Compile Data Set for Download or QSAR
Report error Found 3944 Enz. Inhib. hit(s) with Target = 'Rho-associated protein kinase 1'
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50546246(CHEMBL4753043 | US11608319, Compound AR-13503)
Affinity DataKi:  0.200nMAssay Description:Inhibition of human ROCK1 expressed in baculovirus expression system by Kinase-Glo luminescent AssayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50546246(CHEMBL4753043 | US11608319, Compound AR-13503)
Affinity DataKi:  0.200nMAssay Description:Inhibition of recombinant human GST-tagged ROCK1 catalytic domain expressed in baculovirus expression system by Kinase-Glo luminescent kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM252239(US9458110, 309)
Affinity DataIC50: 0.200nMpH: 7.5Assay Description:The effectiveness of compounds of the present invention as ROCK inhibitors can be determined in a 30 μL assay containing 20 mM HEPES, pH 7.5, 20...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/2/2017
Entry Details
US Patent

TargetRho-associated protein kinase 1 [1-535](Human)
Kadmon

US Patent
LigandPNGBDBM598584(N-(2-(3,6-diazabicyclo[3.1.1]heptan-6-yl)-6-methyl...)
Affinity DataIC50: 0.200nMAssay Description:Recombinant ROCK1 (amino acids 1-535) and ROCK2 (amino acids 1-552) proteins were purchased from ThermoFisher Scientific. Compound's activities w...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/9/2023
Entry Details
US Patent

TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50546246(CHEMBL4753043 | US11608319, Compound AR-13503)
Affinity DataKi:  0.200nMAssay Description:Inhibition of Rock1 (unknown origin) by Kinase Glo luminescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM252174(US9458110, 246)
Affinity DataIC50: 0.260nMpH: 7.5Assay Description:The effectiveness of compounds of the present invention as ROCK inhibitors can be determined in a 30 μL assay containing 20 mM HEPES, pH 7.5, 20...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/2/2017
Entry Details
US Patent

TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataKd:  0.280nMAssay Description:Binding constant for ROCK1 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM252175(US9458110, 247)
Affinity DataIC50: 0.390nMpH: 7.5Assay Description:The effectiveness of compounds of the present invention as ROCK inhibitors can be determined in a 30 μL assay containing 20 mM HEPES, pH 7.5, 20...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/2/2017
Entry Details
US Patent

TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM569251(US11427563, Compound 120 | US11427563, Compound 11...)
Affinity DataIC50: 0.400nMAssay Description:All compounds were initially prepared as 10 mM stocks in anhydrous dimethylsulfoxide (DMSO). A 20 μl aliquot of the 10 mM solutions was transfer...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/7/2022
Entry Details
US Patent

TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM569271(US11427563, Compound 86 | US11427563, Compound 146)
Affinity DataIC50: 0.400nMAssay Description:All compounds were initially prepared as 10 mM stocks in anhydrous dimethylsulfoxide (DMSO). A 20 μl aliquot of the 10 mM solutions was transfer...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/7/2022
Entry Details
US Patent

TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM569271(US11427563, Compound 86 | US11427563, Compound 146)
Affinity DataIC50: 0.400nMAssay Description:All compounds were initially prepared as 10 mM stocks in anhydrous dimethylsulfoxide (DMSO). A 20 μl aliquot of the 10 mM solutions was transfer...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/7/2022
Entry Details
US Patent

TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM252176(US9458110, 248)
Affinity DataIC50: 0.430nMpH: 7.5Assay Description:The effectiveness of compounds of the present invention as ROCK inhibitors can be determined in a 30 μL assay containing 20 mM HEPES, pH 7.5, 20...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/2/2017
Entry Details
US Patent

TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataIC50: 0.444nMAssay Description:Inhibition of human ROCK1 using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/27/2022
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM572304(4-(2,7- diazaspiro[4.4]nonan-2- yl)-3-pyridazin-4-...)
Affinity DataKi:  0.448nMAssay Description:MRCKα, MRCKβ, ROCK1 and ROCK2 assays were performed using an IMAP fluorescence polarization assay format (Molecular Devices Inc.). 8-12 nM ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2022
Entry Details
US Patent

TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM376380(US9914740, VIII-6 | N-((R)-1-(3-methoxyphenyl) eth...)
Affinity DataIC50: 0.490nMAssay Description:Inhibition of ROCK1 (unknown origin) using FITC-AHA-AKRRRLSSLRA-OH as substrate by caliper assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM569350(US11427563, Compound 125)
Affinity DataIC50: 0.5nMAssay Description:All compounds were initially prepared as 10 mM stocks in anhydrous dimethylsulfoxide (DMSO). A 20 μl aliquot of the 10 mM solutions was transfer...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/7/2022
Entry Details
US Patent

TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM199250(US9221808, 1bo-HCl | US9221808, 1bo-Mes | US922180...)
Affinity DataIC50: 0.530nMAssay Description:Inhibition of ROCK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2020
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM412136(US10392402, Compound A | US10738007, Compound A | ...)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of ROCK1 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPurchaseSimilars
In Depth
Date in BDB:
4/19/2024
Entry Details
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM412136(US10392402, Compound A | US10738007, Compound A | ...)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of human ROCK1More data for this Ligand-Target Pair
Ligand InfoPurchaseSimilars
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM139540(US8889696, Staurosporine | US9051313, Staurosporin...)
Affinity DataIC50: 0.627nMAssay 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
US Patent

TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50089584(CHEMBL3578252 | US9914740, VIII-15)
Affinity DataIC50: 0.630nMAssay Description:Inhibition of ROCK1 (unknown origin) using FITC-AHA-AKRRRLSSLRA-OH as substrate by caliper assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataIC50: 0.640nMAssay Description:Inhibition of ROCK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/26/2020
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50089584(CHEMBL3578252 | US9914740, VIII-15)
Affinity DataIC50: 0.670nMAssay Description:Inhibition of ROCK1 (unknown origin) using FITC-AHA-AKRRRLSSLRA-OH as substrate by caliper assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50089584(CHEMBL3578252 | US9914740, VIII-15)
Affinity DataIC50: 0.670nMAssay Description:Inhibition of ROCK1 (unknown origin) using FITC-AHA-AKRRRLSSLRA-OH as substrate by caliper assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataIC50: 0.680nMAssay Description:Inhibition of ROCK1 (unknown origin) by mobility shift assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2017
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM252182(US9458110, 254)
Affinity DataIC50: 0.770nMpH: 7.5Assay Description:The effectiveness of compounds of the present invention as ROCK inhibitors can be determined in a 30 μL assay containing 20 mM HEPES, pH 7.5, 20...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/2/2017
Entry Details
US Patent

TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataIC50: 0.799nMAssay Description:Inhibition of human ROCK1 using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50546544(CHEMBL4791701)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of ROCK1 (unknown origin) using FITC-AHA-AKRRRLSSLRA-OH peptide substrate by caliper assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM252182(US9458110, 254)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of ROCK1 (unknown origin) using FITC-AHA-AKRRRLSSLRA-OH peptide substrate by caliper assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM251934(US9458110, 6)
Affinity DataIC50: 0.850nMpH: 7.5Assay Description:The effectiveness of compounds of the present invention as ROCK inhibitors can be determined in a 30 μL assay containing 20 mM HEPES, pH 7.5, 20...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/2/2017
Entry Details
US Patent

TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM251935(US9458110, 7)
Affinity DataIC50: 0.900nMAssay Description:Inhibition of ROCK1 (unknown origin) using FITC-AHA-AKRRRLSSLRA-OH peptide substrate by caliper assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM597767(US11608319, Compound 13)
Affinity DataIC50: 1nMAssay Description:Table 2: Inhibitory effect of each compound synthesized above on Rho-associated protein kinase (ROCK) was tested.Method 1. 10 mM test compound was di...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/5/2023
Entry Details
US Patent

TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50087130(CHEMBL3426625)
Affinity DataIC50: 1nMAssay Description:Inhibition of human N-terminal GST-tagged ROCK1 expressed in insect cells using long S6 kinase peptide as substrate by radiometric assay in presence ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/6/2016
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50549385(CHEMBL4777515)
Affinity DataKi:  1nMAssay Description:Inhibition of ROCK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50515430(NETARSUDIL | US11608319, Compound AR-13324)
Affinity DataKi:  1nMAssay Description:Inhibition of ROCK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50087131(CHEMBL3426624)
Affinity DataIC50: 1nMAssay Description:Inhibition of human N-terminal GST-tagged ROCK1 expressed in insect cells using long S6 kinase peptide as substrate by radiometric assay in presence ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/6/2016
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM14042(N-(3-{[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H...)
Affinity DataIC50: 1nMpH: 7.4 T: 2°CAssay Description:The assay of Rock-1 activity involved incubation with peptide substrate and ATP/[gamma-33P] ATP, the subsequent incorporation of 33P into the peptid...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/6/2007
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50087132(CHEMBL3426623)
Affinity DataIC50: 1nMAssay Description:Inhibition of human N-terminal GST-tagged ROCK1 expressed in insect cells using long S6 kinase peptide as substrate by radiometric assay in presence ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/6/2016
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM14043(N-(3-{[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H...)
Affinity DataIC50: 1nMpH: 7.4 T: 2°CAssay Description:The assay of Rock-1 activity involved incubation with peptide substrate and ATP/[gamma-33P] ATP, the subsequent incorporation of 33P into the peptid...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/6/2007
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50546247(Netarsudil | AR-11324 FREE BASE | AR-13324 | US114...)
Affinity DataKi:  1nMAssay Description:Inhibition of recombinant human GST-tagged ROCK1 catalytic domain expressed in baculovirus expression system by Kinase-Glo luminescent kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50087133(CHEMBL3426622)
Affinity DataIC50: 1nMAssay Description:Inhibition of human N-terminal GST-tagged ROCK1 expressed in insect cells using long S6 kinase peptide as substrate by radiometric assay in presence ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/6/2016
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM14044(N-(3-{[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H...)
Affinity DataIC50: 1nMpH: 7.4 T: 2°CAssay Description:The assay of Rock-1 activity involved incubation with peptide substrate and ATP/[gamma-33P] ATP, the subsequent incorporation of 33P into the peptid...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/6/2007
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM14045(N-(3-{[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H...)
Affinity DataIC50: 1nMpH: 7.4 T: 2°CAssay Description:The assay of Rock-1 activity involved incubation with peptide substrate and ATP/[gamma-33P] ATP, the subsequent incorporation of 33P into the peptid...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/6/2007
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50463484(CHEMBL4248525)
Affinity DataKi: <1nMAssay Description:Inhibition of ROCK1 (6 to 553 residues) (unknown origin) using Lys-Lys-Arg-Asn-Arg-Thr-Leu-Ser-Val as substrate in presence of ATP by spectrophotomet...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM14046(N-(3-{[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H...)
Affinity DataIC50: 1nMpH: 7.4 T: 2°CAssay Description:The assay of Rock-1 activity involved incubation with peptide substrate and ATP/[gamma-33P] ATP, the subsequent incorporation of 33P into the peptid...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/6/2007
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50546247(Netarsudil | AR-11324 FREE BASE | AR-13324 | US114...)
Affinity DataKi:  1nMAssay Description:Binding affinity to ROCK1 (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50506948(CHEMBL4448806)
Affinity DataIC50: 1nMAssay Description:Inhibition of ROCK1 (unknown origin) incubated for 2 hrs by AbbVie kinase panel assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50463499(CHEMBL4250547)
Affinity DataKi: <1nMAssay Description:Inhibition of ROCK1 (6 to 553 residues) (unknown origin) using Lys-Lys-Arg-Asn-Arg-Thr-Leu-Ser-Val as substrate in presence of ATP by spectrophotomet...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50430377(CHEMBL2333898)
Affinity DataIC50: 1nMAssay Description:Inhibition of ROCK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Taipei Medical University

Curated by ChEMBL
LigandPNGBDBM50546246(CHEMBL4753043 | US11608319, Compound AR-13503)
Affinity DataIC50: 1nMAssay Description:Table 2: Inhibitory effect of each compound synthesized above on Rho-associated protein kinase (ROCK) was tested.Method 1. 10 mM test compound was di...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/5/2023
Entry Details
US Patent

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