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TargetRhodopsin kinase GRK1
LigandBDBM50173329
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1581284 (CHEMBL3811361)
IC50>100000±n/a nM
Citation Waldschmidt, HVHoman, KTCruz-Rodríguez, OCato, MCWaninger-Saroni, JLarimore, KMCannavo, ASong, JCheung, JYKirchhoff, PDKoch, WJTesmer, JJLarsen, SD Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J Med Chem59:3793-807 (2016) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Rhodopsin kinase GRK1
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:
MDFGSLETVVANSAFIAARGSFDGSSSQPSRDKKYLAKLKLPPLSKCESLRDSLSLEFES
VCLEQPIGKKLFQQFLQSAEKHLPALELWKDIEDYDTADNDLQPQKAQTILAQYLDPQAK
LFCSFLDEGIVAKFKEGPVEIQDGLFQPLLQATLAHLGQAPFQEYLGSLYFLRFLQWKWL
EAQPMGEDWFLDFRVLGKGGFGEVSACQMKATGKLYACKKLNKKRLKKRKGYQGAMVEKK
ILMKVHSRFIVSLAYAFETKADLCLVMTIMNGGDIRYHIYNVNEENPGFPEPRALFYTAQ
IICGLEHLHQRRIVYRDLKPENVLLDNDGNVRISDLGLAVELLDGQSKTKGYAGTPGFMA
PELLQGEEYDFSVDYFALGVTLYEMIAARGPFRARGEKVENKELKHRIISEPVKYPDKFS
QASKDFCEALLEKDPEKRLGFRDETCDKLRAHPLFKDLNWRQLEAGMLMPPFIPDSKTVY
AKDIQDVGAFSTVKGVAFDKTDTEFFQEFATGNCPIPWQEEMIETGIFGELNVWRSDGQM
PDDMKGISGGSSSSSKSGMCLVS
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  Blast E-value cutoff:
BDBM50173329
n/a
NameBDBM50173329
Synonyms:CHEMBL3809697 | US10023564, Example 15
TypeSmall organic molecule
Emp. Form.C27H24FN7O3
Mol. Mass.513.523
SMILESCC1=C(C(NC(=O)N1)c1ccc(F)c(c1)C(=O)NCc1ncccc1C)C(=O)Nc1ccc2[nH]ncc2c1 |t:1|
Structure
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