Affinity DataKi: 1.72E+4nMAssay Description:Binding affinity to BRD2 BD1 (unknown origin) by fluorescence anisotropy competition binding assayMore data for this Ligand-Target Pair
Affinity DataKi: 1.72E+4nMAssay Description:Binding affinity to BRD4 BD1 (unknown origin) by fluorescence anisotropy competition binding assayMore data for this Ligand-Target Pair
Affinity DataKi: 1.72E+4nMAssay Description:Binding affinity to BRD3 BD1 (unknown origin) by fluorescence anisotropy competition binding assayMore data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 1nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 5nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 5nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 5nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 5nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 6nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 7nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 7nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD4 BD1 (1 to 477 residues)/BD2 Y390A mutant expressed in Escher...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD3 BD1 (1 to 435 residues)/BD2 Y348A mutant expressed in Escher...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Displacement of Alexa Fluor 647 labelled ligand from recombinant human N-terminal His6-tagged BRD4 BD1 (1 to 477 residues)/BD2 Y390A mutant incubated...More data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 12nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 13nMAssay Description:Displacement of Alexa Fluor 647 labelled ligand from recombinant human N-terminal His6-tagged BRD4 BD1 (1 to 477 residues)/BD2 Y390A mutant incubated...More data for this Ligand-Target Pair
Affinity DataIC50: 13nMAssay Description:Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD2 BD1 (1 to 473 residues)/BD2 Y386A mutant expressed in Escher...More data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 15nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 16nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 16nMAssay Description:Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD3 BD2 (1 to 435 residues)/BD1 Y73A mutant expressed in Escheri...More data for this Ligand-Target Pair
Affinity DataIC50: 20nMAssay Description:Inhibition of BRD4 BD2 (unknown origin) incubated for 30 mins in presence of fluorescent ligand by TR-FRET methodMore data for this Ligand-Target Pair
Affinity DataIC50: 20nMAssay Description:Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FL...More data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 21nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 23nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 25nMAssay Description:Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FL...More data for this Ligand-Target Pair
Affinity DataIC50: 25nMAssay Description:Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRDT BD1 (1 to 397 residues)/BD2 Y309A mutant expressed in Escher...More data for this Ligand-Target Pair
Affinity DataIC50: 25nMAssay Description:Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD4 BD1 (1 to 477 residues)/BD2 Y390A mutant expressed in Escher...More data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 29nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 31.6nMAssay Description:Displacement of Alexa Fluor 647 labelled ligand from recombinant human N-terminal His6-tagged BRD4 BD1 (1 to 477 residues)/BD2 Y390A mutant incubated...More data for this Ligand-Target Pair
Affinity DataIC50: 32nMAssay Description:Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FL...More data for this Ligand-Target Pair
Affinity DataIC50: 32nMAssay Description:Displacement of Alexa Fluor 647 labelled ligand from recombinant human N-terminal His6-tagged BRD4 BD1 (1 to 477 residues)/BD2 Y390A mutant incubated...More data for this Ligand-Target Pair
Affinity DataIC50: 32nMAssay Description:Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD3 BD1 (1 to 435 residues)/BD2 Y348A mutant expressed in Escher...More data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 34nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 39nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 40nMAssay Description:Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FL...More data for this Ligand-Target Pair
Affinity DataIC50: 40nMAssay Description:Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD4 BD1 (1 to 477 residues)/BD2 Y390A mutant expressed in Escher...More data for this Ligand-Target Pair
Affinity DataIC50: 40nMAssay Description:Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD4 BD2 (1 to 477 residues)/BD1 Y97A mutant expressed in Escheri...More data for this Ligand-Target Pair
Affinity DataIC50: 40nMAssay Description:Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD2 BD2 (1 to 473 residues)/BD1 Y113A mutant expressed in Escher...More data for this Ligand-Target Pair
Affinity DataIC50: 40nMAssay Description:Displacement of Alexa Fluor 647 labelled ligand from recombinant human N-terminal His6-tagged BRD4 BD1 (1 to 477 residues)/BD2 Y390A mutant incubated...More data for this Ligand-Target Pair
Affinity DataIC50: 40nMAssay Description:Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD3 BD1 (1 to 435 residues)/BD2 Y348A mutant expressed in Escher...More data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 41nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 50nMAssay Description:Antagonist activity at human recombinant CCR8 expressed in RBL cells assessed as inhibition of I-309-induced intracellular calcium mobilization by FL...More data for this Ligand-Target Pair
Affinity DataIC50: 50nMAssay Description:Displacement of Alexa Fluor 647 labelled ligand from recombinant human N-terminal His6-tagged BRD4 BD1 (1 to 477 residues)/BD2 Y390A mutant incubated...More data for this Ligand-Target Pair
Affinity DataIC50: 50nMAssay Description:Displacement of bromosporine-tracer from BRD4 (unknown origin) expressed in HEK293 cells by NanoBRET NanoGlo substrate based NanoBRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 50nMAssay Description:Displacement of Alexa Fluor 647 labelled ligand from recombinant human N-terminal His6-tagged BRD4 BD1 (1 to 477 residues)/BD2 Y390A mutant incubated...More data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 50nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 50nMAssay Description:Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD2 BD1 (1 to 473 residues)/BD2 Y386A mutant expressed in Escher...More data for this Ligand-Target Pair
Affinity DataIC50: 50nMAssay Description:Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD4 BD1 (1 to 477 residues)/BD2 Y390A mutant expressed in Escher...More data for this Ligand-Target Pair
TargetGamma-secretase subunit APH-1A/Gamma-secretase subunit APH-1B/Gamma-secretase subunit PEN-2/Nicastrin/Presenilin-1/Presenilin-2(Homo sapiens (Human))
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Merck Sharp & Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 62nMAssay Description:Inhibitory concentration against Gamma-secretase in whole cell inhibition assay using SH-SY5Y cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 63nMAssay Description:Inhibition of BRD4 BD2 (unknown origin) incubated for 30 mins in presence of fluorescent ligand by TR-FRET methodMore data for this Ligand-Target Pair