Reaction Details |
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Target | Beta-adrenergic receptor kinase 1 |
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Ligand | BDBM50444101 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1280628 (CHEMBL3096889) |
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IC50 | 3060±n/a nM |
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Citation | Cho, SY; Lee, BH; Jung, H; Yun, CS; Ha, JD; Kim, HR; Chae, CH; Lee, JH; Seo, HW; Oh, KS Design and synthesis of novel 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine derivatives as selective G-protein-coupled receptor kinase-2 and -5 inhibitors. Bioorg Med Chem Lett23:6711-6 (2013) [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 |
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 |
Type: | Enzyme |
Mol. Mass.: | 79581.30 |
Organism: | Homo sapiens (Human) |
Description: | P25098 |
Residue: | 689 |
Sequence: | MADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFS
QKLGYLLFRDFCLNHLEEARPLVEFYEEIKKYEKLETEEERVARSREIFDSYIMKELLAC
SHPFSKSATEHVQGHLGKKQVPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNV
ELNIHLTMNDFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNER
IMLSLVSTGDCPFIVCMSYAFHTPDKLSFILDLMNGGDLHYHLSQHGVFSEADMRFYAAE
IILGLEHMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHASVGTHGYMAPE
VLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAVELPDSFSPE
LRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMVFLQKYPPPLIPPRGEVNAA
DAFDIGSFDEEDTKGIKLLDSDQELYRNFPLTISERWQQEVAETVFDTINAETDRLEARK
KAKNKQLGHEEDYALGKDCIMHGYMSKMGNPFLTQWQRRYFYLFPNRLEWRGEGEAPQSL
LTMEEIQSVEETQIKERKCLLLKIRGGKQFILQCDSDPELVQWKKELRDAYREAQQLVQR
VPKMKNKPRSPVVELSKVPLVQRGSANGL
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BDBM50444101 |
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n/a |
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Name | BDBM50444101 |
Synonyms: | CHEMBL3093250 |
Type | Small organic molecule |
Emp. Form. | C27H26N6O2 |
Mol. Mass. | 466.5343 |
SMILES | COc1ccc(cc1)-c1ccc2nc(oc2c1)-c1cc(cnc1N)-c1cnn(c1)C1CCNCC1 |
Structure |
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