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TargetRho-associated protein kinase 1 (ROCK I)
LigandBDBM24995
Substrate/CompetitorROCK1 Substrate Peptide
Meas. Tech.In Vitro Kinase Inhibition Assay
IC50 6±n/a nM
Citation Heerding, DARhodes, NLeber, JDClark, TJKeenan, RMLafrance, LVLi, MSafonov, IGTakata, DTVenslavsky, JWYamashita, DSChoudhry, AECopeland, RALai, ZSchaber, MDTummino, PJStrum, SLWood, ERDuckett, DREberwein, DKnick, VBLansing, TJMcConnell, RTZhang, SMinthorn, EAConcha, NOWarren, GLKumar, 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 Chem51:5663-79 (2008) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Rho-associated protein kinase 1 (ROCK I)
Name:Rho-associated protein kinase 1 (ROCK I)
Synonyms:Liver regenerat ion-related protein LRRG199 | Liver regeneration-related protein LRRG199 | Rho-associated protein kinase 1 | Rho-associated, coiled-coil-containing protein kinase 1 | Rho-kinase (ROCK I) | p150 RhoA-binding kinase ROK beta | p160 ROCK-1
Type:Protein
Mol. Mass.:159610.34
Organism:Rattus norvegicus (Rat)
Description:Q63644
Residue:1369
Sequence:
MSTGDSFETRFEKIDNLLRDPKSEVNSDCLLDGLDALVYDLDFPALRKNKNIDNFLSRYK
DTINKIRDLRMKAEDYEVVKVIGRGAFGEVQLVRHKSTRKVYAMKLLSKFEMIKRSDSAF
FWEERDIMAFANSPWVVQLFYAFQDDRYLYMVMEYMPGGDLVNLMSNYDVPEKWARFYTA
EVVLALDAIHSMGFIHRDVKPDNMLLDKSGHLKLADFGTCMKMNKEGMVRCDTAVGTPDY
ISPEVLKSQGGDGYYGRECDWWSVGVFLYEMLVGDTPFYADSLVGTYSKIMNHKNSLTFP
DDNDISKEAKNLICAFLTDREVRLGRNGVEEIKRHLFFKNDQWAWETLRDTVAPVVPDLS
SDIDTSNFDDLEEDKGDEETFPIPKAFVGNQLPFVGFTYYSNRRYLPSANPSENRSSSNV
DKNVQESLQKTIYKLEEQLHNEMQLKDEMEQKCRTSNIKLDKIMKELDEEGNQRRNLESA
VSQIEKEKMLLQHRINEYQRKVEQENEKRRNVENEVSTLKDQLEDLRKASQSSQLANEKL
TQLQKQLEEANDLLRTESDTAVRLRKSHTEMSKSVSQLESLNRELQERNRMLENSKSQAD
KDYYQLQAVLEAERRDRGHDSEMIGDLQARITSLQEEVKHLKHNLERVEGERKEAQDMLN
HSEKEKNNLEIDLNYKLKSIQQRLEQEVNEHKVTKARLTDKHQSIEEAKSVAMCEMEKKL
KEEREAREKAENRVVETEKQCSMLDVDLKQSQQKLEHLTENKERLEDAVKSLTLQLEQES
NKRILLQSELKTQAFEADNLKGLEKQMKQEINTLLEAKRLLEFELAQLTKQYRGNEGQMR
ELQDQLEAEQYFSTLYKTQVKELKEEIEEKNRENLRKIQELQSEKETLSTQLDLAETKAE
SEQLARGILEEQYFELTQESKKAASRNRQEITDKDHTVSRLEEANNALTKDIELLRKENE
ELNERMRTAEEEYKLKKEEEISNLKAAFEKNISTERTLKTQAVNKLAEIMNRKDFKIDRK
KANTQDLRKKEKENRKLQLELNQEREKFNQMVVKHQKELNDMQAQLVEECTHRNELQMQL
ASKESDIEQLRAKLLDLSDSTSVASFPSADETDGNLPVGSACIPYLFIFYSSSSRIEGWL
SVPNRGNIKRYGWKKQYVVVSSKKMLFYNDEQDKEQSSPSMVLDIDKLFHVRPVTQGDVY
RAETEEIPKIFQILYANEGECRKDIEVEPVQQGEKTNFQNHKGHEFIPTLYHFPANCEAC
AKPLWHVFKPPPALECRRCHVKSHRDHLDKKEDLIPPCKVSYDVTSARDMLLLACPQDEQ
KKWVTHLVKKIPKKAPSGFVRASPRTLSTRSTANQSFRKVVKNTSGKTS
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM24995
NameBDBM24995
Synonyms:2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-N-(piperidin-4-yl)-1H-imidazo[4,5-c]pyridine-7-carboxamide | oxadiazole-containing compound, 8
TypeSmall organic molecule
Emp. Form.C16H20N8O2
Mol. Mass.356.3824
SMILESCCn1c(nc2cncc(C(=O)NC3CCNCC3)c12)-c1nonc1N
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
ROCK1 Substrate Peptide
Name:ROCK1 Substrate Peptide
Synonyms:RSK1 Substrate Peptide
Type:Peptide
Mol. Mass.:1318.60
Organism:n/a
Description:n/a
Residue:11
Sequence:
AKRRRLSSLRA