Target
5-hydroxytryptamine receptor 2A
Ligand
BDBM50137981
Substrate
n/a
Meas. Tech.
ChEBML_2670
Ki
0.340000±n/a nM
Citation
 Campiani, GButini, SFattorusso, CCatalanotti, BGemma, SNacci, VMorelli, ECagnotto, AMereghetti, IMennini, TCarli, MMinetti, PDi Cesare, MAMastroianni, DScafetta, NGalletti, BStasi, MACastorina, MPacifici, LVertechy, MDi Serio, SGhirardi, OTinti, OCarminati, P Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. J Med Chem 47:143-57 (2003) [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:
BDBM50137981
Synonyms:
7-Chloro-9-(4-methyl-piperazin-1-yl)-4-thia-10a-aza-benzo[f]azulene | CHEMBL426763
Type:
Small organic molecule
Emp. Form.:
C17H18ClN3S
Mol. Mass.:
331.863
SMILES:
CN1CCN(CC1)C1=Cn2cccc2Sc2ccc(Cl)cc12 |t:8|
Structure:
Search PDB for entries with ligand similarity: