Reaction Details |
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Target | Corticotropin-releasing factor receptor 1/2 |
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Ligand | BDBM50218683 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_217368 (CHEMBL822880) |
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Ki | 324±n/a nM |
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Citation | Hartz, RA; Gilligan, PJ; Nanda, KK; Tebben, AJ; Fitzgerald, LW; Miller, K Synthesis and evaluation of imidazo[1,5-a]pyrazines as corticotropin releasing hormone receptor ligands. Bioorg Med Chem Lett12:291-4 (2002) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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Corticotropin-releasing factor receptor 1/2 |
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Name: | Corticotropin-releasing factor receptor 1/2 |
Synonyms: | Corticotropin releasing factor receptor |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 217368 |
Components: | This complex has 2 components. |
Component 1 |
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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Component 2 |
Name: | Corticotropin-releasing factor receptor 2 |
Synonyms: | CRF-R-2 | CRF-R2 | CRF2 Beta | CRFR-2 | CRFR2_RAT | CRH-R-2 | CRH-R2 | Corticotropin releasing factor receptor | Corticotropin-releasing factor receptor 2 | Corticotropin-releasing hormone receptor 2 | Crf2r | Crhr2 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 47697.09 |
Organism: | RAT |
Description: | CRF2 Beta 0 RAT::P47866 |
Residue: | 411 |
Sequence: | MDAALLLSLLEANCSLALAEELLLDGWGEPPDPEGPYSYCNTTLDQIGTCWPQSAPGALV
ERPCPEYFNGIKYNTTRNAYRECLENGTWASRVNYSHCEPILDDKQRKYDLHYRIALIIN
YLGHCVSVVALVAAFLLFLVLRSIRCLRNVIHWNLITTFILRNITWFLLQLIDHEVHEGN
EVWCRCVTTIFNYFVVTNFFWMFVEGCYLHTAIVMTYSTEHLRKWLFLFIGWCIPCPIIV
AWAVGKLYYENEQCWFGKEPGDLVDYIYQGPIILVLLINFVFLFNIVRILMTKLRASTTS
ETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDDLSQIVFIYFNSFLQSFQGFFVSVFYC
FFNGEVRSALRKRWHRWQDHHALRVPVARAMSIPTSPTRISFHSIKQTAAV
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BDBM50218683 |
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n/a |
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Name | BDBM50218683 |
Synonyms: | CHEMBL98643 |
Type | Small organic molecule |
Emp. Form. | C20H25Cl2N5 |
Mol. Mass. | 406.352 |
SMILES | CCCc1nc(N(C)c2ccc(Cl)cc2Cl)n2ccnc(N(CC)CC)c12 |
Structure |
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