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Target
Beta-adrenergic receptor kinase 1
Ligand
BDBM50173326
Substrate
n/a
Meas. Tech.
Assays for Inhibition of GRKs
pH
7±n/a
IC50
>100000±n/a nM
Comments
extracted
Citation
 Larsen, SD; Homan, K; Waldschmidt, H; Tesmer, JJ G protein-coupled receptor kinase 2 inhibitors and methods for use of the same US Patent  US10023564 Publication Date 7/17/2018 
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:
BDBM50173326
Synonyms:
CHEMBL3809604 | US10023564, Example 29
Type:
Small organic molecule
Emp. Form.:
C30H23F7N6O3
Mol. Mass.:
648.5308
SMILES:
CC1=C(C(NC(=O)N1)c1ccc(F)c(CC(=O)NCc2c(cccc2C(F)(F)F)C(F)(F)F)c1)C(=O)Nc1ccc2[nH]ncc2c1 |t:1|
Structure:
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