BDBM16173 3,5-diamino-6-chloro-N-(diaminomethylene)pyrazinamide;hydrochloride::3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-carboxamide::Amiloride::Amipramidin::CHEMBL945

SMILES NC(=N)NC(=O)c1nc(Cl)c(N)nc1N

InChI Key InChIKey=XSDQTOBWRPYKKA-UHFFFAOYSA-N

Data  45 KI  31 IC50

PDB links: 2 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 76 hits for monomerid = 16173   

TargetUrokinase-type plasminogen activator(Human)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 2.40E+3nMAssay Description:Inhibition of human kidney uPA using chromogenic H-D-Ile-L-propyl-L-arginine-p-nitroaniline as substrateMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetUrokinase-type plasminogen activator(Human)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 1.07E+5nMAssay Description:Inhibitory activity against Urokinase-type plasminogen activatorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetAmiloride-sensitive sodium channel subunit alpha(Human)
Parion Sciences

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 776nMAssay Description:Inhibition of dog bronchi prototypical epithelial sodium channel by electrophysiological assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium/hydrogen exchanger(three-toed salamander)
University of California

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 9.80E+4nMAssay Description:Inhibition of Amphiuma tridactylum wild type NHE1 expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammonium chloride ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium/hydrogen exchanger 1(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 6.00E+4nMAssay Description:Inhibition of human wild type NHE1 expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammonium chloride prepulse protoc...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetAcid-sensing ion channel 3(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 4.40E+3nMAssay Description:Inhibition of ASIC3 assessed as inhibition of peak current by patch clamp electrophysiologyMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSolute carrier family 22 member 1(Human)
Uppsala University

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 5.70E+4nMAssay Description:Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopyMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTissue-type plasminogen activator(Human)
University of Louisville

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 2.20E+5nMAssay Description:Inhibition of tPA using CH3SO2-D-HHT-Gly-Arg-pNA as substrate by spectrofluorometryMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetUrokinase-type plasminogen activator(Human)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 7.00E+3nMAssay Description:Inhibition of urokinase-type plasminogen activator using Glt-Gly-Arg-AMC as substrate by spectrofluorometryMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetPlasminogen(Human)
University of Louisville

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 2.50E+5nMAssay Description:Inhibition of plasmin using tosyl-Gly-Pro-Lys-pNA as substrate by spectrofluorometryMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium/hydrogen exchanger 1(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 6.67E+4nMAssay Description:Inhibition of platelet NHE1 in human platelet rich plasma assessed as decrease in platelet swelling preincubated for 3 mins followed by sodium propio...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBile salt export pump(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 1.00E+6nMAssay Description:Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetAcid-sensing ion channel 1(Rat)
Anhui Medical University

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 3.02E+4nMAssay Description:Inhibition of ASIC1 in Sprague-Dawley rat articular chondrocytes assessed as decrease in acid-induced intracellular calcium level by Fluo-3AM dye bas...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetSodium channel protein type 5 subunit alpha(Human)
Parion Sciences

US Patent
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 781nMAssay Description:One assay used to assess mechanism of action and/or potency of the compounds of the present invention involves the determination of lumenal drug inhi...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetUrokinase-type plasminogen activator(Human)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 1.20E+4nMAssay Description:Inhibition of human uPA using pyro-Glu-Gly-Arg-pNA as substrate assessed as para-nitroaniline release from substrate measured for 5 mins by spectroph...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetUrokinase-type plasminogen activator(Human)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 7.00E+3nMAssay Description:Inhibitory activity against Urokinase-type plasminogen activatorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetUrokinase-type plasminogen activator(Human)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 2.40E+3nMAssay Description:Inhibition of human uPAMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetUrokinase-type plasminogen activator(Mouse)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 2.30E+3nMAssay Description:Inhibition of mouse uPAMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetVitamin K-dependent protein C(Human)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of activated protein C (unknown origin) using chromogenic L-pyroGlu-L-Pro-L-Arg-p-nitroaniline as substrateMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCoagulation factor X(Human)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of factor Xa (unknown origin)More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPlasma kallikrein(Human)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of human plasma kallikrein using chromogenic L-pyroGlu-L-Pro-L-Arg-p-nitroaniline as substrateMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetProthrombin(Human)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of thrombin (unknown origin) using chromogenic H-D-Ile-L-propyl-L-arginine-p-nitroaniline as substrateMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPlasminogen(Human)
University of Louisville

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of plasmin (unknown origin) using chromogenic H-D-Ile-L-propyl-L-arginine-p-nitroaniline as substrateMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTissue-type plasminogen activator(Human)
University of Louisville

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of tissue-type plasminogen activator (unknown origin) using chromogenic H-D-Ile-L-propyl-L-arginine-p-nitroaniline as substrateMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCoagulation factor XI(Human)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of factor 11a (unknown origin) using chromogenic L-pyroGlu-L-Pro-L-Arg-p-nitroaniline as substrateMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTrypsin(Human)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of trypsin (unknown origin) using chromogenic H-D-Ile-L-propyl-L-arginine-p-nitroaniline as substrateMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of recombinant human ERG expressed in CHO cells incubated for 12 mins by whole cell voltage clamp methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 5 subunit alpha(Human)
Parion Sciences

US Patent
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of recombinant human Nav1.5alpha expressed in HEK293 cells incubated for 10 mins by voltage clamp methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetAlpha-ketoglutarate-dependent dioxygenase FTO(Human)
University College London

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 4.74E+3nMAssay Description:Inhibition of FTO (unknown origin) demethylation activity using m6A7-Broccoli RNA as substrate incubated for 3 mins under shaking condition and measu...More data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetSerine/threonine-protein kinase D1(Human)
University of Pittsburgh

Curated by PubChem BioAssay
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 6.88E+3nMpH: 7.2 T: 2°CAssay Description:The PKD HTS assay was developed and run at the University of Pittsburgh Molecular Screening Center (PMLSC) as part of the Molecular Library Screening...More data for this Ligand-Target Pair
In DepthDetails
PCBioAssay
TargetSerine/threonine-protein kinase PLK1(Human)
University of Pittsburgh

Curated by PubChem BioAssay
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataIC50: 6.63E+3nMAssay Description:The PKD HTS assay was developed and run at the University of Pittsburgh Molecular Screening Center (PMLSC) as part of the Molecular Library Screening...More data for this Ligand-Target Pair
In DepthDetails
PCBioAssay
TargetAdenosine receptor A1(Bovine)
Center For Bio-Pharmaceutical Sciences

Curated by PDSP Ki Database
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi:  2.00E+3nMMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetUrokinase-type plasminogen activator(Mouse)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi:  2.31E+3nMAssay Description:Inhibition of mouse uPA using Z-Gly-Gly-Arg-AMC as substrate after 15 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetUrokinase-type plasminogen activator(Human)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi:  2.43E+3nMAssay Description:Inhibition of human kidney uPA using Z-Gly-Gly-Arg-AMC as substrate measured over 15 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetUrokinase-type plasminogen activator(Human)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi:  2.51E+3nMAssay Description:Inhibition of urokinaseMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetAdenosine receptor A2a(Human)
Niddk

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi:  3.28E+3nMAssay Description:Binding affinity for HA-tagged mutant human Adenosine A2A receptor (H250N) using [3H]-CGS-21,680 as radioligand expressed in COS-7 cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSolute carrier family 22 member 2(Rat)
Kyoto University Hospital

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi:  4.70E+3nMAssay Description:TP_TRANSPORTER: inhibition of TEA uptake in OCT2-expressing MDCK cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetUrokinase-type plasminogen activator(Human)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi:  5.30E+3nM ΔG°:  -7.19kcal/molepH: 8.0 T: 2°CAssay Description:The measurements were carried out on a microplate reader. Two concentrations of the substrate and five concentrations of the inhibitor were used in t...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetSolute carrier family 22 member 1(Rat)
Kyoto University Hospital

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi:  6.90E+3nMAssay Description:TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing MDCK cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetUrokinase-type plasminogen activator(Human)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi:  7.00E+3nMAssay Description:Inhibition of uPA (unknown origin) using L-pyroglutamyl-glycyl-L-arginine-p-nitroanilide as substrate by Lineweaver-Burk plot analysisMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetUrokinase-type plasminogen activator(Human)
University of Wollongong

Curated by ChEMBL
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi:  7.00E+3nMAssay Description:Inhibition of uPA (unknown origin) using L-pyroglutamyl-glycyl-L-arginine-p-nitro-anilide as susbtrate by Lineweaver-Burk plot analysisMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetVoltage-dependent calcium channel gamma-1 subunit(Human)
Center For Bio-Pharmaceutical Sciences

Curated by PDSP Ki Database
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCysteinyl leukotriene receptor 1(Guinea pig)
Center For Bio-Pharmaceutical Sciences

Curated by PDSP Ki Database
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBeta-1 adrenergic receptor(Rat)
Center For Bio-Pharmaceutical Sciences

Curated by PDSP Ki Database
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetAlpha-2C adrenergic receptor(Rat)
Center For Bio-Pharmaceutical Sciences

Curated by PDSP Ki Database
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetAlpha-1A adrenergic receptor(Rat)
Center For Bio-Pharmaceutical Sciences

Curated by PDSP Ki Database
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetAdenosine receptor A2a(Rat)
Center For Bio-Pharmaceutical Sciences

Curated by PDSP Ki Database
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetAdenosine receptor A1(Rat)
Center For Bio-Pharmaceutical Sciences

Curated by PDSP Ki Database
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 3A(Mouse)
Center For Bio-Pharmaceutical Sciences

Curated by PDSP Ki Database
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2C(Pig)
Center For Bio-Pharmaceutical Sciences

Curated by PDSP Ki Database
LigandPNGBDBM16173(3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-car...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
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