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Target
Rhodopsin kinase GRK1
Ligand
BDBM50173324
Substrate
n/a
Meas. Tech.
ChEMBL_1581284 (CHEMBL3811361)
IC50
>100000±n/a nM
Citation
 Waldschmidt, HV; Homan, KT; Cruz-Rodríguez, O; Cato, MC; Waninger-Saroni, J; Larimore, KM; Cannavo, A; Song, J; Cheung, JY; Kirchhoff, PD; Koch, WJ; Tesmer, JJ; Larsen, SD Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J Med Chem 59:3793-807 (2016) [PubMed]  Article 
Target
Name:
Rhodopsin kinase GRK1
Synonyms:
G protein-coupled receptor kinase 1 | GRK1 | GRK1_HUMAN | PK | RHOK | Rhodopsin kinase
Type:
PROTEIN
Mol. Mass.:
63520.09
Organism:
Homo sapiens (Human)
Description:
ChEMBL_774378
Residue:
563
Sequence:
MDFGSLETVVANSAFIAARGSFDGSSSQPSRDKKYLAKLKLPPLSKCESLRDSLSLEFESVCLEQPIGKKLFQQFLQSAEKHLPALELWKDIEDYDTADNDLQPQKAQTILAQYLDPQAKLFCSFLDEGIVAKFKEGPVEIQDGLFQPLLQATLAHLGQAPFQEYLGSLYFLRFLQWKWLEAQPMGEDWFLDFRVLGKGGFGEVSACQMKATGKLYACKKLNKKRLKKRKGYQGAMVEKKILMKVHSRFIVSLAYAFETKADLCLVMTIMNGGDIRYHIYNVNEENPGFPEPRALFYTAQIICGLEHLHQRRIVYRDLKPENVLLDNDGNVRISDLGLAVELLDGQSKTKGYAGTPGFMAPELLQGEEYDFSVDYFALGVTLYEMIAARGPFRARGEKVENKELKHRIISEPVKYPDKFSQASKDFCEALLEKDPEKRLGFRDETCDKLRAHPLFKDLNWRQLEAGMLMPPFIPDSKTVYAKDIQDVGAFSTVKGVAFDKTDTEFFQEFATGNCPIPWQEEMIETGIFGELNVWRSDGQMPDDMKGISGGSSSSSKSGMCLVS
  
Inhibitor
Name:
BDBM50173324
Synonyms:
CHEMBL3809124 | US10023564, Example 30
Type:
Small organic molecule
Emp. Form.:
C30H29FN6O5
Mol. Mass.:
572.5869
SMILES:
COc1cccc(OC)c1CNC(=O)Cc1cc(ccc1F)C1NC(=O)NC(C)=C1C(=O)Nc1ccc2[nH]ncc2c1 |c:30|
Structure:
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