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TargetBeta-adrenergic receptor kinase 1
LigandBDBM50257385
Substrate/Competitorn/a
Meas. Tech.ChEBML_1689808
IC50 54±n/a nM
Citation Okawa, TAramaki, YYamamoto, MKobayashi, TFukumoto, SToyoda, YHenta, THata, AIkeda, SKaneko, MHoffman, IDSang, BCZou, HKawamoto, T Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. J Med Chem60:6942-6990 (2017) [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_HUMAN | BARK | BARK1 | Beta-ARK-1 | Beta-adrenergic receptor kinase 1 | G-protein coupled receptor kinase 2 | G-protein coupled receptor kinase 2 (GRK2) | GRK2
Type:Enzyme
Mol. Mass.:79581.30
Organism:Homo sapiens (Human)
Description:P25098
Residue:689
Sequence:
MADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFS
QKLGYLLFRDFCLNHLEEARPLVEFYEEIKKYEKLETEEERVARSREIFDSYIMKELLAC
SHPFSKSATEHVQGHLGKKQVPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNV
ELNIHLTMNDFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNER
IMLSLVSTGDCPFIVCMSYAFHTPDKLSFILDLMNGGDLHYHLSQHGVFSEADMRFYAAE
IILGLEHMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHASVGTHGYMAPE
VLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAVELPDSFSPE
LRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMVFLQKYPPPLIPPRGEVNAA
DAFDIGSFDEEDTKGIKLLDSDQELYRNFPLTISERWQQEVAETVFDTINAETDRLEARK
KAKNKQLGHEEDYALGKDCIMHGYMSKMGNPFLTQWQRRYFYLFPNRLEWRGEGEAPQSL
LTMEEIQSVEETQIKERKCLLLKIRGGKQFILQCDSDPELVQWKKELRDAYREAQQLVQR
VPKMKNKPRSPVVELSKVPLVQRGSANGL
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50257385
n/a
NameBDBM50257385
Synonyms:CHEMBL4076320
TypeSmall organic molecule
Emp. Form.C21H18N6O
Mol. Mass.370.4072
SMILESO=C(Nc1ccccc1)c1cccc(NCc2nc(n[nH]2)-c2ccncc2)c1
Structure
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