Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Fibroblast growth factor receptor 1 (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | US Patent | n/a | n/a | 0.600 | n/a | n/a | n/a | n/a | n/a | 25 |
Principia Biopharma, Inc. US Patent | Assay Description A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin... | US Patent US9567334 (2017) BindingDB Entry DOI: 10.7270/Q2XK8HKQ | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Fibroblast growth factor receptor 1 (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 0.600 | n/a | n/a | n/a | n/a | n/a | n/a |
Principia Biopharma, Inc. Curated by ChEMBL | Assay 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... | J Med Chem 60: 6516-6527 (2017) Article DOI: 10.1021/acs.jmedchem.7b00360 BindingDB Entry DOI: 10.7270/Q2C53P3H | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Fibroblast growth factor receptor 1 (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | US Patent | n/a | n/a | 0.600 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin... | Citation and Details BindingDB Entry DOI: 10.7270/Q2DB850W | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Fibroblast growth factor receptor 1 (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | US Patent | n/a | n/a | 0.600 | n/a | n/a | n/a | n/a | n/a | n/a |
Boehringer Ingelheim Pharmaceuticals Inc. | Assay Description A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin... | Bioorg Med Chem Lett 19: 773-7 (2009) BindingDB Entry DOI: 10.7270/Q2GX4DVZ | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Fibroblast growth factor receptor 1 (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 0.600 | n/a | n/a | n/a | n/a | n/a | n/a |
Principia Biopharma, Inc. Curated by ChEMBL | Assay 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... | J Med Chem 60: 6516-6527 (2017) Article DOI: 10.1021/acs.jmedchem.7b00360 BindingDB Entry DOI: 10.7270/Q2C53P3H | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Fibroblast growth factor receptor 2 (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 1.30 | n/a | n/a | n/a | n/a | n/a | n/a |
Principia Biopharma, Inc. Curated by ChEMBL | Assay Description Inhibition of human FGFR2 preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis m... | J Med Chem 60: 6516-6527 (2017) Article DOI: 10.1021/acs.jmedchem.7b00360 BindingDB Entry DOI: 10.7270/Q2C53P3H | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Fibroblast growth factor receptor 1 (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | US Patent | n/a | n/a | 2.60 | n/a | n/a | n/a | n/a | n/a | n/a |
PRINCIPIA BIOPHARMA, INC. US Patent | Assay Description A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin... | US Patent US9815834 (2017) BindingDB Entry DOI: 10.7270/Q2B85B83 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Fibroblast growth factor receptor 2 (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | US Patent | n/a | n/a | 2.60 | n/a | n/a | n/a | n/a | n/a | n/a |
Boehringer Ingelheim Pharmaceuticals Inc. | Assay 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 ... | Bioorg Med Chem Lett 19: 773-7 (2009) BindingDB Entry DOI: 10.7270/Q2GX4DVZ | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Fibroblast growth factor receptor 3 (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 4.10 | n/a | n/a | n/a | n/a | n/a | n/a |
Principia Biopharma, Inc. Curated by ChEMBL | Assay Description Inhibition of human FGFR3 preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis m... | J Med Chem 60: 6516-6527 (2017) Article DOI: 10.1021/acs.jmedchem.7b00360 BindingDB Entry DOI: 10.7270/Q2C53P3H | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Macrophage colony-stimulating factor 1 receptor (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 8.10 | n/a | n/a | n/a | n/a | n/a | n/a |
Principia Biopharma, Inc. Curated by ChEMBL | Assay Description Inhibition of human CSF1R preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis m... | J Med Chem 60: 6516-6527 (2017) Article DOI: 10.1021/acs.jmedchem.7b00360 BindingDB Entry DOI: 10.7270/Q2C53P3H | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Fibroblast growth factor receptor 4 (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 19 | n/a | n/a | n/a | n/a | n/a | n/a |
Principia Biopharma, Inc. Curated by ChEMBL | Assay Description Inhibition of human FGFR4 preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis m... | J Med Chem 60: 6516-6527 (2017) Article DOI: 10.1021/acs.jmedchem.7b00360 BindingDB Entry DOI: 10.7270/Q2C53P3H | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Cytoplasmic tyrosine-protein kinase BMX (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 272 | n/a | n/a | n/a | n/a | n/a | n/a |
Principia Biopharma, Inc. Curated by ChEMBL | Assay Description Inhibition of human BMX preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis met... | J Med Chem 60: 6516-6527 (2017) Article DOI: 10.1021/acs.jmedchem.7b00360 BindingDB Entry DOI: 10.7270/Q2C53P3H | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Tyrosine-protein kinase Blk (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | Reactome pathway KEGG UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 371 | n/a | n/a | n/a | n/a | n/a | n/a |
Principia Biopharma, Inc. Curated by ChEMBL | Assay Description Inhibition of human BLK preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis met... | J Med Chem 60: 6516-6527 (2017) Article DOI: 10.1021/acs.jmedchem.7b00360 BindingDB Entry DOI: 10.7270/Q2C53P3H | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Vascular endothelial growth factor receptor 3 (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 410 | n/a | n/a | n/a | n/a | n/a | n/a |
Principia Biopharma, Inc. Curated by ChEMBL | Assay Description Inhibition of human FLT4 preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis me... | J Med Chem 60: 6516-6527 (2017) Article DOI: 10.1021/acs.jmedchem.7b00360 BindingDB Entry DOI: 10.7270/Q2C53P3H | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Tyrosine-protein kinase JAK3 (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 556 | n/a | n/a | n/a | n/a | n/a | n/a |
Principia Biopharma, Inc. Curated by ChEMBL | Assay Description Inhibition of human JAK3 preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis me... | J Med Chem 60: 6516-6527 (2017) Article DOI: 10.1021/acs.jmedchem.7b00360 BindingDB Entry DOI: 10.7270/Q2C53P3H | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Tyrosine-protein kinase Lyn (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 631 | n/a | n/a | n/a | n/a | n/a | n/a |
Principia Biopharma, Inc. Curated by ChEMBL | Assay Description Inhibition of human LYN-B preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis m... | J Med Chem 60: 6516-6527 (2017) Article DOI: 10.1021/acs.jmedchem.7b00360 BindingDB Entry DOI: 10.7270/Q2C53P3H | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Tyrosine-protein kinase Lyn (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 639 | n/a | n/a | n/a | n/a | n/a | n/a |
Principia Biopharma, Inc. Curated by ChEMBL | Assay Description Inhibition of human LYN-A preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis m... | J Med Chem 60: 6516-6527 (2017) Article DOI: 10.1021/acs.jmedchem.7b00360 BindingDB Entry DOI: 10.7270/Q2C53P3H | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Vascular endothelial growth factor receptor 2 (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 705 | n/a | n/a | n/a | n/a | n/a | n/a |
Principia Biopharma, Inc. Curated by ChEMBL | Assay Description Inhibition of human VEGFR2 preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis ... | J Med Chem 60: 6516-6527 (2017) Article DOI: 10.1021/acs.jmedchem.7b00360 BindingDB Entry DOI: 10.7270/Q2C53P3H | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Eukaryotic translation initiation factor 2-alpha kinase 3 (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 792 | n/a | n/a | n/a | n/a | n/a | n/a |
Principia Biopharma, Inc. Curated by ChEMBL | Assay Description Inhibition of human PERK preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis me... | J Med Chem 60: 6516-6527 (2017) Article DOI: 10.1021/acs.jmedchem.7b00360 BindingDB Entry DOI: 10.7270/Q2C53P3H | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Serine/threonine-protein kinase TAO2 (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 1.18E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Principia Biopharma, Inc. Curated by ChEMBL | Assay Description Inhibition of human TAOK2 preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis m... | J Med Chem 60: 6516-6527 (2017) Article DOI: 10.1021/acs.jmedchem.7b00360 BindingDB Entry DOI: 10.7270/Q2C53P3H | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Macrophage colony-stimulating factor 1 receptor (Homo sapiens (Human)) | BDBM286984 (8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | >1.50E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Principia Biopharma, Inc. Curated by ChEMBL | Assay Description Inhibition of human CSF1R by cell based assay | J Med Chem 60: 6516-6527 (2017) Article DOI: 10.1021/acs.jmedchem.7b00360 BindingDB Entry DOI: 10.7270/Q2C53P3H | |||||||||||
More data for this Ligand-Target Pair |