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TargetBeta-adrenergic receptor kinase 1
LigandBDBM50444090
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1280628
IC50 460±n/a nM
Citation Cho, SYLee, BHJung, HYun, CSHa, JDKim, HRChae, CHLee, JHSeo, HWOh, KS Design and synthesis of novel 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine derivatives as selective G-protein-coupled receptor kinase-2 and -5 inhibitors. Bioorg Med Chem Lett23:6711-6 (2013) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Beta-adrenergic receptor kinase 1
Name:Beta-adrenergic receptor kinase 1
Synonyms:ADRBK1 | BARK | BARK1 | Beta-ARK-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:
MADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFS
QKLGYLLFRDFCLNHLEEARPLVEFYEEIKKYEKLETEEERVARSREIFDSYIMKELLAC
SHPFSKSATEHVQGHLGKKQVPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNV
ELNIHLTMNDFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNER
IMLSLVSTGDCPFIVCMSYAFHTPDKLSFILDLMNGGDLHYHLSQHGVFSEADMRFYAAE
IILGLEHMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHASVGTHGYMAPE
VLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAVELPDSFSPE
LRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMVFLQKYPPPLIPPRGEVNAA
DAFDIGSFDEEDTKGIKLLDSDQELYRNFPLTISERWQQEVAETVFDTINAETDRLEARK
KAKNKQLGHEEDYALGKDCIMHGYMSKMGNPFLTQWQRRYFYLFPNRLEWRGEGEAPQSL
LTMEEIQSVEETQIKERKCLLLKIRGGKQFILQCDSDPELVQWKKELRDAYREAQQLVQR
VPKMKNKPRSPVVELSKVPLVQRGSANGL
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50444090
NameBDBM50444090
Synonyms:CHEMBL3093151
TypeSmall organic molecule
Emp. Form.C24H27N7O
Mol. Mass.429.5175
SMILESNc1ncc(cc1-c1nc2ccc(cc2o1)N1CCCC1)-c1cnn(c1)C1CCNCC1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
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