Found 4 hits Enz. Inhib. hit(s) with Target = 'Fibroblast growth factor receptor 1' and Ligand = 'BDBM286999' 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)) | BDBM286999
(8-((1-((4-acryloylpiperazin-1-yl)methyl)cyclopropy...)Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CC3(CN4CCN(CC4)C(=O)C=C)CC3)c2n1 |(-6.67,-.77,;-6.67,.77,;-5.33,1.54,;-5.33,3.08,;-4,3.85,;-2.67,3.08,;-1.33,3.85,;,3.08,;1.33,3.85,;1.33,5.39,;,6.16,;2.67,6.16,;2.67,7.7,;1.33,8.47,;4,5.39,;4,3.85,;5.33,3.08,;6.67,3.85,;2.67,3.08,;2.67,1.54,;,1.54,;1.33,.77,;-1.33,.77,;-1.33,-.77,;,-1.54,;,-3.08,;1.33,-3.85,;1.33,-5.39,;2.67,-6.16,;4,-5.39,;4,-3.85,;2.67,-3.08,;5.33,-6.16,;6.67,-5.39,;5.33,-7.7,;6.67,-8.47,;1.54,-1.54,;.77,-.21,;-2.67,1.54,;-4,.77,)| Show InChI InChI=1S/C28H32Cl2N6O4/c1-5-21(37)35-10-8-34(9-11-35)15-28(6-7-28)16-36-25-17(14-32-27(31-2)33-25)12-18(26(36)38)22-23(29)19(39-3)13-20(40-4)24(22)30/h5,12-14H,1,6-11,15-16H2,2-4H3,(H,31,32,33) | 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 | 0.900 | 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)) | BDBM286999
(8-((1-((4-acryloylpiperazin-1-yl)methyl)cyclopropy...)Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CC3(CN4CCN(CC4)C(=O)C=C)CC3)c2n1 |(-6.67,-.77,;-6.67,.77,;-5.33,1.54,;-5.33,3.08,;-4,3.85,;-2.67,3.08,;-1.33,3.85,;,3.08,;1.33,3.85,;1.33,5.39,;,6.16,;2.67,6.16,;2.67,7.7,;1.33,8.47,;4,5.39,;4,3.85,;5.33,3.08,;6.67,3.85,;2.67,3.08,;2.67,1.54,;,1.54,;1.33,.77,;-1.33,.77,;-1.33,-.77,;,-1.54,;,-3.08,;1.33,-3.85,;1.33,-5.39,;2.67,-6.16,;4,-5.39,;4,-3.85,;2.67,-3.08,;5.33,-6.16,;6.67,-5.39,;5.33,-7.7,;6.67,-8.47,;1.54,-1.54,;.77,-.21,;-2.67,1.54,;-4,.77,)| Show InChI InChI=1S/C28H32Cl2N6O4/c1-5-21(37)35-10-8-34(9-11-35)15-28(6-7-28)16-36-25-17(14-32-27(31-2)33-25)12-18(26(36)38)22-23(29)19(39-3)13-20(40-4)24(22)30/h5,12-14H,1,6-11,15-16H2,2-4H3,(H,31,32,33) | 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 | 0.900 | 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)) | BDBM286999
(8-((1-((4-acryloylpiperazin-1-yl)methyl)cyclopropy...)Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CC3(CN4CCN(CC4)C(=O)C=C)CC3)c2n1 |(-6.67,-.77,;-6.67,.77,;-5.33,1.54,;-5.33,3.08,;-4,3.85,;-2.67,3.08,;-1.33,3.85,;,3.08,;1.33,3.85,;1.33,5.39,;,6.16,;2.67,6.16,;2.67,7.7,;1.33,8.47,;4,5.39,;4,3.85,;5.33,3.08,;6.67,3.85,;2.67,3.08,;2.67,1.54,;,1.54,;1.33,.77,;-1.33,.77,;-1.33,-.77,;,-1.54,;,-3.08,;1.33,-3.85,;1.33,-5.39,;2.67,-6.16,;4,-5.39,;4,-3.85,;2.67,-3.08,;5.33,-6.16,;6.67,-5.39,;5.33,-7.7,;6.67,-8.47,;1.54,-1.54,;.77,-.21,;-2.67,1.54,;-4,.77,)| Show InChI InChI=1S/C28H32Cl2N6O4/c1-5-21(37)35-10-8-34(9-11-35)15-28(6-7-28)16-36-25-17(14-32-27(31-2)33-25)12-18(26(36)38)22-23(29)19(39-3)13-20(40-4)24(22)30/h5,12-14H,1,6-11,15-16H2,2-4H3,(H,31,32,33) | 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 | 0.900 | 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)) | BDBM286999
(8-((1-((4-acryloylpiperazin-1-yl)methyl)cyclopropy...)Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CC3(CN4CCN(CC4)C(=O)C=C)CC3)c2n1 |(-6.67,-.77,;-6.67,.77,;-5.33,1.54,;-5.33,3.08,;-4,3.85,;-2.67,3.08,;-1.33,3.85,;,3.08,;1.33,3.85,;1.33,5.39,;,6.16,;2.67,6.16,;2.67,7.7,;1.33,8.47,;4,5.39,;4,3.85,;5.33,3.08,;6.67,3.85,;2.67,3.08,;2.67,1.54,;,1.54,;1.33,.77,;-1.33,.77,;-1.33,-.77,;,-1.54,;,-3.08,;1.33,-3.85,;1.33,-5.39,;2.67,-6.16,;4,-5.39,;4,-3.85,;2.67,-3.08,;5.33,-6.16,;6.67,-5.39,;5.33,-7.7,;6.67,-8.47,;1.54,-1.54,;.77,-.21,;-2.67,1.54,;-4,.77,)| Show InChI InChI=1S/C28H32Cl2N6O4/c1-5-21(37)35-10-8-34(9-11-35)15-28(6-7-28)16-36-25-17(14-32-27(31-2)33-25)12-18(26(36)38)22-23(29)19(39-3)13-20(40-4)24(22)30/h5,12-14H,1,6-11,15-16H2,2-4H3,(H,31,32,33) | 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 | 1.80 | 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 | |