BDBM286388 8-(2-(4-acryloylpiperazin-1-yl)ethyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one::US10294223, Cpd No. 2::US9567334, Example 2::US9815834, Compound 2
SMILES: CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCN3CCN(CC3)C(=O)C=C)c2n1
InChI Key: InChIKey=PZMMTZOZIZQHCK-UHFFFAOYSA-N
Data: 6 IC50
Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kcal/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)) | BDBM286388 (8-(2-(4-acryloylpiperazin-1-yl)ethyl)-6-(2,6-dichl...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | US Patent | n/a | n/a | 2.30 | 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)) | BDBM286388 (8-(2-(4-acryloylpiperazin-1-yl)ethyl)-6-(2,6-dichl...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | Article PubMed | n/a | n/a | 11 | 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)) | BDBM286388 (8-(2-(4-acryloylpiperazin-1-yl)ethyl)-6-(2,6-dichl...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | Article PubMed | n/a | n/a | 2.30 | 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 1 (Homo sapiens (Human)) | US11078199, Cpd 2 (8-(2-(4-acryloylpiperazin-1-yl)ethyl)-6-(2,6-dichl...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | n/a | n/a | 2.30 | n/a | n/a | n/a | n/a | n/a | n/a | |
TBA | Citation and Details | ||||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Fibroblast growth factor receptor 2 (Homo sapiens (Human)) | BDBM286388 (8-(2-(4-acryloylpiperazin-1-yl)ethyl)-6-(2,6-dichl...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | US Patent | n/a | n/a | 1.20 | 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 1 (Homo sapiens (Human)) | BDBM286388 (8-(2-(4-acryloylpiperazin-1-yl)ethyl)-6-(2,6-dichl...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | US Patent | n/a | n/a | 1.20 | 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 1 (Homo sapiens (Human)) | BDBM286388 (8-(2-(4-acryloylpiperazin-1-yl)ethyl)-6-(2,6-dichl...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | US Patent | n/a | n/a | 2.30 | 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 |