Target
Beta-adrenergic receptor kinase 1
Ligand
BDBM50715
Substrate
n/a
Meas. Tech.
Dose Response of inhibitors of GRK2 binding with RNA aptamer, Cherry Pick 1
EC50
21280±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:
BDBM50715
Synonyms:
(8R)-3-[3-[(2-methyl-1-oxoprop-2-enyl)amino]phenyl]-7-[(E)-1-oxobut-2-enyl]-1-oxa-2,7-diazaspiro[4.4]non-2-ene-8-carboxamide | (8R)-7-[(E)-but-2-enoyl]-3-(3-methacrylamidophenyl)-1-oxa-2,7-diazaspiro[4.4]non-2-ene-8-carboxamide | (8R)-7-[(E)-but-2-enoyl]-3-[3-(2-methylprop-2-enoylamino)phenyl]-1-oxa-2,7-diazaspiro[4.4]non-2-ene-8-carboxamide | MLS000561975 | SMR000390639 | cid_16745482
Type:
Small organic molecule
Emp. Form.:
C21H24N4O4
Mol. Mass.:
396.4397
SMILES:
C\C=C\C(=O)N1CC2(C[C@@H]1C(N)=O)CC(=NO2)c1cccc(NC(=O)C(C)=C)c1 |c:15|
Structure:
Search PDB for entries with ligand similarity: