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Target
Rhodopsin kinase GRK1
Ligand
BDBM50554258
Substrate
n/a
Meas. Tech.
ChEMBL_2048919 (CHEMBL4703618)
IC50
>10000±n/a nM
Citation
 Xu, G; Gaul, MD; Liu, Z; DesJarlais, RL; Qi, J; Wang, W; Krosky, D; Petrounia, I; Milligan, CM; Hermans, A; Lu, HR; Huang, DZ; Xu, JZ; Spurlino, JC Hit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor. Bioorg Med Chem Lett 30:0 (2020) [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:
BDBM50554258
Synonyms:
CHEMBL4744858
Type:
Small organic molecule
Emp. Form.:
C19H16N4O2
Mol. Mass.:
332.3559
SMILES:
COc1cccc(Cn2ncc3ccc(cc3c2=O)-c2cn[nH]c2)c1
Structure:
Search PDB for entries with ligand similarity: