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Target
Beta-adrenergic receptor kinase 1
Ligand
BDBM50566215
Substrate
n/a
Meas. Tech.
ChEMBL_2094567 (CHEMBL4775830)
IC50
23000±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:
Beta-adrenergic receptor kinase 1
Synonyms:
ADRBK1 | ARBK1_BOVIN | Beta-ARK-1 | Beta-adrenergic receptor kinase 1 | G-protein-coupled receptor kinase 2 | GRK2
Type:
PROTEIN
Mol. Mass.:
79654.58
Organism:
Bos taurus
Description:
ChEMBL_113511
Residue:
689
Sequence:
MADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFSQKLGYLLFRDFCLKHLEEAKPLVEFYEEIKKYEKLETEEERLVCSREIFDTYIMKELLACSHPFSKSAIEHVQGHLVKKQVPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNVELNIHLTMNDFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNERIMLSLVSTGDCPFIVCMSYAFHTPDKLSFILDLMNGGDLHYHLSQHGVFSEADMRFYAAEIILGLEHMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHASVGTHGYMAPEVLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAVELPDSFSPELRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMVFLQKYPPPLIPPRGEVNAADAFDIGSFDEEDTKGIKLLDSDQELYRNFPLTISERWQQEVAETVFDTINAETDRLEARKKTKNKQLGHEEDYALGKDCIMHGYMSKMGNPFLTQWQRRYFYLFPNRLEWRGEGEAPQSLLTMEEIQSVEETQIKERKCLLLKIRGGKQFVLQCDSDPELVQWKKELRDAYREAQQLVQRVPKMKNKPRSPVVELSKVPLIQRGSANGL
  
Inhibitor
Name:
BDBM50566215
Synonyms:
CHEMBL4779427
Type:
Small organic molecule
Emp. Form.:
C29H31ClN4O3
Mol. Mass.:
519.034
SMILES:
CC(C)[C@H](Cc1ccccc1)NC(=O)c1ccc2NC(=O)\C(=C/c3[nH]c(C)c(NC(=O)CCl)c3C)c2c1 |r|
Structure:
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