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Target
Rho-associated protein kinase 1
Ligand
BDBM25004
Substrate
ROCK1 Substrate Peptide
Meas. Tech.
In Vitro Kinase Inhibition Assay
IC50
20±n/a nM
Citation
 Heerding, DA; Rhodes, N; Leber, JD; Clark, TJ; Keenan, RM; Lafrance, LV; Li, M; Safonov, IG; Takata, DT; Venslavsky, JW; Yamashita, DS; Choudhry, AE; Copeland, RA; Lai, Z; Schaber, MD; Tummino, PJ; Strum, SL; Wood, ER; Duckett, DR; Eberwein, D; Knick, VB; Lansing, TJ; McConnell, RT; Zhang, S; Minthorn, EA; Concha, NO; Warren, GL; Kumar, R Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase. J Med Chem 51:5663-79 (2008) [PubMed]  Article 
Target
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:
MSTGDSFETRFEKMDNLLRDPKSEVNSDCLLDGLDALVYDLDFPALRKNKNIDNFLSRYKDTINKIRDLRMKAEDYEVVKVIGRGAFGEVQLVRHKSTRKVYAMKLLSKFEMIKRSDSAFFWEERDIMAFANSPWVVQLFYAFQDDRYLYMVMEYMPGGDLVNLMSNYDVPEKWARFYTAEVVLALDAIHSMGFIHRDVKPDNMLLDKSGHLKLADFGTCMKMNKEGMVRCDTAVGTPDYISPEVLKSQGGDGYYGRECDWWSVGVFLYEMLVGDTPFYADSLVGTYSKIMNHKNSLTFPDDNDISKEAKNLICAFLTDREVRLGRNGVEEIKRHLFFKNDQWAWETLRDTVAPVVPDLSSDIDTSNFDDLEEDKGEEETFPIPKAFVGNQLPFVGFTYYSNRRYLSSANPNDNRTSSNADKSLQESLQKTIYKLEEQLHNEMQLKDEMEQKCRTSNIKLDKIMKELDEEGNQRRNLESTVSQIEKEKMLLQHRINEYQRKAEQENEKRRNVENEVSTLKDQLEDLKKVSQNSQLANEKLSQLQKQLEEANDLLRTESDTAVRLRKSHTEMSKSISQLESLNRELQERNRILENSKSQTDKDYYQLQAILEAERRDRGHDSEMIGDLQARITSLQEEVKHLKHNLEKVEGERKEAQDMLNHSEKEKNNLEIDLNYKLKSLQQRLEQEVNEHKVTKARLTDKHQSIEEAKSVAMCEMEKKLKEEREAREKAENRVVQIEKQCSMLDVDLKQSQQKLEHLTGNKERMEDEVKNLTLQLEQESNKRLLLQNELKTQAFEADNLKGLEKQMKQEINTLLEAKRLLEFELAQLTKQYRGNEGQMRELQDQLEAEQYFSTLYKTQVKELKEEIEEKNRENLKKIQELQNEKETLATQLDLAETKAESEQLARGLLEEQYFELTQESKKAASRNRQEITDKDHTVSRLEEANSMLTKDIEILRRENEELTEKMKKAEEEYKLEKEEEISNLKAAFEKNINTERTLKTQAVNKLAEIMNRKDFKIDRKKANTQDLRKKEKENRKLQLELNQEREKFNQMVVKHQKELNDMQAQLVEECAHRNELQMQLASKESDIEQLRAKLLDLSDSTSVASFPSADETDGNLPESRIEGWLSVPNRGNIKRYGWKKQYVVVSSKKILFYNDEQDKEQSNPSMVLDIDKLFHVRPVTQGDVYRAETEEIPKIFQILYANEGECRKDVEMEPVQQAEKTNFQNHKGHEFIPTLYHFPANCDACAKPLWHVFKPPPALECRRCHVKCHRDHLDKKEDLICPCKVSYDVTSARDMLLLACSQDEQKKWVTHLVKKIPKNPPSGFVRASPRTLSTRSTANQSFRKVVKNTSGKTS
  
Inhibitor
Name:
BDBM25004
Synonyms:
3-[2-(4-amino-1,2,5-oxadiazol-3-yl)-7-(3-aminopropoxy)-1-ethyl-1H-imidazo[4,5-c]pyridin-4-yl]prop-2-yn-1-ol | oxadiazole-containing compound, 12c
Type:
Small organic molecule
Emp. Form.:
C16H19N7O3
Mol. Mass.:
357.3672
SMILES:
CCn1c(nc2c(ncc(OCCCN)c12)C#CCO)-c1nonc1N
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
ROCK1 Substrate Peptide
Synonyms:
RSK1 Substrate Peptide
Type:
Peptide
Mol. Mass.:
1318.60
Organism:
n/a
Description:
n/a
Residue:
11
Sequence:
AKRRRLSSLRA