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Target
Beta-adrenergic receptor kinase 1
Ligand
BDBM258595
Substrate
n/a
Meas. Tech.
Competition Binding Assay
Temperature
298.15±n/a K
IC50
>20±n/a nM
Comments
extracted
Citation
 Akama, T; Jarnagin, K; Zhang, Y; Zhou, Y; Plattner, JJ; Sullivan, DC Boron-containing small molecules US Patent  US9493490 Publication Date 11/15/2016 
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:
BDBM258595
Synonyms:
US9493490, 6-(4-(aminomethyl)-2-fluorophenoxy)-7-methylbenzo[c][1,2]oxaborol-1(3H)-ol | US9493490, D | US9493490, Example 4
Type:
Small organic molecule
Emp. Form.:
C15H15BFNO3
Mol. Mass.:
287.094
SMILES:
Cc1c2B(O)OCc2ccc1Oc1ccc(CN)cc1F
Structure:
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