Target
G protein-coupled receptor kinase 5
Ligand
BDBM50444097
Substrate
n/a
Meas. Tech.
ChEMBL_1280627 (CHEMBL3096888)
IC50
530±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:
BDBM50444097
Synonyms:
CHEMBL3093254
Type:
Small organic molecule
Emp. Form.:
C27H24N8O2
Mol. Mass.:
492.5319
SMILES:
Nc1ncc(cc1-c1nc2ccc(O)c(-c3ccc4cn[nH]c4c3)c2o1)-c1cnn(c1)C1CCNCC1
Structure:
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