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Target
Histamine H1 receptor
Ligand
BDBM50212239
Substrate
n/a
Meas. Tech.
ChEMBL_466551 (CHEMBL935643)
IC50
>10000±n/a nM
Citation
 Jarvis, MF; Honore, P; Shieh, CC; Chapman, M; Joshi, S; Zhang, XF; Kort, M; Carroll, W; Marron, B; Atkinson, R; Thomas, J; Liu, D; Krambis, M; Liu, Y; McGaraughty, S; Chu, K; Roeloffs, R; Zhong, C; Mikusa, JP; Hernandez, G; Gauvin, D; Wade, C; Zhu, C; Pai, M; Scanio, M; Shi, L; Drizin, I; Gregg, R; Matulenko, M; Hakeem, A; Gross, M; Johnson, M; Marsh, K; Wagoner, PK; Sullivan, JP; Faltynek, CR; Krafte, DS A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc Natl Acad Sci U S A 104:8520-5 (2007) [PubMed]  Article 
Target
Name:
Histamine H1 receptor
Synonyms:
H1R | HH1R | HISTAMINE H1 | HRH1 | HRH1_HUMAN
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
55808.72
Organism:
Homo sapiens (Human)
Description:
Cell pellets from SK-N-MC cells transfected with human H1 receptor were used in binding assay.
Residue:
487
Sequence:
MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHTVGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFILCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKCETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLRPENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKLYCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSRTDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFIMAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFKRILHIRS
  
Inhibitor
Name:
BDBM50212239
Synonyms:
5-(4-chlorophenyl)-N-(3,5-dimethoxyphenyl)furan-2-carboxamide | A-803467 | CHEMBL250699
Type:
Small organic molecule
Emp. Form.:
C19H16ClNO4
Mol. Mass.:
357.788
SMILES:
COc1cc(NC(=O)c2ccc(o2)-c2ccc(Cl)cc2)cc(OC)c1
Structure:
Search PDB for entries with ligand similarity: