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Target
Beta-adrenergic receptor kinase 1
Ligand
BDBM22416
Substrate
n/a
Meas. Tech.
ChEMBL_2236421 (CHEMBL5150317)
IC50
1100±n/a nM
Citation
 Xie, Z; Yang, X; Duan, Y; Han, J; Liao, C Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases. J Med Chem 64:1283-1345 (2021) [PubMed] 
Target
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:
MADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFSQKLGYLLFRDFCLNHLEEARPLVEFYEEIKKYEKLETEEERVARSREIFDSYIMKELLACSHPFSKSATEHVQGHLGKKQVPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNVELNIHLTMNDFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNERIMLSLVSTGDCPFIVCMSYAFHTPDKLSFILDLMNGGDLHYHLSQHGVFSEADMRFYAAEIILGLEHMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHASVGTHGYMAPEVLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAVELPDSFSPELRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMVFLQKYPPPLIPPRGEVNAADAFDIGSFDEEDTKGIKLLDSDQELYRNFPLTISERWQQEVAETVFDTINAETDRLEARKKAKNKQLGHEEDYALGKDCIMHGYMSKMGNPFLTQWQRRYFYLFPNRLEWRGEGEAPQSLLTMEEIQSVEETQIKERKCLLLKIRGGKQFILQCDSDPELVQWKKELRDAYREAQQLVQRVPKMKNKPRSPVVELSKVPLVQRGSANGL
  
Inhibitor
Name:
BDBM22416
Synonyms:
(3S,4R)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)piperidine | (3S,4R)-3-[(2H-1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)piperidine | CHEMBL490 | PAROXETINE | US09969700, Paroxetine | US9944618, Compound ID No. 182 | [3H]Paroxetine
Type:
radiolabeled ligand
Emp. Form.:
C19H20FNO3
Mol. Mass.:
329.3654
SMILES:
Fc1ccc(cc1)[C@@H]1CCNC[C@H]1COc1ccc2OCOc2c1
Structure:
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