Receptor for trace amines, including beta-phenylethylamine (b-PEA), p-tyramine (p-TYR), octopamine and tryptamine, with highest affinity for b-PEA and p-TYR. Unresponsive to classical biogenic amines, such as epinephrine and histamine and only partially activated by dopamine and serotonin. Trace amines are biogenic amines present in very low levels in mammalian tissues. Although some trace amines have clearly defined roles as neurotransmitters in invertebrates, the extent to which they function as true neurotransmitters in vertebrates has remained speculative. Trace amines are likely to be involved in a variety of physiological functions that have yet to be fully understood. The signal transduced by this receptor is mediated by the G(s)-class of G-proteins which activate adenylate cyclase.
TTD ID
T99524
Uniprot ID
Q96RJ0
DrugMap ID
TTIU98M
Ensemble ID
ENST00000275216.3
HGNC ID
HGNC:17734
ChEMBL ID
CHEMBL5857

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
BTD
 Probe Info 
C13(1.25)  LDD2094  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0548  1-(4-(Benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)-2-nitroethan-1-one MDA-MB-231 C13(0.88)  LDD2142  [1]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C13(1.20)  LDD2112  [1]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C13(1.25)  LDD2094  [1]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C13(0.64)  LDD2104  [1]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C13(1.00)  LDD2105  [1]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C13(0.95)  LDD2106  [1]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C13(0.94)  LDD2141  [1]

References

1 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761