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Target5-hydroxytryptamine receptor 1A/1B/1D/1F/2A/2B/2C/3A/3B/4/5A/5B/6/7
LigandBDBM50231569
Substrate/Competitorn/a
Meas. Tech.ChEMBL_3525 (CHEMBL619195)
Ki>10000±n/a nM
Citation van Wijngaarden, I; Hamminga, D; van Hes, R; Standaar, PJ; Tipker, J; Tulp, MT; Mol, F; Olivier, B; de Jonge, A Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives. J Med Chem36:3693-9 (1994) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
5-hydroxytryptamine receptor 1A/1B/1D/1F/2A/2B/2C/3A/3B/4/5A/5B/6/7
Name:5-hydroxytryptamine receptor 1A/1B/1D/1F/2A/2B/2C/3A/3B/4/5A/5B/6/7
Synonyms:Serotonin (5-HT) receptor
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of ChEMBL is 3517
Components:This complex has 14 components.
Component 1
Name:5-hydroxytryptamine receptor 3B
Synonyms:5HT3B_RAT | Htr3b | Serotonin (5-HT) receptor
Type:PROTEIN
Mol. Mass.:50328.78
Organism:Rattus norvegicus
Description:EBI_11885
Residue:437
Sequence:
MILLWSCLLVAVVGILGTATPQPGNSSLHRLTRQLLQQYHKEVRPVYNWAEATTVYLDLC
VHAVLDVDVQNQKLKTSMWYREVWNDEFLSWNSSLFDDIQEISLPLSAIWAPDIIINEFV
DVERSPDLPYVYVNSSGTIRNHKPIQVVSACSLQTYAFPFDIQNCSLTFNSILHTVEDID
LGFLRNQEDIENDKRSFLNDSEWQLLSVTSTYHIRQSSAGDFAQIRFNVVIRRCPLAYVV
SLLIPSIFLMLVDLGSFYLPPNCRARIVFKTNVLVGYTVFRVNMSDEVPRSAGCTSLIGV
FFTVCMALLVLSLSKSILLIKFLYEERHSEQERPLMCLRGDSDANESRLYLRAPCAEDTE
SPVRQEHQVPSDTLKDFWFQLQSINNSLRTRDQVYQKEVEWLAILCHFDQLLFRIYLAVL
GLYTVTLCSLWALWSRM
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Component 2
Name:5-hydroxytryptamine receptor 7
Synonyms:5-HT-7 | 5-HT-X | 5-HT7 | 5-HT7L | 5-HT7S | 5-Hydroxytryptamine receptor 7 (5-HT7) | 5-hydroxytryptamine receptor 7 | 5-hydroxytryptamine receptor 7 (5-HT-7) | 5HT7R_RAT | Adrenergic Alpha | GPRFO | Htr7 | Serotonin (5-HT) receptor | Serotonin Receptor 7
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:49852.62
Organism:Rattus norvegicus (rat)
Description:Rat cloned 5-HT7R.
Residue:448
Sequence:
MMDVNSSGRPDLYGHLRSLILPEVGRGLQDLSPDGGAHPVVSSWMPHLLSGFLEVTASPA
PTWDAPPDNVSGCGEQINYGRVEKVVIGSILTLITLLTIAGNCLVVISVCFVKKLRQPSN
YLIVSLALADLSVAVAVMPFVSVTDLIGGKWIFGHFFCNVFIAMDVMCCTASIMTLCVIS
IDRYLGITRPLTYPVRQNGKCMAKMILSVWLLSASITLPPLFGWAQNVNDDKVCLISQDF
GYTIYSTAVAFYIPMSVMLFMYYQIYKAARKSAAKHKFPGFPRVQPESVISLNGVVKLQK
EVEECANLSRLLKHERKNISIFKREQKAATTLGIIVGAFTVCWLPFFLLSTARPFICGTS
CSCIPLWVERTCLWLGYANSLINPFIYAFFNRDLRTTYRSLLQCQYRNINRKLSAAGMHE
ALKLAERPERSEFVLQNSDHCGKKGHDT
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Component 3
Name:5-hydroxytryptamine receptor 1F
Synonyms:5-HT-1F | 5-HT1F | 5-hydroxytryptamine receptor 1F | 5HT1F_RAT | 5ht1f | Htr1f | Serotonin 1 (5-HT1) receptor | Serotonin 1f (5-HT1f) receptor | Serotonin receptor 1F
Type:Enzyme Catalytic Domain
Mol. Mass.:41896.93
Organism:RAT
Description:5-HT1F HTR1F RAT::P30940
Residue:366
Sequence:
MDFLNSSDQNLTSEELLNRMPSKILVSLTLSGLALMTTTINCLVITAIIVTRKLHHPANY
LICSLAVTDFLVAVLVMPFSIVYIVRESWIMGQGLCDLWLSVDIICCTCSILHLSAIALD
RYRAITDAVEYARKRTPRHAGITITTVWVISVFISVPPLFWRHQGNSRDDQCIIKHDHIV
STIYSTFGAFYIPLVLILILYYKIYRAARTLYHKRQASRMIKEELNGQVLLESGEKSIKL
VSTSYMLEKSLSDPSTDFDRIHSTVKSPRSELKHEKSWRRQKISGTRERKAATTLGLILG
AFVICWLPFFVKELVVNICEKCKISEEMSNFLAWLGYLNSLINPLIYTIFNEDFKKAFQK
LVRCRN
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Component 4
Name:5-hydroxytryptamine receptor 4
Synonyms:5-HT-4 | 5-HT4 | 5-HT4L | 5-HT4S | 5-hydroxytryptamine receptor 4 | 5HT4R_RAT | Htr4 | Serotonin (5-HT) receptor | Serotonin 4 (5-HT4) receptor
Type:Enzyme Catalytic Domain
Mol. Mass.:46117.31
Organism:RAT
Description:5-HT4 HTR4 RAT::Q62758
Residue:406
Sequence:
MDRLDANVSSNEGFGSVEKVVLLTFFAMVILMAILGNLLVMVAVCRDRQLRKIKTNYFIV
SLAFADLLVSVLVNAFGAIELVQDIWFYGEMFCLVRTSLDVLLTTASIFHLCCISLDRYY
AICCQPLVYRNKMTPLRIALMLGGCWVIPMFISFLPIMQGWNNIGIVDVIEKRKFNHNSN
STFCVFMVNKPYAITCSVVAFYIPFLLMVLAYYRIYVTAKEHAQQIQMLQRAGATSESRP
QTADQHSTHRMRTETKAAKTLCVIMGCFCFCWAPFFVTNIVDPFIDYTVPEKVWTAFLWL
GYINSGLNPFLYAFLNKSFRRAFLIILCCDDERYKRPPILGQTVPCSTTTINGSTHVLRD
TVECGGQWESRCHLTATSPLVAAQPVIRRPQDNDLEDSCSLKRSQS
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Component 5
Name:5-hydroxytryptamine receptor 2B
Synonyms:5-HT2B | 5-hydroxytryptamine receptor 2B | 5HT2B_RAT | Htr2b | Serotonin 2b (5-HT2b) receptor | Serotonin receptor 2a and 2b (5HT2A and 5HT2B) | Srl
Type:Enzyme Catalytic Domain
Mol. Mass.:53668.47
Organism:RAT
Description:5-HT2B HTR2B RAT::P30994
Residue:479
Sequence:
MASSYKMSEQSTISEHILQKTCDHLILTDRSGLKAESAAEEMKQTAENQGNTVHWAALLI
FAVIIPTIGGNILVILAVSLEKRLQYATNYFLMSLAVADLLVGLFVMPIALLTIMFEATW
PLPLALCPAWLFLDVLFSTASIMHLCAISLDRYIAIKKPIQANQCNSRTTAFVKITVVWL
ISIGIAIPVPIKGIEADVVNAHNITCELTKDRFGSFMLFGSLAAFFAPLTIMIVTYFLTI
HALRKKAYLVRNRPPQRLTRWTVSTVLQREDSSFSSPEKMVMLDGSHKDKILPNSTDETL
MRRMSSAGKKPAQTISNEQRASKVLGIVFLFFLLMWCPFFITNVTLALCDSCNQTTLKTL
LQIFVWVGYVSSGVNPLIYTLFNKTFREAFGRYITCNYQATKSVKVLRKCSSTLYFGNSM
VENSKFFTKHGIRNGINPAMYQSPVRLRSSTIQSSSIILLNTFLTENDGDKVEDQVSYI
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Component 6
Name:5-hydroxytryptamine receptor 1A
Synonyms:5-HT-1A | 5-HT1 | 5-HT1A | 5-Hydroxytryptamine receptor 1A (5-HT1A) | 5-hydroxytryptamine receptor 1A (5HT1A) | 5HT1A_RAT | 5ht1a | G-21 | Htr1a | Serotonin 1 (5-HT1) receptor | Serotonin 1a (5-HT1a) receptor/Adrenergic receptor alpha-1 | Serotonin receptor 1A
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:46445.29
Organism:Rattus norvegicus (rat)
Description:Binding assays were performed using rat hippocampal membranes.
Residue:422
Sequence:
MDVFSFGQGNNTTASQEPFGTGGNVTSISDVTFSYQVITSLLLGTLIFCAVLGNACVVAA
IALERSLQNVANYLIGSLAVTDLMVSVLVLPMAALYQVLNKWTLGQVTCDLFIALDVLCC
TSSILHLCAIALDRYWAITDPIDYVNKRTPRRAAALISLTWLIGFLISIPPMLGWRTPED
RSDPDACTISKDHGYTIYSTFGAFYIPLLLMLVLYGRIFRAARFRIRKTVRKVEKKGAGT
SLGTSSAPPPKKSLNGQPGSGDWRRCAENRAVGTPCTNGAVRQGDDEATLEVIEVHRVGN
SKEHLPLPSESGSNSYAPACLERKNERNAEAKRKMALARERKTVKTLGIIMGTFILCWLP
FFIVALVLPFCESSCHMPALLGAIINWLGYSNSLLNPVIYAYFNKDFQNAFKKIIKCKFC
RR
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Component 7
Name:5-hydroxytryptamine receptor 2A
Synonyms:5-HT-2A | 5-HT2 | 5-HT2A | 5-hydroxytryptamine receptor 2A (5-HT2A) | 5-hydroxytryptamine receptor 2A (5HT2A) | 5HT2A_RAT | Htr2 | Htr2a | Serotonin Receptor 2A
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:52852.05
Organism:Rattus norvegicus (rat)
Description:Rat cortex membranes 5-HT2A receptors.
Residue:471
Sequence:
MEILCEDNISLSSIPNSLMQLGDGPRLYHNDFNSRDANTSEASNWTIDAENRTNLSCEGY
LPPTCLSILHLQEKNWSALLTTVVIILTIAGNILVIMAVSLEKKLQNATNYFLMSLAIAD
MLLGFLVMPVSMLTILYGYRWPLPSKLCAIWIYLDVLFSTASIMHLCAISLDRYVAIQNP
IHHSRFNSRTKAFLKIIAVWTISVGISMPIPVFGLQDDSKVFKEGSCLLADDNFVLIGSF
VAFFIPLTIMVITYFLTIKSLQKEATLCVSDLSTRAKLASFSFLPQSSLSSEKLFQRSIH
REPGSYAGRRTMQSISNEQKACKVLGIVFFLFVVMWCPFFITNIMAVICKESCNENVIGA
LLNVFVWIGYLSSAVNPLVYTLFNKTYRSAFSRYIQCQYKENRKPLQLILVNTIPALAYK
SSQLQVGQKKNSQEDAEQTVDDCSMVTLGKQQSEENCTDNIETVNEKVSCV
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Component 8
Name:5-hydroxytryptamine receptor 5B
Synonyms:5-HT5B | 5-hydroxytryptamine receptor 5B | 5HT5B_RAT | 5ht5b | Htr5b | Serotonin (5-HT) receptor | Serotonin 5b (5-HT5b) receptor
Type:Enzyme Catalytic Domain
Mol. Mass.:41141.95
Organism:RAT
Description:5-HT5B 0 RAT::P35365
Residue:370
Sequence:
MEVSNLSGATPGIAFPPGPESCSDSPSSGRSMGSTPGGLILSGREPPFSAFTVLVVTLLV
LLIAATFLWNLLVLVTILRVRAFHRVPHNLVASTAVSDVLVAALVMPLSLVSELSAGRRW
QLGRSLCHVWISFDVLCCTASIWNVAAIALDRYWTITRHLQYTLRTRRRASALMIAITWA
LSALIALAPLLFGWGEAYDARLQRCQVSQEPSYAVFSTCGAFYVPLAVVLFVYWKIYKAA
KFRFGRRRRAVVPLPATTQAKEAPQESETVFTARCRATVAFQTSGDSWREQKEKRAAMMV
GILIGVFVLCWIPFFLTELVSPLCACSLPPIWKSIFLWLGYSNSFFNPLIYTAFNKNYNN
AFKSLFTKQR
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Component 9
Name:5-hydroxytryptamine receptor 1D
Synonyms:5-HT-1D | 5-HT1D | 5-hydroxytryptamine receptor 1D | 5HT1D_RAT | Htr1d | Serotonin 1 (5-HT1) receptor | Serotonin 1B/1D receptor | Serotonin receptor 1D
Type:Enzyme Catalytic Domain
Mol. Mass.:41551.75
Organism:RAT
Description:5-HT1D HTR1D RAT::P28565
Residue:374
Sequence:
MSLPNQSLEGLPQEASNRSLNATGAWDPEVLQALRISLVVVLSIITLATVLSNAFVLTTI
LLTKKLHTPANYLIGSLATTDLLVSILVMPISIAYTTTRTWNFGQILCDIWVSSDITCCT
ASILHLCVIALDRYWAITDALEYSKRRTAGHAAAMIAAVWAISICISIPPLFWRQATAHE
EMSDCLVNTSQISYTIYSTCGAFYIPSILLIILYGRIYVAARSRILNPPSLYGKRFTTAQ
LITGSAGSSLCSLNPSLHESHTHTVGSPLFFNQVKIKLADSILERKRISAARERKATKTL
GIILGAFIICWLPFFVVSLVLPICRDSCWIHPALFDFFTWLGYLNSLINPVIYTVFNEDF
RQAFQRVVHFRKAS
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Component 10
Name:5-hydroxytryptamine receptor 2C
Synonyms:5-HT2C | 5-hydroxytryptamine receptor 2C | 5-hydroxytryptamine receptor 2C (5HT2c) | 5HT2C_RAT | 5ht1c | Htr1c | Htr2c | Serotonin (5-HT) receptor | Serotonin receptor 2a and 2c (5HT2A and 5HT2C)
Type:Enzyme
Mol. Mass.:51935.10
Organism:Rattus norvegicus (Rat)
Description:P08909
Residue:460
Sequence:
MVNLGNAVRSLLMHLIGLLVWQFDISISPVAAIVTDTFNSSDGGRLFQFPDGVQNWPALS
IVVIIIMTIGGNILVIMAVSMEKKLHNATNYFLMSLAIADMLVGLLVMPLSLLAILYDYV
WPLPRYLCPVWISLDVLFSTASIMHLCAISLDRYVAIRNPIEHSRFNSRTKAIMKIAIVW
AISIGVSVPIPVIGLRDESKVFVNNTTCVLNDPNFVLIGSFVAFFIPLTIMVITYFLTIY
VLRRQTLMLLRGHTEEELANMSLNFLNCCCKKNGGEEENAPNPNPDQKPRRKKKEKRPRG
TMQAINNEKKASKVLGIVFFVFLIMWCPFFITNILSVLCGKACNQKLMEKLLNVFVWIGY
VCSGINPLVYTLFNKIYRRAFSKYLRCDYKPDKKPPVRQIPRVAATALSGRELNVNIYRH
TNERVARKANDPEPGIEMQVENLELPVNPSNVVSERISSV
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Component 11
Name:5-hydroxytryptamine receptor 5A
Synonyms:5-HT-5A | 5-HT5a | 5-hydroxytryptamine receptor 5A | 5HT5A_RAT | 5ht5a | Htr5a | REC17 | Serotonin (5-HT) receptor | Serotonin receptor 5A
Type:Enzyme Catalytic Domain
Mol. Mass.:40684.21
Organism:RAT
Description:5-HT5a HTR5A RAT::P35364
Residue:357
Sequence:
MDLPINLTSFSLSTPSTLEPNRSLDTEALRTSQSFLSAFRVLVLTLLGFLAAATFTWNLL
VLATILRVRTFHRVPHNLVASMAISDVLVAVLVMPLSLVHELSGRRWQLGRRLCQLWIAC
DVLCCTASIWNVTAIALDRYWSITRHLEYTLRARKRVSNVMILLTWALSAVISLAPLLFG
WGETYSELSEECQVSREPSYTVFSTVGAFYLPLCVVLFVYWKIYKAAKFRMGSRKTNSVS
PIPEAVEVKDASQHPQMVFTVRHATVTFQTEGDTWREQKEQRAALMVGILIGVFVLCWFP
FFVTELISPLCSWDIPALWKSIFLWLGYSNSFFNPLIYTAFNRSYSSAFKVFFSKQQ
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Component 12
Name:5-hydroxytryptamine receptor 6
Synonyms:5-HT-6 | 5-HT6 | 5-hydroxytryptamine receptor 6 | 5HT6R_RAT | Htr6 | ST-B17 | Serotonin (5-HT) receptor | Serotonin 6 (5-HT6) receptor | Serotonin receptor 6
Type:Enzyme Catalytic Domain
Mol. Mass.:46945.51
Organism:RAT
Description:5-HT6 HTR6 RAT::P31388
Residue:436
Sequence:
MVPEPGPVNSSTPAWGPGPPPAPGGSGWVAAALCVVIVLTAAANSLLIVLICTQPALRNT
SNFFLVSLFTSDLMVGLVVMPPAMLNALYGRWVLARGLCLLWTAFDVMCCSASILNLCLI
SLDRYLLILSPLRYKLRMTAPRALALILGAWSLAALASFLPLLLGWHELGKARTPAPGQC
RLLASLPFVLVASGVTFFLPSGAICFTYCRILLAARKQAVQVASLTTGTAGQALETLQVP
RTPRPGMESADSRRLATKHSRKALKASLTLGILLGMFFVTWLPFFVANIAQAVCDCISPG
LFDVLTWLGYCNSTMNPIIYPLFMRDFKRALGRFLPCVHCPPEHRPALPPPPCGPLTAVP
DQASACSRCCLCLCRQTQIQTPLQGAPRACSSQPSFCCLERPPGTPRHPPGPPLWSTSLS
QTLWSLRYGRIHSVPP
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Component 13
Name:5-hydroxytryptamine receptor 3A
Synonyms:5-HT3 | 5-hydroxytryptamine receptor 3A | 5HT3A_RAT | 5ht3 | Htr3 | Htr3a | Serotonin (5-HT) receptor | Zacopride site-R
Type:Enzyme Catalytic Domain
Mol. Mass.:55428.70
Organism:RAT
Description:5-HT3 HTR3A RAT::P35563
Residue:483
Sequence:
MPLCIPQVLLALFLSVLIAQGEGSRRRATQAHSTTQPALLRLSDHLLANYKKGVRPVRDW
RKPTLVSIDVIMYAILNVDEKNQVLTTYIWYRQFWTDEFLQWTPEDFDNVTKLSIPTDSI
WVPDILINEFVDVGKSPSIPYVYVHHQGEVQNYKPLQLVTACSLDIYNFPFDVQNCSLTF
TSWLHTIQDINISLWRTPEEVRSDKSIFINQGEWELLGVFTKFQEFSIETSNSYAEMKFY
VVIRRRPLFYAVSLLLPSIFLMVVDIVGFCLPPDSGERVSFKITLLLGYSVFLIIVSDTL
PATAIGTPLIGVYFVVCMALLVISLAETIFIVQLVHKQDLQRPVPDWLRHLVLDRIAWLL
CLGEQPMAHRPPATFQANKTDDCSAMGNHCSHVGSPQDLEKTSRSRDSPLPPPREASLAV
RGLLQELSSIRHSLEKRDEMREVARDWLRVGYVLDRLLFRIYLLAVLAYSITLVTLWSIW
HYS
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Component 14
Name:5-hydroxytryptamine receptor 1B
Synonyms:5-HT-1B | 5-HT1B | 5-hydroxytryptamine receptor 1B (5HT1B) | 5HT1B_RAT | 5ht1b | Htr1b | Serotonin 1 (5-HT1) receptor | Serotonin 1B/1D receptor | Serotonin receptor 1B
Type:Protein
Mol. Mass.:43173.33
Organism:Rattus norvegicus (Rat)
Description:P28564
Residue:386
Sequence:
MEEQGIQCAPPPPATSQTGVPLANLSHNCSADDYIYQDSIALPWKVLLVALLALITLATT
LSNAFVIATVYRTRKLHTPANYLIASLAVTDLLVSILVMPISTMYTVTGRWTLGQVVCDF
WLSSDITCCTASIMHLCVIALDRYWAITDAVDYSAKRTPKRAAIMIVLVWVFSISISLPP
FFWRQAKAEEEVLDCFVNTDHVLYTVYSTVGAFYLPTLLLIALYGRIYVEARSRILKQTP
NKTGKRLTRAQLITDSPGSTSSVTSINSRVPEVPSESGSPVYVNQVKVRVSDALLEKKKL
MAARERKATKTLGIILGAFIVCWLPFFIISLVMPICKDACWFHMAIFDFFNWLGYLNSLI
NPIIYTMSNEDFKQAFHKLIRFKCTG
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BDBM50231569
n/a
NameBDBM50231569
Synonyms:Cilansetron | KC-9946
TypeSmall organic molecule
Emp. Form.C20H21N3O
Mol. Mass.319.4002
SMILESCc1nccn1C[C@H]1CCc2c(C1=O)c1cccc3CCCn2c13
Structure
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