Reaction Details
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Target
Beta-adrenergic receptor kinase 1
Ligand
BDBM48373
Substrate
n/a
Meas. Tech.
Dose Response of inhibitors of GRK2 binding with RNA aptamer, Cherry Pick 1
EC50
22080±n/a nM
Citation
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More Info.:
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:
BDBM48373
Synonyms:
MLS000081944 | N-(2-furanylmethyl)-2-[(6-methyl-4-oxo-1H-pyrimidin-2-yl)thio]acetamide | N-(2-furfuryl)-2-[(4-keto-6-methyl-1H-pyrimidin-2-yl)thio]acetamide | N-(furan-2-ylmethyl)-2-[(6-methyl-4-oxidanylidene-1H-pyrimidin-2-yl)sulfanyl]ethanamide | N-(furan-2-ylmethyl)-2-[(6-methyl-4-oxo-1H-pyrimidin-2-yl)sulfanyl]acetamide | SMR000061049 | cid_586221
Type:
Small organic molecule
Emp. Form.:
C12H13N3O3S
Mol. Mass.:
279.315
SMILES:
Cc1cc(=O)[nH]c(SCC(=O)NCc2ccco2)n1