| Reaction Details |
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| Target | Histamine H3 Receptor |
| Ligand | JNJ 7777120 |
| Substrate/Competitor | [3H]N-alpha-methyl histamine |
| Meas. Tech. | Radioligand Binding Assay |
| pH | 7.4±n/a |
| Temperature | 298.15±n/a K |
| Ki | 1318±260 nM |
| Citation | Altenbach, RJ; Adair, RM; Bettencourt, BM; Black, LA; Fix-Stenzel, SR; Gopalakrishnan, SM; Hsieh, GC; Liu, H; Marsh, KC; McPherson, MJ; Milicic, I; Miller, TR; Vortherms, TA; Warrior, U; Wetter, JM; Wishart, N; Witte, DG; Honore, P; Esbenshade, TA; Hancock, AA; Brioni, JD; Cowart, MD Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands.J Med Chem.51:6571-80(2008)[PubMed] |
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, Solution Info
, Assay Method
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| Histamine H3 Receptor |
| Name | Histamine H3 Receptor |
| Synonyms | HH3R |
| Type | G Protein-Coupled Receptor (GPCR) |
| Mol. Mass. | 48588 |
| Organism | Rattus norvegicus (rat) |
| Description | Radioligand binding assays were using rat cortical membranes. |
| Residue | 445 |
| Sequence | MERAPPDGLMNASGTLAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCAS
SVFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMALVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGGREAG
PEPPPDAQPSPPPAPPSCWGCWPKGHGEAMPLHRYGVGEAGPGVEAGEAALGGGSGGGAA
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSITQRFRLSRDKKVAKSL
AIIVSIFGLCWAPYTLLMIIRAACHGRCIPDYWYETSFWLLWANSAVNPVLYPLCHYSFR
RAFTKLLCPQKLKVQPHGSLEQCWK
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| JNJ 7777120 |
| Name | JNJ 7777120 |
| Synonyms: | 5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-indole |
| Type | Small organic molecule |
| Emp. Form. | C14H16ClN3O |
| Mol. Mass. | 277.749 |
| SMILES | CN1CCN(CC1)C(=O)c1cc2cc(Cl)ccc2[nH]1 |
| Structure | |
| [3H]N-alpha-methyl histamine |
| Name | [3H]N-alpha-methyl histamine |
| Synonyms: | N-alpha-methylhistamine | N-methylhistamine | [2-(1H-imidazol-5-yl)ethyl](methyl)amine |
| Type | radiolabeled ligand |
| Emp. Form. | C6H11N3 |
| Mol. Mass. | 125.1716 |
| SMILES | CNCCc1cnc[nH]1 |
| Structure | |