Target
5-hydroxytryptamine receptor 2A
Ligand
BDBM50001276
Substrate
n/a
Meas. Tech.
ChEMBL_2527 (CHEMBL616877)
Ki
1259±n/a nM
Citation
 Bromidge, SMDabbs, SDavies, DTDavies, SDuckworth, DMForbes, ITGaster, LMHam, PJones, GEKing, FDMulholland, KRSaunders, DVWyman, PABlaney, FEClarke, SEBlackburn, TPHolland, VKennett, GALightowler, SMiddlemiss, DNTrail, BRiley, GJWood, MD Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent. J Med Chem 43:1123-34 (2000) [PubMed]  Article 
Target
Name:
5-hydroxytryptamine receptor 2A
Synonyms:
5-HT-2 | 5-HT-2A | 5-HT2A | 5-hydroxytryptamine receptor 2A (5-HT-2A) | 5-hydroxytryptamine receptor 2A (5HT-2A) | 5-hydroxytryptamine receptor 2A (5HT2A) | 5HT2A_HUMAN | HTR2 | HTR2A | Serotonin receptor 2A
Type:
undefined
Mol. Mass.:
52607.65
Organism:
Homo sapiens (Human)
Description:
P28223
Residue:
471
Sequence:
MDILCEENTSLSSTTNSLMQLNDDTRLYSNDFNSGEANTSDAFNWTVDSENRTNLSCEGCLSPSCLSLLHLQEKNWSALLTAVVIILTIAGNILVIMAVSLEKKLQNATNYFLMSLAIADMLLGFLVMPVSMLTILYGYRWPLPSKLCAVWIYLDVLFSTASIMHLCAISLDRYVAIQNPIHHSRFNSRTKAFLKIIAVWTISVGISMPIPVFGLQDDSKVFKEGSCLLADDNFVLIGSFVSFFIPLTIMVITYFLTIKSLQKEATLCVSDLGTRAKLASFSFLPQSSLSSEKLFQRSIHREPGSYTGRRTMQSISNEQKACKVLGIVFFLFVVMWCPFFITNIMAVICKESCNEDVIGALLNVFVWIGYLSSAVNPLVYTLFNKTYRSAFSRYIQCQYKENKKPLQLILVNTIPALAYKSSQLQMGQKKNSKQDAKTTDNDCSMVALGKQHSEEASKDNSDGVNEKVSCV
  
Inhibitor
Name:
BDBM50001276
Synonyms:
CHEMBL277732
Type:
Small organic molecule
Emp. Form.:
C22H16F5N3O2
Mol. Mass.:
449.3734
SMILES:
COc1cc2CCN(C(=O)Nc3cncc(c3)-c3cc(F)cc(F)c3)c2cc1C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: