| Reaction Details |
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 | Report a problem with these data |
| Target | Beta-adrenergic receptor kinase 2 |
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| Ligand | BDBM50257344 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEBML_1689810 |
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| IC50 | 4.3±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 2 |
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| Name: | Beta-adrenergic receptor kinase 2 |
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| Synonyms: | ADRBK2 | ARBK2_HUMAN | BARK2 | GRK3 |
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| Type: | PROTEIN |
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| Mol. Mass.: | 79721.92 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_615172 |
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| Residue: | 688 |
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| Sequence: | MADLEAVLADVSYLMAMEKSKATPAARASKRIVLPEPSIRSVMQKYLAERNEITFDKIFN
QKIGFLLFKDFCLNEINEAVPQVKFYEEIKEYEKLDNEEDRLCRSRQIYDAYIMKELLSC
SHPFSKQAVEHVQSHLSKKQVTSTLFQPYIEEICESLRGDIFQKFMESDKFTRFCQWKNV
ELNIHLTMNEFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNER
IMLSLVSTGDCPFIVCMTYAFHTPDKLCFILDLMNGGDLHYHLSQHGVFSEKEMRFYATE
IILGLEHMHNRFVVYRDLKPANILLDEHGHARISDLGLACDFSKKKPHASVGTHGYMAPE
VLQKGTAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTVNVELPDTFSPE
LKSLLEGLLQRDVSKRLGCHGGGSQEVKEHSFFKGVDWQHVYLQKYPPPLIPPRGEVNAA
DAFDIGSFDEEDTKGIKLLDCDQELYKNFPLVISERWQQEVTETVYEAVNADTDKIEARK
RAKNKQLGHEEDYALGKDCIMHGYMLKLGNPFLTQWQRRYFYLFPNRLEWRGEGESRQNL
LTMEQILSVEETQIKDKKCILFRIKGGKQFVLQCESDPEFVQWKKELNETFKEAQRLLRR
APKFLNKPRSGTVELPKPSLCHRNSNGL
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| BDBM50257344 |
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| n/a |
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| Name | BDBM50257344 |
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| Synonyms: | CHEMBL4065690 |
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| Type | Small organic molecule |
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| Emp. Form. | C24H23N5O |
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| Mol. Mass. | 397.4723 |
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| SMILES | Cc1c(CNc2cccc(c2)C(=O)NCc2ccccc2)[nH]nc1-c1ccncc1 |
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| Structure | 
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