BDBM610439 1-{(R)-2-(2-Hydroxy-ethyl)-4-[2-trifluoromethyl-4-(2-trifluoromethyl-pyrimidin-5-yl)-thiazol-5-yl]-piperazin-1-yl}-2-(3-methyl-[1,2,4]triazol-1-yl)-ethanone::US10053457, Example 35
SMILES Cc1ncn(CC(=O)N2CCN(C[C@H]2CCO)c2sc(nc2-c2cnc(nc2)C(F)(F)F)C(F)(F)F)n1
InChI Key InChIKey=FDZFVXKCJKOSRC-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 25 hits for monomerid = 610439
Affinity DataIC50: 1.5nMAssay Description:Antagonist activity at mouse CXCR3 expressed in CHO-K1 cells assessed as reduction in CXCL10 induced calcium flux by FLIPR methodMore data for this Ligand-Target Pair
Affinity DataIC50: 2.20nMAssay Description:Antagonist activity at rat CXCR3 expressed in CHO-K1 cells assessed as reduction in CXCL10 induced calcium flux by FLIPR methodMore data for this Ligand-Target Pair
Affinity DataIC50: 2.80nMAssay Description:Antagonist activity at dog CXCR3 expressed in CHO-K1 cells assessed as reduction in CXCL10 induced calcium flux by FLIPR methodMore data for this Ligand-Target Pair
Affinity DataIC50: 2.90nMAssay Description:The bioactivity of compounds is tested in a fluorometric imaging plate reader (FLIPR: Molecular Devices) using engineered CHO-K1 cells expressing the...More data for this Ligand-Target Pair
Affinity DataIC50: 3.20nMAssay Description:Antagonist activity at human CXCR3 expressed in CHO-K1 cells assessed as reduction in CXCL10 induced calcium flux by FLIPR methodMore data for this Ligand-Target Pair
Affinity DataIC50: 3.30nMAssay Description:Antagonist activity at human CXCR3 expressed in CHO-K1 cells assessed as reduction in CXCL9 induced calcium flux by FLIPR methodMore data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Antagonist activity at dog CXCR3 expressed in CHO-K1 cells assessed as reduction in CXCL11 induced calcium flux by FLIPR methodMore data for this Ligand-Target Pair
Affinity DataIC50: 4.40nMAssay Description:Antagonist activity at mouse CXCR3 expressed in CHO-K1 cells assessed as reduction in CXCL11 induced calcium flux by FLIPR methodMore data for this Ligand-Target Pair
Affinity DataKd: 4.60nMAssay Description:Binding affinity to human CXCR3 expressed in CHO-K1 cell membrane assessed as dissociation constant using tritium-labeled ligand by FLIPR assayMore data for this Ligand-Target Pair
Affinity DataIC50: 5.30nMAssay Description:Antagonist activity at human CXCR3 expressed in CHO-K1 cells assessed as reduction in CXCL11 induced calcium flux by FLIPR methodMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Idorsia Pharmaceuticals
Curated by ChEMBL
Idorsia Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 8.5nMAssay Description:Inhibition of human ERG K+ currents by GLP assayMore data for this Ligand-Target Pair
Affinity DataIC50: 11nMAssay Description:Antagonist activity at human CXCR3-mediated chemotaxis expressed in CD3/CD28-activated primary human T cells assessed as inhibition of CXCLI1 mediate...More data for this Ligand-Target Pair
Affinity DataIC50: 11nMAssay Description:Antagonist activity at mouse CXCR3-mediated chemotaxis expressed in CD3/CD28-activated primary mouse T cells assessed as inhibition of CXCLI1 mediate...More data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Idorsia Pharmaceuticals
Curated by ChEMBL
Idorsia Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 26nMAssay Description:Inhibition of human ERG stably expressed in CHO cells at -80 mV holding voltage by automated QPatch electrophysiological assayMore data for this Ligand-Target Pair
Affinity DataIC50: 56nMAssay Description:Antagonist activity at CXCR3 in human whole blood assessed as receptor internalization incubated for 30 mins in presence of CXCL10 by flow cytometric...More data for this Ligand-Target Pair
Affinity DataIC50: 56nMAssay Description:Antagonist activity at CXCR3 (unknown origin) in human T cells in venous blood assessed as receptor internalization incubated for 30 mins in presence...More data for this Ligand-Target Pair
Affinity DataIC50: 102nMAssay Description:Stock solutions of test compounds are made up at a concentration of 10 mM in DMSO, and serially diluted in PBS containing 0.5% BSA to concentrations ...More data for this Ligand-Target Pair
Affinity DataIC50: 161nMAssay Description:Antagonist activity at CXCR3 in DBA/1 mouse whole blood assessed as receptor internalization incubated for 30 mins in presence of CXCL10 by flow cyto...More data for this Ligand-Target Pair
Affinity DataIC50: 291nMAssay Description:Antagonist activity at CXCR3 in Wistar rat whole blood assessed as receptor internalization incubated for 30 mins in presence of CXCL10 by flow cytom...More data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+4nMAssay Description:Time dependent inhibition of CYP2D6 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+4nMAssay Description:Time dependent inhibition of CYP3A4 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+4nMAssay Description:Time dependent inhibition of CYP2C9 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+4nMAssay Description:Competitive inhibition of CYP2C9 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+4nMAssay Description:Competitive inhibition of CYP2D6 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+4nMAssay Description:Competitive inhibition of CYP3A4 (unknown origin)More data for this Ligand-Target Pair