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TargetRhodopsin kinase
LigandBDBM50173325
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1581284
IC50 16000±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 Chem 59:3793-807 (2016) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
Rhodopsin kinase
Name:Rhodopsin kinase
Synonyms:G protein-coupled receptor kinase 1 | GRK1 | PK | RHOK
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:
BDBM50173325
n/a
NameBDBM50173325
Synonyms:CHEMBL3809965 | US10023564, Example 5
TypeSmall organic molecule
Emp. Form.C28H25FN6O4
Mol. Mass.528.5343
SMILESCOc1ccccc1CNC(=O)c1cc(ccc1F)C1NC(=O)NC(C)=C1C(=O)Nc1ccc2[nH]ncc2c1 |c:27|
Structure
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