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Found 3740 with Last Name = 'luo' and Initial = 'c'
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
University of Pennsylvania

LigandPNGBDBM25391(CHEMBL200622 | SB-590885 | SB590885 | [2-(4-{4-[(1...)
Affinity DataKi:  0.160nM ΔG°:  -58.2kJ/molepH: 7.0 T: 2°CAssay Description:BRAF kinase activity was quantified using an ELISA-based MEK phosphorylation assay. IC50 values were derived from the sigmoidal dose-response curve f...More data for this Ligand-Target Pair
TargetCoagulation factor X(Homo sapiens (Human))
Axys Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50101871(3-[3-(3-Benzyl-5-carbamimidoyl-1H-indol-2-yl)-5-br...)
Affinity DataKi:  0.5nMAssay Description:Inhibitory activity against Coagulation factor X in human plasmaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCoagulation factor X(Homo sapiens (Human))
Axys Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50101882(CHEMBL53829 | Phosphoric acid mono-{2-[3-(3-benzyl...)
Affinity DataKi:  0.5nMAssay Description:Inhibitory activity against Coagulation factor X in human plasmaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCoagulation factor X(Homo sapiens (Human))
Axys Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50101881(4-[3-(3-Benzyl-5-carbamimidoyl-1H-indol-2-yl)-5-br...)
Affinity DataKi:  0.700nMAssay Description:Inhibitory activity against Coagulation factor X in human plasmaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetWD repeat-containing protein 5(Homo sapiens (Human))
Zhejiang Sci-Tech University

Curated by ChEMBL
LigandPNGBDBM200723(US9233086, 10L)
Affinity DataKi: <1nMAssay Description:Displacement of 5-FAM labelled tracer from WDR5 (unknown origin) by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCoagulation factor X(Homo sapiens (Human))
Axys Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM16127(2,2 -methanediylbis(1H-benzimidazole-6-carboximida...)
Affinity DataKi:  1nM ΔG°:  -50.9kJ/molepH: 8.2 T: 2°CAssay Description:Enzymes were incubated with inhibitors at eight inhibitor concentrations bracketing the Ki, prepared by serial dilution along with control lacking th...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetWD repeat-containing protein 5(Homo sapiens (Human))
Zhejiang Sci-Tech University

Curated by ChEMBL
LigandPNGBDBM200712(US9233086, 10A)
Affinity DataKi: <1nMAssay Description:Displacement of 5-FAM labelled tracer from WDR5 (unknown origin) by fluorescence polarization assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetWD repeat-containing protein 5(Homo sapiens (Human))
Zhejiang Sci-Tech University

Curated by ChEMBL
LigandPNGBDBM200722(US9233086, 10K)
Affinity DataKi: <1nMAssay Description:Displacement of 5-FAM labelled tracer from WDR5 (unknown origin) by fluorescence polarization assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSerine protease 1(Bos taurus (bovine))
Celera

LigandPNGBDBM14338(2-{5-[amino(iminiumyl)methyl]-1H-indol-2-yl}-4-nit...)
Affinity DataKi:  1.30nMAssay Description:Each enzyme was assayed with a set of different concentrations of each inhibitor. After addition of the appropriate substrate, the rate of hydrolysis...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM92906(CHK1 compound 1)
Affinity DataKi:  1.75nM ΔG°:  -49.5kJ/molepH: 7.4 T: 2°CAssay Description:The inhibitors reported in this study bind to CHK1 according to a general mechanism illustrated in Scheme 1 where E, S, and I stand for enzyme, subst...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCoagulation factor X(Homo sapiens (Human))
Axys Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50101883(2-[3-(3-Benzyl-5-carbamimidoyl-1H-indol-2-yl)-5-br...)
Affinity DataKi:  2nMAssay Description:Inhibitory activity against Coagulation factor X in human plasmaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCoagulation factor X(Homo sapiens (Human))
Axys Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50101885(2-[3-(3-Benzyl-5-carbamimidoyl-1H-indol-2-yl)-5-br...)
Affinity DataKi:  2nMAssay Description:Inhibitory activity against Coagulation factor X in human plasmaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Celera

LigandPNGBDBM14352(2-{5-[amino(iminiumyl)methyl]-6-chloro-1H-indol-2-...)
Affinity DataKi:  2.20nMAssay Description:Each enzyme was assayed with a set of different concentrations of each inhibitor. After addition of the appropriate substrate, the rate of hydrolysis...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Celera

LigandPNGBDBM14351(2-{5-[amino(iminiumyl)methyl]-6-chloro-1H-indol-2-...)
Affinity DataKi:  2.60nMAssay Description:Each enzyme was assayed with a set of different concentrations of each inhibitor. After addition of the appropriate substrate, the rate of hydrolysis...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCoagulation factor X(Homo sapiens (Human))
Axys Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50101880(CHEMBL416127 | [3-(3-Benzyl-5-carbamimidoyl-1H-ind...)
Affinity DataKi:  3nMAssay Description:Inhibitory activity against Coagulation factor X in human plasmaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCoagulation factor X(Homo sapiens (Human))
Axys Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50101879(CHEMBL50924 | [3-(3-Benzyl-5-carbamimidoyl-1H-indo...)
Affinity DataKi:  3nMAssay Description:Inhibitory activity against Coagulation factor X in human plasmaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 2(Homo sapiens (Human))
University Of Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50515771(CHEMBL4528047)
Affinity DataKi:  3.10nMAssay Description:Binding affinity to human recombinant BRD2 BD2 (349 to 460 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Celera

LigandPNGBDBM14354(2-{5-[amino(iminiumyl)methyl]-1H-indol-2-yl}-4-(di...)
Affinity DataKi:  3.20nMAssay Description:Each enzyme was assayed with a set of different concentrations of each inhibitor. After addition of the appropriate substrate, the rate of hydrolysis...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCoagulation factor X(Homo sapiens (Human))
Axys Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50101870(3-(3-Benzyl-5-carbamimidoyl-1H-indol-2-yl)-5-bromo...)
Affinity DataKi:  4nMAssay Description:Inhibitory activity against Coagulation factor X in human plasmaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTryptase beta-2(Homo sapiens (Human))
Arris

LigandPNGBDBM16127(2,2 -methanediylbis(1H-benzimidazole-6-carboximida...)
Affinity DataKi:  5nM ΔG°:  -46.9kJ/molepH: 8.2 T: 2°CAssay Description:Enzymes were incubated with inhibitors at eight inhibitor concentrations bracketing the Ki, prepared by serial dilution along with control lacking th...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM92906(CHK1 compound 1)
Affinity DataKi:  5.14nM ΔG°:  -46.5kJ/molepH: 8.0 T: 2°CAssay Description:Surface plasmon resonance (SPR) biosensor binding studies were conducted using a Biacore 3000 instrument (GE Healtchare).More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSerine protease 1(Homo sapiens (Human))
Arris

LigandPNGBDBM16304(2-(1H-1,3-benzodiazol-2-ylcarbonyl)-1H-1,3-benzodi...)
Affinity DataKi:  5.20nM ΔG°:  -46.8kJ/molepH: 8.2 T: 2°CAssay Description:Enzymes were incubated with inhibitors at eight inhibitor concentrations bracketing the Ki, prepared by serial dilution along with control lacking th...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3(Homo sapiens (Human))
University Of Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50515771(CHEMBL4528047)
Affinity DataKi:  5.30nMAssay Description:Binding affinity to human recombinant BRD3 BD2 (306 to 417 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Arris

LigandPNGBDBM16303(2-(1H-1,3-benzodiazol-2-ylmethyl)-1H-1,3-benzodiaz...)
Affinity DataKi:  5.60nM ΔG°:  -46.6kJ/molepH: 8.2 T: 2°CAssay Description:Enzymes were incubated with inhibitors at eight inhibitor concentrations bracketing the Ki, prepared by serial dilution along with control lacking th...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
University Of Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50515771(CHEMBL4528047)
Affinity DataKi:  7.30nMAssay Description:Binding affinity to human recombinant BRD4 BD2 (333 to 460 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Celera

LigandPNGBDBM14142(2-{5-[amino(iminiumyl)methyl]-1H-indol-2-yl}-6-phe...)
Affinity DataKi:  8nM ΔG°:  -45.7kJ/molepH: 7.4 T: 2°CAssay Description:Each enzyme was assayed with a set of different concentrations of each inhibitor. After addition of the appropriate substrate, the rate of hydrolysis...More data for this Ligand-Target Pair
TargetProthrombin(Homo sapiens (Human))
Arris

LigandPNGBDBM13940(2-(3-HYDROXY-PYRIDIN-2-YL)-1H-BENZOIMIDAZOLE-5-CAR...)
Affinity DataKi:  8nMAssay Description:Each enzyme was assayed with a set of different concentrations of each inhibitor. After addition of the appropriate substrate, the rate of hydrolysis...More data for this Ligand-Target Pair
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Celera

LigandPNGBDBM50102780(2-(2-Hydroxy-3-phenyl-phenyl)-1H-indole-5-carboxam...)
Affinity DataKi:  8nMAssay Description:Inhibitory concentration against Human Serine Protease Urokinase Plasminogen ActivatorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Celera

LigandPNGBDBM50102780(2-(2-Hydroxy-3-phenyl-phenyl)-1H-indole-5-carboxam...)
Affinity DataKi:  8nMAssay Description:The compound was tested for inhibition of human urokinase type plasminogen activator (microPa)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Celera

LigandPNGBDBM50115874(2-(2-Hydroxy-3-phenoxy-phenyl)-1H-indole-5-carboxa...)
Affinity DataKi:  8nMAssay Description:Inhibition of urokinase-type plasminogen activatorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3(Homo sapiens (Human))
University Of Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50515795(CHEMBL4438006)
Affinity DataKi:  8.20nMAssay Description:Binding affinity to human recombinant BRD3 BD2 (306 to 417 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3(Homo sapiens (Human))
University Of Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  8.70nMAssay Description:Binding affinity to human recombinant BRD3 BD1 (24 to 144 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 2(Homo sapiens (Human))
University Of Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50515795(CHEMBL4438006)
Affinity DataKi:  8.90nMAssay Description:Binding affinity to human recombinant BRD2 BD2 (349 to 460 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Celera

LigandPNGBDBM14152(6-CHLORO-2-(2-HYDROXY-BIPHENYL-3-YL)-1H-INDOLE-5-C...)
Affinity DataKi:  9nM ΔG°:  -45.5kJ/molepH: 7.4 T: 2°CAssay Description:Each enzyme was assayed with a set of different concentrations of each inhibitor. After addition of the appropriate substrate, the rate of hydrolysis...More data for this Ligand-Target Pair
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Celera

LigandPNGBDBM50106240(6-Chloro-2-(2-hydroxy-biphenyl-3-yl)-1H-indole-5-c...)
Affinity DataKi:  9nMAssay Description:The compound was tested for inhibition of human urokinase type plasminogen activator (microPa)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 2(Homo sapiens (Human))
University Of Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50515772(CHEMBL4471776)
Affinity DataKi:  9.10nMAssay Description:Binding affinity to human recombinant BRD2 BD2 (349 to 460 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
University Of Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  9.90nMAssay Description:Binding affinity to human recombinant BRD4 BD2 (333 to 460 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetCoagulation factor X(Homo sapiens (Human))
Axys Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50101869(2-[3-(3-Benzyl-5-carbamimidoyl-1H-indol-2-yl)-5-br...)
Affinity DataKi:  10nMAssay Description:Inhibitory activity against Coagulation factor X in human plasmaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 2(Homo sapiens (Human))
University Of Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  10nMAssay Description:Binding affinity to human recombinant BRD2 BD2 (349 to 460 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCoagulation factor X(Homo sapiens (Human))
Axys Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50101867(3-Benzyl-2-[3-bromo-2-hydroxy-5-(2H-tetrazol-5-yl)...)
Affinity DataKi:  10nMAssay Description:Inhibitory activity against Coagulation factor X in human plasmaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Celera

LigandPNGBDBM14149(6-fluoro-2-(2-hydroxy-3-{[(1S,2S)-2-methylcyclohex...)
Affinity DataKi:  11nM ΔG°:  -45.0kJ/molepH: 7.4 T: 2°CAssay Description:Each enzyme was assayed with a set of different concentrations of each inhibitor. After addition of the appropriate substrate, the rate of hydrolysis...More data for this Ligand-Target Pair
TargetBeta-secretase 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM17786((4S)-4-(2-amino-6-phenoxy-3,4-dihydroquinazolin-3-...)
Affinity DataKi:  11nM ΔG°:  -45.0kJ/molepH: 5.0 T: 2°CAssay Description:BACE-1 activity was measured at pH 5 using the FS1 FRET substrate. Compounds were preincubated with recombinant BACE-1 for 20 min before adding subst...More data for this Ligand-Target Pair
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Celera

LigandPNGBDBM50115868(2-{5-[AMINO(IMINIO)METHYL]-6-FLUORO-1H-BENZIMIDAZO...)
Affinity DataKi:  11nMAssay Description:Inhibition of urokinase-type plasminogen activatorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3(Homo sapiens (Human))
University Of Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  11nMAssay Description:Binding affinity to human recombinant BRD3 BD2 (306 to 417 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3(Homo sapiens (Human))
University Of Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50515772(CHEMBL4471776)
Affinity DataKi:  11nMAssay Description:Binding affinity to human recombinant BRD3 BD2 (306 to 417 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetSerine protease 1(Bos taurus (bovine))
Celera

LigandPNGBDBM14142(2-{5-[amino(iminiumyl)methyl]-1H-indol-2-yl}-6-phe...)
Affinity DataKi:  11nM ΔG°:  -45.0kJ/molepH: 7.45 T: 2°CAssay Description:Each enzyme was assayed with a set of different concentrations of each inhibitor. After addition of the appropriate substrate, the rate of hydrolysis...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
University Of Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50515770(CHEMBL4547454)
Affinity DataKi:  12nMAssay Description:Binding affinity to human recombinant BRD4 BD2 (333 to 460 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
University Of Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  12nMAssay Description:Binding affinity to human recombinant BRD4 BD1 (44 to 168 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetCoagulation factor X(Homo sapiens (Human))
Axys Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM14338(2-{5-[amino(iminiumyl)methyl]-1H-indol-2-yl}-4-nit...)
Affinity DataKi:  13nMAssay Description:Each enzyme was assayed with a set of different concentrations of each inhibitor. After addition of the appropriate substrate, the rate of hydrolysis...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine protease 1(Bos taurus (bovine))
Celera

LigandPNGBDBM14335(2-{5-[amino(iminiumyl)methyl]-1H-indol-2-yl}-4-chl...)
Affinity DataKi:  13nMAssay Description:Each enzyme was assayed with a set of different concentrations of each inhibitor. After addition of the appropriate substrate, the rate of hydrolysis...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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