Target
5-hydroxytryptamine receptor 2A
Ligand
BDBM50097224
Substrate
n/a
Meas. Tech.
ChEMBL_1589563 (CHEMBL3829238)
Ki
2.5±n/a nM
Citation
 Fujiwara, TOhira, KUrushibara, KIto, AYoshida, MKanai, MTanatani, AKagechika, HHirano, T Steric structure-activity relationship of cyproheptadine derivatives as inhibitors of histone methyltransferase Set7/9. Bioorg Med Chem 24:4318-4323 (2016) [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:
BDBM50097224
Synonyms:
1-Methyl-4-thioxanthen-9-ylidene-piperidine | 1-methyl-4-(9H-thioxanthen-9-ylidene)piperidine | CHEMBL152408 | Pimethixene
Type:
Small organic molecule
Emp. Form.:
C19H19NS
Mol. Mass.:
293.426
SMILES:
[#6]-[#7]-1-[#6]-[#6]\[#6](-[#6]-[#6]-1)=[#6]-1\c2ccccc2-[#16]-c2ccccc-12
Structure:
Search PDB for entries with ligand similarity: