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TargetG protein-coupled receptor kinase 4
LigandBDBM50566947
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2102046 (CHEMBL4810442)
IC50 190±n/a nM
Citation Uehling, DEJoseph, BChung, KCZhang, AXLer, SPrakesch, MAPoda, GGrouleff, JAman, AKiyota, TLeung-Hagesteijn, CKonda, JDMarcellus, RGriffin, CSubramaniam, RAbibi, AStrathdee, CAIsaac, MBAl-Awar, RTiedemann, RE Design, Synthesis, and Characterization of 4-Aminoquinazolines as Potent Inhibitors of the G Protein-Coupled Receptor Kinase 6 (GRK6) for the Treatment of Multiple Myeloma. J Med Chem64:11129-11147 (2021) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
G protein-coupled receptor kinase 4
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:
MELENIVANSLLLKARQGGYGKKSGRSKKWKEILTLPPVSQCSELRHSIEKDYSSLCDKQ
PIGRRLFRQFCDTKPTLKRHIEFLDAVAEYEVADDEDRSDCGLSILDRFFNDKLAAPLPE
IPPDVVTECRLGLKEENPSKKAFEECTRVAHNYLRGEPFEEYQESSYFSQFLQWKWLERQ
PVTKNTFRHYRVLGKGGFGEVCACQVRATGKMYACKKLQKKRIKKRKGEAMALNEKRILE
KVQSRFVVSLAYAYETKDALCLVLTIMNGGDLKFHIYNLGNPGFDEQRAVFYAAELCCGL
EDLQRERIVYRDLKPENILLDDRGHIRISDLGLATEIPEGQRVRGRVGTVGYMAPEVVNN
EKYTFSPDWWGLGCLIYEMIQGHSPFKKYKEKVKWEEVDQRIKNDTEEYSEKFSEDAKSI
CRMLLTKNPSKRLGCRGEGAAGVKQHPVFKDINFRRLEANMLEPPFCPDPHAVYCKDVLD
IEQFSVVKGIYLDTADEDFYARFATGCVSIPWQNEMIESGCFKDINKSESEEALPLDLDK
NIHTPVSRPNRGFFYRLFRRGGCLTMVPSEKEVEPKQC
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50566947
n/a
NameBDBM50566947
Synonyms:CHEMBL4847703
TypeSmall organic molecule
Emp. Form.C20H20FN7O
Mol. Mass.393.4175
SMILESCCc1cc(Nc2nc(NCc3ccc(F)cn3)nc3cccc(OC)c23)n[nH]1
Structure
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