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Target
Rho-associated protein kinase 1/2
Ligand
BDBM148421
Substrate
n/a
Meas. Tech.
MLC Phosphorylation Assay
EC50
<100±n/a nM
Citation
 Boland, S; Bourin, A; Defert, O; Leysen, D Pyridine derivatives as soft rock inhibitors US Patent  US9682963 Publication Date 6/20/2017 
Target
Name:
Rho-associated protein kinase 1/2
Synonyms:
ROCK Complex
Type:
Protein
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
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
  
Component 2
Name:
Rho-associated protein kinase 2
Synonyms:
ROCK2_RAT | Rho Kinase | Rho-associated protein kinase 2 | Rho-associated protein kinase 2 (ROCK II) | Rho-associated, coiled-coil-containing protein kinase 2 | Rho-associated, coiled-coil-containing protein kinase II | RhoA-binding kinase 2 | Rock2 | p150 ROK-alpha
Type:
Protein
Mol. Mass.:
160370.90
Organism:
Rattus norvegicus (Rat)
Description:
Q62868
Residue:
1388
Sequence:
MSRPPPTGKMPGAPEAAAGDGAGAGRQRKLEALIRDPRSPINVESLLDGLNSLVLDLDFPALRKNKNIDNFLNRYEKIVKKIRGLQMKAEDYDVVKVIGRGAFGEVQLVRHKASQKVYAMKLLSKFEMIKRSDSAFFWEERDIMAFANSPWVVQLFCAFQDDRYLYMVMEYMPGGDLVNLMSNYDVPEKWAKFYTAEVVLALDAIHSMGLIHRDVKPDNMLLDKHGHLKLADFGTCMKMDETGMVHCDTAVGTPDYISPEVLKSQGGDGYYGRECDWWSVGVFLFEMLVGDTPFYADSLVGTYSKIMDHKNSLCFPEDTEISKHAKNLICAFLTDREVRLGRNGVEEIKSASFFKNDQWNWDNIRETAAPVVPELSSDIDSSNFDDIEDDKGDVETFPIPKAFVGNQLPFIGFTYFRENLLLSDSPPCRENDAIQTRKSEESQEIQKKLYALEEHLSSEVQAKEELEQKCKSINTRLEKTAKELEEEITFRKNVESTLRQLEREKALLQHKNAEYQRKADHEADKKRNLENDVNSLKDQLEDLKKRNQSSQISTEKVNQLQKQLDEANALLRTESDTAARLRKTQAESSKQIQQLESNNRDLQDKNCLLETAKLKLEKEFINLQSALESERRDRTHGSEIINDLQGRISGLEEDLKTGKTLLAKVELEKRQLQEKLTDLEKEKSNMEIDMTYQLKVIQQSLEQEEAEHKTTKARLADKNKIYESIEEAKSEAMKEMEKKLLEERSLKQKVENLLLEAEKRCSILDCDLKQSQQKLNELLKQKDVLNEDVRNLTLKIEQETQKRCLMQNDLKMQTQQVNTLKMSEKQIKQENNHLMEMKMNLEKQNAELRKERQDADGQMKELQDQLEAEQYFSTLYKTQVRELKEENEEKTKLCKELQQKKQDLQDERDSLAAQLEITLTKADSEQLARSIAEEQYSDLEKEKIMKELEIKEMMARHKQELTEKDATIASLEETNRTLTSDVANLANEKEELNNKLKDTQEQLSKLKDEEISAAAIKAQFEKQLLTERTLKTQAVNKLAEIMNRKEPVKRGSDTDVRRKEKENRKLHMELKSEREKLTQQMIKYQKELNEMQAQIAEESQIRIELQMTLDSKDSDIEQLRSQLQALHIGMDSSSIGSGPGDAEPDDGFPESRLEGWLSLPVRNNTKKFGWVKKYVIVSSKKILFYDSEQDKEQSNPYMVLDIDKLFHVRPVTQTDVYRADAKEIPRIFQILYANEGESKKEPEFPVEPVGEKSNYICHKGHEFIPTLYHFPTNCEACMKPLWHMFKPPPALECSRCHIKCHKDHMDKKEEIIAPCKVYYDISSAKNLLLLANSTEEQQKWVSRLVKKIPKKPPAPDPFARSSPRTSMKIQQNQSIRRPSRQLAPNKPS
  
Inhibitor
Name:
BDBM148421
Synonyms:
US9682963, 11
Type:
Small organic molecule
Emp. Form.:
C30H25FN4O4S
Mol. Mass.:
556.607
SMILES:
NCc1ccc(cc1-c1cccc(c1)C(=O)Nc1ccc(SC2COC(=O)C2)cc1)C(=O)Nc1ccncc1F
Structure:
Search PDB for entries with ligand similarity: