Reaction Details |
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Target | Beta-adrenergic receptor kinase 1 |
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Ligand | BDBM50173311 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Assays for Inhibition of GRKs |
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pH | 7±n/a |
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IC50 | 460±n/a nM |
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Comments | extracted |
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Citation | Larsen, SD; Homan, K; Waldschmidt, H; Tesmer, JJ G protein-coupled receptor kinase 2 inhibitors and methods for use of the same US Patent US10023564 Publication Date 7/17/2018 |
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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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BDBM50173311 |
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n/a |
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Name | BDBM50173311 |
Synonyms: | CHEMBL3810073 | US10023564, Example 6 |
Type | Small organic molecule |
Emp. Form. | C28H25FN6O4 |
Mol. Mass. | 528.5343 |
SMILES | COc1ccc(CNC(=O)c2cc(ccc2F)C2NC(=O)NC(C)=C2C(=O)Nc2ccc3[nH]ncc3c2)cc1 |c:24| |
Structure |
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