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Target
Histamine H1 receptor
Ligand
BDBM22566
Substrate
BDBM22567
Meas. Tech.
Radioligand Binding Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
977±n/a nM
Citation
Liu, H; Altenbach, RJ; Carr, TL; Chandran, P; Hsieh, GC; Lewis, LG; Manelli, AM; Milicic, I; Marsh, KC; Miller, TR; Strakhova, MI; Vortherms, TA; Wakefield, BD; Wetter, JM; Witte, DG; Honore, P; Esbenshade, TA; Brioni, JD; Cowart, MD cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), A New Histamine H4R Antagonist that Blocks Pain Responses against Carrageenan-Induced Hyperalgesia. J Med Chem 51:7094-8 (2008) [PubMed] Article
More Info.:
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:
BDBM22566
Synonyms:
5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-indole | CHEMBL129198 | JNJ 7777120
Type:
Small organic molecule
Emp. Form.:
C14H16ClN3O
Mol. Mass.:
277.749
SMILES:
CN1CCN(CC1)C(=O)c1cc2cc(Cl)ccc2[nH]1
Substrate
Name:
BDBM22567
Synonyms:
3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramine | N-(4-methoxybenzyl)-N ,N -dimethyl-N-pyridin-2-ylethane-1,2-diamine | N-[2-(dimethylamino)ethyl]-N-[(4-methoxyphenyl)methyl]pyridin-2-amine | PYRILAMINE | Pyranisamine | [3H]mepyramine | [3H]pyrilamine
Type:
radiolabeled ligand
Emp. Form.:
C17H23N3O
Mol. Mass.:
285.384
SMILES:
COc1ccc(CN(CCN(C)C)c2ccccn2)cc1