Reaction Details Report a problem with these data
Target
Histamine H2 receptor
Ligand
BDBM50394695
Substrate
n/a
Meas. Tech.
ChEMBL_858640 (CHEMBL2166522)
EC50
331.13±n/a nM
Citation
 Birnkammer, T; Spickenreither, A; Brunskole, I; Lopuch, M; Kagermeier, N; Bernhardt, G; Dove, S; Seifert, R; Elz, S; Buschauer, A The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H2 receptor agonists. J Med Chem 55:1147-60 (2012) [PubMed]  Article 
Target
Name:
Histamine H2 receptor
Synonyms:
Gastric receptor I | H2R | HISTAMINE H2 | HRH2 | HRH2_CAVPO | Histamine H2-Gs alpha S
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
40567.22
Organism:
Cavia porcellus (domestic guinea pig)
Description:
For the H2 receptor-binding assays, guinea pig striatum was used.
Residue:
359
Sequence:
MAFNGTVPSFCMDFTVYKVTISVILIILILVTVAGNVVVCLAVGLNRRLRSLTNCFIVSLAVTDLLLGLLVLPFSAIYQLSCKWSFSKVFCNIYTSLDVMLCTASILNLFMISLDRYCAVTDPLRYPVLITPARVAISLVFIWVISITLSFLSIHLGWNSRNETSKDNDTIVKCKVQVNEVYGLVDGLVTFYLPLLIMCITYFRIFKIAREQARRINHIGSWKAATIREHKATVTLAAVMGAFIICWFPYFTVFVYRGLKGDDAVNEVFEDVVLWLGYANSALNPILYAALNRDFRTAYHQLFCCRLASHNSHETSLRLNNSQLNRSQCQEPRWQEDKPLNLQVWSGTEVTAPQGATNR
  
Inhibitor
Name:
BDBM50394695
Synonyms:
CHEMBL2165635
Type:
Small organic molecule
Emp. Form.:
C38H68N10O2S2
Mol. Mass.:
761.142
SMILES:
Cc1nc(N)sc1CCCNC(=N)NC(=O)CCCCCCCCCCCCCCCCCCCCC(=O)NC(N)=NCCCc1sc(N)nc1C |w:41.42|
Structure:
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