| Reaction Details |
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 | Report a problem with these data |
| Target | Beta-adrenergic receptor kinase 1 |
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| Ligand | BDBM283996 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1771205 (CHEMBL4223317) |
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| IC50 | 160±n/a nM |
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| Citation |  Waldschmidt, HV; Bouley, R; Kirchhoff, PD; Lee, P; Tesmer, JJG; Larsen, SD Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors. Bioorg Med Chem Lett28:1507-1515 (2018) [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_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 |
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| Type: | Enzyme |
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| Mol. Mass.: | 79581.30 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P25098 |
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| Residue: | 689 |
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| Sequence: | MADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFS
QKLGYLLFRDFCLNHLEEARPLVEFYEEIKKYEKLETEEERVARSREIFDSYIMKELLAC
SHPFSKSATEHVQGHLGKKQVPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNV
ELNIHLTMNDFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNER
IMLSLVSTGDCPFIVCMSYAFHTPDKLSFILDLMNGGDLHYHLSQHGVFSEADMRFYAAE
IILGLEHMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHASVGTHGYMAPE
VLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAVELPDSFSPE
LRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMVFLQKYPPPLIPPRGEVNAA
DAFDIGSFDEEDTKGIKLLDSDQELYRNFPLTISERWQQEVAETVFDTINAETDRLEARK
KAKNKQLGHEEDYALGKDCIMHGYMSKMGNPFLTQWQRRYFYLFPNRLEWRGEGEAPQSL
LTMEEIQSVEETQIKERKCLLLKIRGGKQFILQCDSDPELVQWKKELRDAYREAQQLVQR
VPKMKNKPRSPVVELSKVPLVQRGSANGL
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| BDBM283996 |
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| n/a |
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| Name | BDBM283996 |
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| Synonyms: | E22 | US10023564, Example 22 |
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| Type | Small organic molecule |
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| Emp. Form. | C25H23FN8O4 |
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| Mol. Mass. | 518.4997 |
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| SMILES | CCc1nc(CNC(=O)c2cc(ccc2F)C2NC(=O)NC(C)=C2C(=O)Nc2ccc3[nH]ncc3c2)no1 |c:23| |
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| Structure | 
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