Target
5-hydroxytryptamine receptor 2A
Ligand
BDBM50324542
Substrate
n/a
Meas. Tech.
ChEMBL_649428 (CHEMBL1219126)
Ki
2.4±n/a nM
Citation
 Xiong, YUllman, BChoi, JSCherrier, MStrah-Pleynet, SDecaire, MDosa, PIFeichtinger, KTeegarden, BRFrazer, JMYoon, WHShan, YWhelan, KHauser, EKGrottick, AJSemple, GAl-Shamma, H Synthesis and in vivo evaluation of phenethylpiperazine amides: selective 5-hydroxytryptamine(2A) receptor antagonists for the treatment of insomnia. J Med Chem 53:5696-706 (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:
BDBM50324542
Synonyms:
2-[4-(4-Chloro-1-methyl-1H-pyrazole-3-carbonyl)piperazin-1-yl]-1-(4-fluorophenyl)ethanone | CHEMBL1214946
Type:
Small organic molecule
Emp. Form.:
C17H18ClFN4O2
Mol. Mass.:
364.802
SMILES:
Cn1cc(Cl)c(n1)C(=O)N1CCN(CC(=O)c2ccc(F)cc2)CC1
Structure:
Search PDB for entries with ligand similarity: