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TargetBeta-adrenergic receptor kinase 1
LigandBDBM50260126
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1692744 (CHEMBL4043634)
IC50 2680±n/a nM
Citation Waldschmidt, HVHoman, KTCato, MCCruz-Rodríguez, OCannavo, AWilson, MWSong, JCheung, JYKoch, WJTesmer, JJLarsen, SD Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. J Med Chem60:3052-3069 (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_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:
BDBM50260126
n/a
NameBDBM50260126
Synonyms:CHEMBL4073639
TypeSmall organic molecule
Emp. Form.C28H29FN2O4
Mol. Mass.476.5393
SMILESFc1ccc(cc1C(=O)NCCc1ccccc1)[C@@H]1CCNC[C@H]1COc1ccc2OCOc2c1 |r|
Structure
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