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Target
Beta-adrenergic receptor kinase 1
Ligand
BDBM54754
Substrate
n/a
Meas. Tech.
Dose Response of inhibitors of GRK2 binding with RNA aptamer, Cherry Pick 1
EC50
33270±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:
BDBM54754
Synonyms:
3-[(4-ketocyclohexa-2,5-dien-1-ylidene)methyl]-2,4-dihydro-1H-cyclopenta[b]quinoline-9-carboxylic acid | 3-[(4-oxidanylidenecyclohexa-2,5-dien-1-ylidene)methyl]-2,4-dihydro-1H-cyclopenta[b]quinoline-9-carboxylic acid | 3-[(4-oxo-1-cyclohexa-2,5-dienylidene)methyl]-2,4-dihydro-1H-cyclopenta[b]quinoline-9-carboxylic acid | 3-[(4-oxocyclohexa-2,5-dien-1-ylidene)methyl]-2,4-dihydro-1H-cyclopenta[b]quinoline-9-carboxylic acid | MLS000776136 | SMR000371150 | cid_5908804
Type:
Small organic molecule
Emp. Form.:
C20H15NO3
Mol. Mass.:
317.338
SMILES:
OC(=O)c1c2CCC(=Cc3ccc(O)cc3)c2nc2ccccc12 |w:8.8|
Structure:
Search PDB for entries with ligand similarity: