Details of the Target

General Information of Target

Target ID LDTP12409
Target Name Transient receptor potential cation channel subfamily V member 5 (TRPV5)
Gene Name TRPV5
Gene ID 56302
Synonyms
ECAC1; Transient receptor potential cation channel subfamily V member 5; TrpV5; Calcium transport protein 2; CaT2; Epithelial calcium channel 1; ECaC; ECaC1; Osm-9-like TRP channel 3; OTRPC3
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MESNHKSGDGLSGTQKEAALRALVQRTGYSLVQENGQRKYGGPPPGWDAAPPERGCEIFI
GKLPRDLFEDELIPLCEKIGKIYEMRMMMDFNGNNRGYAFVTFSNKVEAKNAIKQLNNYE
IRNGRLLGVCASVDNCRLFVGGIPKTKKREEILSEMKKVTEGVVDVIVYPSAADKTKNRG
FAFVEYESHRAAAMARRKLLPGRIQLWGHGIAVDWAEPEVEVDEDTMSSVKILYVRNLML
STSEEMIEKEFNNIKPGAVERVKKIRDYAFVHFSNREDAVEAMKALNGKVLDGSPIEVTL
AKPVDKDSYVRYTRGTGGRGTMLQGEYTYSLGQVYDPTTTYLGAPVFYAPQTYAAIPSLH
FPATKGHLSNRAIIRAPSVREIYMNVPVGAAGVRGLGGRGYLAYTGLGRGYQVKGDKRED
KLYDILPGMELTPMNPVTLKPQGIKLAPQILEEICQKNNWGQPVYQLHSAIGQDQRQLFL
YKITIPALASQNPAIHPFTPPKLSAFVDEAKTYAAEYTLQTLGIPTDGGDGTMATAAAAA
TAFPGYAVPNATAPVSAAQLKQAVTLGQDLAAYTTYEVYPTFAVTARGDGYGTF
Target Bioclass
Transporter and channel
Family
Transient receptor (TC 1.A.4) family, TrpV subfamily, TRPV5 sub-subfamily
Subcellular location
Apical cell membrane
Function
Constitutively active calcium selective cation channel thought to be involved in Ca(2+) reabsorption in kidney and intestine. Required for normal Ca(2+) reabsorption in the kidney distal convoluted tubules. The channel is activated by low internal calcium level and the current exhibits an inward rectification. A Ca(2+)-dependent feedback regulation includes fast channel inactivation and slow current decay. Heteromeric assembly with TRPV6 seems to modify channel properties. TRPV5-TRPV6 heteromultimeric concatemers exhibit voltage-dependent gating.
Uniprot ID
Q9NQA5
Ensemble ID
ENST00000265310.6
HGNC ID
HGNC:3145
ChEMBL ID
CHEMBL1628474

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
HHS-475
 Probe Info  		Y647(0.91)  LDD0264  [1]
HHS-465
 Probe Info  		Y647(9.31)  LDD2237  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0116  HHS-0101 DM93 Y647(0.91)  LDD0264  [1]
 LDCM0117  HHS-0201 DM93 Y647(0.85)  LDD0265  [1]
 LDCM0118  HHS-0301 DM93 Y647(0.96)  LDD0266  [1]
 LDCM0119  HHS-0401 DM93 Y647(0.84)  LDD0267  [1]
 LDCM0120  HHS-0701 DM93 Y647(1.06)  LDD0268  [1]

References

1 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
2 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.