Target
Rhodopsin kinase GRK1
Ligand
BDBM50173327
Substrate
n/a
Meas. Tech.
Assays for Inhibition of GRKs
pH
7±n/a
IC50
>100000±n/a nM
Comments
extracted
Citation
 Larsen, SDHoman, KWaldschmidt, HTesmer, 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:
BDBM50173327
Synonyms:
CHEMBL3808499 | US10023564, Example 28
Type:
Small organic molecule
Emp. Form.:
C30H29FN6O3
Mol. Mass.:
540.5881
SMILES:
CC1=C(C(NC(=O)N1)c1ccc(F)c(CC(=O)NCc2c(C)cccc2C)c1)C(=O)Nc1ccc2[nH]ncc2c1 |t:1|
Structure:
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