Reaction Details |
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Target | Rhodopsin kinase GRK1 |
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Ligand | BDBM50529469 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1908745 (CHEMBL4411103) |
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IC50 | 760±n/a nM |
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Citation | Rowlands, RA; Cato, MC; Waldschmidt, HV; Bouley, RA; Chen, Q; Avramova, L; Larsen, SD; Tesmer, JJG; White, AD Structure-Based Design of Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. ACS Med Chem Lett10:1628-1634 (2019) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Rhodopsin kinase GRK1 |
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Name: | Rhodopsin kinase GRK1 |
Synonyms: | G protein-coupled receptor kinase 1 | GRK1 | GRK1_BOVIN | RHOK | Rhodopsin kinase |
Type: | PROTEIN |
Mol. Mass.: | 62931.24 |
Organism: | Bos taurus |
Description: | ChEMBL_116985 |
Residue: | 561 |
Sequence: | MDFGSLETVVANSAFIAARGSFDASSGPASRDRKYLARLKLPPLSKCEALRESLDLGFEG
MCLEQPIGKRLFQQFLRTHEQHGPALQLWKDIEDYDTADDALRPQKAQALRAAYLEPQAQ
LFCSFLDAETVARARAGAGDGLFQPLLRAVLAHLGQAPFQEFLDSLYFLRFLQWKWLEAQ
PMGEDWFLDFRVLGRGGFGEVFACQMKATGKLYACKKLNKKRLKKRKGYQGAMVEKKILA
KVHSRFIVSLAYAFETKTDLCLVMTIMNGGDIRYHIYNVDEDNPGFQEPRAIFYTAQIVS
GLEHLHQRNIIYRDLKPENVLLDDDGNVRISDLGLAVELKAGQTKTKGYAGTPGFMAPEL
LLGEEYDFSVDYFALGVTLYEMIAARGPFRARGEKVENKELKQRVLEQAVTYPDKFSPAS
KDFCEALLQKDPEKRLGFRDGSCDGLRTHPLFRDISWRQLEAGMLTPPFVPDSRTVYAKN
IQDVGAFSTVKGVAFEKADTEFFQEFASGTCPIPWQEEMIETGVFGDLNVWRPDGQMPDD
MKGVSGQEAAPSSKSGMCVLS
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BDBM50529469 |
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n/a |
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Name | BDBM50529469 |
Synonyms: | CHEMBL4456539 |
Type | Small organic molecule |
Emp. Form. | C26H28N8O3 |
Mol. Mass. | 500.5523 |
SMILES | COc1cc(NC(=O)\C=C\CN(C)C)ccc1Nc1nc(Nc2ccccc2C(N)=O)c2cc[nH]c2n1 |
Structure |
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