BDBM364746 6-(4-((3-(Benzyloxy)benzyl)oxy)-6-methoxybenzofuran-2-yl)-2-methoxyimidazo[2,1-b][1,3,4]thiadiazole::US9862730, Example 205

SMILES COc1nn2cc(nc2s1)-c1cc2c(OCc3cccc(OCc4ccccc4)c3)cc(OC)cc2o1

InChI Key InChIKey=LFOIDLOIBZFWDO-UHFFFAOYSA-N

Data  10 IC50  2 Kd  1 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 13 hits for monomerid = 364746   

TargetProteinase-activated receptor 4(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM364746(US9862730, Example 205 | 6-(4-((3-(Benzyloxy)benzy...)
Affinity DataIC50: 2.42nMAssay Description:The FLIPR assay is an exemplary in vitro assay for measuring the activity of the PAR4 antagonists of the present invention. In this assay, intracellu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/3/2019
Entry Details
Go to US Patent

TargetProteinase-activated receptor 4(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM364746(US9862730, Example 205 | 6-(4-((3-(Benzyloxy)benzy...)
Affinity DataIC50: 8nMAssay Description:Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins f...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetCytochrome P450 4B1(Human)
Bristol-Myers Squibb Research & Development

Curated by ChEMBL
LigandPNGBDBM364746(US9862730, Example 205 | 6-(4-((3-(Benzyloxy)benzy...)
Affinity DataIC50: 4.00E+4nMAssay Description:Inhibition of CYP450 in human liver microsomesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetProteinase-activated receptor 4(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM364746(US9862730, Example 205 | 6-(4-((3-(Benzyloxy)benzy...)
Affinity DataIC50: 25nMAssay 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
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetProteinase-activated receptor 1(Human)
Bristol-Myers Squibb Research & Development

Curated by ChEMBL
LigandPNGBDBM364746(US9862730, Example 205 | 6-(4-((3-(Benzyloxy)benzy...)
Affinity DataIC50: 3.00E+4nMAssay Description:Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of SFFLRR-induced platelet aggregation preincubated for 5 mins follo...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetProteinase-activated receptor 1(Human)
Bristol-Myers Squibb Research & Development

Curated by ChEMBL
LigandPNGBDBM364746(US9862730, Example 205 | 6-(4-((3-(Benzyloxy)benzy...)
Affinity DataIC50: 3.00E+4nMAssay Description:Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation preincubated for 5 mins followed...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetProteinase-activated receptor 1(Human)
Bristol-Myers Squibb Research & Development

Curated by ChEMBL
LigandPNGBDBM364746(US9862730, Example 205 | 6-(4-((3-(Benzyloxy)benzy...)
Affinity DataIC50: 3.00E+4nMAssay Description:Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of U46619-induced platelet aggregation preincubated for 5 mins follo...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetProteinase-activated receptor 4(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM364746(US9862730, Example 205 | 6-(4-((3-(Benzyloxy)benzy...)
Affinity DataIC50: 2.40nMAssay Description:Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization p...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetNuclear receptor subfamily 1 group I member 2(Human)
Bristol-Myers Squibb Research & Development

Curated by ChEMBL
LigandPNGBDBM364746(US9862730, Example 205 | 6-(4-((3-(Benzyloxy)benzy...)
Affinity DataEC50: >5.00E+4nMAssay Description:Activation of human PXRMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetProteinase-activated receptor 4(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM364746(US9862730, Example 205 | 6-(4-((3-(Benzyloxy)benzy...)
Affinity DataKd:  1.40nMAssay Description:Displacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranes measured after 2 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetProteinase-activated receptor 4(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM364746(US9862730, Example 205 | 6-(4-((3-(Benzyloxy)benzy...)
Affinity DataKd:  3nMAssay Description:Displacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetProteinase-activated receptor 1(Human)
Bristol-Myers Squibb Research & Development

Curated by ChEMBL
LigandPNGBDBM364746(US9862730, Example 205 | 6-(4-((3-(Benzyloxy)benzy...)
Affinity DataIC50: 3.00E+4nMAssay Description:Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of collagen-induced platelet aggregation preincubated for 5 mins fol...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetProteinase-activated receptor 4(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM364746(US9862730, Example 205 | 6-(4-((3-(Benzyloxy)benzy...)
Affinity DataIC50: 2.40nMAssay 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
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed