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Target
Rhodopsin kinase GRK1
Ligand
BDBM50529469
Substrate
n/a
Meas. Tech.
ChEMBL_1908745 (CHEMBL4411103)
IC50
760±n/a nM
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 Lett 10:1628-1634 (2019) [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:
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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