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Target
Rho-associated protein kinase 2 [1-543,T431N]
Ligand
BDBM25474
Substrate
STK substrate 2-biotin
Meas. Tech.
ROCK-II Inhibition Assay
pH
7±n/a
Temperature
295.15±n/a K
IC50
3.2±2.3 nM
Citation
 Feng, Y; Yin, Y; Weiser, A; Griffin, E; Cameron, MD; Lin, L; Ruiz, C; Schürer, SC; Inoue, T; Rao, PV; Schröter, T; Lograsso, P Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. J Med Chem 51:6642-5 (2008) [PubMed]  Article 
Target
Name:
Rho-associated protein kinase 2 [1-543,T431N]
Synonyms:
KIAA0619 | ROCK2 | ROCK2_HUMAN | Rho-associated, coiled-coil-containing protein kinase 2 | Rho-kinase (ROCK II) | p164 ROCK-2
Type:
Serine/threonine-protein kinase
Mol. Mass.:
62266.25
Organism:
Homo sapiens (Human)
Description:
The truncated human Rho-kinase II (1-543) expressed in Sf-21 cell.
Residue:
543
Sequence:
MSRPPPTGKMPGAPETAPGDGAGASRQRKLEALIRDPRSPINVESLLDGLNSLVLDLDFPALRKNKNIDNFLNRYEKIVKKIRGLQMKAEDYDVVKVIGRGAFGEVQLVRHKASQKVYAMKLLSKFEMIKRSDSAFFWEERDIMAFANSPWVVQLFYAFQDDRYLYMVMEYMPGGDLVNLMSNYDVPEKWAKFYTAEVVLALDAIHSMGLIHRDVKPDNMLLDKHGHLKLADFGTCMKMDETGMVHCDTAVGTPDYISPEVLKSQGGDGFYGRECDWWSVGVFLYEMLVGDTPFYADSLVGTYSKIMDHKNSLCFPEDAEISKHAKNLICAFLTDREVRLGRNGVEEIRQHPFFKNDQWHWDNIRETAAPVVPELSSDIDSSNFDDIEDDKGDVETFPIPKAFVGNQLPFIGFTYYRENLLLSDSPSCRENDSIQSRKNEESQEIQKKLYTLEEHLSNEMQAKEELEQKCKSVNTRLEKTAKELEEEITLRKSVESALRQLEREKALLQHKNAEYQRKADHEADKKRNLENDVNSLKDQLEDL
  
Inhibitor
Name:
BDBM25474
Synonyms:
JMC516642 Compound 5 | N-{2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl}-2,3-dihydro-1,4-benzodioxine-2-carboxamide | SR3677
Type:
Small organic molecule
Emp. Form.:
C22H24N4O4
Mol. Mass.:
408.4504
SMILES:
CN(C)CCOc1cc(ccc1NC(=O)C1COc2ccccc2O1)-c1cn[nH]c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
STK substrate 2-biotin
Synonyms:
n/a
Type:
biotinylated peptide substrate
Mol. Mass.:
358.43
Organism:
n/a
Description:
HTRF KinEASE-STK S2 Assay Kit (Cisbio, Bedford, MA)
Residue:
3
Sequence:
NA