BDBM14027 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline::5-(1,4-diazepane-1-sulfonyl)isoquinoline::AT877::CHEMBL38380::CHEMBL541388::Fasudil (HA-1077)::HA-1077::US9687483, Fasudil::cid_163751

SMILES O=S(=O)(N1CCCNCC1)c1cccc2cnccc12

InChI Key InChIKey=NGOGFTYYXHNFQH-UHFFFAOYSA-N

Data  11 KI  62 IC50  3 Kd  1 EC50

PDB links: 15 PDB IDs match this monomer.

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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 15 hits for monomerid = 14027   

TargetRho-associated protein kinase 1(Homo sapiens (Human))
Msd

Curated by ChEMBL
LigandPNGBDBM14027(5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 5-(1,4...)
Affinity DataKi:  100nMAssay Description:Inhibition of ROCK-1More data for this Ligand-Target Pair
TargetRho-associated protein kinase 1(Homo sapiens (Human))
Msd

Curated by ChEMBL
LigandPNGBDBM14027(5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 5-(1,4...)
Affinity DataKi:  330nMAssay Description:In vitro inhibition of angiotensin I converting enzyme in rabbit lung with hippuryl-histidyl-leucine as substrateMore data for this Ligand-Target Pair
TargetRho-associated protein kinase 1(Homo sapiens (Human))
Msd

Curated by ChEMBL
LigandPNGBDBM14027(5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 5-(1,4...)
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
TargetRho-associated protein kinase 1(Homo sapiens (Human))
Msd

Curated by ChEMBL
LigandPNGBDBM14027(5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 5-(1,4...)
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
TargetRho-associated protein kinase 1(Homo sapiens (Human))
Msd

Curated by ChEMBL
LigandPNGBDBM14027(5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 5-(1,4...)
Affinity DataIC50:  3.16E+3nMAssay Description:Inhibition of ROCK-1 by Immobilized metal ion affinity-based fluorescence polarization assayMore data for this Ligand-Target Pair
TargetRho-associated protein kinase 1(Homo sapiens (Human))
Msd

Curated by ChEMBL
LigandPNGBDBM14027(5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 5-(1,4...)
Affinity DataIC50:  4.30E+3nMAssay Description:Inhibition of human ROCK1 by homogenous luciferase assayMore data for this Ligand-Target Pair
TargetRho-associated protein kinase 1(Homo sapiens (Human))
Msd

Curated by ChEMBL
LigandPNGBDBM14027(5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 5-(1,4...)
Affinity DataIC50:  260nMAssay Description:Inhibition of ROCK1 (unknown origin)More data for this Ligand-Target Pair
TargetRho-associated protein kinase 1(Homo sapiens (Human))
Msd

Curated by ChEMBL
LigandPNGBDBM14027(5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 5-(1,4...)
Affinity DataIC50:  660nMAssay Description:Inhibition of ROCK1More data for this Ligand-Target Pair
TargetRho-associated protein kinase 1(Homo sapiens (Human))
Msd

Curated by ChEMBL
LigandPNGBDBM14027(5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 5-(1,4...)
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
TargetRho-associated protein kinase 1(Homo sapiens (Human))
Msd

Curated by ChEMBL
LigandPNGBDBM14027(5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 5-(1,4...)
Affinity DataIC50:  4.30E+3nMAssay Description:Inhibition of human ROCK1 by homogenous luciferase assayMore data for this Ligand-Target Pair
TargetRho-associated protein kinase 1(Rattus norvegicus (Rat))
Bioaxone Biosciences

US Patent
LigandPNGBDBM14027(5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 5-(1,4...)
Affinity DataIC50:  2.10E+3nMT: 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
TargetRho-associated protein kinase 1(Homo sapiens (Human))
Msd

Curated by ChEMBL
LigandPNGBDBM14027(5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 5-(1,4...)
Affinity DataIC50:  260nMAssay Description:Inhibition of ROCK1 (unknown origin)More data for this Ligand-Target Pair
TargetRho-associated protein kinase 1(Homo sapiens (Human))
Msd

Curated by ChEMBL
LigandPNGBDBM14027(5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 5-(1,4...)
Affinity DataIC50:  260nMAssay Description:Inhibition of ROCK1 (unknown origin)More data for this Ligand-Target Pair
TargetRho-associated protein kinase 1(Homo sapiens (Human))
Msd

Curated by ChEMBL
LigandPNGBDBM14027(5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 5-(1,4...)
Affinity DataIC50:  940nMAssay Description:Inhibition of ROCK1 (unknown origin)More data for this Ligand-Target Pair
TargetRho-associated protein kinase 1(Homo sapiens (Human))
Msd

Curated by ChEMBL
LigandPNGBDBM14027(5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 5-(1,4...)
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