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TargetEnzymes

Rho-associated protein kinase 2

Named enzymes, including the metabolising cytochromes and the monoamine oxidases.

Measurements
5
Compounds
4
Binding constants
0
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

ROCK2_HUMANROCK2Homo sapiens

Rho-associated protein kinase 2

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

Quoted from UniProt’s FUNCTION annotation for O75116 (reviewed).

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
RHOA0.9980.5410.9000.974
ROCK10.9880.7810.9000.409
MYL20.9840.3340.9000.791
PPP1R12A0.9750.0950.9000.700
MYL12B0.9540.1060.9000.530
MYL90.9510.1060.9000.502
CTNNB10.9450.0980.9000.438
PTEN0.9370.0920.9000.351
LIMK10.9370.1310.9000.334
LIMK20.9320.1310.9000.280

Where it sits in the cell

  • Cytosol

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Cytoplasm · Cell membrane · Nucleus · Cytoplasm, cytoskeleton, microtubule organizing center, centrosome

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Functional readouts 1

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

TargetClassTypeValue (nM)pXOrganismAssay
Rho-associated protein kinase 2EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5235539

Other measurements 4

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
Rho-associated protein kinase 2EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1063671
Rho-associated protein kinase 2EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1063671
Rho-associated protein kinase 2EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1063671
Rho-associated protein kinase 2EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1063671