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Target
G protein-coupled receptor kinase 5
Ligand
BDBM50566213
Substrate
n/a
Meas. Tech.
ChEMBL_2094566 (CHEMBL4775829)
IC50
130±n/a nM
Citation
 Rowlands, RA; Chen, Q; Bouley, RA; Avramova, LV; Tesmer, JJG; White, AD Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. J Med Chem 64:566-585 (2021) [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:
BDBM50566213
Synonyms:
CHEMBL4784634
Type:
Small organic molecule
Emp. Form.:
C26H25ClN4O3
Mol. Mass.:
476.955
SMILES:
Cc1[nH]c(\C=C2/C(=O)Nc3ccc(cc23)C(=O)NCCc2ccccc2)c(C)c1NC(=O)CCl
Structure:
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