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TargetBeta-adrenergic receptor kinase 1
LigandBDBM50566212
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2094567 (CHEMBL4775830)
IC50 3600±n/a nM
Citation Rowlands, RAChen, QBouley, RAAvramova, LVTesmer, JJGWhite, AD Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. J Med Chem64:566-585 (2021) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Beta-adrenergic receptor kinase 1
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:
MADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFS
QKLGYLLFRDFCLKHLEEAKPLVEFYEEIKKYEKLETEEERLVCSREIFDTYIMKELLAC
SHPFSKSAIEHVQGHLVKKQVPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNV
ELNIHLTMNDFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNER
IMLSLVSTGDCPFIVCMSYAFHTPDKLSFILDLMNGGDLHYHLSQHGVFSEADMRFYAAE
IILGLEHMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHASVGTHGYMAPE
VLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAVELPDSFSPE
LRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMVFLQKYPPPLIPPRGEVNAA
DAFDIGSFDEEDTKGIKLLDSDQELYRNFPLTISERWQQEVAETVFDTINAETDRLEARK
KTKNKQLGHEEDYALGKDCIMHGYMSKMGNPFLTQWQRRYFYLFPNRLEWRGEGEAPQSL
LTMEEIQSVEETQIKERKCLLLKIRGGKQFVLQCDSDPELVQWKKELRDAYREAQQLVQR
VPKMKNKPRSPVVELSKVPLIQRGSANGL
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50566212
n/a
NameBDBM50566212
Synonyms:CHEMBL4780266
TypeSmall organic molecule
Emp. Form.C27H26BrFN4O3
Mol. Mass.553.423
SMILESC[C@H](Cc1ccc(F)cc1)NC(=O)c1ccc2NC(=O)\C(=C/c3[nH]c(C)c(NC(=O)CBr)c3C)c2c1 |r|
Structure
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