Reaction Details |
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Target | Rho-associated protein kinase 1 |
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Ligand | BDBM14039 |
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Substrate/Competitor | Biotinylated Peptide Substrate |
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Meas. Tech. | ROCK 1 Kinase Activity Assay |
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pH | 7.4±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 18±n/a nM |
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Citation | Stavenger, RA; Cui, H; Dowdell, SE; Franz, RG; Gaitanopoulos, DE; Goodman, KB; Hilfiker, MA; Ivy, RL; Leber, JD; Marino, JP; Oh, HJ; Viet, AQ; Xu, W; Ye, G; Zhang, D; Zhao, Y; Jolivette, LJ; Head, MS; Semus, SF; Elkins, PA; Kirkpatrick, RB; Dul, E; Khandekar, SS; Yi, T; Jung, DK; Wright, LL; Smith, GK; Behm, DJ; Doe, CP; Bentley, R; Chen, ZX; Hu, E; Lee, D Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity. J Med Chem50:2-5 (2007) [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 1 |
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Name: | Rho-associated protein kinase 1 |
Synonyms: | ROCK-I | ROCK1 | ROCK1_HUMAN | Renal carcinoma antigen NY-REN-35 | Rho-associated protein kinase | Rho-associated protein kinase 1 (ROCK1) | Rho-associated, coiled-coil-containing protein kinase 1 | Rho-associated, coiled-coil-containing protein kinase I | Rho-kinase (ROCK I) | Serine/threonine-protein kinase RIO1 | p160 ROCK-1 | p160ROCK |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 158156.77 |
Organism: | Homo sapiens (Human) |
Description: | Q13464 |
Residue: | 1354 |
Sequence: | MSTGDSFETRFEKMDNLLRDPKSEVNSDCLLDGLDALVYDLDFPALRKNKNIDNFLSRYK
DTINKIRDLRMKAEDYEVVKVIGRGAFGEVQLVRHKSTRKVYAMKLLSKFEMIKRSDSAF
FWEERDIMAFANSPWVVQLFYAFQDDRYLYMVMEYMPGGDLVNLMSNYDVPEKWARFYTA
EVVLALDAIHSMGFIHRDVKPDNMLLDKSGHLKLADFGTCMKMNKEGMVRCDTAVGTPDY
ISPEVLKSQGGDGYYGRECDWWSVGVFLYEMLVGDTPFYADSLVGTYSKIMNHKNSLTFP
DDNDISKEAKNLICAFLTDREVRLGRNGVEEIKRHLFFKNDQWAWETLRDTVAPVVPDLS
SDIDTSNFDDLEEDKGEEETFPIPKAFVGNQLPFVGFTYYSNRRYLSSANPNDNRTSSNA
DKSLQESLQKTIYKLEEQLHNEMQLKDEMEQKCRTSNIKLDKIMKELDEEGNQRRNLEST
VSQIEKEKMLLQHRINEYQRKAEQENEKRRNVENEVSTLKDQLEDLKKVSQNSQLANEKL
SQLQKQLEEANDLLRTESDTAVRLRKSHTEMSKSISQLESLNRELQERNRILENSKSQTD
KDYYQLQAILEAERRDRGHDSEMIGDLQARITSLQEEVKHLKHNLEKVEGERKEAQDMLN
HSEKEKNNLEIDLNYKLKSLQQRLEQEVNEHKVTKARLTDKHQSIEEAKSVAMCEMEKKL
KEEREAREKAENRVVQIEKQCSMLDVDLKQSQQKLEHLTGNKERMEDEVKNLTLQLEQES
NKRLLLQNELKTQAFEADNLKGLEKQMKQEINTLLEAKRLLEFELAQLTKQYRGNEGQMR
ELQDQLEAEQYFSTLYKTQVKELKEEIEEKNRENLKKIQELQNEKETLATQLDLAETKAE
SEQLARGLLEEQYFELTQESKKAASRNRQEITDKDHTVSRLEEANSMLTKDIEILRRENE
ELTEKMKKAEEEYKLEKEEEISNLKAAFEKNINTERTLKTQAVNKLAEIMNRKDFKIDRK
KANTQDLRKKEKENRKLQLELNQEREKFNQMVVKHQKELNDMQAQLVEECAHRNELQMQL
ASKESDIEQLRAKLLDLSDSTSVASFPSADETDGNLPESRIEGWLSVPNRGNIKRYGWKK
QYVVVSSKKILFYNDEQDKEQSNPSMVLDIDKLFHVRPVTQGDVYRAETEEIPKIFQILY
ANEGECRKDVEMEPVQQAEKTNFQNHKGHEFIPTLYHFPANCDACAKPLWHVFKPPPALE
CRRCHVKCHRDHLDKKEDLICPCKVSYDVTSARDMLLLACSQDEQKKWVTHLVKKIPKNP
PSGFVRASPRTLSTRSTANQSFRKVVKNTSGKTS
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BDBM14039 |
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Biotinylated Peptide Substrate |
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Name: | Biotinylated Peptide Substrate |
Synonyms: | n/a |
Type: | Peptide |
Mol. Mass.: | 2323.73 |
Organism: | n/a |
Description: | n/a |
Residue: | 20 |
Sequence: | biotin-Ahx-AKRRRLSSLRA-CONH2
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