Target
5-hydroxytryptamine receptor 2A/2B/2C
Ligand
BDBM50001121
Substrate
n/a
Meas. Tech.
ChEMBL_2214 (CHEMBL617039)
Ki
>1722±n/a nM
Citation
 Ennis, MDBaze, MESmith, MWLawson, CFMcCall, RBLahti, RAPiercey, MF Novel indolodioxanes with antihypertensive effects: potent ligands for the 5-HT1A receptor. J Med Chem 35:3058-66 (1992) [PubMed]  Article 
Target
Name:
5-hydroxytryptamine receptor 2A/2B/2C
Synonyms:
Serotonin 2 (5-HT2) receptor
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of ChEMBL is 306637
Components:
This complex has 3 components.
Component 1
Name:
5-hydroxytryptamine receptor 2B
Synonyms:
5-HT-2B | 5-HT2B | 5-hydroxytryptamine (serotonin) receptor 2B [Homo sapiens] | 5-hydroxytryptamine receptor 2B (5-HT2B) | 5-hydroxytryptamine receptor 2C (5HT2C) | 5HT2B_HUMAN | HTR2B | Serotonin (5-HT3) receptor | Serotonin 2b (5-HT2b) receptor | Serotonin Receptor 2B
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
54312.47
Organism:
Homo sapiens (Human)
Description:
Receptor binding assays were performed using human clone stably expressed in CHO cells.
Residue:
481
Sequence:
MALSYRVSELQSTIPEHILQSTFVHVISSNWSGLQTESIPEEMKQIVEEQGNKLHWAALLILMVIIPTIGGNTLVILAVSLEKKLQYATNYFLMSLAVADLLVGLFVMPIALLTIMFEAMWPLPLVLCPAWLFLDVLFSTASIMHLCAISVDRYIAIKKPIQANQYNSRATAFIKITVVWLISIGIAIPVPIKGIETDVDNPNNITCVLTKERFGDFMLFGSLAAFFTPLAIMIVTYFLTIHALQKKAYLVKNKPPQRLTWLTVSTVFQRDETPCSSPEKVAMLDGSRKDKALPNSGDETLMRRTSTIGKKSVQTISNEQRASKVLGIVFFLFLLMWCPFFITNITLVLCDSCNQTTLQMLLEIFVWIGYVSSGVNPLVYTLFNKTFRDAFGRYITCNYRATKSVKTLRKRSSKIYFRNPMAENSKFFKKHGIRNGINPAMYQSPMRLRSSTIQSSSIILLDTLLLTENEGDKTEEQVSYV
  
Component 2
Name:
5-hydroxytryptamine receptor 2C
Synonyms:
5-HT-2C | 5-HT2C | 5-HT2C-INI | 5-HT2c VGI | 5-HTR2C | 5-hydroxytryptamine receptor 1C | 5-hydroxytryptamine receptor 2C (5-HT-2C) | 5-hydroxytryptamine receptor 2C (5HT-2C) | 5HT-1C | 5HT2C_HUMAN | HTR1C | HTR2C | Serotonin (5-HT3) receptor | Serotonin 2c (5-HT2c) receptor | Serotonin Receptor 2C
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
51836.79
Organism:
Homo sapiens (Human)
Description:
P28335
Residue:
458
Sequence:
MVNLRNAVHSFLVHLIGLLVWQCDISVSPVAAIVTDIFNTSDGGRFKFPDGVQNWPALSIVIIIIMTIGGNILVIMAVSMEKKLHNATNYFLMSLAIADMLVGLLVMPLSLLAILYDYVWPLPRYLCPVWISLDVLFSTASIMHLCAISLDRYVAIRNPIEHSRFNSRTKAIMKIAIVWAISIGVSVPIPVIGLRDEEKVFVNNTTCVLNDPNFVLIGSFVAFFIPLTIMVITYCLTIYVLRRQALMLLHGHTEEPPGLSLDFLKCCKRNTAEEENSANPNQDQNARRRKKKERRPRGTMQAINNERKASKVLGIVFFVFLIMWCPFFITNILSVLCEKSCNQKLMEKLLNVFVWIGYVCSGINPLVYTLFNKIYRRAFSNYLRCNYKVEKKPPVRQIPRVAATALSGRELNVNIYRHTNEPVIEKASDNEPGIEMQVENLELPVNPSSVVSERISSV
  
Component 3
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:
BDBM50001121
Synonyms:
8-(4-Oxo-1-phenyl-1,3,8-triaza-spiro[4.5]dec-8-ylmethyl)-7,8-dihydro-3H-6,9-dioxa-3-aza-cyclopenta[a]naphthalene-2-carboxylic acid | CHEMBL106283
Type:
Small organic molecule
Emp. Form.:
C25H26N4O5
Mol. Mass.:
462.4977
SMILES:
OC(=O)c1cc2c3OC(CN4CCC5(CC4)N(CNC5=O)c4ccccc4)COc3ccc2[nH]1
Structure:
Search PDB for entries with ligand similarity: