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Target
G protein-coupled receptor kinase 4
Ligand
BDBM50536678
Substrate
n/a
Meas. Tech.
ChEMBL_1934070 (CHEMBL4479722)
IC50
19000±n/a nM
Citation
 Sloman, DL; Noucti, N; Altman, MD; Chen, D; Mislak, AC; Szewczak, A; Hayashi, M; Warren, L; Dellovade, T; Wu, Z; Marcus, J; Walker, D; Su, HP; Edavettal, SC; Munshi, S; Hutton, M; Nuthall, H; Stanton, MG Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties. Bioorg Med Chem Lett 26:4362-6 (2016) [PubMed]  Article 
Target
Name:
G protein-coupled receptor kinase 4
Synonyms:
GPRK2L | GPRK4 | GRK4 | GRK4_HUMAN
Type:
PROTEIN
Mol. Mass.:
66590.61
Organism:
Homo sapiens (Human)
Description:
ChEMBL_774219
Residue:
578
Sequence:
MELENIVANSLLLKARQGGYGKKSGRSKKWKEILTLPPVSQCSELRHSIEKDYSSLCDKQPIGRRLFRQFCDTKPTLKRHIEFLDAVAEYEVADDEDRSDCGLSILDRFFNDKLAAPLPEIPPDVVTECRLGLKEENPSKKAFEECTRVAHNYLRGEPFEEYQESSYFSQFLQWKWLERQPVTKNTFRHYRVLGKGGFGEVCACQVRATGKMYACKKLQKKRIKKRKGEAMALNEKRILEKVQSRFVVSLAYAYETKDALCLVLTIMNGGDLKFHIYNLGNPGFDEQRAVFYAAELCCGLEDLQRERIVYRDLKPENILLDDRGHIRISDLGLATEIPEGQRVRGRVGTVGYMAPEVVNNEKYTFSPDWWGLGCLIYEMIQGHSPFKKYKEKVKWEEVDQRIKNDTEEYSEKFSEDAKSICRMLLTKNPSKRLGCRGEGAAGVKQHPVFKDINFRRLEANMLEPPFCPDPHAVYCKDVLDIEQFSVVKGIYLDTADEDFYARFATGCVSIPWQNEMIESGCFKDINKSESEEALPLDLDKNIHTPVSRPNRGFFYRLFRRGGCLTMVPSEKEVEPKQC
  
Inhibitor
Name:
BDBM50536678
Synonyms:
CHEMBL4550702
Type:
Small organic molecule
Emp. Form.:
C17H13F3N6OS
Mol. Mass.:
406.385
SMILES:
Cn1cc(cn1)-c1cnc2c(cnn2c1)-c1csc(c1)C(=O)NCC(F)(F)F
Structure:
Search PDB for entries with ligand similarity: