| Reaction Details |
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 | Report a problem with these data |
| Target | Beta-adrenergic receptor kinase 1 |
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| Ligand | BDBM22416 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEBML_1692743 |
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| IC50 | 1380±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 |
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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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| BDBM22416 |
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| n/a |
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| Name | BDBM22416 |
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| Synonyms: | (3S,4R)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)piperidine | (3S,4R)-3-[(2H-1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)piperidine | CHEMBL490 | PAROXETINE | US09969700, Paroxetine | US9944618, Compound ID No. 182 | [3H]Paroxetine |
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| Type | radiolabeled ligand |
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| Emp. Form. | C19H20FNO3 |
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| Mol. Mass. | 329.3654 |
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| SMILES | Fc1ccc(cc1)[C@@H]1CCNC[C@H]1COc1ccc2OCOc2c1 |
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| Structure | 
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