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Target
G protein-coupled receptor kinase 5
Ligand
BDBM50173319
Substrate
n/a
Meas. Tech.
Assays for Inhibition of GRKs
pH
7±n/a
IC50
>100000±n/a nM
Comments
extracted
Citation
 Larsen, SD; Homan, K; Waldschmidt, H; Tesmer, JJ G protein-coupled receptor kinase 2 inhibitors and methods for use of the same US Patent  US10023564 Publication Date 7/17/2018 
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:
BDBM50173319
Synonyms:
CHEMBL3809020 | US10023564, Example 11
Type:
Small organic molecule
Emp. Form.:
C29H27FN6O5
Mol. Mass.:
558.5603
SMILES:
COc1cccc(OC)c1CNC(=O)c1cc(ccc1F)C1NC(=O)NC(C)=C1C(=O)Nc1ccc2[nH]ncc2c1 |c:29|
Structure:
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