Reaction Details |
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Target | Corticotropin-releasing factor receptor 1 |
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Ligand | BDBM29453 |
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Substrate/Competitor | 125I-Tyr(0)-ovine-CRF |
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Meas. Tech. | In Vitro Binding Autoradiography |
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pH | 7.2±n/a |
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Temperature | 296.15±n/a K |
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IC50 | 1.48±0.5 nM |
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Citation | Gilligan, PJ; He, L; Clarke, T; Tivitmahaisoon, P; Lelas, S; Li, YW; Heman, K; Fitzgerald, L; Miller, K; Zhang, G; Marshall, A; Krause, C; McElroy, J; Ward, K; Shen, H; Wong, H; Grossman, S; Nemeth, G; Zaczek, R; Arneric, SP; Hartig, P; Robertson, DW; Trainor, G 8-(4-Methoxyphenyl)pyrazolo[1,5-a]-1,3,5-triazines: selective and centrally active corticotropin-releasing factor receptor-1 (CRF1) antagonists. J Med Chem52:3073-83 (2009) [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 |
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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BDBM29453 |
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125I-Tyr(0)-ovine-CRF |
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Name: | 125I-Tyr(0)-ovine-CRF |
Synonyms: | Ovine Tyr-CRF | oCRF |
Type: | radiolabeled substrate |
Mol. Mass.: | 4833.46 |
Organism: | Ovis aries (sheep) |
Description: | n/a |
Residue: | 42 |
Sequence: | YSQE PPISLDLTFH LLREVLEMTK ADQLAQQAHS NRKLLDIA
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