Reaction Details |
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Target | Serotonin 2 (5-HT2) receptor |
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Ligand | BDBM21395 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1927 (CHEMBL616981) |
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IC50 | 1.7±n/a nM |
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Citation | Bøgesø, KP; Arnt, J; Boeck, V; Christensen, AV; Hyttel, J; Jensen, KG Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity. J Med Chem31:2247-56 (1989) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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Serotonin 2 (5-HT2) receptor |
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Name: | Serotonin 2 (5-HT2) receptor |
Synonyms: | 5-hydroxytryptamine receptor 2A/2B/2C |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 2197419 |
Components: | This complex has 3 components. |
Component 1 |
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 2 |
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 3 |
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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BDBM21395 |
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n/a |
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Name | BDBM21395 |
Synonyms: | 3-(2-(4-(4-Fluorobenzoyl)piperidinol)ethyl)-2,4(1H,3H)-quinazolinedione | 3-(2-{4-[(4-fluorophenyl)carbonyl]piperidin-1-yl}ethyl)-1,2,3,4-tetrahydroquinazoline-2,4-dione | CHEMBL1628637 | CHEMBL51 | Ketanserin | R-41,468 | R-41-468 | R41,468 | [3H]-Ketanserin |
Type | radiolabeled ligand |
Emp. Form. | C22H22FN3O3 |
Mol. Mass. | 395.4268 |
SMILES | Fc1ccc(cc1)C(=O)C1CCN(CCn2c(=O)[nH]c3ccccc3c2=O)CC1 |
Structure |
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