Reaction Details |
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Target | Rho-associated protein kinase 1 |
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Ligand | BDBM50315069 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_624654 (CHEMBL1111614) |
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IC50 | <50000±n/a nM |
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Citation | Verheijen, JC; Richard, DJ; Curran, K; Kaplan, J; Yu, K; Zask, A 2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability. Bioorg Med Chem Lett20:2648-53 (2010) [PubMed] Article |
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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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BDBM50315069 |
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n/a |
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Name | BDBM50315069 |
Synonyms: | 1-(4-(4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)-6-(tetrahydro-2H-pyran-4-yl)-1,3,5-triazin-2-yl)phenyl)-3-(4-(4-isopropylpiperazine-1-carbonyl)phenyl)urea | CHEMBL1091356 |
Type | Small organic molecule |
Emp. Form. | C35H44N8O4 |
Mol. Mass. | 640.7751 |
SMILES | CC(C)N1CCN(CC1)C(=O)c1ccc(NC(=O)Nc2ccc(cc2)-c2nc(nc(n2)N2C3CCC2COC3)C2CCOCC2)cc1 |
Structure |
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