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Target
Rho-associated protein kinase 2
Ligand
BDBM15211
Substrate
BDBM27221
Meas. Tech.
Fluorescence Polarization-Based Binding Displacement Kinase Assay
pH
7.5±n/a
Temperature
303.15±n/a K
Kd
31±3 nM
Citation
 Lavogina, D; Lust, M; Viil, I; König, N; Raidaru, G; Rogozina, J; Enkvist, E; Uri, A; Bossemeyer, D Structural analysis of ARC-type inhibitor (ARC-1034) binding to protein kinase A catalytic subunit and rational design of bisubstrate analogue inhibitors of basophilic protein kinases. J Med Chem 52:308-21 (2009) [PubMed]  Article 
Target
Name:
Rho-associated protein kinase 2
Synonyms:
KIAA0619 | ROCK-II | ROCK2 | ROCK2_HUMAN | Rho kinase 2 (ROCKII) | Rho-associated protein kinase 2 (ROCK-2) | Rho-associated protein kinase 2 (ROCK2) | Rho-associated protein kinase 2 (ROCKII) | Rho-associated protein kinase 2/Transforming protein RhoA | Rho-associated, coiled-coil-containing protein kinase 2 | Rho-associated, coiled-coil-containing protein kinase II | Serine/threonine-protein kinase RIO2 | p164 ROCK-2
Type:
Protein
Mol. Mass.:
160885.43
Organism:
Homo sapiens (Human)
Description:
O75116
Residue:
1388
Sequence:
MSRPPPTGKMPGAPETAPGDGAGASRQRKLEALIRDPRSPINVESLLDGLNSLVLDLDFPALRKNKNIDNFLNRYEKIVKKIRGLQMKAEDYDVVKVIGRGAFGEVQLVRHKASQKVYAMKLLSKFEMIKRSDSAFFWEERDIMAFANSPWVVQLFYAFQDDRYLYMVMEYMPGGDLVNLMSNYDVPEKWAKFYTAEVVLALDAIHSMGLIHRDVKPDNMLLDKHGHLKLADFGTCMKMDETGMVHCDTAVGTPDYISPEVLKSQGGDGFYGRECDWWSVGVFLYEMLVGDTPFYADSLVGTYSKIMDHKNSLCFPEDAEISKHAKNLICAFLTDREVRLGRNGVEEIRQHPFFKNDQWHWDNIRETAAPVVPELSSDIDSSNFDDIEDDKGDVETFPIPKAFVGNQLPFIGFTYYRENLLLSDSPSCRETDSIQSRKNEESQEIQKKLYTLEEHLSNEMQAKEELEQKCKSVNTRLEKTAKELEEEITLRKSVESALRQLEREKALLQHKNAEYQRKADHEADKKRNLENDVNSLKDQLEDLKKRNQNSQISTEKVNQLQRQLDETNALLRTESDTAARLRKTQAESSKQIQQLESNNRDLQDKNCLLETAKLKLEKEFINLQSALESERRDRTHGSEIINDLQGRICGLEEDLKNGKILLAKVELEKRQLQERFTDLEKEKSNMEIDMTYQLKVIQQSLEQEEAEHKATKARLADKNKIYESIEEAKSEAMKEMEKKLLEERTLKQKVENLLLEAEKRCSLLDCDLKQSQQKINELLKQKDVLNEDVRNLTLKIEQETQKRCLTQNDLKMQTQQVNTLKMSEKQLKQENNHLMEMKMNLEKQNAELRKERQDADGQMKELQDQLEAEQYFSTLYKTQVRELKEECEEKTKLGKELQQKKQELQDERDSLAAQLEITLTKADSEQLARSIAEEQYSDLEKEKIMKELEIKEMMARHKQELTEKDATIASLEETNRTLTSDVANLANEKEELNNKLKDVQEQLSRLKDEEISAAAIKAQFEKQLLTERTLKTQAVNKLAEIMNRKEPVKRGNDTDVRRKEKENRKLHMELKSEREKLTQQMIKYQKELNEMQAQIAEESQIRIELQMTLDSKDSDIEQLRSQLQALHIGLDSSSIGSGPGDAEADDGFPESRLEGWLSLPVRNNTKKFGWVKKYVIVSSKKILFYDSEQDKEQSNPYMVLDIDKLFHVRPVTQTDVYRADAKEIPRIFQILYANEGESKKEQEFPVEPVGEKSNYICHKGHEFIPTLYHFPTNCEACMKPLWHMFKPPPALECRRCHIKCHKDHMDKKEEIIAPCKVYYDISTAKNLLLLANSTEEQQKWVSRLVKKIPKKPPAPDPFARSSPRTSMKIQQNQSIRRPSRQLAPNKPS
  
Inhibitor
Name:
BDBM15211
Synonyms:
CHEMBL104264 | H-89 | H89 | HT-89 (H-89) | N-(2-{[(2E)-3-(4-bromophenyl)prop-2-en-1-yl]amino}ethyl)isoquinoline-5-sulfonamide | N-[2-[[(E)-3-(4-bromophenyl)prop-2-enyl]amino]ethyl]isoquinoline-5-sulfonamide
Type:
Small organic molecule
Emp. Form.:
C20H20BrN3O2S
Mol. Mass.:
446.361
SMILES:
Brc1ccc(\C=C\CNCCNS(=O)(=O)c2cccc3cnccc23)cc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM27221
Synonyms:
Adc-Ahx-(D-Arg)(6)-D-Lys(5-TAMRA)-NH2 | Fluorescent probe ARC-583
Type:
5-TAMRA labeled compound
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
n/a
Structure: