Target
G protein-coupled receptor kinase 5
Ligand
BDBM50444133
Substrate
n/a
Meas. Tech.
ChEMBL_1280627 (CHEMBL3096888)
IC50
5050±n/a nM
Citation
 Cho, SYLee, BHJung, HYun, CSHa, JDKim, HRChae, CHLee, JHSeo, HWOh, KS Design and synthesis of novel 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine derivatives as selective G-protein-coupled receptor kinase-2 and -5 inhibitors. Bioorg Med Chem Lett 23:6711-6 (2013) [PubMed]  Article 
Target
Name:
G protein-coupled receptor kinase 5
Synonyms:
G protein-coupled receptor kinase GRK5 | GPRK5 | GRK5 | GRK5_HUMAN
Type:
PROTEIN
Mol. Mass.:
67798.93
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1280627
Residue:
590
Sequence:
MELENIVANTVLLKAREGGGGKRKGKSKKWKEILKFPHISQCEDLRRTIDRDYCSLCDKQPIGRLLFRQFCETRPGLECYIQFLDSVAEYEVTPDEKLGEKGKEIMTKYLTPKSPVFIAQVGQDLVSQTEEKLLQKPCKELFSACAQSVHEYLRGEPFHEYLDSMFFDRFLQWKWLERQPVTKNTFRQYRVLGKGGFGEVCACQVRATGKMYACKRLEKKRIKKRKGESMALNEKQILEKVNSQFVVNLAYAYETKDALCLVLTIMNGGDLKFHIYNMGNPGFEEERALFYAAEILCGLEDLHRENTVYRDLKPENILLDDYGHIRISDLGLAVKIPEGDLIRGRVGTVGYMAPEVLNNQRYGLSPDYWGLGCLIYEMIEGQSPFRGRKEKVKREEVDRRVLETEEVYSHKFSEEAKSICKMLLTKDAKQRLGCQEEGAAEVKRHPFFRNMNFKRLEAGMLDPPFVPDPRAVYCKDVLDIEQFSTVKGVNLDHTDDDFYSKFSTGSVSIPWQNEMIETECFKELNVFGPNGTLPPDLNRNHPPEPPKKGLLQRLFKRQHQNNSKSSPSSKTSFNHHINSNHVSSNSTGSS
  
Inhibitor
Name:
BDBM50444133
Synonyms:
CHEMBL3093261
Type:
Small organic molecule
Emp. Form.:
C27H27N7O
Mol. Mass.:
465.5496
SMILES:
CN(c1ccccc1)c1ccc2oc(nc2c1)-c1cc(cnc1N)-c1cnn(c1)C1CCNCC1
Structure:
Search PDB for entries with ligand similarity: