| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Beta-adrenergic receptor kinase 2 |
|---|
| Ligand | BDBM50257340 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | ChEBML_1689810 |
|---|
| IC50 | 0.650000±n/a nM |
|---|
| Citation |  Okawa, T; Aramaki, Y; Yamamoto, M; Kobayashi, T; Fukumoto, S; Toyoda, Y; Henta, T; Hata, A; Ikeda, S; Kaneko, M; Hoffman, ID; Sang, BC; Zou, H; Kawamoto, T Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. J Med Chem60:6942-6990 (2017) [PubMed] Article |
|---|
| More Info.: | Get all data from this article, Assay Method |
|---|
| |
| Beta-adrenergic receptor kinase 2 |
|---|
| Name: | Beta-adrenergic receptor kinase 2 |
|---|
| Synonyms: | ADRBK2 | ARBK2_HUMAN | BARK2 | GRK3 |
|---|
| Type: | PROTEIN |
|---|
| Mol. Mass.: | 79721.92 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | ChEMBL_615172 |
|---|
| Residue: | 688 |
|---|
| Sequence: | MADLEAVLADVSYLMAMEKSKATPAARASKRIVLPEPSIRSVMQKYLAERNEITFDKIFN
QKIGFLLFKDFCLNEINEAVPQVKFYEEIKEYEKLDNEEDRLCRSRQIYDAYIMKELLSC
SHPFSKQAVEHVQSHLSKKQVTSTLFQPYIEEICESLRGDIFQKFMESDKFTRFCQWKNV
ELNIHLTMNEFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNER
IMLSLVSTGDCPFIVCMTYAFHTPDKLCFILDLMNGGDLHYHLSQHGVFSEKEMRFYATE
IILGLEHMHNRFVVYRDLKPANILLDEHGHARISDLGLACDFSKKKPHASVGTHGYMAPE
VLQKGTAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTVNVELPDTFSPE
LKSLLEGLLQRDVSKRLGCHGGGSQEVKEHSFFKGVDWQHVYLQKYPPPLIPPRGEVNAA
DAFDIGSFDEEDTKGIKLLDCDQELYKNFPLVISERWQQEVTETVYEAVNADTDKIEARK
RAKNKQLGHEEDYALGKDCIMHGYMLKLGNPFLTQWQRRYFYLFPNRLEWRGEGESRQNL
LTMEQILSVEETQIKDKKCILFRIKGGKQFVLQCESDPEFVQWKKELNETFKEAQRLLRR
APKFLNKPRSGTVELPKPSLCHRNSNGL
|
|
|
|---|
| BDBM50257340 |
|---|
| n/a |
|---|
| Name | BDBM50257340 |
|---|
| Synonyms: | CHEMBL4072828 |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C25H21F3N6O2 |
|---|
| Mol. Mass. | 494.4684 |
|---|
| SMILES | FC(F)(F)c1ccccc1CNC(=O)c1cccc(NCc2nnc3-c4ccncc4OCCn23)c1 |
|---|
| Structure | 
|
|---|
Search and Browse
