BDBM287559 8-(2-((1-acryloylpiperidin-4-yl)(methyl)amino)ethyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one::US10294223, Cpd No. 127::US11078199, Cpd 127::US9567334, Example 127::US9815834, Compound 127

SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCN(C)C3CCN(CC3)C(=O)C=C)c2n1

InChI Key InChIKey=ZVFYULVCRUAESA-UHFFFAOYSA-N

Data  7 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 7 hits for monomerid = 287559   

TargetFibroblast growth factor receptor 1(Human)
Principia Biopharma

US Patent
LigandPNGBDBM287559(8-(2-((1-acryloylpiperidin-4-yl)(methyl)amino)ethy...)
Affinity DataIC50: 1.5nMT: 2°CAssay Description:A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/17/2019
Entry Details
Go to US Patent

TargetFibroblast growth factor receptor 1(Human)
Principia Biopharma

US Patent
LigandPNGBDBM287559(8-(2-((1-acryloylpiperidin-4-yl)(methyl)amino)ethy...)
Affinity DataIC50: 4.10nMAssay Description:Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/13/2019
Entry Details Article
PubMed
TargetFibroblast growth factor receptor 1(Human)
Principia Biopharma

US Patent
LigandPNGBDBM287559(8-(2-((1-acryloylpiperidin-4-yl)(methyl)amino)ethy...)
Affinity DataIC50: 4.10nMAssay Description:Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/13/2019
Entry Details Article
PubMed
TargetFibroblast growth factor receptor 1(Human)
Principia Biopharma

US Patent
LigandPNGBDBM287559(8-(2-((1-acryloylpiperidin-4-yl)(methyl)amino)ethy...)
Affinity DataIC50: 1.5nMAssay Description:A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2020
Entry Details
Go to US Patent

TargetFibroblast growth factor receptor 2(Human)
Principia Biopharma

US Patent
LigandPNGBDBM287559(8-(2-((1-acryloylpiperidin-4-yl)(methyl)amino)ethy...)
Affinity DataIC50: 3.40nMAssay Description:The cell-based effects of FGFR inhibitors were determined by measuring inhibition of FGFR-dependent cell line growth. The cell lines SNU-16 was used ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2020
Entry Details
Go to US Patent

TargetFibroblast growth factor receptor 1(Human)
Principia Biopharma

US Patent
LigandPNGBDBM287559(8-(2-((1-acryloylpiperidin-4-yl)(methyl)amino)ethy...)
Affinity DataIC50: 3.40nMAssay Description:A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2019
Entry Details
Go to US Patent

TargetFibroblast growth factor receptor 1(Human)
Principia Biopharma

US Patent
LigandPNGBDBM287559(8-(2-((1-acryloylpiperidin-4-yl)(methyl)amino)ethy...)
Affinity DataIC50: 1.5nMAssay Description:A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/16/2022
Entry Details
Go to US Patent