Reaction Details Report a problem with these data
Target
Rho-associated protein kinase 1
Ligand
BDBM14027
Substrate
n/a
Meas. Tech.
Fluorescent Polarization Assay
Temperature
296.15±n/a K
IC50
2100±200 nM
Comments
extracted
Citation
 McKerracher, L; Bond, LM Treatment of cerebral cavernous malformations and cerebral aneurysms with Rho kinase inhibitors US Patent  US9687483 Publication Date 6/27/2017 
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:
BDBM14027
Synonyms:
5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 5-(1,4-diazepane-1-sulfonyl)isoquinoline | AT877 | CHEMBL38380 | CHEMBL541388 | Fasudil (HA-1077) | HA-1077 | US9687483, Fasudil | cid_163751
Type:
Small organic molecule
Emp. Form.:
C14H17N3O2S
Mol. Mass.:
291.369
SMILES:
O=S(=O)(N1CCCNCC1)c1cccc2cnccc12
Structure:
Search PDB for entries with ligand similarity: