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Target
Beta-adrenergic receptor kinase 1
Ligand
BDBM79503
Substrate
n/a
Meas. Tech.
Dose Response of inhibitors of GRK2 binding with RNA aptamer, Cherry Pick 1
EC50
4380±n/a nM
Citation
 PubChem, PC Dose Response of inhibitors of GRK2 binding with RNA aptamer, Cherry Pick 1 PubChem Bioassay (2011)[AID] 
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:
BDBM79503
Synonyms:
(8S)-3-[3-(caproylamino)phenyl]-7-p-anisoyl-1-oxa-2,7-diazaspiro[4.4]non-2-ene-8-carboxamide | (8S)-3-[3-(hexanoylamino)phenyl]-7-(4-methoxybenzoyl)-1-oxa-2,7-diazaspiro[4.4]non-2-ene-8-carboxamide | (8S)-3-[3-(hexanoylamino)phenyl]-7-(4-methoxyphenyl)carbonyl-1-oxa-2,7-diazaspiro[4.4]non-2-ene-8-carboxamide | (8S)-7-[(4-methoxyphenyl)-oxomethyl]-3-[3-(1-oxohexylamino)phenyl]-1-oxa-2,7-diazaspiro[4.4]non-2-ene-8-carboxamide | MLS000561965 | SMR000390668 | cid_16745480
Type:
Small organic molecule
Emp. Form.:
C27H32N4O5
Mol. Mass.:
492.5668
SMILES:
CCCCCC(=O)Nc1cccc(c1)C1=NOC2(C[C@H](N(C2)C(=O)c2ccc(OC)cc2)C(N)=O)C1 |t:15|
Structure:
Search PDB for entries with ligand similarity: