| Reaction Details |
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 | Report a problem with these data |
| Target | Beta-adrenergic receptor kinase 1 |
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| Ligand | BDBM50554258 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2048915 (CHEMBL4703614) |
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| IC50 | 19±n/a nM |
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| Citation |  Xu, G; Gaul, MD; Liu, Z; DesJarlais, RL; Qi, J; Wang, W; Krosky, D; Petrounia, I; Milligan, CM; Hermans, A; Lu, HR; Huang, DZ; Xu, JZ; Spurlino, JC Hit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor. Bioorg Med Chem Lett30:0 (2020) [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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| BDBM50554258 |
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| n/a |
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| Name | BDBM50554258 |
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| Synonyms: | CHEMBL4744858 |
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| Type | Small organic molecule |
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| Emp. Form. | C19H16N4O2 |
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| Mol. Mass. | 332.3559 |
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| SMILES | COc1cccc(Cn2ncc3ccc(cc3c2=O)-c2cn[nH]c2)c1 |
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| Structure | 
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