Reaction Details |
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Target | Rho-associated protein kinase 2 [1-543,T431N] |
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Ligand | BDBM25472 |
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Substrate/Competitor | STK substrate 2-biotin |
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Meas. Tech. | ROCK-II Inhibition Assay |
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pH | 7±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 1.5±0.7 nM |
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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 Chem51:6642-5 (2008) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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Rho-associated protein kinase 2 [1-543,T431N] |
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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: | MSRPPPTGKMPGAPETAPGDGAGASRQRKLEALIRDPRSPINVESLLDGLNSLVLDLDFP
ALRKNKNIDNFLNRYEKIVKKIRGLQMKAEDYDVVKVIGRGAFGEVQLVRHKASQKVYAM
KLLSKFEMIKRSDSAFFWEERDIMAFANSPWVVQLFYAFQDDRYLYMVMEYMPGGDLVNL
MSNYDVPEKWAKFYTAEVVLALDAIHSMGLIHRDVKPDNMLLDKHGHLKLADFGTCMKMD
ETGMVHCDTAVGTPDYISPEVLKSQGGDGFYGRECDWWSVGVFLYEMLVGDTPFYADSLV
GTYSKIMDHKNSLCFPEDAEISKHAKNLICAFLTDREVRLGRNGVEEIRQHPFFKNDQWH
WDNIRETAAPVVPELSSDIDSSNFDDIEDDKGDVETFPIPKAFVGNQLPFIGFTYYRENL
LLSDSPSCRENDSIQSRKNEESQEIQKKLYTLEEHLSNEMQAKEELEQKCKSVNTRLEKT
AKELEEEITLRKSVESALRQLEREKALLQHKNAEYQRKADHEADKKRNLENDVNSLKDQL
EDL
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BDBM25472 |
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STK substrate 2-biotin |
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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: | |