BDBM286984 8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one::US10294223, Cpd No. 6::US11078199, Cpd 6::US9567334, Example 6::US9815834, Compound 6

SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCCN3CCN(CC3)C(=O)C=C)c2n1

InChI Key InChIKey=PUIXMSRTTHLNKI-UHFFFAOYSA-N

Data  4 KI  21 IC50

PDB links: 1 PDB ID matches this monomer.

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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 25 hits for monomerid = 286984   

TargetFibroblast growth factor receptor 2(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataKi:  1.30nMAssay Description:Irreversible inhibition of human FGFR2 preincubated with enzyme followed by peptide substrate addition by caliper capillary electrophoresis methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFibroblast growth factor receptor 1(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataKi:  1.60nMAssay Description:Irreversible inhibition of human FGFR1 using 5-FAM-KKKKEEIYFFF-NH2 as substrate preincubated with enzyme followed by peptide substrate addition by ca...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFibroblast growth factor receptor 3(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataKi:  2.20nMAssay Description:Irreversible inhibition of human FGFR3 preincubated with enzyme followed by peptide substrate addition by caliper capillary electrophoresis methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFibroblast growth factor receptor 4(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataKi:  73nMAssay Description:Irreversible inhibition of human FGFR4 preincubated with enzyme followed by peptide substrate addition by caliper capillary electrophoresis methodMore data for this Ligand-Target Pair
TargetCytoplasmic tyrosine-protein kinase BMX(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  272nMAssay Description:Inhibition of human BMX preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis met...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFibroblast growth factor receptor 4(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  19nMAssay Description:Inhibition of human FGFR4 preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis m...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Blk(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  371nMAssay Description:Inhibition of human BLK preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis met...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  705nMAssay Description:Inhibition of human VEGFR2 preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Lyn(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  631nMAssay Description:Inhibition of human LYN-B preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  556nMAssay Description:Inhibition of human JAK3 preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis me...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEukaryotic translation initiation factor 2-alpha kinase 3(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  792nMAssay Description:Inhibition of human PERK preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis me...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase TAO2(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  1.18E+3nMAssay Description:Inhibition of human TAOK2 preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFibroblast growth factor receptor 1(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of human FGFR1 using 5-FAM-KKKKEEIYFFF-NH2 as substrate preincubated for 15 mins followed by peptide substrate addition measured after 3 h...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 3(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  410nMAssay Description:Inhibition of human FLT4 preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis me...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMacrophage colony-stimulating factor 1 receptor(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  8.10nMAssay Description:Inhibition of human CSF1R preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMacrophage colony-stimulating factor 1 receptor(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50: >1.50E+3nMAssay Description:Inhibition of human CSF1R by cell based assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Lyn(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  639nMAssay Description:Inhibition of human LYN-A preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFibroblast growth factor receptor 1(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  0.600nMAssay 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 DepthDetails US Patent
TargetFibroblast growth factor receptor 2(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  2.60nMAssay 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 DepthDetails US Patent
TargetFibroblast growth factor receptor 1(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  2.60nMAssay 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 DepthDetails US Patent
TargetFibroblast growth factor receptor 3(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  4.10nMAssay Description:Inhibition of human FGFR3 preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFibroblast growth factor receptor 2(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  1.30nMAssay Description:Inhibition of human FGFR2 preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFibroblast growth factor receptor 1(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  0.600nMAssay 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 DepthDetails US Patent
TargetFibroblast growth factor receptor 1(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  0.600nMT: 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 DepthDetails US Patent
TargetFibroblast growth factor receptor 1(Homo sapiens (Human))
Principia Biopharma

Curated by ChEMBL
LigandPNGBDBM286984(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Affinity DataIC50:  0.600nMAssay 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 DepthDetails ArticlePubMed