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Target
Rhodopsin kinase GRK1
Ligand
BDBM284001
Substrate
n/a
Meas. Tech.
Assays for Inhibition of GRKs
pH
7±n/a
IC50
14000±n/a nM
Comments
extracted
Citation
 Larsen, SD; Homan, K; Waldschmidt, H; Tesmer, JJ G protein-coupled receptor kinase 2 inhibitors and methods for use of the same US Patent  US10023564 Publication Date 7/17/2018
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:
BDBM284001
Synonyms:
E27 | US10023564, Example 27
Type:
Small organic molecule
Emp. Form.:
C29H27FN6O4
Mol. Mass.:
542.5609
SMILES:
COc1ccccc1C(C)NC(=O)c1cc(ccc1F)C1NC(=O)NC(C)=C1C(=O)Nc1ccc2[nH]ncc2c1 |c:28|
Structure:
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