Reaction Details |
| Report a problem with these data |
Target | Histamine H1 receptor |
---|
Ligand | BDBM50290708 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_84420 (CHEMBL691452) |
---|
IC50 | 473±n/a nM |
---|
Citation | Maynard, GD; Bratton, LD; Kane, JM; Burkholder, TP; Santiago, B; Stewart, KT; Kudlacz, EM; Shatzer, SA; Knippenberg, RW; Farrell, AM; Logan, DE Synthesis and sar of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/tachykinin NK1 receptor antagonist activity Bioorg Med Chem Lett7:2819-2824 (1997) Article |
---|
More Info.: | Get all data from this article, Assay Method |
---|
|
Histamine H1 receptor |
---|
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: | MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHT
VGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFI
LCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKC
ETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLR
PENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKL
YCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSR
TDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFI
MAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFK
RILHIRS
|
|
|
BDBM50290708 |
---|
n/a |
---|
Name | BDBM50290708 |
Synonyms: | CHEMBL94834 | [3-(2-{4-[1-(4-Fluoro-benzyl)-1H-benzoimidazole-2-carbonyl]-piperidin-1-yl}-ethyl)-3-(4-trifluoromethyl-phenyl)-pyrrolidin-1-yl]-(3,4,5-trimethoxy-phenyl)-methanone |
Type | Small organic molecule |
Emp. Form. | C43H44F4N4O5 |
Mol. Mass. | 772.8269 |
SMILES | COc1cc(cc(OC)c1OC)C(=O)N1CCC(CCN2CCC(CC2)C(=O)c2nc3ccccc3n2Cc2ccc(F)cc2)(C1)c1ccc(cc1)C(F)(F)F |
Structure |
|