Reaction Details |
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Target | Rho-associated protein kinase 1 |
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Ligand | BDBM380152 |
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Substrate/Competitor | n/a |
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Meas. Tech. | In Vitro Assay |
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IC50 | <100±n/a nM |
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Citation | Glunz, PW; Zou, Y; Quan, ML; Ladziata, V Phthalazinones and isoquinolinones as rock inhibitors US Patent US9926282 Publication Date 3/27/2018 |
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More Info.: | Get all data from this article, 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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BDBM380152 |
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n/a |
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Name | BDBM380152 |
Synonyms: | 1-[3-(benzyloxy)-2- hydroxypropyl]-N-[4-(4- oxo-3,4- dihydrophthalazin-1- yl)phenyl]-1H-indazole- 3-carboxamide | US9926282, Example 147 |
Type | Small organic molecule |
Emp. Form. | C32H27N5O4 |
Mol. Mass. | 545.5879 |
SMILES | OC(COCc1ccccc1)Cn1nc(C(=O)Nc2ccc(cc2)-c2n[nH]c(=O)c3ccccc23)c2ccccc12 |
Structure |
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