Compile Data Set for Download or QSAR
Report error Found 27 Enz. Inhib. hit(s) for PDB: 2F2U
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataKd:  78nMAssay Description:Displacement of fluorescent-ARC-1063 from His6-tagged recombinant human ROCK2 by luminescence intensity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataKd:  45nMAssay Description:Compounds were tested using an 11-point curve with 3-fold serial dilutions. IC50 determinations were made using an ATP concentration of 10 uM. The hi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2022
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 71nMAssay Description:Source (MLSCN Center Name): The Scripps Research Institute Molecular Screening Center Center Affiliation: The Scripps Research Institute, TSRI Assay ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2011
Entry Details
PCBioAssayPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 158nMAssay Description:Inhibition of ROCK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/18/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 158nMAssay Description:Inhibition of ROCK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/25/2014
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 158nMAssay Description:Inhibition of human ROCK2More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 164nMAssay Description:Compounds as a powder were dissolved in dimethyl sulfoxide to make a 10 mM stock. Compounds were tested in 10-dose IC50 triplicate mode with a 3-fold...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/7/2024
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetRho-associated protein kinase 1/2(Human)
Kirin Brewery

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 180nMAssay Description:Inhibition of Rho kinaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 1/2(Human)
Kirin Brewery

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 180nMAssay Description:Inhibition of Rho kinaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/10/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 220nMAssay Description:Inhibition of ROCK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 320nMAssay Description:Inhibition of ROCK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 320nMAssay Description:Inhibition of ROCK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 320nMAssay Description:Inhibition of ROCK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 370nMAssay Description:Inhibition of ROCK2 (unknown origin) using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK-peptide as substrate incubated for 30 mins in presence of [gamma-33P]-ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 400nMAssay Description:Inhibition of ROCK2More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2010
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Bovine)
German Cancer Research Center

LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 485nMAssay Description:The enzyme activity was assayed by using an ATP regenerative NADH consuming system. The reaction was started with adding ATP to the mixture containin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2007
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 509nMAssay Description:Inhibition of ROCK2 (unknown origin) using 2-biotin as substrate measured after 15 to 60 mins by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 659nMAssay Description:Inhibition of ROCK2 (unknown origin) using 2-biotin as substrate measured after 15 to 60 mins by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 660nMAssay Description:Inhibition of human ROCK2 by IMAP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/28/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Rat)
Bioaxone Biosciences

US Patent
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 820nMT: 2°CAssay Description:The inhibitor potency of BA-1049 (racemic mixture) and Fasudil (Calbiochem) were compared by fluorescent polarization assays performed using a Biomek...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2018
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 1.35E+3nMAssay Description:Inhibition of ROCK-2 by Immobilized metal ion affinity-based fluorescence polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 1.90E+3nMAssay Description:Inhibition of Protein kinase ROCK2 (ROCKII)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Rat)
Bioaxone Biosciences

US Patent
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 1.90E+3nMAssay Description:Inhibition of rat ROCK2 expressed in Sf9 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/10/2011
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataIC50: 1.17E+4nMAssay Description:Displacement of fluorescent-ARC-1063 from His6-tagged recombinant human ROCK2 by luminescence intensity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 1/2(Human)
Kirin Brewery

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataKi:  330nMAssay Description:Inhibition of ROCK (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Rat)
Bioaxone Biosciences

US Patent
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataKi:  330nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/10/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetRho-associated protein kinase 2(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM14027(AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl...)
Affinity DataKi:  330nMAssay Description:Inhibition of ROCK2 (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMedPDB3D3D Structure (crystal)