| Reaction Details |
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 | Report a problem with these data |
| Target | Histamine H3 receptor |
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| Ligand | BDBM22566 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_789899 (CHEMBL1925206) |
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| Ki | 5011.87±n/a nM |
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| Citation |  Istyastono, EP; Nijmeijer, S; Lim, HD; van de Stolpe, A; Roumen, L; Kooistra, AJ; Vischer, HF; de Esch, IJ; Leurs, R; de Graaf, C Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies. J Med Chem54:8136-47 (2011) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Histamine H3 receptor |
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| Name: | Histamine H3 receptor |
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| Synonyms: | G-protein coupled receptor 97 | GPCR97 | HH3R | HISTAMINE H3 | HRH3 | HRH3_HUMAN | Histamine H3 receptor (H3) | Histamine H3L | Histamine receptor (H3 and H4) |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 48691.47 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Binding assays were using CHO cells stably expressing hH3R receptors. |
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| Residue: | 445 |
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| Sequence: | MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTS
SAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAA
GPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSV
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSL
AVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFR
RAFTKLLCPQKLKIQPHSSLEHCWK
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| BDBM22566 |
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| n/a |
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| Name | BDBM22566 |
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| Synonyms: | 5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-indole | CHEMBL129198 | JNJ 7777120 |
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| Type | Small organic molecule |
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| Emp. Form. | C14H16ClN3O |
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| Mol. Mass. | 277.749 |
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| SMILES | CN1CCN(CC1)C(=O)c1cc2cc(Cl)ccc2[nH]1 |
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| Structure | 
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