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Target
Rhodopsin kinase GRK1
Ligand
BDBM50260141
Substrate
n/a
Meas. Tech.
ChEBML_1692745
IC50
86500±n/a nM
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 Chem 60:3052-3069 (2017) [PubMed]  Article
Target
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:
MDFGSLETVVANSAFIAARGSFDASSGPASRDRKYLARLKLPPLSKCEALRESLDLGFEGMCLEQPIGKRLFQQFLRTHEQHGPALQLWKDIEDYDTADDALRPQKAQALRAAYLEPQAQLFCSFLDAETVARARAGAGDGLFQPLLRAVLAHLGQAPFQEFLDSLYFLRFLQWKWLEAQPMGEDWFLDFRVLGRGGFGEVFACQMKATGKLYACKKLNKKRLKKRKGYQGAMVEKKILAKVHSRFIVSLAYAFETKTDLCLVMTIMNGGDIRYHIYNVDEDNPGFQEPRAIFYTAQIVSGLEHLHQRNIIYRDLKPENVLLDDDGNVRISDLGLAVELKAGQTKTKGYAGTPGFMAPELLLGEEYDFSVDYFALGVTLYEMIAARGPFRARGEKVENKELKQRVLEQAVTYPDKFSPASKDFCEALLQKDPEKRLGFRDGSCDGLRTHPLFRDISWRQLEAGMLTPPFVPDSRTVYAKNIQDVGAFSTVKGVAFEKADTEFFQEFASGTCPIPWQEEMIETGVFGDLNVWRPDGQMPDDMKGVSGQEAAPSSKSGMCVLS
  
Inhibitor
Name:
BDBM50260141
Synonyms:
CHEMBL4097393
Type:
Small organic molecule
Emp. Form.:
C25H27FN4O4
Mol. Mass.:
466.5047
SMILES:
Cc1cc(CNC(=O)c2cc(ccc2F)[C@@H]2CCNC[C@H]2COc2ccc3OCOc3c2)n[nH]1 |r|
Structure:
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