Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)
Found 106 hits in this display
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Protease(Human immunodeficiency virus 1 (HIV-1))Dainippon Sumitomo Pharma
Curated by ChEMBL
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 0.150nM ΔG°: -58.3kJ/molepH: 4.7 T: 2°CAssay Description:The inhibition constant, Ki was determined by monitoring the competitive inhibition of the hydrolysis of the chromogenic substrate.More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 0.230nM ΔG°: -57.2kJ/molepH: 4.7 T: 2°CAssay Description:The inhibition constant, Ki was determined by monitoring the competitive inhibition of the hydrolysis of the chromogenic substrate.More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 0.5nM ΔG°: -55.2kJ/molepH: 4.7 T: 2°CAssay Description:The inhibition constant, Ki was determined by monitoring the competitive inhibition of the hydrolysis of the chromogenic substrate.More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 0.700nM ΔG°: -54.4kJ/molepH: 4.7 T: 2°CAssay Description:The inhibition constant, Ki was determined by monitoring the competitive inhibition of the hydrolysis of the chromogenic substrate.More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 0.700nM ΔG°: -54.4kJ/molepH: 4.7 T: 2°CAssay Description:The inhibition constants Ki were determined by monitoring the inhibition of hydrolysis of the chromogenic substrate using a Hewlett-Packard 8452A spe...More data for this Ligand-Target Pair
Protease(Human immunodeficiency virus 1 (HIV-1))Dainippon Sumitomo Pharma
Curated by ChEMBL
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 0.910nM ΔG°: -51.6kJ/molepH: 5.0 T: 2°CAssay Description:Protease activity was determined by following the increase in fluorescence with hydrolysis of the fluorogenic substrate Arg-Glu(EDANS)-Ser-Gln-Asn-Ty...More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 1.10nM ΔG°: -53.2kJ/molepH: 4.7 T: 2°CAssay Description:The inhibition constant, Ki was determined by monitoring the competitive inhibition of the hydrolysis of the chromogenic substrate.More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 2.40nM ΔG°: -51.2kJ/molepH: 4.7 T: 2°CAssay Description:The inhibition constant, Ki was determined by monitoring the competitive inhibition of the hydrolysis of the chromogenic substrate.More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 2.81nMAssay Description:HIV-1 protease inhibitor activities were determined by the fluorescence resonance energy transfer (FRET) method. The energy transfer donor (EDANS) an...More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 3.02nMAssay Description:HIV-1 protease inhibitor activities were determined by the fluorescence resonance energy transfer (FRET) method. The energy transfer donor (EDANS) an...More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 3.10nMAssay Description:The inhibition constants Ki were determined by monitoring the inhibition of hydrolysis of the chromogenic substrate using a Hewlett-Packard 8452A spe...More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 4nM ΔG°: -49.9kJ/molepH: 4.7 T: 2°CAssay Description:The inhibition constants Ki were determined by monitoring the inhibition of hydrolysis of the chromogenic substrate using a Hewlett-Packard 8452A spe...More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 4.5nM ΔG°: -49.6kJ/molepH: 4.7 T: 2°CAssay Description:The inhibition constant, Ki was determined by monitoring the competitive inhibition of the hydrolysis of the chromogenic substrate.More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 13nM ΔG°: -46.8kJ/molepH: 4.7 T: 2°CAssay Description:The inhibition constant, Ki was determined by monitoring the competitive inhibition of the hydrolysis of the chromogenic substrate.More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 30nM ΔG°: -44.7kJ/molepH: 4.7 T: 2°CAssay Description:The inhibition constants Ki were determined by monitoring the inhibition of hydrolysis of the chromogenic substrate using a Hewlett-Packard 8452A spe...More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 32nMAssay Description:The inhibition constants Ki were determined by monitoring the inhibition of hydrolysis of the chromogenic substrate using a Hewlett-Packard 8452A spe...More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 65nM ΔG°: -42.7kJ/molepH: 4.7 T: 2°CAssay Description:The inhibition constants Ki were determined by monitoring the inhibition of hydrolysis of the chromogenic substrate using a Hewlett-Packard 8452A spe...More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 109nM ΔG°: -41.3kJ/molepH: 4.7 T: 2°CAssay Description:The inhibition constants Ki were determined by monitoring the inhibition of hydrolysis of the chromogenic substrate using a Hewlett-Packard 8452A spe...More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Dimer of Gag-Pol polyprotein [489-587,Q496K,L499I,M525I,S526D,M535I,R546K,L552P,A560V,G562S,L579M,I582L](Human immunodeficiency virus type 1)The Johns Hopkins University
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 340nM ΔG°: -36.9kJ/molepH: 5.0 T: 2°CAssay Description:Protease activity was determined by following the increase in fluorescence with hydrolysis of the fluorogenic substrate Arg-Glu(EDANS)-Ser-Gln-Asn-Ty...More data for this Ligand-Target Pair
Dimer of Gag-Pol polyprotein [489-587,K509R,V521I,L522F,M525I,M535I,L552P,A560V,V571A,I573V,L579M](Human immunodeficiency virus type 1)University of Florida College of Medicine
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 345nMAssay Description:The inhibition constants Ki were determined by monitoring the inhibition of hydrolysis of the chromogenic substrate using a Hewlett-Packard 8452A spe...More data for this Ligand-Target Pair
Dimer of Gag-Pol polyprotein [489-587,K509R,V521I,L522F,M525I,M535I,I543V,L552P,A560V,V571A,I573V,L579M](Human immunodeficiency virus type 1)University of Florida College of Medicine
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 624nMAssay Description:The inhibition constants Ki were determined by monitoring the inhibition of hydrolysis of the chromogenic substrate using a Hewlett-Packard 8452A spe...More data for this Ligand-Target Pair
Dimer of Gag-Pol polyprotein [489-587,K509R,V521I,L522F,M525I,I543V,L552P,A560V,V571A,I573V,L579M](Human immunodeficiency virus type 1)University of Florida College of Medicine
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 932nMAssay Description:The inhibition constants Ki were determined by monitoring the inhibition of hydrolysis of the chromogenic substrate using a Hewlett-Packard 8452A spe...More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 1.30E+3nMAssay Description:Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation countingMore data for this Ligand-Target Pair
Dimer of Gag-Pol polyprotein [489-587,Q496K,L499I,M525I,S526D,M535I,R546K,L552P,A560V,G562S,I573V,L579M,I582L](Human immunodeficiency virus type 1)The Johns Hopkins University
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Ki: 2.11E+3nM ΔG°: -32.4kJ/molepH: 5.0 T: 2°CAssay Description:Protease activity was determined by following the increase in fluorescence with hydrolysis of the fluorogenic substrate Arg-Glu(EDANS)-Ser-Gln-Asn-Ty...More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
IC50: 80nMAssay Description:Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysisMore data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
IC50: 1.30E+3nMAssay Description:Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation countingMore data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
IC50: 1.70E+3nMAssay Description:Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS methodMore data for this Ligand-Target Pair
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
IC50: 2.10E+3nMAssay Description:Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysisMore data for this Ligand-Target Pair
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
IC50: 3.00E+3nMAssay Description:Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS methodMore data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
IC50: 4.40E+3nMAssay Description:Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillatio...More data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
IC50: 4.40E+3nMAssay Description:Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assayMore data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
IC50: 6.10E+3nMAssay Description:Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation coun...More data for this Ligand-Target Pair
Protease(Human immunodeficiency virus 1 (HIV-1))Dainippon Sumitomo Pharma
Curated by ChEMBL
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
IC50: 1.20E+4nMAssay Description:Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assayMore data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
IC50: >5.00E+4nMAssay Description:Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assayMore data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
IC50: >5.00E+4nMAssay Description:Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assayMore data for this Ligand-Target Pair
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
EC50: 4.00E+3nMAssay Description:Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysisMore data for this Ligand-Target Pair
BDBM520(1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[...)
Protease(Human immunodeficiency virus 1 (HIV-1))Dainippon Sumitomo Pharma
Curated by ChEMBL
BDBM50088504(A-84538 | ABBOTT-84538 | CHEBI:45409 | Norvir | Ri...)
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