Assay Detail

CHEMBL2024951

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Binding

Displacement of fluorescent-ARC-583/ARC-1042/ARC-1059 from His6-tagged recombinant human ROCK2 by fluorescence anisotropy assay

ChEMBL ↗

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Target

Rho-associated protein kinase 2 (CHEMBL2973) ↗

Open DB target context

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Rho-associated protein kinase 2 (CHEMBL2973) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Rho-associated protein kinase 2

CHEMBL2973

Anchored from Assay target.

Protein identity Rho-associated protein kinase 2

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Rho-associated protein kinase 2 (CHEMBL2973) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Conjugates of 5-isoquinolinesulfonylamides and oligo-D-arginine possess high affinity and selectivity towards Rho kinase (ROCK).

Lavogina D, Kalind K, Bredihhina J, Hurt M, Vaasa A, Kasari M, Enkvist E, Raidaru G, Uri A.
Bioorg Med Chem Lett (2012) 22 : 3425 -3430
PubMed 22521647 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Kd	2	7.57	7.57
IC50	2	7.41	8.61

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2023714	—	—	2	8.61
CHEMBL2023842	—	—	2	7.57

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2023714	—	IC50	=	2.455	nM	8.61
CHEMBL2023842	—	Kd	=	27.0	nM	7.57
CHEMBL2023842	—	IC50	=	630.96	nM	6.20
CHEMBL2023714	—	Kd	<	0.5	nM	-