Target
Beta-adrenergic receptor kinase 1
Ligand
BDBM79499
Substrate
n/a
Meas. Tech.
Dose Response of inhibitors of GRK2 binding with RNA aptamer, Cherry Pick 1
EC50
9420±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:
BDBM79499
Synonyms:
MLS001004100 | N-[1-oxo-2-[(4-oxo-3-phenyl-2-quinazolinyl)thio]ethyl]-2-(2-oxo-1-pyrrolidinyl)acetamide | N-[2-(4-oxidanylidene-3-phenyl-quinazolin-2-yl)sulfanylethanoyl]-2-(2-oxidanylidenepyrrolidin-1-yl)ethanamide | N-[2-(4-oxo-3-phenylquinazolin-2-yl)sulfanylacetyl]-2-(2-oxopyrrolidin-1-yl)acetamide | N-[2-[(4-keto-3-phenyl-quinazolin-2-yl)thio]acetyl]-2-(2-ketopyrrolidino)acetamide | SMR000377687 | cid_2566682
Type:
Small organic molecule
Emp. Form.:
C22H20N4O4S
Mol. Mass.:
436.484
SMILES:
O=C(CSc1nc2ccccc2c(=O)n1-c1ccccc1)NC(=O)CN1CCCC1=O
Structure:
Search PDB for entries with ligand similarity: