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Target
Beta-adrenergic receptor kinase 1
Ligand
BDBM50257426
Substrate
n/a
Meas. Tech.
ChEMBL_1689805 (CHEMBL4040375)
IC50
3.9±n/a nM
Citation
 Okawa, T; Aramaki, Y; Yamamoto, M; Kobayashi, T; Fukumoto, S; Toyoda, Y; Henta, T; Hata, A; Ikeda, S; Kaneko, M; Hoffman, ID; Sang, BC; Zou, H; Kawamoto, T Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. J Med Chem 60:6942-6990 (2017) [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:
BDBM50257426
Synonyms:
CHEMBL4077447
Type:
Small organic molecule
Emp. Form.:
C22H19ClN6O
Mol. Mass.:
418.879
SMILES:
Clc1ccccc1CNC(=O)c1cccc(NCc2nnc([nH]2)-c2ccncc2)c1
Structure:
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