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Target
Rhodopsin kinase GRK1
Ligand
BDBM284006
Substrate
n/a
Meas. Tech.
ChEMBL_1771206 (CHEMBL4223318)
IC50
26000±n/a nM
Citation
 Waldschmidt, HV; Bouley, R; Kirchhoff, PD; Lee, P; Tesmer, JJG; Larsen, SD Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors. Bioorg Med Chem Lett 28:1507-1515 (2018) [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:
BDBM284006
Synonyms:
E32 | US10023564, Example 32
Type:
Small organic molecule
Emp. Form.:
C28H27FN6O5
Mol. Mass.:
546.5496
SMILES:
CC1=C(C(NC(=O)N1)c1ccc(F)c(CC(=O)N(CCO)Cc2ccco2)c1)C(=O)Nc1ccc2[nH]ncc2c1 |t:1|
Structure:
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