| Reaction Details |
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 | Report a problem with these data |
| Target | Beta-adrenergic receptor kinase 1 |
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| Ligand | BDBM50529469 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1908746 (CHEMBL4411104) |
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| IC50 | 680±n/a nM |
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| Citation |  Rowlands, RA; Cato, MC; Waldschmidt, HV; Bouley, RA; Chen, Q; Avramova, L; Larsen, SD; Tesmer, JJG; White, AD Structure-Based Design of Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. ACS Med Chem Lett10:1628-1634 (2019) [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 |
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| Synonyms: | ADRBK1 | ARBK1_BOVIN | Beta-ARK-1 | Beta-adrenergic receptor kinase 1 | G-protein-coupled receptor kinase 2 | GRK2 |
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| Type: | PROTEIN |
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| Mol. Mass.: | 79654.58 |
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| Organism: | Bos taurus |
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| Description: | ChEMBL_113511 |
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| Residue: | 689 |
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| Sequence: | MADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFS
QKLGYLLFRDFCLKHLEEAKPLVEFYEEIKKYEKLETEEERLVCSREIFDTYIMKELLAC
SHPFSKSAIEHVQGHLVKKQVPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNV
ELNIHLTMNDFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNER
IMLSLVSTGDCPFIVCMSYAFHTPDKLSFILDLMNGGDLHYHLSQHGVFSEADMRFYAAE
IILGLEHMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHASVGTHGYMAPE
VLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAVELPDSFSPE
LRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMVFLQKYPPPLIPPRGEVNAA
DAFDIGSFDEEDTKGIKLLDSDQELYRNFPLTISERWQQEVAETVFDTINAETDRLEARK
KTKNKQLGHEEDYALGKDCIMHGYMSKMGNPFLTQWQRRYFYLFPNRLEWRGEGEAPQSL
LTMEEIQSVEETQIKERKCLLLKIRGGKQFVLQCDSDPELVQWKKELRDAYREAQQLVQR
VPKMKNKPRSPVVELSKVPLIQRGSANGL
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| BDBM50529469 |
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| n/a |
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| Name | BDBM50529469 |
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| Synonyms: | CHEMBL4456539 |
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| Type | Small organic molecule |
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| Emp. Form. | C26H28N8O3 |
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| Mol. Mass. | 500.5523 |
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| SMILES | COc1cc(NC(=O)\C=C\CN(C)C)ccc1Nc1nc(Nc2ccccc2C(N)=O)c2cc[nH]c2n1 |
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| Structure | 
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