Reaction Details Report a problem with these data
Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50313852
Substrate
n/a
Meas. Tech.
ChEMBL_615438 (CHEMBL1106905)
IC50
2.9±n/a nM
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 Lett 20:1890-4 (2010) [PubMed]  Article 
Target
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
  
Inhibitor
Name:
BDBM50313852
Synonyms:
8-(2,4-dichlorophenyl)-N-(1,3-dimethoxypropan-2-yl)-2,7-dimethyl-3,4-dihydropyrazolo[1,5-a][1,3,5]triazin-4-amine | CHEMBL1091818
Type:
Small organic molecule
Emp. Form.:
C18H23Cl2N5O2
Mol. Mass.:
412.314
SMILES:
COCC(COC)NC1N=C(C)Nc2c(c(C)nn12)-c1ccc(Cl)cc1Cl |t:9,(16.61,.95,;15.27,1.72,;13.94,.95,;13.95,-.59,;15.28,-1.36,;16.61,-.59,;17.95,-1.35,;12.61,-1.37,;12.62,-2.91,;11.29,-3.68,;11.29,-5.22,;9.95,-5.99,;12.62,-5.99,;13.95,-5.22,;15.43,-5.69,;16.33,-4.44,;17.87,-4.44,;15.42,-3.2,;13.95,-3.67,;16.17,-7.04,;15.37,-8.36,;16.11,-9.71,;17.65,-9.74,;18.39,-11.09,;18.45,-8.41,;17.7,-7.07,;18.49,-5.75,)|
Structure:
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