Target
Rhodopsin kinase GRK1
Ligand
BDBM50173313
Substrate
n/a
Meas. Tech.
ChEMBL_1581284 (CHEMBL3811361)
IC50
9000±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]  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:
BDBM50173313
Synonyms:
CHEMBL1738878
Type:
Small organic molecule
Emp. Form.:
C24H23F2N7O
Mol. Mass.:
463.4825
SMILES:
CCCn1c(CNc2cccc(c2)C(=O)NCc2c(F)cccc2F)nnc1-c1ccncn1
Structure:
Search PDB for entries with ligand similarity: