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Target
Beta-adrenergic receptor kinase 1
Ligand
BDBM50540741
Substrate
n/a
Meas. Tech.
ChEMBL_1982692 (CHEMBL4615954)
IC50
11±n/a nM
Citation
 Prati, F; Buonfiglio, R; Furlotti, G; Cavarischia, C; Mangano, G; Picollo, R; Oggianu, L; di Matteo, A; Olivieri, S; Bovi, G; Porceddu, PF; Reggiani, A; Garrone, B; Di Giorgio, FP; Ombrato, R Optimization of Indazole-Based GSK-3 Inhibitors with Mitigated hERG Issue and  ACS Med Chem Lett 11:825-831 (2020) [PubMed]  Article 
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:
BDBM50540741
Synonyms:
CHEMBL4640019
Type:
Small organic molecule
Emp. Form.:
C20H22N4O3
Mol. Mass.:
366.4137
SMILES:
OCc1cncc(c1)-c1ccc2[nH]nc(C(=O)NCC3CCOCC3)c2c1
Structure:
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