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TargetDihydrofolate reductase(Mouse)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50043393(2-({4-[(2,4-Diamino-pyrido[2,3-d]pyrimidin-6-ylmet...)
Affinity DataKi:  0.00365nMAssay Description:Inhibitory activity of Dihydrofolate reductase in L1210 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDihydrofolate reductase(Mouse)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50043396(2-({4-[(2,4-Diamino-pteridin-6-ylmethyl)-amino]-na...)
Affinity DataKi:  0.00455nMAssay Description:Inhibitory activity of Dihydrofolate reductase in L1210 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDihydrofolate reductase(Mouse)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50043399(2-({4-[(2,4-Diamino-pyrido[2,3-d]pyrimidin-6-ylmet...)
Affinity DataKi:  0.00465nMAssay Description:Inhibitory activity of Dihydrofolate reductase in L1210 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDihydrofolate reductase(Mouse)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM18050(2-[(4-{[(2,4-diaminopteridin-6-yl)methyl](methyl)a...)
Affinity DataKi:  0.00480nMAssay Description:Compound was evaluated in vitro for the inhibition of dihydrofolate reductase (DHFR) in L1210 cellsMore data for this Ligand-Target Pair
TargetDihydrofolate reductase(Mouse)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM18050(2-[(4-{[(2,4-diaminopteridin-6-yl)methyl](methyl)a...)
Affinity DataKi:  0.00482nMAssay Description:Inhibitory activity of Dihydrofolate reductase in L1210 cellsMore data for this Ligand-Target Pair
TargetDihydrofolate reductase(Mouse)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50043395(2-({4-[(2,4-Diamino-5-methyl-pyrido[2,3-d]pyrimidi...)
Affinity DataKi:  0.00484nMAssay Description:Inhibitory activity of Dihydrofolate reductase in L1210 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDihydrofolate reductase(Mouse)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50043400(2-({4-[(2,4-Diamino-5-methyl-pyrido[2,3-d]pyrimidi...)
Affinity DataKi:  0.00508nMAssay Description:Inhibitory activity of Dihydrofolate reductase in L1210 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDihydrofolate reductase(Mouse)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50043398(2-({4-[(2,4-Diamino-quinazolin-6-ylmethyl)-amino]-...)
Affinity DataKi:  0.00520nMAssay Description:Inhibitory activity of Dihydrofolate reductase in L1210 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDihydrofolate reductase(Mouse)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50043394(2-({4-[(2,4-Diamino-pteridin-6-ylmethyl)-methyl-am...)
Affinity DataKi:  0.00522nMAssay Description:Inhibitory activity of Dihydrofolate reductase in L1210 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029704(2-(4-Benzyl-5-oxo-2,5-dihydro-furan-3-yloxymethyl)...)
Affinity DataKi:  0.0130nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDihydrofolate reductase(Mouse)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50043397(2-({4-[(2,4-Diamino-pyrido[2,3-d]pyrimidin-6-ylmet...)
Affinity DataKi:  0.0131nMAssay Description:Inhibitory activity of Dihydrofolate reductase in L1210 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029709(2-(4-Benzyl-2-methyl-5-oxo-2,5-dihydro-furan-3-ylo...)
Affinity DataKi:  0.0160nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCoagulation factor VII(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM189451(US9174974, Example 39)
Affinity DataKi:  0.0200nMAssay Description:FVIIa-Xase Ki (37° C.): S2765 (0.5 mM), PCPS (25 μM), calcium chloride (5 mM), full-length human TF (3 nM), human FVIIa (5 pM), and FVIIa inhibi...More data for this Ligand-Target Pair
In DepthDetails US Patent

TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029710(4-Isopropyl-6-methoxy-2-(2-methyl-5-oxo-4-phenyl-2...)
Affinity DataKi:  0.0210nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029699(2,6-Dichloro-benzoic acid 4-isopropyl-6-methoxy-1,...)
Affinity DataKi:  0.0230nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029698(4-Isopropyl-6-methoxy-1,1-dioxo-2-(5-oxo-4-phenyl-...)
Affinity DataKi:  0.0250nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029717(2-(3-Chloro-6-methyl-2-oxo-2H-pyran-4-yloxymethyl)...)
Affinity DataKi:  0.0250nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029696(2-(3-Benzoyl-6-methyl-2-oxo-2H-pyran-4-yloxymethyl...)
Affinity DataKi:  0.0270nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029712(2-(4-Chloro-5-oxo-2,5-dihydro-furan-3-yloxymethyl)...)
Affinity DataKi:  0.0300nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029713(4-Isopropyl-6-methoxy-1,1-dioxo-2-(3-oxo-cyclobut-...)
Affinity DataKi:  0.0330nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029691(2-(2-Benzyl-3-oxo-cyclopent-1-enyloxymethyl)-4-iso...)
Affinity DataKi:  0.0340nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLethal factor(Bacillus anthracis)
Panthera Biopharma

Curated by ChEMBL
LigandPNGBDBM50379543(CHEMBL2012752)
Affinity DataKi:  0.0400nMAssay Description:Inhibition of N-terminal 6-histine tagged Bacillus anthracis LF 263-C terminal catalytic domain using MCA-KKVYPYPME-Dap(Dnp)-NH2 as substrate after 4...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50545960(CHEMBL4740778 | US11649241, Example 9)
Affinity DataKi:  0.0420nMAssay Description:Inhibition of recombinant human JAK2 (812 to 1132 residues) expressed in insect cells using Y1-B as substrate incubated for 30 mins by microfluidic m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50545980(CHEMBL4764019)
Affinity DataKi:  0.0450nMAssay Description:Inhibition of recombinant human JAK2 (812 to 1132 residues) expressed in insect cells using Y1-B as substrate incubated for 30 mins by microfluidic m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50545979(CHEMBL4742159)
Affinity DataKi:  0.0470nMAssay Description:Inhibition of recombinant human JAK2 (812 to 1132 residues) expressed in insect cells using Y1-B as substrate incubated for 30 mins by microfluidic m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCoagulation factor VII(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM189454(US9174974, Example 38)
Affinity DataKi:  0.0500nMAssay Description:FVIIa-Xase Ki (37° C.): S2765 (0.5 mM), PCPS (25 μM), calcium chloride (5 mM), full-length human TF (3 nM), human FVIIa (5 pM), and FVIIa inhibi...More data for this Ligand-Target Pair
In DepthDetails US Patent

TargetLethal factor(Bacillus anthracis)
Panthera Biopharma

Curated by ChEMBL
LigandPNGBDBM50329261((R)-2-(4-fluoro-3,5-dimethylphenylamino)-6-(4-fluo...)
Affinity DataKi:  0.0500nMAssay Description:Inhibition of Bacillus anthracis lethal factor assessed as proteolysis using MCA-KKVYPYPME-Dap(Dnp)-NH2 peptide substrate after 4 hrs by FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLethal factor(Bacillus anthracis)
Panthera Biopharma

Curated by ChEMBL
LigandPNGBDBM50329261((R)-2-(4-fluoro-3,5-dimethylphenylamino)-6-(4-fluo...)
Affinity DataKi:  0.0500nMAssay Description:Inhibition of Bacillus anthracis lethal factor assessed as proteolysis using MCA-KKVYPYPME-Dap(Dnp)-NH2 peptide substrate by FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029692(4-Isopropyl-6-methoxy-2-(6-methyl-2-oxo-2H-pyran-4...)
Affinity DataKi:  0.0500nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50545987(CHEMBL4746726)
Affinity DataKi:  0.0520nMAssay Description:Inhibition of recombinant human JAK2 (812 to 1132 residues) expressed in insect cells using Y1-B as substrate incubated for 30 mins by microfluidic m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029695(4-Isopropyl-6-methoxy-1,1-dioxo-2-(5-oxo-2,5-dihyd...)
Affinity DataKi:  0.0520nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50545986(CHEMBL4789075)
Affinity DataKi:  0.0570nMAssay Description:Inhibition of recombinant human JAK2 (812 to 1132 residues) expressed in insect cells using Y1-B as substrate incubated for 30 mins by microfluidic m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029711(3-Bromo-2-(4-isopropyl-6-methoxy-1,1,3-trioxo-1,3-...)
Affinity DataKi:  0.0580nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029720(4-Isopropyl-6-methoxy-2-(2-methyl-3-oxo-cyclopent-...)
Affinity DataKi:  0.0600nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029707(3-Chloro-2-(4-isopropyl-6-methoxy-1,1,3-trioxo-1,3...)
Affinity DataKi:  0.0660nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50545961(CHEMBL4793262)
Affinity DataKi:  0.0710nMAssay Description:Inhibition of recombinant human JAK2 (812 to 1132 residues) expressed in insect cells using Y1-B as substrate incubated for 30 mins by microfluidic m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50545944(CHEMBL4744172)
Affinity DataKi:  0.0710nMAssay Description:Inhibition of recombinant human JAK2 (812 to 1132 residues) expressed in insect cells using Y1-B as substrate incubated for 30 mins by microfluidic m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetApelin receptor(Human)
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50567169(CHEMBL4873876)
Affinity DataKi:  0.0740nMAssay Description:Displacement of [3H]Apelin-13 from human APJ receptor stably expressed in human HEK293 cell membrane incubated for 120 mins by TopCount scintillation...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50545987(CHEMBL4746726)
Affinity DataKi:  0.0750nMAssay Description:Inhibition of recombinant human JAK1 (854 to 1154 residues) expressed in insect cells using Y1-B as substrate incubated for 30 mins by microfluidic m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029721(2-(4-Isopropyl-6-methoxy-1,1,3-trioxo-1,3-dihydro-...)
Affinity DataKi:  0.0780nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50545964(CHEMBL4746416)
Affinity DataKi:  0.0780nMAssay Description:Inhibition of recombinant human JAK2 (812 to 1132 residues) expressed in insect cells using Y1-B as substrate incubated for 30 mins by microfluidic m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029715(4-Isopropyl-6-methoxy-1,1-dioxo-2-(3-oxo-3H-inden-...)
Affinity DataKi:  0.0830nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50545965(CHEMBL4788860 | US11649241, Example 7)
Affinity DataKi:  0.0850nMAssay Description:Inhibition of recombinant human JAK2 (812 to 1132 residues) expressed in insect cells using Y1-B as substrate incubated for 30 mins by microfluidic m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50545945(CHEMBL4777342)
Affinity DataKi:  0.0880nMAssay Description:Inhibition of recombinant human JAK2 (812 to 1132 residues) expressed in insect cells using Y1-B as substrate incubated for 30 mins by microfluidic m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029718(4-Isopropyl-6-methoxy-1,1-dioxo-2-(2-oxo-2H-chrome...)
Affinity DataKi:  0.0900nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Human)
Sterling Winthrop Pharmaceuticals Research Division

Curated by ChEMBL
LigandPNGBDBM50029700(4-Isopropyl-6-methoxy-2-(2-methyl-5-oxo-2,5-dihydr...)
Affinity DataKi:  0.0930nMAssay Description:Potency of inhibition of human leukocyte elastase is expressed as apparent binding constantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ITK/TSK(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50015266(CHEMBL3263053)
Affinity DataKi:  0.100nMAssay Description:Inhibition of GST-tagged full length ITK (unknown origin) using BLK peptide as substrate after 35 minsMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase ITK/TSK(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50015266(CHEMBL3263053)
Affinity DataKi:  0.100nMAssay Description:Inhibition of full-length ITK (unknown origin) using biotin-EQEDEPEGIYGVLF-NH2 as substrate by plate reader analysisMore data for this Ligand-Target Pair
TargetDihydrofolate reductase(Mouse)
Southern Research Institute

Curated by ChEMBL
LigandPNGBDBM50004544(2-{4-[1-(2,4-Diamino-pteridin-6-ylmethyl)-propyl]-...)
Affinity DataKi:  0.100nMAssay Description:Compound was evaluated in vitro for the inhibition of dihydrofolate reductase (DHFR) in L1210 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50545963(CHEMBL4760406 | US11649241, Example 13)
Affinity DataKi:  0.100nMAssay Description:Inhibition of recombinant human JAK2 (812 to 1132 residues) expressed in insect cells using Y1-B as substrate incubated for 30 mins by microfluidic m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
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