Compile Data Set for Download or QSAR
Report error Found 34 Enz. Inhib. hit(s) with all data for entry = 248
TargetSerine/threonine-protein kinase MARK2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247036((1R,3aR, 6S,7R,7aS)- 5,5-difluoro- 7-((E)-2-(5- (3...)
Affinity DataIC50: 1.37nMAssay Description:This assay measures the potency of the inventive compounds as PAR-1 receptor antagonists.Frozen HEK 293 Cells were plated in 384-well PDL coated plat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetSerine/threonine-protein kinase MARK2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247038(2-((1R,3aR, 6S,7R,7aS)-5,5- difluoro-7- ((E)-2-(5-...)
Affinity DataIC50: 2.62nMAssay Description:This assay measures the potency of the inventive compounds as PAR-1 receptor antagonists.Frozen HEK 293 Cells were plated in 384-well PDL coated plat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetSerine/threonine-protein kinase MARK2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247035((1R,3aR,6S,7R, 7aS)-5,5-difluoro- 7-((E)-2-(5- (2-...)
Affinity DataIC50: 3.80nMAssay Description:This assay measures the potency of the inventive compounds as PAR-1 receptor antagonists.Frozen HEK 293 Cells were plated in 384-well PDL coated plat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetSerine/threonine-protein kinase MARK2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247039(US9701669, 8 | 2-((1R,3aR, 6S,7R,7aS)-7- ((E)-2-(5...)
Affinity DataIC50: 4.07nMAssay Description:This assay measures the potency of the inventive compounds as PAR-1 receptor antagonists.Frozen HEK 293 Cells were plated in 384-well PDL coated plat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetSerine/threonine-protein kinase MARK2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247047((S and R)-2- ((1R,3aR,6S, 7R,7aS)-7- ((E)-2-(5-(2-...)
Affinity DataIC50: 4.41nMAssay Description:This assay measures the potency of the inventive compounds as PAR-1 receptor antagonists.Frozen HEK 293 Cells were plated in 384-well PDL coated plat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetSerine/threonine-protein kinase MARK2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247039(US9701669, 8 | 2-((1R,3aR, 6S,7R,7aS)-7- ((E)-2-(5...)
Affinity DataIC50: 4.43nMAssay Description:This assay measures the potency of the inventive compounds as PAR-1 receptor antagonists.Frozen HEK 293 Cells were plated in 384-well PDL coated plat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetSerine/threonine-protein kinase MARK2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247044(3-((1R,3aR,6S, 7R,7aS)-7 -((E)- 2- (2'-cyano-[...)
Affinity DataIC50: 6.34nMAssay Description:This assay measures the potency of the inventive compounds as PAR-1 receptor antagonists.Frozen HEK 293 Cells were plated in 384-well PDL coated plat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetSerine/threonine-protein kinase MARK2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247037((1R,3aR,6S,7R, 7aS)-7-((E)-2-(5- (2-cyanophenyl)- ...)
Affinity DataIC50: 6.92nMAssay Description:This assay measures the potency of the inventive compounds as PAR-1 receptor antagonists.Frozen HEK 293 Cells were plated in 384-well PDL coated plat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetSerine/threonine-protein kinase MARK2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247042(1R,3aR,6S, 7R,7aS)-7-((E)-2- (2'-cyano-[3,3...)
Affinity DataIC50: 9.68nMAssay Description:This assay measures the potency of the inventive compounds as PAR-1 receptor antagonists.Frozen HEK 293 Cells were plated in 384-well PDL coated plat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetSerine/threonine-protein kinase MARK2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247039(US9701669, 8 | 2-((1R,3aR, 6S,7R,7aS)-7- ((E)-2-(5...)
Affinity DataIC50: 11.3nMAssay Description:This assay measures the potency of the inventive compounds as PAR-1 receptor antagonists.Frozen HEK 293 Cells were plated in 384-well PDL coated plat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetSerine/threonine-protein kinase MARK2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247043(1-((1R,3aS,6S, 7R,7aS)-5,5- difluoro-7- ((E)-2-(5-...)
Affinity DataIC50: 13.9nMAssay Description:This assay measures the potency of the inventive compounds as PAR-1 receptor antagonists.Frozen HEK 293 Cells were plated in 384-well PDL coated plat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetSerine/threonine-protein kinase MARK2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247046(2-((1R,3aR,6S, 7R,7aS)-7-((E)- 2- (2'-cyano-[3...)
Affinity DataIC50: 21.2nMAssay Description:This assay measures the potency of the inventive compounds as PAR-1 receptor antagonists.Frozen HEK 293 Cells were plated in 384-well PDL coated plat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetSerine/threonine-protein kinase MARK2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247045(2-((1R,3aR,6S, 7R,7aS)-5,5- difluoro-7- ((E)-2-(2&...)
Affinity DataIC50: 104nMAssay Description:This assay measures the potency of the inventive compounds as PAR-1 receptor antagonists.Frozen HEK 293 Cells were plated in 384-well PDL coated plat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247043(1-((1R,3aS,6S, 7R,7aS)-5,5- difluoro-7- ((E)-2-(5-...)
Affinity DataIC50: 3.00E+3nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247036((1R,3aR, 6S,7R,7aS)- 5,5-difluoro- 7-((E)-2-(5- (3...)
Affinity DataIC50: 1.20E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247035((1R,3aR,6S,7R, 7aS)-5,5-difluoro- 7-((E)-2-(5- (2-...)
Affinity DataIC50: 1.30E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247052(US9701669, 14)
Affinity DataIC50: 1.44E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247050(US9701669, 10)
Affinity DataIC50: 1.54E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247051(US9701669, 12)
Affinity DataIC50: 1.63E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247038(2-((1R,3aR, 6S,7R,7aS)-5,5- difluoro-7- ((E)-2-(5-...)
Affinity DataIC50: 2.04E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247046(2-((1R,3aR,6S, 7R,7aS)-7-((E)- 2- (2'-cyano-[3...)
Affinity DataIC50: 2.19E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247055(US9701669, 21)
Affinity DataIC50: 2.34E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247045(2-((1R,3aR,6S, 7R,7aS)-5,5- difluoro-7- ((E)-2-(2&...)
Affinity DataIC50: 2.59E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247039(US9701669, 8 | 2-((1R,3aR, 6S,7R,7aS)-7- ((E)-2-(5...)
Affinity DataIC50: 2.63E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247039(US9701669, 8 | 2-((1R,3aR, 6S,7R,7aS)-7- ((E)-2-(5...)
Affinity DataIC50: 3.91E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247048(US9701669, 1)
Affinity DataIC50: 4.39E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247053(US9701669, 18)
Affinity DataIC50: 4.68E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247054(US9701669, 19)
Affinity DataIC50: 4.77E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247039(US9701669, 8 | 2-((1R,3aR, 6S,7R,7aS)-7- ((E)-2-(5...)
Affinity DataIC50: 5.97E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247044(3-((1R,3aR,6S, 7R,7aS)-7 -((E)- 2- (2'-cyano-[...)
Affinity DataIC50: 6.00E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247042(1R,3aR,6S, 7R,7aS)-7-((E)-2- (2'-cyano-[3,3...)
Affinity DataIC50: 6.00E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247049(US9701669, 5)
Affinity DataIC50: 6.00E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247037((1R,3aR,6S,7R, 7aS)-7-((E)-2-(5- (2-cyanophenyl)- ...)
Affinity DataIC50: 6.00E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Sharp & Dohme

US Patent
LigandPNGBDBM247047((S and R)-2- ((1R,3aR,6S, 7R,7aS)-7- ((E)-2-(5-(2-...)
Affinity DataIC50: 6.00E+4nMpH: 7.4 T: 2°CAssay Description:Drug cardiac arrhythmia is an important safety concern for pharmaceutical development and health regulatory authorities. Blockade of heterologously-e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
US Patent