Reaction Details |
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Target | Beta-adrenergic receptor kinase 1 |
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Ligand | BDBM50257350 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1692744 (CHEMBL4043634) |
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IC50 | 30±n/a nM |
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Citation | Waldschmidt, HV; Homan, KT; Cato, MC; Cruz-Rodríguez, O; Cannavo, A; Wilson, MW; Song, J; Cheung, JY; Koch, WJ; Tesmer, JJ; Larsen, SD Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. J Med Chem60:3052-3069 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Beta-adrenergic receptor kinase 1 |
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Name: | Beta-adrenergic receptor kinase 1 |
Synonyms: | ADRBK1 | ARBK1_BOVIN | Beta-ARK-1 | Beta-adrenergic receptor kinase 1 | G-protein-coupled receptor kinase 2 | GRK2 |
Type: | PROTEIN |
Mol. Mass.: | 79654.58 |
Organism: | Bos taurus |
Description: | ChEMBL_113511 |
Residue: | 689 |
Sequence: | MADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFS
QKLGYLLFRDFCLKHLEEAKPLVEFYEEIKKYEKLETEEERLVCSREIFDTYIMKELLAC
SHPFSKSAIEHVQGHLVKKQVPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNV
ELNIHLTMNDFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNER
IMLSLVSTGDCPFIVCMSYAFHTPDKLSFILDLMNGGDLHYHLSQHGVFSEADMRFYAAE
IILGLEHMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHASVGTHGYMAPE
VLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAVELPDSFSPE
LRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMVFLQKYPPPLIPPRGEVNAA
DAFDIGSFDEEDTKGIKLLDSDQELYRNFPLTISERWQQEVAETVFDTINAETDRLEARK
KTKNKQLGHEEDYALGKDCIMHGYMSKMGNPFLTQWQRRYFYLFPNRLEWRGEGEAPQSL
LTMEEIQSVEETQIKERKCLLLKIRGGKQFVLQCDSDPELVQWKKELRDAYREAQQLVQR
VPKMKNKPRSPVVELSKVPLIQRGSANGL
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BDBM50257350 |
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n/a |
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Name | BDBM50257350 |
Synonyms: | CHEMBL1738877 |
Type | Small organic molecule |
Emp. Form. | C24H21F3N6O |
Mol. Mass. | 466.4583 |
SMILES | Cn1c(CNc2cccc(c2)C(=O)NCc2ccccc2C(F)(F)F)nnc1-c1ccncc1 |
Structure |
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