BDBM14027 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline::5-(1,4-diazepane-1-sulfonyl)isoquinoline::AT877::CHEMBL38380::CHEMBL541388::Fasudil (HA-1077)::HA-1077::US20240246972, Compound Fasudil::US9687483, Fasudil::cid_163751
SMILES c1cc2cnccc2c(c1)S(=O)(=O)N3CCCNCC3
InChI Key InChIKey=NGOGFTYYXHNFQH-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 79 hits for monomerid = 14027
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
Affinity DataKd: 50nMAssay 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
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
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
Affinity DataIC50: 158nMAssay Description:Inhibition of human ROCK2More data for this Ligand-Target Pair
Affinity DataIC50: 158nMAssay Description:Inhibition of ROCK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 158nMAssay Description:Inhibition of ROCK2 (unknown origin)More data for this Ligand-Target Pair
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
Affinity DataIC50: 180nMAssay Description:Inhibition of Rho kinaseMore data for this Ligand-Target Pair
Affinity DataIC50: 180nMAssay Description:Inhibition of Rho kinaseMore data for this Ligand-Target Pair
Affinity DataIC50: 220nMAssay Description:Inhibition of ROCK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 260nMAssay Description:Inhibition of ROCK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 260nMAssay Description:Inhibition of ROCK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 260nMAssay Description:Inhibition of ROCK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 300nMAssay Description:Inhibition of human recombinant N-terminal his-tagged ROCK1 (3-543) expressed in baculovirus infected Sf9 cells using Biotin-Ahx-AKRRLSSLRA-CONH2 sub...More data for this Ligand-Target Pair
Affinity DataIC50: 320nMAssay Description:Inhibition of ROCK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 320nMAssay Description:Inhibition of ROCK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 320nMAssay Description:Inhibition of ROCK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 330nMAssay Description:Binding affinity to human ROCK1 assessed as inhibition constantMore data for this Ligand-Target Pair
Affinity DataKi: 330nMAssay Description:Inhibition of ROCK2 (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
Affinity DataKi: 330nMAssay Description:Inhibition of ROCK (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 367nMAssay 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
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
Affinity DataKi: 460nM ΔG°: -8.78kcal/molepH: 7.6 T: 2°CAssay 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
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
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
Affinity DataKi: 530nM ΔG°: -8.70kcal/molepH: 7.6 T: 2°CAssay 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
Affinity DataKi: 530nMAssay Description:Inhibition of human leukocytic ROCK1 expressed in insect cells using KKRNRTLSV as substrate after 10 mins by pyruvate kinase/lactate dehydrogenase co...More data for this Ligand-Target Pair
TargetcAMP-dependent protein kinase catalytic subunit alpha [Q181K,T183A](Bovine)
German Cancer Research Center
German Cancer Research Center
Affinity DataIC50: 541nMAssay 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
TargetcAMP-dependent protein kinase catalytic subunit alpha [T183A](Bovine)
German Cancer Research Center
German Cancer Research Center
Affinity DataIC50: 607nMAssay 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
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
Affinity DataIC50: 660nMAssay Description:Inhibition of human ROCK2 by IMAP assayMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase N2(Human)
Boehringer Ingelheim Pharmaceuticals
Curated by ChEMBL
Boehringer Ingelheim Pharmaceuticals
Curated by ChEMBL
TargetSerine/threonine-protein kinase N2(Human)
Boehringer Ingelheim Pharmaceuticals
Curated by ChEMBL
Boehringer Ingelheim Pharmaceuticals
Curated by ChEMBL
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
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
The Scripps Research Institute Molecular Screening Center
Curated by PubChem BioAssay
The Scripps Research Institute Molecular Screening Center
Curated by PubChem BioAssay
Affinity DataIC50: 853nMAssay 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
TargetcAMP-dependent protein kinase catalytic subunit alpha [L49I,Q181K,T183A](Bovine)
German Cancer Research Center
German Cancer Research Center
Affinity DataIC50: 870nMAssay 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
TargetcAMP-dependent protein kinase catalytic subunit alpha [L49I](Bovine)
German Cancer Research Center
German Cancer Research Center
Affinity DataIC50: 893nMpH: 6.8 T: 2°CAssay 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
Affinity DataIC50: 940nMAssay Description:Inhibition of ROCK1 (unknown origin)More data for this Ligand-Target Pair
TargetcAMP-dependent protein kinase catalytic subunit alpha [L49I,V123M,Q181K,T183A](Bovine)
German Cancer Research Center
German Cancer Research Center
Affinity DataIC50: 1.13E+3nMAssay 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
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
TargetcAMP-dependent protein kinase catalytic subunit alpha [V123M,T183A](Bovine)
German Cancer Research Center
German Cancer Research Center
Affinity DataIC50: 1.35E+3nMAssay 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
Affinity DataIC50: 1.49E+3nMpH: 6.8 T: 2°CAssay 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
TargetcAMP-dependent protein kinase catalytic subunit beta(Rat)
Temple University
Curated by PDSP Ki Database
Temple University
Curated by PDSP Ki Database
Affinity DataIC50: 1.70E+3nMAssay Description:Inhibition of Protein kinase C related kinase 1 (PRK1)More data for this Ligand-Target Pair

3D Structure (crystal)