BDBM176061 US10047103, 94::US9688695, 94
SMILES COc1nn2cc(nc2s1)-c1cc2c(OCc3nc(sc3C)N3CCOCC3)cc(OC)cc2o1
InChI Key InChIKey=MINMDCMSHDBHKG-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 22 hits for monomerid = 176061
Affinity DataEC50: 0.430nMT: 25°CAssay Description:The activity of the PAR4 antagonists of the present invention were tested in PAR4 expressing cells by monitoring H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-L...More data for this Ligand-Target Pair
TargetNuclear receptor subfamily 1 group I member 2(Human)
Bristol-Myers Squibb Research & Early Development
Curated by ChEMBL
Bristol-Myers Squibb Research & Early Development
Curated by ChEMBL
Affinity DataEC50: >5.00E+3nMAssay Description:Agonist activity at PXR (unknown origin)More data for this Ligand-Target Pair
Affinity DataEC50: 7.60nMT: 25°CAssay Description:Briefly, PRP or washed platelet suspension (100 μl) was pre-incubated for 5 minutes at room temperature with varying concentrations of compounds...More data for this Ligand-Target Pair
Affinity DataIC50: 7.60nMT: 25°CAssay Description:The ability of the compounds of the current invention to inhibit platelet aggregation induced by gamma-thrombin was tested in a 96-well microplate ag...More data for this Ligand-Target Pair
Affinity DataIC50: 0.560nMAssay Description:Inhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobiliza...More data for this Ligand-Target Pair
Affinity DataIC50: 7.30nMAssay Description:Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mi...More data for this Ligand-Target Pair
Affinity DataIC50: 9.5nMAssay Description:Antagonist activity at PAR4 in human whole blood assessed as inhibition of Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced platelet aggregati...More data for this Ligand-Target Pair
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of PAR1 in human whole blood assessed as inhibition of PAR1 AP (Ala-Phe (4fluro) Arg-Cha-homo Arg-Tyr-NH2)-induced platelet aggregation pr...More data for this Ligand-Target Pair
Affinity DataIC50: 9.70nMAssay Description:Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidim...More data for this Ligand-Target Pair
Affinity DataIC50: 0.700nMAssay Description:Antagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for ...More data for this Ligand-Target Pair
Affinity DataIC50: >3.16E+3nMAssay Description:Antagonist activity at human PAR1 expressed in Ga15-HEK293 cells assessed as reduction in PAR1 AP SFFLRR-NH2-induced cytosolic calcium incubated for ...More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+3nMAssay Description:Antagonist activity at human PAR2 expressed in Ga15-HEK293 cells assessed as reduction in PAR2 AP 2-furoyl-LIGRLO-NH2-induced cytosolic calcium incub...More data for this Ligand-Target Pair
Affinity DataIC50: 0.400nMAssay Description:Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 i...More data for this Ligand-Target Pair
Affinity DataKd: 0.0980nMAssay Description:Binding affinity to PAR4 (unknown origin) assessed as saturation bindingMore data for this Ligand-Target Pair
Affinity DataKd: 0.0700nMAssay Description:Binding affinity to PAR4 (unknown origin) assessed as association constantMore data for this Ligand-Target Pair
Affinity DataIC50: >6.00E+3nMAssay Description:Inhibition of CYP2B6 in human liver microsomesMore data for this Ligand-Target Pair
Affinity DataIC50: >2.00E+3nMAssay Description:Inhibition of CYP2C8 in human liver microsomesMore data for this Ligand-Target Pair
Affinity DataIC50: >6.00E+3nMAssay Description:Inhibition of CYP2C9 in human liver microsomesMore data for this Ligand-Target Pair
Affinity DataIC50: >6.00E+3nMAssay Description:Inhibition of CYP2C19 in human liver microsomesMore data for this Ligand-Target Pair
Affinity DataIC50: >6.00E+3nMAssay Description:Inhibition of CYP2D6 in human liver microsomesMore data for this Ligand-Target Pair
Affinity DataIC50: >6.00E+3nMAssay Description:Inhibition of CYP3A4 in human liver microsomesMore data for this Ligand-Target Pair
Affinity DataEC50: 0.430nMT: 25°CAssay Description:Briefly, HEK293 EBNA PAR4 clone 20664.1J cells were plated 24 hrs. prior to experiment in 384 well, Poly-D-Lysine coated, black, clear bottom plates ...More data for this Ligand-Target Pair