Details of the Target

General Information of Target

Target ID LDTP03112
Target Name Substance-K receptor (TACR2)
Gene Name TACR2
Gene ID 6865
Synonyms
NK2R; NKNAR; TAC2R; Substance-K receptor; SKR; NK-2 receptor; NK-2R; Neurokinin A receptor; Tachykinin receptor 2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGTCDIVTEANISSGPESNTTGITAFSMPSWQLALWATAYLALVLVAVTGNAIVIWIILA
HRRMRTVTNYFIVNLALADLCMAAFNAAFNFVYASHNIWYFGRAFCYFQNLFPITAMFVS
IYSMTAIAADRYMAIVHPFQPRLSAPSTKAVIAGIWLVALALASPQCFYSTVTMDQGATK
CVVAWPEDSGGKTLLLYHLVVIALIYFLPLAVMFVAYSVIGLTLWRRAVPGHQAHGANLR
HLQAMKKFVKTMVLVVLTFAICWLPYHLYFILGSFQEDIYCHKFIQQVYLALFWLAMSST
MYNPIIYCCLNHRFRSGFRLAFRCCPWVTPTKEDKLELTPTTSLSTRVNRCHTKETLFMA
GDTAPSEATSGEAGRPQDGSGLWFGYGLLAPTKTHVEI
Target Type
Clinical trial
Target Bioclass
GPCR
Family
G-protein coupled receptor 1 family
Subcellular location
Cell membrane
Function
This is a receptor for the tachykinin neuropeptide substance K (neurokinin A). It is associated with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of affinity of this receptor to tachykinins is: substance K > neuromedin-K > substance P.
TTD ID
T52790
Uniprot ID
P21452
DrugMap ID
TTYO0A3
Ensemble ID
ENST00000373306.5
HGNC ID
HGNC:11527
ChEMBL ID
CHEMBL2327

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
BTD
 Probe Info  		C281(1.30)  LDD1700  [1]
Acrolein
 Probe Info  		N.A.  LDD0221  [2]

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 C281(0.67)  LDD2142  [1]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C281(0.76)  LDD2112  [1]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [2]
 LDCM0107  IAA HeLa N.A.  LDD0221  [2]
 LDCM0109  NEM HeLa N.A.  LDD0223  [2]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C281(0.54)  LDD2100  [1]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C281(0.57)  LDD2106  [1]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C281(0.63)  LDD2108  [1]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C281(0.53)  LDD2114  [1]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C281(1.30)  LDD1700  [1]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C281(0.73)  LDD2141  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ibodutant Small molecular drug D0XS4X
Phase 2
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Nepadutant Small molecular drug D0S6JV
Pmx-53 Small molecular drug D0G2XE
Rambazole Small molecular drug D0AA6Z
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Slv-332 Small molecular drug D02NMG
Investigative
Click To Hide/Show 15 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Small molecular drug D0T2RY
A-987306 Small molecular drug D0F9QT
Gr100679 Small molecular drug D08SGF
Gr94800 Small molecular drug D0RR7X
Hoo-phe-orn-pro-hle-pff-phe-nh2 Small molecular drug D00HAJ
Neurokinin A Small molecular drug D01NPA
R396 Small molecular drug D07CVE
Sch 206272 Small molecular drug D07JAN
Way-207024 Small molecular drug D0C7LY
Ym44778 Small molecular drug D0ZJ6Y
Ym44781 Small molecular drug D0U4WP
Ym49598 Small molecular drug D0N1PH
Zd-6021 Small molecular drug D0Z6TG
Zm 253270 Small molecular drug D05DYX
Zm-274773 Small molecular drug D0KX3C
Discontinued
Click To Hide/Show 14 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cs-003 Small molecular drug D03ZKE
Dnk-333 Small molecular drug D0C9FF
Fk-224 Small molecular drug D02FIJ
Gr-159897 Small molecular drug D02YWV
L-732138 Small molecular drug D08ZBV
Men-10627 Small molecular drug D04RCG
Saredutant Small molecular drug D05WJQ
Sr 144190 Small molecular drug D0E9EE
Uk-224671 Small molecular drug D08WVA
Zd-7944 Small molecular drug D0J3QU
Ave-5883 . D0Y4GJ
Azd-5106 . D09KLO
Men-10207 . D0IW0Y
Uk-290795 . D0S1RT

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
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.