Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50116105
Substrate
n/a
Meas. Tech.
ChEMBL_685890
Ki
3.98±n/a nM
Citation
 Tellew, JELanier, MMoorjani, MLin, ELuo, ZSlee, DHZhang, XHoare, SRGrigoriadis, DESt Denis, YDi Fabio, RDi Modugno, ESaunders, JWilliams, JP Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties. Bioorg Med Chem Lett 20:7259-64 (2010) [PubMed]  Article
Target
Name:
Corticotropin-releasing factor receptor 1
Synonyms:
CRF-R | CRF-R2 Alpha | CRF1 | CRH-R 1 | CRHR1 | Corticotropin releasing factor receptor 1 | Corticotropin-releasing factor receptor 1 (CRF-1) | Corticotropin-releasing factor receptor 1 (CRF1) | Corticotropin-releasing hormone receptor 1
Type:
Enzyme
Mol. Mass.:
50744.31
Organism:
Homo sapiens (Human)
Description:
P34998
Residue:
444
Sequence:
MGGHPQLRLVKALLLLGLNPVSASLQDQHCESLSLASNISGLQCNASVDLIGTCWPRSPAGQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYSECQEILNEEKKSKVHYHVAVIINYLGHCISLVALLVAFVLFLRLRPGCTHWGDQADGALEVGAPWSGAPFQVRRSIRCLRNIIHWNLISAFILRNATWFVVQLTMSPEVHQSNVGWCRLVTAAYNYFHVTNFFWMFGEGCYLHTAIVLTYSTDRLRKWMFICIGWGVPFPIIVAWAIGKLYYDNEKCWFGKRPGVYTDYIYQGPMILVLLINFIFLFNIVRILMTKLRASTTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDEVSRVVFIYFNSFLESFQGFFVSVFYCFLNSEVRSAIRKRWHRWQDKHSIRARVARAMSIPTSPTRVSFHSIKQSTAV
  
Inhibitor
Name:
BDBM50116105
Synonyms:
3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine | CHEMBL309138 | R-121919 | [3-(6-Dimethylamino-4-methyl-pyridin-3-yl)-2,5-dimethyl-4H-pyrazolo[1,5-a]pyrimidin-7-yl]-dipropyl-amine | [3-(6-Dimethylamino-4-methyl-pyridin-3-yl)-2,5-dimethyl-pyrazolo[1,5-a]pyrimidin-7-yl]-dipropyl-amine
Type:
Small organic molecule
Emp. Form.:
C22H32N6
Mol. Mass.:
380.5297
SMILES:
CCCN(CCC)c1cc(C)nc2c(c(C)nn12)-c1cnc(cc1C)N(C)C |(-1.91,-13.39,;-3.24,-14.16,;-4.58,-13.4,;-5.91,-14.18,;-7.24,-13.41,;-8.57,-14.19,;-9.91,-13.42,;-5.9,-15.72,;-7.22,-16.49,;-7.23,-18.03,;-8.56,-18.8,;-5.9,-18.8,;-4.55,-18.03,;-3.07,-18.5,;-2.16,-17.24,;-.62,-17.23,;-3.09,-15.99,;-4.56,-16.48,;-2.58,-19.96,;-3.61,-21.11,;-3.13,-22.57,;-1.62,-22.88,;-.59,-21.72,;-1.08,-20.27,;-.06,-19.11,;-1.13,-24.34,;.38,-24.65,;-2.15,-25.5,)|
Structure:
Search PDB for entries with ligand similarity: