Reaction Details |
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Target | Rhodopsin kinase GRK1 |
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Ligand | BDBM50173320 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEBML_1692745 |
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IC50 | >100000±n/a nM |
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Citation | Waldschmidt, HV; Homan, KT; Cato, MC; Cruz-Rodríguez, O; Cannavo, A; Wilson, MW; Song, J; Cheung, JY; Koch, WJ; Tesmer, JJ; Larsen, SD Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. J Med Chem60:3052-3069 (2017) [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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BDBM50173320 |
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n/a |
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Name | BDBM50173320 |
Synonyms: | GSK-180736A | GSK180736A | US10023564, Compound GSK180736A |
Type | Small organic molecule |
Emp. Form. | C19H16FN5O2 |
Mol. Mass. | 365.361 |
SMILES | CC1=C(C(NC(=O)N1)c1ccc(F)cc1)C(=O)Nc1ccc2[nH]ncc2c1 |t:1| |
Structure |
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