Reaction Details |
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Target | Rho-associated protein kinase 1 |
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Ligand | BDBM50173307 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Assays for Inhibition of ROCK |
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IC50 | 17.0±n/a nM |
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Citation | Larsen, SD; Homan, K; Waldschmidt, H; Tesmer, JJ G protein-coupled receptor kinase 2 inhibitors and methods for use of the same US Patent US10023564 Publication Date 7/17/2018 |
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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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BDBM50173307 |
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n/a |
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Name | BDBM50173307 |
Synonyms: | CHEMBL3809796 | US10023564, Example 8 |
Type | Small organic molecule |
Emp. Form. | C30H24FN7O3 |
Mol. Mass. | 549.5551 |
SMILES | CC1=C(C(NC(=O)N1)c1ccc(F)c(c1)C(=O)NCc1nccc2ccccc12)C(=O)Nc1ccc2[nH]ncc2c1 |t:1| |
Structure |
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