Target
5-hydroxytryptamine receptor 2A
Ligand
BDBM84937
Substrate
n/a
Ki
42±n/a nM
Comments
PDSP_1137
Citation
 Nelson, DLLucaites, VLAudia, JENissen, JSWainscott, DB Species differences in the pharmacology of the 5-hydroxytryptamine2 receptor: structurally specific differentiation by ergolines and tryptamines. J Pharmacol Exp Ther 265:1272-9 (1993) [PubMed]
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:
BDBM84937
Synonyms:
6-Methylergoline-8¿¿¿¿-carboxylic acid 4-methoxycyclohexyl ester | 6-Methylergoline-8β-carboxylic acid 4-methoxycyclohexyl ester | LY 254239 | LY-254239
Type:
Small organic molecule
Emp. Form.:
C23H30N2O3
Mol. Mass.:
382.4959
SMILES:
COC1CCC(CC1)OC(=O)[C@@H]1C[C@H]2[C@@H](Cc3c[nH]c4cccc2c34)N(C)C1 |wU:13.24,11.11,wD:14.28,(3.85,8.25,;3.08,6.91,;3.85,5.58,;5.39,5.58,;6.16,4.25,;5.39,2.91,;3.85,2.91,;3.08,4.25,;6.16,1.58,;5.39,.24,;3.85,.24,;6.16,-1.09,;6.16,-2.63,;7.49,-3.4,;8.83,-2.63,;10.16,-3.4,;10.16,-4.94,;11.31,-5.97,;10.68,-7.38,;9.15,-7.22,;8,-8.25,;6.54,-7.77,;6.22,-6.26,;7.49,-4.94,;8.83,-5.71,;8.83,-1.09,;10.16,-.32,;7.49,-.32,)|
Structure:
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