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Target
5-hydroxytryptamine receptor 2A
Ligand
BDBM35254
Substrate
n/a
Meas. Tech.
ChEMBL_643047 (CHEMBL1176238)
Ki
4±n/a nM
Citation
 Butini, S; Campiani, G; Franceschini, S; Trotta, F; Kumar, V; Guarino, E; Borrelli, G; Fiorini, I; Novellino, E; Fattorusso, C; Persico, M; Orteca, N; Sandager-Nielsen, K; Jacobsen, TA; Madsen, K; Scheel-Kruger, J; Gemma, S Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors. J Med Chem 53:4803-7 (2010) [PubMed]  Article 
Target
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:
MEILCEDNISLSSIPNSLMQLGDGPRLYHNDFNSRDANTSEASNWTIDAENRTNLSCEGYLPPTCLSILHLQEKNWSALLTTVVIILTIAGNILVIMAVSLEKKLQNATNYFLMSLAIADMLLGFLVMPVSMLTILYGYRWPLPSKLCAIWIYLDVLFSTASIMHLCAISLDRYVAIQNPIHHSRFNSRTKAFLKIIAVWTISVGISMPIPVFGLQDDSKVFKEGSCLLADDNFVLIGSFVAFFIPLTIMVITYFLTIKSLQKEATLCVSDLSTRAKLASFSFLPQSSLSSEKLFQRSIHREPGSYAGRRTMQSISNEQKACKVLGIVFFLFVVMWCPFFITNIMAVICKESCNENVIGALLNVFVWIGYLSSAVNPLVYTLFNKTYRSAFSRYIQCQYKENRKPLQLILVNTIPALAYKSSQLQVGQKKNSQEDAEQTVDDCSMVTLGKQQSEENCTDNIETVNEKVSCV
  
Inhibitor
Name:
BDBM35254
Synonyms:
2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3-b][1,5]benzodiazepine | CHEMBL715 | Olansek | US8802672, Olanzapine | Zyprexa | olanzapine
Type:
Small organic molecule
Emp. Form.:
C17H20N4S
Mol. Mass.:
312.432
SMILES:
CN1CCN(CC1)C1=Nc2ccccc2Nc2sc(C)cc12 |t:8|
Structure:
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