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Target
Beta-adrenergic receptor kinase 2
Ligand
BDBM50257344
Substrate
n/a
Meas. Tech.
ChEBML_1689810
IC50
4.3±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 2
Synonyms:
ADRBK2 | ARBK2_HUMAN | BARK2 | GRK3
Type:
PROTEIN
Mol. Mass.:
79721.92
Organism:
Homo sapiens (Human)
Description:
ChEMBL_615172
Residue:
688
Sequence:
MADLEAVLADVSYLMAMEKSKATPAARASKRIVLPEPSIRSVMQKYLAERNEITFDKIFNQKIGFLLFKDFCLNEINEAVPQVKFYEEIKEYEKLDNEEDRLCRSRQIYDAYIMKELLSCSHPFSKQAVEHVQSHLSKKQVTSTLFQPYIEEICESLRGDIFQKFMESDKFTRFCQWKNVELNIHLTMNEFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNERIMLSLVSTGDCPFIVCMTYAFHTPDKLCFILDLMNGGDLHYHLSQHGVFSEKEMRFYATEIILGLEHMHNRFVVYRDLKPANILLDEHGHARISDLGLACDFSKKKPHASVGTHGYMAPEVLQKGTAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTVNVELPDTFSPELKSLLEGLLQRDVSKRLGCHGGGSQEVKEHSFFKGVDWQHVYLQKYPPPLIPPRGEVNAADAFDIGSFDEEDTKGIKLLDCDQELYKNFPLVISERWQQEVTETVYEAVNADTDKIEARKRAKNKQLGHEEDYALGKDCIMHGYMLKLGNPFLTQWQRRYFYLFPNRLEWRGEGESRQNLLTMEQILSVEETQIKDKKCILFRIKGGKQFVLQCESDPEFVQWKKELNETFKEAQRLLRRAPKFLNKPRSGTVELPKPSLCHRNSNGL
  
Inhibitor
Name:
BDBM50257344
Synonyms:
CHEMBL4065690
Type:
Small organic molecule
Emp. Form.:
C24H23N5O
Mol. Mass.:
397.4723
SMILES:
Cc1c(CNc2cccc(c2)C(=O)NCc2ccccc2)[nH]nc1-c1ccncc1
Structure:
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