Details of the Target

General Information of Target

Target ID LDTP04357
Target Name 5-hydroxytryptamine receptor 6 (HTR6)
Gene Name HTR6
Gene ID 3362
Synonyms
5-hydroxytryptamine receptor 6; 5-HT-6; 5-HT6; Serotonin receptor 6
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MVPEPGPTANSTPAWGAGPPSAPGGSGWVAAALCVVIALTAAANSLLIALICTQPALRNT
SNFFLVSLFTSDLMVGLVVMPPAMLNALYGRWVLARGLCLLWTAFDVMCCSASILNLCLI
SLDRYLLILSPLRYKLRMTPLRALALVLGAWSLAALASFLPLLLGWHELGHARPPVPGQC
RLLASLPFVLVASGLTFFLPSGAICFTYCRILLAARKQAVQVASLTTGMASQASETLQVP
RTPRPGVESADSRRLATKHSRKALKASLTLGILLGMFFVTWLPFFVANIVQAVCDCISPG
LFDVLTWLGYCNSTMNPIIYPLFMRDFKRALGRFLPCPRCPRERQASLASPSLRTSHSGP
RPGLSLQQVLPLPLPPDSDSDSDAGSGGSSGLRLTAQLLLPGEATQDPPLPTRAAAAVNF
FNIDPAEPELRPHPLGIPTN
Target Type
Clinical trial
Target Bioclass
GPCR
Family
G-protein coupled receptor 1 family
Subcellular location
Cell membrane
Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase. It has a high affinity for tricyclic psychotropic drugs. Controls pyramidal neurons migration during corticogenesis, through the regulation of CDK5 activity. Is an activator of TOR signaling.
TTD ID
T16691
Uniprot ID
P50406
DrugMap ID
TTJS8PY
Ensemble ID
ENST00000289753.2
HGNC ID
HGNC:5301
ChEMBL ID
CHEMBL3371

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
IA-alkyne
 Probe Info  		N.A.  LDD0165  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Tyrosine-protein kinase Fyn (FYN) Tyr protein kinase family P06241
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Microtubule-associated protein 1B (MAP1B) MAP1 family P46821
RNA-binding protein Nova-1 (NOVA1) . P51513

The Drug(s) Related To This Target

Approved
Click To Hide/Show 22 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Amitriptyline Small molecular drug DB00321
Amoxapine Small molecular drug DB00543
Aripiprazole Small molecular drug DB01238
Asenapine Small molecular drug DB06216
Chlorpromazine Small molecular drug DB00477
Chlorprothixene Small molecular drug DB01239
Clozapine Small molecular drug DB00363
Cyclobenzaprine Small molecular drug DB00924
Doxepin Small molecular drug DB01142
Gilteritinib Small molecular drug DB12141
Haloperidol Small molecular drug DB00502
Iloperidone Small molecular drug DB04946
Imipramine Small molecular drug DB00458
Loxapine Small molecular drug DB00408
Mianserin Small molecular drug DB06148
Olanzapine Small molecular drug DB00334
Paroxetine Small molecular drug DB00715
Quetiapine Small molecular drug DB01224
Sertindole Small molecular drug DB06144
Ziprasidone Small molecular drug DB00246
Zotepine Small molecular drug DB09225
Aripiprazole Lauroxil . DB14185
Phase 3
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Lu Ae58054 Small molecular drug D09IRN
Sb-742457 Small molecular drug D0R9HI
Avn 211 . D0WH4L
Phase 2
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Sam-531 Small molecular drug D0V4ZQ
Suvn-502 Small molecular drug D0Z0GX
Syn120 Small molecular drug D9I3WE
Avn 101 . D01NDF
Avn 322 . D0L8IO
Pf-05212377 . D0G1YA
Syn-120 . D07RQR
Phase 1
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Avn-322 Small molecular drug DWD06K
Bvt-74316 Small molecular drug D02KLD
Prx-07034 Small molecular drug D03ZPX
11c-gsk-215083 . D08PIK
Abt-354 . D0X9HF
Investigative
Click To Hide/Show 107 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1-(2-methoxy-phenyl)-piperazine Small molecular drug D0V4RP
1-(3-(Benzyloxy)-2-methylphenyl)Piperazine Small molecular drug D0S4XR
1-(3-(Pentafluorosulfanyl)Phenyl)Propan-2-amine Small molecular drug D0LG8A
1-(Phenylsulfonyl)-4-(Piperazin-1-yl)-1h-indole Small molecular drug D0TG0I
1-benzenesulfonyl-3-piperidin-3-yl-1h-indole Small molecular drug D02LFU
1-benzenesulfonyl-3-piperidin-4-yl-1h-indole Small molecular drug D0H5EP
1-naphthylpiperazine Small molecular drug D03TDN
1-phenylthio-n,N-dimethyltryptamine Small molecular drug D0J7EM
2-(1-(Phenylsulfonyl)-1h-indol-3-yl)Ethanamine Small molecular drug D02VHJ
2-(1-benzyl-1h-inden-3-yl)-n,N-dimethylethanamine Small molecular drug D0PQ1U
2-(1-benzyl-1h-indol-3-yl)-n,N-dimethylethanamine Small molecular drug D0T7VZ
2-(1-tosyl-1h-indol-3-yl)Ethanamine Small molecular drug D08SMK
2-(1h-indol-3-yl)-n,N-dimethylethanamine Small molecular drug D03DLZ
2-(3-(Phenylsulfonyl)-1h-indol-1-yl)Ethanamine Small molecular drug D0Y1LJ
2-(3-benzenesulfonyl)Phenyl-1-aminoethane Small molecular drug D07LIE
2-(3-phenylthio)Phenyl)-1-aminoethane Small molecular drug D0O3GQ
2-(4-(Benzenesulfonyl)Phenyl)-1-aminoethane Small molecular drug D0CY6E
2-benzyl-4-piperazin-1-yl-1h-benzimidazole Small molecular drug D09RXU
2-bromo-lsd Small molecular drug D00VRV
2-ethyl-5-methoxy-3-piperidin-4-yl-1h-indole Small molecular drug D0W2QN
2-methyl-5-ht Small molecular drug D00CRA
3-(Phenylsulfonyl)-1-(Piperidin-3-yl)-1h-indole Small molecular drug D06FXO
3-(Phenylsulfonyl)-1-(Piperidin-4-yl)-1h-indole Small molecular drug D0C4AE
3-(Phenylsulfonyl)-1-(Pyrrolidin-3-yl)-1h-indole Small molecular drug D0Y4WH
4-((1h-indol-1-yl)Methyl)Benzenamine Small molecular drug D0FV7K
4-(1h-inden-1-ylmethyl)-phenylamine Small molecular drug D09LVG
4-(1h-indol-1-ylsulfonyl)Benzenamine Small molecular drug D0R7VT
4-(1h-indol-3-ylmethyl)-phenylamine Small molecular drug D09VSK
4-(2-benzenesulfonylphenyl)Piperazine Small molecular drug D00DZY
4-(3-benzenesulfonamidophenyl)Piperazine Small molecular drug D07DCN
4-(3-benzenesulfonylphenyl)Piperazine Small molecular drug D00OCC
4-(3-methyl-indole-1-sulfonyl)-phenylamine Small molecular drug D0XJ6D
4-(3h-inden-1-ylmethyl)-phenylamine Small molecular drug D01ZMO
4-(4,6-dinitro-1h-indol-1-ylsulfonyl)Benzenamine Small molecular drug D01TYJ
4-(4-benzenesulfonamidophenyl)Piperazine Small molecular drug D0N8AO
4-(4-benzenesulfonylphenyl)Piperazine Small molecular drug D0C8UV
4-(4-methoxy-1h-indol-1-ylsulfonyl)Benzenamine Small molecular drug D0D2XH
4-(6-methoxy-1h-indol-1-ylsulfonyl)Benzenamine Small molecular drug D0G6NV
4-(Indan-1-ylsulfanyl)-phenylamine Small molecular drug D01DCE
4-(Indane-1-sulfonyl)-phenylamine Small molecular drug D0LA4I
4-(Naphthalene-1-sulfonyl)-phenylamine Small molecular drug D06QVB
4-(Piperazin-1-yl)-1h-indole Small molecular drug D0TX8W
4-(Piperazin-1-yl)-3-tosyl-1h-indazole Small molecular drug D0VI0S
4-indan-1-ylmethyl-phenylamine Small molecular drug D0X1IU
4-inden-(1e)-ylidenemethyl-phenylamine Small molecular drug D05HJP
5,6-dichloro-3,4-dihydroquinazolin-2-amine Small molecular drug D08VGJ
5-(4-methylpiperazin-1-yl)-3-tosyl-1h-indazole Small molecular drug D0F6GP
5-ct Small molecular drug D02UWB
5-meo-dmt Small molecular drug D0C5XQ
5-methoxytryptamine Small molecular drug D04AQE
6-(Piperazin-1-yl)-3-tosyl-1h-indazole Small molecular drug D02SBM
6-tosyl-1,2,3,4,5,6-hexahydroazepino[4,5-b]Indole Small molecular drug D0V5AN
Alpha-ergocryptine Small molecular drug D06PXY
Alpha-methyl-5-ht Small molecular drug D09OYA
Brl-15572 Small molecular drug D04TVG
Bufotenine Small molecular drug D0SP2J
Dimebolin Small molecular drug D02YSX
Dm-1451 Small molecular drug D0J0KG
E-6837 Small molecular drug D0Q7AF
E6801 Small molecular drug D0N7NK
Edmt Small molecular drug D0CK9K
Emd-386088 Small molecular drug D0G7QT
Fluperlapine Small molecular drug D0F8TG
Lergotrile Small molecular drug D0DE8K
Ly 165,163 Small molecular drug D0T4PS
M-chlorophenylpiperazine Small molecular drug D0J6JT
Methiothepin Small molecular drug D0X6MT
Mpdt Small molecular drug D0C5GF
N,N-diethyl-2-(1h-indol-3-yl)Ethanamine Small molecular drug D0W2HW
N,N-dimethyl-2-(1-tosyl-1h-indol-3-yl)Ethanamine Small molecular drug D0SJ6E
N-(3-(2-aminoethyl)Phenyl)Benzenesulfonamide Small molecular drug D0E0DR
N-(3-(3-aminopropyl)Phenyl)Benzenesulfonamide Small molecular drug D0J9MP
N-(3-(Aminomethyl)Phenyl)Benzenesulfonamide Small molecular drug D05SAP
N-(3-aminophenyl)Benzenesulfonamide Small molecular drug D05DAF
N-(4-(2-aminoethyl)Phenyl)Benzenesulfonamide Small molecular drug D0D6FC
N-phenyl-3-(2-aminoethyl)Benzenesulfonamide Small molecular drug D0H0IZ
Octoclothepin Small molecular drug D0D3YN
Opc 4392 Small molecular drug D09ULA
Quipazine Small molecular drug D08BCF
Ro-04-6790 Small molecular drug D0P8JA
Sb 258585 Small molecular drug D0L7PA
Sb-214111 Small molecular drug D05XGR
Sb-271046 Small molecular drug D07LRJ
Sb-357134 Small molecular drug D0H7PC
Sb399885 Small molecular drug D02JFD
Serotonin Small molecular drug D0F6CD
Tfmpp Small molecular drug D0V5HV
Tiapride Small molecular drug DB13025
Way-208466 Small molecular drug D0OG0R
Way-466 Small molecular drug D06VPR
[125i]Sb-258585 Small molecular drug D0UB6O
[2-(3-benzyl-3h-inden-1-yl)-ethyl]-methyl-amine Small molecular drug D05JPG
[2-(3-benzyl-3h-indol-1-yl)-ethyl]-dimethyl-amine Small molecular drug D0KD8D
[2-(3-benzyl-indol-1-yl)-ethyl]-dimethyl-amine Small molecular drug D0JT3M
[2-(3h-indol-1-yl)-ethyl]-dimethyl-amine Small molecular drug D0ZC9Q
[3h]5-ct Small molecular drug D08PJK
[3h]Lsd Small molecular drug D07HQZ
[3h]Ro 63-0563 Small molecular drug D0V2PB
[3h]Spiperone Small molecular drug D05EQG
(+/-)-nantenine . D0L5MW
Amr-six-1 . D09CHX
Chlorophenylpiperazine . D0V3XU
Sel-73 . D0P1XQ
Sgs518 . DB05042
Suvn-501 . D00PBI
Suvn-504 . D0K8PH
Suvn-507 . D0S3UH
Patented
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid30124346-compound-13table4 Small molecular drug D0F4NB
Pmid30124346-compound-34table4 Small molecular drug D09BCJ
Discontinued
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dimethyltryptamine Small molecular drug DB01488
Lysergic Acid Diethylamide Small molecular drug DB04829
Way-181187 Small molecular drug D06ZVC
Avn 397 . D0J7EP
Syn-114 . D04VTV

References

1 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060