| Reaction Details |
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 | Report a problem with these data |
| Target | Beta-adrenergic receptor kinase 1 |
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| Ligand | BDBM50257366 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEBML_1689808 |
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| IC50 | 14±n/a nM |
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| Citation |  Okawa, T; Aramaki, Y; Yamamoto, M; Kobayashi, T; Fukumoto, S; Toyoda, Y; Henta, T; Hata, A; Ikeda, S; Kaneko, M; Hoffman, ID; Sang, BC; Zou, H; Kawamoto, T Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. J Med Chem60:6942-6990 (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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| BDBM50257366 |
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| n/a |
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| Name | BDBM50257366 |
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| Synonyms: | CHEMBL4082559 |
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| Type | Small organic molecule |
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| Emp. Form. | C18H20N4O2 |
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| Mol. Mass. | 324.377 |
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| SMILES | COc1cccc(NCC(=O)N\N=C2/CCCc3cnccc23)c1 |
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| Structure | 
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