| Reaction Details |
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 | Report a problem with these data |
| Target | Corticotropin-releasing factor receptor 1 |
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| Ligand | BDBM20986 |
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| Substrate/Competitor | 125I-Tyr(0)-ovine-CRF |
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| Meas. Tech. | Receptor Binding Assay |
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| pH | 7±n/a |
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| Temperature | 296.15±n/a K |
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| IC50 | 3.5±0.4 nM |
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| Citation |  Dzierba, CD; Tebben, AJ; Wilde, RG; Takvorian, AG; Rafalski, M; Kasireddy-Polam, P; Klaczkiewicz, JD; Pechulis, AD; Davis, AL; Sweet, MP; Woo, AM; Yang, Z; Ebeltoft, SM; Molski, TF; Zhang, G; Zaczek, RC; Trainor, GL; Combs, AP; Gilligan, PJ Dihydropyridopyrazinones and dihydropteridinones as corticotropin-releasing factor-1 receptor antagonists: structure-activity relationships and computational modeling. J Med Chem50:2269-72 (2007) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Corticotropin-releasing factor receptor 1 |
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| Name: | Corticotropin-releasing factor receptor 1 |
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| 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 |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 47870.75 |
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| Organism: | Rattus norvegicus (rat) |
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| Description: | Receptor binding assays were performed using rat cortex homogenate. |
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| Residue: | 415 |
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| Sequence: | MGRRPQLRLVKALLLLGLNPVSTSLQDQRCENLSLTSNVSGLQCNASVDLIGTCWPRSPA
GQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYSECQEILNEEKKSKVHYHVAV
IINYLGHCISLVALLVAFVLFLRLRSIRCLRNIIHWNLISAFILRNATWFVVQLTVSPEV
HQSNVAWCRLVTAAYNYFHVTNFFWMFGEGCYLHTAIVLTYSTDRLRKWMFVCIGWGVPF
PIIVAWAIGKLHYDNEKCWFGKRPGVYTDYIYQGPMILVLLINFIFLFNIVRILMTKLRA
STTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDEVSRVVFIYFNSFLESFQGFFVS
VFYCFLNSEVRSAIRKRWRRWQDKHSIRARVARAMSIPTSPTRVSFHSIKQSTAV
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| BDBM20986 |
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| 125I-Tyr(0)-ovine-CRF |
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| Name: | 125I-Tyr(0)-ovine-CRF |
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| Synonyms: | Ovine Tyr-CRF | oCRF |
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| Type: | radiolabeled substrate |
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| Mol. Mass.: | 4833.46 |
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| Organism: | Ovis aries (sheep) |
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| Description: | n/a |
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| Residue: | 42 |
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| Sequence: | YSQE PPISLDLTFH LLREVLEMTK ADQLAQQAHS NRKLLDIA
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