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Target
Histamine H1 receptor
Ligand
BDBM50156898
Substrate
n/a
Meas. Tech.
ChEMBL_429751 (CHEMBL914451)
IC50
145±n/a nM
Citation
Fonquerna, S; Miralpeix, M; Pagès, L; Puig, C; Cardús, A; Antón, F; Cárdenas, A; Vilella, D; Aparici, M; Calaf, E; Prieto, J; Gras, J; Huerta, JM; Warrellow, G; Beleta, J; Ryder, H Synthesis and structure-activity relationships of novel histamine H1 antagonists: indolylpiperidinyl benzoic acid derivatives. J Med Chem 47:6326-37 (2004) [PubMed] Article
More Info.:
Target
Name:
Histamine H1 receptor
Synonyms:
HISTAMINE H1 | HRH1 | HRH1_CAVPO
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
55641.53
Organism:
Guinea pig
Description:
Guinea pig cerebellum was used in binding assay.
Residue:
488
Sequence:
MSFLPGMTPVTLSNFSWALEDRMLEGNSTTTPTRQLMPLVVVLSSVSLVTVALNLLVLYAVRSERKLHTVGNLYIVSLSVADLIVGAVVMPMSILYLHRSAWILGRPLCLFWLSMDYVASTASIFSVFILCIDRYRSVQQPLRYLRYRTKTRASATILGAWLLSFLWVIPILGWHHFMAPTSEPREKKCETDFYDVTWFKVMTAIINFYLPTLLMLWFYIRIYKAVRRHCQHRQLINSSLPSFSEMKLKLENAKVDTRRMGKESPWEDPKRCSKDASGVHTPMPSSQHLVDMPCAAVLSEDEGGEVGTRQMPMLAVGDGRCCEALNHMHSQLELSGQSRATHSISARPEEWTVVDGQSFPITDSDTSTEAAPMGGQPRSGSNSGLDYIKFTWRRLRSHSRQYTSGLHLNRERKAAKQLGCIMAAFILCWIPYFVFFMVIAFCKSCSNEPVHMFTIWLGYLNSTLNPLIYPLCNENFRKTFKRILRIPP
Inhibitor
Name:
BDBM50156898
Synonyms:
5-{4-[1-(2-Ethoxy-ethyl)-1H-indol-3-yl]-piperidin-1-ylmethyl}-2-methoxy-benzoic acid | 5-{4-[1-(2-ethoxyethyl)-1H-indol-3-yl]piperidin-1-ylmethyl}-2-methoxybenzoic acid | CHEMBL360712
Type:
Small organic molecule
Emp. Form.:
C26H32N2O4
Mol. Mass.:
436.5433
SMILES:
CCOCCn1cc(C2CCN(Cc3ccc(OC)c(c3)C(O)=O)CC2)c2ccccc12