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Target
Rhodopsin kinase GRK1
Ligand
BDBM50265871
Substrate
n/a
Meas. Tech.
ChEMBL_1908738 (CHEMBL4411096)
IC50
130±n/a nM
Citation
 Rowlands, RA; Cato, MC; Waldschmidt, HV; Bouley, RA; Chen, Q; Avramova, L; Larsen, SD; Tesmer, JJG; White, AD Structure-Based Design of Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. ACS Med Chem Lett 10:1628-1634 (2019) [PubMed]  Article
Target
Name:
Rhodopsin kinase GRK1
Synonyms:
G protein-coupled receptor kinase 1 | GRK1 | GRK1_BOVIN | RHOK | Rhodopsin kinase
Type:
PROTEIN
Mol. Mass.:
62931.24
Organism:
Bos taurus
Description:
ChEMBL_116985
Residue:
561
Sequence:
MDFGSLETVVANSAFIAARGSFDASSGPASRDRKYLARLKLPPLSKCEALRESLDLGFEGMCLEQPIGKRLFQQFLRTHEQHGPALQLWKDIEDYDTADDALRPQKAQALRAAYLEPQAQLFCSFLDAETVARARAGAGDGLFQPLLRAVLAHLGQAPFQEFLDSLYFLRFLQWKWLEAQPMGEDWFLDFRVLGRGGFGEVFACQMKATGKLYACKKLNKKRLKKRKGYQGAMVEKKILAKVHSRFIVSLAYAFETKTDLCLVMTIMNGGDIRYHIYNVDEDNPGFQEPRAIFYTAQIVSGLEHLHQRNIIYRDLKPENVLLDDDGNVRISDLGLAVELKAGQTKTKGYAGTPGFMAPELLLGEEYDFSVDYFALGVTLYEMIAARGPFRARGEKVENKELKQRVLEQAVTYPDKFSPASKDFCEALLQKDPEKRLGFRDGSCDGLRTHPLFRDISWRQLEAGMLTPPFVPDSRTVYAKNIQDVGAFSTVKGVAFEKADTEFFQEFASGTCPIPWQEEMIETGVFGDLNVWRPDGQMPDDMKGVSGQEAAPSSKSGMCVLS
  
Inhibitor
Name:
BDBM50265871
Synonyms:
3-(2-(1-(2-(dimethylamino)acetyl)-6-methoxy-4,4-dimethyl-1,2,3,4-tetrahydroquinolin-7-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)thiophene-2-carboxamide | CHEMBL463931
Type:
Small organic molecule
Emp. Form.:
C27H32N8O3S
Mol. Mass.:
548.66
SMILES:
COc1cc2c(cc1Nc1nc(Nc3ccsc3C(N)=O)c3cc[nH]c3n1)N(CCC2(C)C)C(=O)CN(C)C
Structure:
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