| Reaction Details |
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 | Report a problem with these data |
| Target | Histamine H3 receptor |
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| Ligand | BDBM50191978 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1613241 (CHEMBL3855041) |
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| IC50 | 5000±n/a nM |
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| Citation |  Shaw, DE; Baig, F; Bruce, I; Chamoin, S; Collingwood, SP; Cross, S; Dayal, S; Drückes, P; Furet, P; Furminger, V; Haggart, D; Hussey, M; Konstantinova, I; Loren, JC; Molteni, V; Roberts, S; Reilly, J; Saunders, AM; Stringer, R; Sviridenko, L; Thomas, M; Thomson, CG; Tomlins, C; Wen, B; Yeh, V; Pearce, AC Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension. J Med Chem59:7901-14 (2016) [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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| BDBM50191978 |
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| n/a |
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| Name | BDBM50191978 |
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| Synonyms: | CHEMBL3915941 |
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| Type | Small organic molecule |
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| Emp. Form. | C27H32N8O2 |
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| Mol. Mass. | 500.5954 |
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| SMILES | Cc1ncc(cc1NC(=O)c1cnn2cc(ccc12)-c1cnn(C)c1)C(=O)NCCN1CCCC1(C)C |
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| Structure | 
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