BDBM254160 US10112937, Example 40::US10150765, Example 40::US10703749, Example 11::US9464084, 40
SMILES C[C@H]1N(CCc2c1ncn2-c1ccc(F)cn1)C(=O)c1cccc(c1Cl)C(F)(F)F
InChI Key InChIKey=PLIXFSPGDVKMDM-LLVKDONJSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 48 hits for monomerid = 254160
Affinity DataKi: 7nMAssay Description:Displacement of [3H]-(S)-7-(2-chloro-3-(trifluoromethyl)benzyl)-6-methyl-3-(pyrazin-2-yl)-6,7-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one from re...More data for this Ligand-Target Pair
Affinity DataKi: 7nMAssay Description:Displacement of [3H]-(S)-7-(2-chloro-3-(trifluoromethyl)benzyl)-6-methyl-3-(pyrazin-2-yl)-6,7-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one from re...More data for this Ligand-Target Pair
Affinity DataKi: 7.10nMAssay Description:human or rat P2X7-1321 N1 cells were collected and frozen @−80° C. On the day of the experiment, cell membrane preparations were made according...More data for this Ligand-Target Pair
Affinity DataKi: 7.10nMAssay Description:Human or rat P2X7-1321 N1 cells were collected and frozen @−80° C. On the day of the experiment, cell membrane preparations were made according...More data for this Ligand-Target Pair
Affinity DataKi: 7.10nMAssay Description:Human or rat P2X7-1321N1 cells were collected and frozen @ −80° C. On the day of the experiment, cell membrane preparations were made according...More data for this Ligand-Target Pair
Affinity DataKi: 7.10nMAssay Description:uman or rat P2X7-1321N1 cells were collected and frozen @−80° C. On the day of the experiment, cell membrane preparations were made according t...More data for this Ligand-Target Pair
Affinity DataKi: 7.10nMAssay Description:uman or rat P2X7-1321N1 cells were collected and frozen @−80° C. On the day of the experiment, cell membrane preparations were made according t...More data for this Ligand-Target Pair
Affinity DataKi: 7.80nMAssay Description:human or rat P2X7-1321 N1 cells were collected and frozen @−80° C. On the day of the experiment, cell membrane preparations were made according...More data for this Ligand-Target Pair
Affinity DataKi: 7.80nMAssay Description:Human or rat P2X7-1321 N1 cells were collected and frozen @−80° C. On the day of the experiment, cell membrane preparations were made according...More data for this Ligand-Target Pair
Affinity DataKi: 7.80nMAssay Description:Human or rat P2X7-1321N1 cells were collected and frozen @ −80° C. On the day of the experiment, cell membrane preparations were made according...More data for this Ligand-Target Pair
Affinity DataKi: 7.80nMAssay Description:uman or rat P2X7-1321N1 cells were collected and frozen @−80° C. On the day of the experiment, cell membrane preparations were made according t...More data for this Ligand-Target Pair
Affinity DataKi: 7.80nMAssay Description:uman or rat P2X7-1321N1 cells were collected and frozen @−80° C. On the day of the experiment, cell membrane preparations were made according t...More data for this Ligand-Target Pair
Affinity DataKi: 126nMAssay Description:Human or rat P2X7-1321 N1 cells were collected and frozen @−80° C. On the day of the experiment, cell membrane preparations were made according...More data for this Ligand-Target Pair
Affinity DataKi: 126nMAssay Description:uman or rat P2X7-1321N1 cells were collected and frozen @−80° C. On the day of the experiment, cell membrane preparations were made according t...More data for this Ligand-Target Pair
Affinity DataKi: 126nMAssay Description:Human or rat P2X7-1321N1 cells were collected and frozen @ −80° C. On the day of the experiment, cell membrane preparations were made according...More data for this Ligand-Target Pair
Affinity DataKi: 126nMAssay Description:uman or rat P2X7-1321N1 cells were collected and frozen @−80° C. On the day of the experiment, cell membrane preparations were made according t...More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 15 mins by LC/MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 72nMAssay Description:Antagonist activity at recombinant mouse P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of Bz-ATP-induced Ca2+ flux preincubate...More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 15 mins by LC/MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as reduction in 4-OH-midazolam formation by LC/MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 92nMAssay Description:Antagonist activity at P2X7 receptor in LPS-stimulated human PBMC assessed as inhibition of Bz-ATP-induced IL-1beta release incubated for 30 mins aft...More data for this Ligand-Target Pair
Affinity DataIC50: 115nMAssay Description:Antagonist activity at recombinant rat P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of Bz-ATP-induced Ca2+ flux preincubated ...More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate after 15 mins by LC/MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 2.00E+3nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate after 15 mins by HPLC analysisMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP2C8 in human liver microsomes using paclitaxel as substrate after 15 mins by LC/MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 160nMAssay Description:Antagonist activity at P2X7 receptor in LPS-stimulated mouse whole blood assessed as inhibition of Bz-ATP-induced IL-1beta release incubated for 30 m...More data for this Ligand-Target Pair
Affinity DataIC50: 22.3nMpH: 7.4Assay Description:1321N1 cells expressing the recombinant human or rat P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high glucose...More data for this Ligand-Target Pair
Affinity DataIC50: 671nMpH: 7.4Assay Description:1321N1 cells expressing the recombinant human or rat P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high glucose...More data for this Ligand-Target Pair
Affinity DataIC50: 115nMpH: 7.4Assay Description:1321 N1 cells expressing the recombinant human, rat or mouse P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high glu...More data for this Ligand-Target Pair
Affinity DataIC50: 671nMAssay Description:Human or rat P2X7-1321 N1 cells were collected and frozen @−80° C. On the day of the experiment, cell membrane preparations were made according...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMpH: 7.4Assay Description:1321N1 cells expressing the recombinant human or rat P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high glucose...More data for this Ligand-Target Pair
Affinity DataIC50: 115nMpH: 7.4Assay Description:1321N1 cells expressing the recombinant human or rat P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high glucose...More data for this Ligand-Target Pair
Affinity DataIC50: 22.3nMAssay Description:1321N1 cells expressing the recombinant human, rat or mouse P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high ...More data for this Ligand-Target Pair
Affinity DataIC50: 671nMAssay Description:1321N1 cells expressing the recombinant human, rat or mouse P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high ...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMpH: 7.4Assay Description:1321 N1 cells expressing the recombinant human, rat or mouse P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high glu...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Human or rat P2X7-1321 N1 cells were collected and frozen @−80° C. On the day of the experiment, cell membrane preparations were made according...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:1321N1 cells expressing the recombinant human, rat or mouse P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high ...More data for this Ligand-Target Pair
Affinity DataIC50: 115nMAssay Description:1321N1 cells expressing the recombinant human, rat or mouse P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high ...More data for this Ligand-Target Pair
Affinity DataIC50: 115nMAssay Description:Human or rat P2X7-1321 N1 cells were collected and frozen @−80° C. On the day of the experiment, cell membrane preparations were made according...More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate after 15 mins by LC/MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 115nMpH: 7.4Assay Description:1321N1 cells expressing the recombinant human or rat P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high glucose...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMpH: 7.4Assay Description:1321N1 cells expressing the recombinant human or rat P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high glucose...More data for this Ligand-Target Pair
Affinity DataIC50: 22.3nMAssay Description:Human or rat P2X7-1321 N1 cells were collected and frozen @−80° C. On the day of the experiment, cell membrane preparations were made according...More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Antagonist activity at recombinant human P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of Bz-ATP-induced Ca2+ flux preincubate...More data for this Ligand-Target Pair
Affinity DataIC50: 2.20E+3nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as reduction in 1-OH-midazolam formation by LC/MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 592nMpH: 7.4Assay Description:1321N1 cells expressing the recombinant human or rat P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high glucose...More data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Janssen Research And Development
Curated by ChEMBL
Janssen Research And Development
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Displacement of [3H]astemizole from human ERG expressed in HEK293 cells by competitive binding assayMore data for this Ligand-Target Pair
Affinity DataIC50: 14.2nMpH: 7.4Assay Description:1321N1 cells expressing the recombinant human or rat P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high glucose...More data for this Ligand-Target Pair