Reaction Details Report a problem with these data
Target
Rho-associated protein kinase 1
Ligand
BDBM24995
Substrate
ROCK1 Substrate Peptide
Meas. Tech.
In Vitro Kinase Inhibition Assay
IC50
6±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:
Liver regenerat ion-related protein LRRG199 | Liver regeneration-related protein LRRG199 | ROCK1_RAT | Rho-associated protein kinase 1 | Rho-associated protein kinase 1 (ROCK I) | Rho-associated, coiled-coil-containing protein kinase 1 | Rho-kinase (ROCK I) | Rock1 | p150 RhoA-binding kinase ROK beta | p160 ROCK-1
Type:
Protein
Mol. Mass.:
159610.34
Organism:
Rattus norvegicus (Rat)
Description:
Q63644
Residue:
1369
Sequence:
MSTGDSFETRFEKIDNLLRDPKSEVNSDCLLDGLDALVYDLDFPALRKNKNIDNFLSRYKDTINKIRDLRMKAEDYEVVKVIGRGAFGEVQLVRHKSTRKVYAMKLLSKFEMIKRSDSAFFWEERDIMAFANSPWVVQLFYAFQDDRYLYMVMEYMPGGDLVNLMSNYDVPEKWARFYTAEVVLALDAIHSMGFIHRDVKPDNMLLDKSGHLKLADFGTCMKMNKEGMVRCDTAVGTPDYISPEVLKSQGGDGYYGRECDWWSVGVFLYEMLVGDTPFYADSLVGTYSKIMNHKNSLTFPDDNDISKEAKNLICAFLTDREVRLGRNGVEEIKRHLFFKNDQWAWETLRDTVAPVVPDLSSDIDTSNFDDLEEDKGDEETFPIPKAFVGNQLPFVGFTYYSNRRYLPSANPSENRSSSNVDKNVQESLQKTIYKLEEQLHNEMQLKDEMEQKCRTSNIKLDKIMKELDEEGNQRRNLESAVSQIEKEKMLLQHRINEYQRKVEQENEKRRNVENEVSTLKDQLEDLRKASQSSQLANEKLTQLQKQLEEANDLLRTESDTAVRLRKSHTEMSKSVSQLESLNRELQERNRMLENSKSQADKDYYQLQAVLEAERRDRGHDSEMIGDLQARITSLQEEVKHLKHNLERVEGERKEAQDMLNHSEKEKNNLEIDLNYKLKSIQQRLEQEVNEHKVTKARLTDKHQSIEEAKSVAMCEMEKKLKEEREAREKAENRVVETEKQCSMLDVDLKQSQQKLEHLTENKERLEDAVKSLTLQLEQESNKRILLQSELKTQAFEADNLKGLEKQMKQEINTLLEAKRLLEFELAQLTKQYRGNEGQMRELQDQLEAEQYFSTLYKTQVKELKEEIEEKNRENLRKIQELQSEKETLSTQLDLAETKAESEQLARGILEEQYFELTQESKKAASRNRQEITDKDHTVSRLEEANNALTKDIELLRKENEELNERMRTAEEEYKLKKEEEISNLKAAFEKNISTERTLKTQAVNKLAEIMNRKDFKIDRKKANTQDLRKKEKENRKLQLELNQEREKFNQMVVKHQKELNDMQAQLVEECTHRNELQMQLASKESDIEQLRAKLLDLSDSTSVASFPSADETDGNLPVGSACIPYLFIFYSSSSRIEGWLSVPNRGNIKRYGWKKQYVVVSSKKMLFYNDEQDKEQSSPSMVLDIDKLFHVRPVTQGDVYRAETEEIPKIFQILYANEGECRKDIEVEPVQQGEKTNFQNHKGHEFIPTLYHFPANCEACAKPLWHVFKPPPALECRRCHVKSHRDHLDKKEDLIPPCKVSYDVTSARDMLLLACPQDEQKKWVTHLVKKIPKKAPSGFVRASPRTLSTRSTANQSFRKVVKNTSGKTS
  
Inhibitor
Name:
BDBM24995
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
Type:
Small organic molecule
Emp. Form.:
C16H20N8O2
Mol. Mass.:
356.3824
SMILES:
CCn1c(nc2cncc(C(=O)NC3CCNCC3)c12)-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