Reaction Details |
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Target | Corticotropin-releasing factor receptor 1 |
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Ligand | BDBM50313866 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_615438 (CHEMBL1106905) |
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IC50 | 1.2±n/a nM |
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Citation | Hartz, RA; Ahuja, VT; Schmitz, WD; Molski, TF; Mattson, GK; Lodge, NJ; Bronson, JJ; Macor, JE Synthesis and structure-activity relationships of N3-pyridylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists. Bioorg Med Chem Lett20:1890-4 (2010) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Corticotropin-releasing factor receptor 1 |
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Name: | Corticotropin-releasing factor receptor 1 |
Synonyms: | CRF-R | CRF1 | CRFR1_RAT | CRH-R 1 | Corticotropin releasing factor receptor | Corticotropin releasing factor receptor 1 | Corticotropin-releasing Factor Receptor 1 | Corticotropin-releasing hormone receptor 1 | Crhr | Crhr1 |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 47870.75 |
Organism: | Rattus norvegicus (rat) |
Description: | Receptor binding assays were performed using rat cortex homogenate. |
Residue: | 415 |
Sequence: | MGRRPQLRLVKALLLLGLNPVSTSLQDQRCENLSLTSNVSGLQCNASVDLIGTCWPRSPA
GQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYSECQEILNEEKKSKVHYHVAV
IINYLGHCISLVALLVAFVLFLRLRSIRCLRNIIHWNLISAFILRNATWFVVQLTVSPEV
HQSNVAWCRLVTAAYNYFHVTNFFWMFGEGCYLHTAIVLTYSTDRLRKWMFVCIGWGVPF
PIIVAWAIGKLHYDNEKCWFGKRPGVYTDYIYQGPMILVLLINFIFLFNIVRILMTKLRA
STTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDEVSRVVFIYFNSFLESFQGFFVS
VFYCFLNSEVRSAIRKRWRRWQDKHSIRARVARAMSIPTSPTRVSFHSIKQSTAV
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BDBM50313866 |
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n/a |
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Name | BDBM50313866 |
Synonyms: | (R)-5-chloro-1-(1-cyclopropylethyl)-3-(6-methoxy-5-methyl-2-(trifluoromethyl)pyridin-3-ylamino)pyrazin-2(1H)-one | CHEMBL1086179 |
Type | Small organic molecule |
Emp. Form. | C17H18ClF3N4O2 |
Mol. Mass. | 402.799 |
SMILES | COc1nc(c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C)C(F)(F)F |r| |
Structure |
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