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TargetBeta-adrenergic receptor kinase 1
LigandBDBM50173325
Substrate/Competitorn/a
Meas. Tech.Assays for Inhibition of GRKs
pH7±n/a
IC50 60.0±n/a nM
Commentsextracted
Citation Larsen, SDHoman, KWaldschmidt, HTesmer, JJ G protein-coupled receptor kinase 2 inhibitors and methods for use of the same US Patent US10023564 Publication Date 7/17/2018
More Info.:Get all data from this article,  Assay Method
 
Beta-adrenergic receptor kinase 1
Name:Beta-adrenergic receptor kinase 1
Synonyms:ADRBK1 | BARK | BARK1 | Beta-ARK-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:
BDBM50173325
NameBDBM50173325
Synonyms:CHEMBL3809965 | US10023564, Example 5
TypeSmall organic molecule
Emp. Form.C28H25FN6O4
Mol. Mass.528.5343
SMILESCOc1ccccc1CNC(=O)c1cc(ccc1F)C1NC(=O)NC(C)=C1C(=O)Nc1ccc2[nH]ncc2c1 |c:27|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
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