General Information of the Protein
Protein ID
PT00890
Protein Name
Rho-associated protein kinase 2
Secondarily
Protein Name
Rho kinase 2
Rho-associated
coiled-coil-containing protein kinase 2
Rho-associated
coiled-coil-containing protein kinase II
p164 ROCK-2
Gene Name
ROCK2
Secondarily
Gene Name
KIAA0619
Sequence
MSRPPPTGKMPGAPETAPGDGAGASRQRKLEALIRDPRSPINVESLLDGLNSLVLDLDFPALRKNKNIDNFLNRYEKIVKKIRGLQMKAEDYDVVKVIGRGAFGEVQLVRHKASQKVYAMKLLSKFEMIKRSDSAFFWEERDIMAFANSPWVVQLFYAFQDDRYLYMVMEYMPGGDLVNLMSNYDVPEKWAKFYTAEVVLALDAIHSMGLIHRDVKPDNMLLDKHGHLKLADFGTCMKMDETGMVHCDTAVGTPDYISPEVLKSQGGDGFYGRECDWWSVGVFLYEMLVGDTPFYADSLVGTYSKIMDHKNSLCFPEDAEISKHAKNLICAFLTDREVRLGRNGVEEIRQHPFFKNDQWHWDNIRETAAPVVPELSSDIDSSNFDDIEDDKGDVETFPIPKAFVGNQLPFIGFTYYRENLLLSDSPSCRETDSIQSRKNEESQEIQKKLYTLEEHLSNEMQAKEELEQKCKSVNTRLEKTAKELEEEITLRKSVESALRQLEREKALLQHKNAEYQRKADHEADKKRNLENDVNSLKDQLEDLKKRNQNSQISTEKVNQLQRQLDETNALLRTESDTAARLRKTQAESSKQIQQLESNNRDLQDKNCLLETAKLKLEKEFINLQSALESERRDRTHGSEIINDLQGRICGLEEDLKNGKILLAKVELEKRQLQERFTDLEKEKSNMEIDMTYQLKVIQQSLEQEEAEHKATKARLADKNKIYESIEEAKSEAMKEMEKKLLEERTLKQKVENLLLEAEKRCSLLDCDLKQSQQKINELLKQKDVLNEDVRNLTLKIEQETQKRCLTQNDLKMQTQQVNTLKMSEKQLKQENNHLMEMKMNLEKQNAELRKERQDADGQMKELQDQLEAEQYFSTLYKTQVRELKEECEEKTKLGKELQQKKQELQDERDSLAAQLEITLTKADSEQLARSIAEEQYSDLEKEKIMKELEIKEMMARHKQELTEKDATIASLEETNRTLTSDVANLANEKEELNNKLKDVQEQLSRLKDEEISAAAIKAQFEKQLLTERTLKTQAVNKLAEIMNRKEPVKRGNDTDVRRKEKENRKLHMELKSEREKLTQQMIKYQKELNEMQAQIAEESQIRIELQMTLDSKDSDIEQLRSQLQALHIGLDSSSIGSGPGDAEADDGFPESRLEGWLSLPVRNNTKKFGWVKKYVIVSSKKILFYDSEQDKEQSNPYMVLDIDKLFHVRPVTQTDVYRADAKEIPRIFQILYANEGESKKEQEFPVEPVGEKSNYICHKGHEFIPTLYHFPTNCEACMKPLWHMFKPPPALECRRCHIKCHKDHMDKKEEIIAPCKVYYDISTAKNLLLLANSTEEQQKWVSRLVKKIPKKPPAPDPFARSSPRTSMKIQQNQSIRRPSRQLAPNKPS
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
AGC protein kinase group
>
AGC protein kinase DMPK family
>
AGC protein kinase ROCK subfamily
Function
Protein kinase which is a key regulator of actin cytoskeleton and cell polarity. Involved in regulation of smooth muscle contraction, actin cytoskeleton organization, stress fiber and focal adhesion formation, neurite retraction, cell adhesion and motility via phosphorylation of ADD1, BRCA2, CNN1, EZR, DPYSL2, EP300, MSN, MYL9/MLC2, NPM1, RDX, PPP1R12A and VIM. Phosphorylates SORL1 and IRF4. Acts as a negative regulator of VEGF-induced angiogenic endothelial cell activation. Positively regulates the activation of p42/MAPK1-p44/MAPK3 and of p90RSK/RPS6KA1 during myogenic differentiation. Plays an important role in the timely initiation of centrosome duplication. Inhibits keratinocyte terminal differentiation. May regulate closure of the eyelids and ventral body wall through organization of actomyosin bundles. Plays a critical role in the regulation of spine and synaptic properties in the hippocampus. Plays an important role in generating the circadian rhythm of the aortic myofilament Ca(2+) sensitivity and vascular contractility by modulating the myosin light chain phosphorylation.
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Uniprot ID
Primary ID:
O75116

Secondarily ID:
Q53QZ0
Q53SJ7
Q9UQN5
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Ensembl ID
ENSG00000134318
HGNC ID
HGNC:10252
Subcellular Location
Cytoplasm
Cell membrane
Nucleus
Cytoplasm
Cytoskeleton
Microtubule organizing center
Centrosome
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000333 , GTM-3
Compound ID Compound Name Compound Formula
CP0060392
(R)-4-(1-aminoethyl)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzamide
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C16H16N4O
 1
1
EC50 = 150 nM
   TI
   LI
   LO
   TS
CP0058927
5-[6-(1,4-diazepan-1-yl)pyrazin-2-yl]-1H-indazole
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C16H18N6
 1
1
EC50 = 260 nM
   TI
   LI
   LO
   TS
CP0225487
5-[6-(1,4-diazepan-1-yl)pyrazin-2-yl]-3-methyl-2H-indazole
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C17H20N6
 1
1
EC50 = 380 nM
   TI
   LI
   LO
   TS
CP0060393
5-[6-(1,4-diazepan-1-yl)-5-pyrrolidin-1-ylpyrazin-2-yl]-1H-pyrazolo[3,4-c]pyridine
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C19H24N8
 1
1
EC50 = 416 nM
   TI
   LI
   LO
   TS
CP0035246
2-(4-(6-(pyridin-4-yl)-3-(pyrrolidin-1-yl)pyrazin-2-yl)piperazin-1-yl)ethanol
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C19H26N6O
 1
1
EC50 = 680 nM
   TI
   LI
   LO
   TS
CP0209095
N-[3-[4-(6-pyridin-4-yl-3-pyrrolidin-1-ylpyrazin-2-yl)piperazin-1-yl]propyl]acetamide
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C22H31N7O
 1
1
EC50 = 760 nM
   TI
   LI
   LO
   TS
CP0225486
1-(dimethylamino)-3-[4-(6-pyridin-4-yl-3-pyrrolidin-1-ylpyrazin-2-yl)piperazin-1-yl]propan-2-ol
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C22H33N7O
 1
1
EC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0058928
N-[2-hydroxy-3-[4-(6-pyridin-4-yl-3-pyrrolidin-1-ylpyrazin-2-yl)piperazin-1-yl]propyl]acetamide
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C22H31N7O2
 1
1
EC50 = 1700 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0060212
N-[(3-methoxyphenyl)methyl]-6-(1H-pyrazol-4-yl)-1H-indole-3-carboxamide
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C20H18N4O2
 1
1 IC50 < 1 nM
CP0140194
N-[(1R)-1-(3-methoxyphenyl)ethyl]-4-pyridin-4-ylbenzamide
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C21H20N2O2
 1
1 IC50 = 1 nM
CP0070702
N-[(3-methoxyphenyl)methyl]-6-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine-3-carboxamide
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C19H17N5O2
 1
1 IC50 = 2 nM
CP0083275
N-[(3-methoxyphenyl)methyl]-6-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine-2-carboxamide
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C19H17N5O2
 1
1 IC50 = 2 nM
CP0130674
N-[(3-methoxyphenyl)methyl]-6-(1H-pyrazol-4-yl)-1H-indole-2-carboxamide
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C20H18N4O2
 1
1 IC50 = 2 nM
CP0016240
(R)-TRANS-4-(1-AMINOETHYL)-N-(4-PYRIDYL) CYCLOHEXANECARBOXAMIDE
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C14H21N3O
 7
1 IC50 = 8.3 nM
2 IC50 = 54 nM
3 IC50 = 89 nM
4 IC50 = 245.47 nM
5 IC50 = 260 nM
6 IC50 = 700 nM
7 Ki = 300 nM
CP0058927
5-[6-(1,4-diazepan-1-yl)pyrazin-2-yl]-1H-indazole
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C16H18N6
 1
1 IC50 = 24 nM
CP0225487
5-[6-(1,4-diazepan-1-yl)pyrazin-2-yl]-3-methyl-2H-indazole
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C17H20N6
 1
1 IC50 = 36 nM
CP0035246
2-(4-(6-(pyridin-4-yl)-3-(pyrrolidin-1-yl)pyrazin-2-yl)piperazin-1-yl)ethanol
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C19H26N6O
 2
1 IC50 = 39 nM
2 IC50 = 78 nM
CP0060392
(R)-4-(1-aminoethyl)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzamide
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C16H16N4O
 2
1 IC50 = 58 nM
2 Ki = 2.4 nM
CP0060393
5-[6-(1,4-diazepan-1-yl)-5-pyrrolidin-1-ylpyrazin-2-yl]-1H-pyrazolo[3,4-c]pyridine
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C19H24N8
 1
1 IC50 = 65 nM
CP0058928
N-[2-hydroxy-3-[4-(6-pyridin-4-yl-3-pyrrolidin-1-ylpyrazin-2-yl)piperazin-1-yl]propyl]acetamide
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C22H31N7O2
 1
1 IC50 = 68 nM
CP0209095
N-[3-[4-(6-pyridin-4-yl-3-pyrrolidin-1-ylpyrazin-2-yl)piperazin-1-yl]propyl]acetamide
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C22H31N7O
 1
1 IC50 = 75 nM
CP0225486
1-(dimethylamino)-3-[4-(6-pyridin-4-yl-3-pyrrolidin-1-ylpyrazin-2-yl)piperazin-1-yl]propan-2-ol
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C22H33N7O
 1
1 IC50 = 76 nM
CP0231361
5-(1,4-diazepane-1-sulfonyl)-1,2-dihydroisoquinolin-1-one
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C14H17N3O3S
 2
1 IC50 = 575.44 nM
2 IC50 = 600 nM
Clinical Information about the Protein
Target 1 ( Rho-associated protein kinase 2 (ROCK2) )
Target Type Successful Target
Disease 2 Target-related Diseases  2
1 Graft-versus-host disease [ICD-11: 4B24]
2 Inflammation [ICD-11: 1A00-CA43.1]
Approved Drug(s) 1 Approved Drug  1
1 Belumosudil Approved
Graft-versus-host disease
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 GSK269962A Clinical trial
Inflammation