Reaction Details Report a problem with these data
Target
Corticotropin-releasing factor receptor 1/2
Ligand
BDBM50218797
Substrate
n/a
Meas. Tech.
ChEMBL_217368 (CHEMBL822880)
Ki
2420±n/a nM
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 Lett 12:291-4 (2002) [PubMed]  Article 
Target
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:
MGRRPQLRLVKALLLLGLNPVSTSLQDQRCENLSLTSNVSGLQCNASVDLIGTCWPRSPAGQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYSECQEILNEEKKSKVHYHVAVIINYLGHCISLVALLVAFVLFLRLRSIRCLRNIIHWNLISAFILRNATWFVVQLTVSPEVHQSNVAWCRLVTAAYNYFHVTNFFWMFGEGCYLHTAIVLTYSTDRLRKWMFVCIGWGVPFPIIVAWAIGKLHYDNEKCWFGKRPGVYTDYIYQGPMILVLLINFIFLFNIVRILMTKLRASTTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDEVSRVVFIYFNSFLESFQGFFVSVFYCFLNSEVRSAIRKRWRRWQDKHSIRARVARAMSIPTSPTRVSFHSIKQSTAV
  
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:
MDAALLLSLLEANCSLALAEELLLDGWGEPPDPEGPYSYCNTTLDQIGTCWPQSAPGALVERPCPEYFNGIKYNTTRNAYRECLENGTWASRVNYSHCEPILDDKQRKYDLHYRIALIINYLGHCVSVVALVAAFLLFLVLRSIRCLRNVIHWNLITTFILRNITWFLLQLIDHEVHEGNEVWCRCVTTIFNYFVVTNFFWMFVEGCYLHTAIVMTYSTEHLRKWLFLFIGWCIPCPIIVAWAVGKLYYENEQCWFGKEPGDLVDYIYQGPIILVLLINFVFLFNIVRILMTKLRASTTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDDLSQIVFIYFNSFLQSFQGFFVSVFYCFFNGEVRSALRKRWHRWQDHHALRVPVARAMSIPTSPTRISFHSIKQTAAV
  
Inhibitor
Name:
BDBM50218797
Synonyms:
CHEMBL320384
Type:
Small organic molecule
Emp. Form.:
C19H23Cl2N5
Mol. Mass.:
392.325
SMILES:
CCCc1nc(N(CC)c2ccc(Cl)cc2Cl)n2ccnc(N(C)C)c12
Structure:
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