Found 5 hits Enz. Inhib. hit(s) with Target = 'Fibroblast growth factor receptor 1' and Ligand = 'BDBM287067' 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)) | BDBM287067
(8-(2-((1-acryloylazetidin-3-yl)(methyl)amino)ethyl...)Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCN(C)C3CN(C3)C(=O)C=C)c2n1 |(-6.94,-1.38,;-6.94,.16,;-5.61,.93,;-5.61,2.47,;-4.28,3.24,;-2.94,2.47,;-1.61,3.24,;-.28,2.47,;1.06,3.24,;1.06,4.78,;-.28,5.55,;2.39,5.55,;2.39,7.09,;1.06,7.86,;3.72,4.78,;3.72,3.24,;5.06,2.47,;6.39,3.24,;2.39,2.47,;2.39,.93,;-.28,.93,;1.06,.16,;-1.61,.16,;-1.61,-1.38,;-.28,-2.15,;-.28,-3.69,;-1.61,-4.46,;1.06,-4.46,;1.46,-5.95,;2.94,-5.55,;2.55,-4.06,;4.28,-6.32,;4.28,-7.86,;5.61,-5.55,;6.94,-6.32,;-2.94,.93,;-4.28,.16,)| Show InChI InChI=1S/C25H28Cl2N6O4/c1-6-19(34)32-12-15(13-32)31(3)7-8-33-23-14(11-29-25(28-2)30-23)9-16(24(33)35)20-21(26)17(36-4)10-18(37-5)22(20)27/h6,9-11,15H,1,7-8,12-13H2,2-5H3,(H,28,29,30) | 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 | 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)) | BDBM287067
(8-(2-((1-acryloylazetidin-3-yl)(methyl)amino)ethyl...)Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCN(C)C3CN(C3)C(=O)C=C)c2n1 |(-6.94,-1.38,;-6.94,.16,;-5.61,.93,;-5.61,2.47,;-4.28,3.24,;-2.94,2.47,;-1.61,3.24,;-.28,2.47,;1.06,3.24,;1.06,4.78,;-.28,5.55,;2.39,5.55,;2.39,7.09,;1.06,7.86,;3.72,4.78,;3.72,3.24,;5.06,2.47,;6.39,3.24,;2.39,2.47,;2.39,.93,;-.28,.93,;1.06,.16,;-1.61,.16,;-1.61,-1.38,;-.28,-2.15,;-.28,-3.69,;-1.61,-4.46,;1.06,-4.46,;1.46,-5.95,;2.94,-5.55,;2.55,-4.06,;4.28,-6.32,;4.28,-7.86,;5.61,-5.55,;6.94,-6.32,;-2.94,.93,;-4.28,.16,)| Show InChI InChI=1S/C25H28Cl2N6O4/c1-6-19(34)32-12-15(13-32)31(3)7-8-33-23-14(11-29-25(28-2)30-23)9-16(24(33)35)20-21(26)17(36-4)10-18(37-5)22(20)27/h6,9-11,15H,1,7-8,12-13H2,2-5H3,(H,28,29,30) | 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 | 1 | 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)) | BDBM287067
(8-(2-((1-acryloylazetidin-3-yl)(methyl)amino)ethyl...)Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCN(C)C3CN(C3)C(=O)C=C)c2n1 |(-6.94,-1.38,;-6.94,.16,;-5.61,.93,;-5.61,2.47,;-4.28,3.24,;-2.94,2.47,;-1.61,3.24,;-.28,2.47,;1.06,3.24,;1.06,4.78,;-.28,5.55,;2.39,5.55,;2.39,7.09,;1.06,7.86,;3.72,4.78,;3.72,3.24,;5.06,2.47,;6.39,3.24,;2.39,2.47,;2.39,.93,;-.28,.93,;1.06,.16,;-1.61,.16,;-1.61,-1.38,;-.28,-2.15,;-.28,-3.69,;-1.61,-4.46,;1.06,-4.46,;1.46,-5.95,;2.94,-5.55,;2.55,-4.06,;4.28,-6.32,;4.28,-7.86,;5.61,-5.55,;6.94,-6.32,;-2.94,.93,;-4.28,.16,)| Show InChI InChI=1S/C25H28Cl2N6O4/c1-6-19(34)32-12-15(13-32)31(3)7-8-33-23-14(11-29-25(28-2)30-23)9-16(24(33)35)20-21(26)17(36-4)10-18(37-5)22(20)27/h6,9-11,15H,1,7-8,12-13H2,2-5H3,(H,28,29,30) | 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 | 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)) | BDBM287067
(8-(2-((1-acryloylazetidin-3-yl)(methyl)amino)ethyl...)Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCN(C)C3CN(C3)C(=O)C=C)c2n1 |(-6.94,-1.38,;-6.94,.16,;-5.61,.93,;-5.61,2.47,;-4.28,3.24,;-2.94,2.47,;-1.61,3.24,;-.28,2.47,;1.06,3.24,;1.06,4.78,;-.28,5.55,;2.39,5.55,;2.39,7.09,;1.06,7.86,;3.72,4.78,;3.72,3.24,;5.06,2.47,;6.39,3.24,;2.39,2.47,;2.39,.93,;-.28,.93,;1.06,.16,;-1.61,.16,;-1.61,-1.38,;-.28,-2.15,;-.28,-3.69,;-1.61,-4.46,;1.06,-4.46,;1.46,-5.95,;2.94,-5.55,;2.55,-4.06,;4.28,-6.32,;4.28,-7.86,;5.61,-5.55,;6.94,-6.32,;-2.94,.93,;-4.28,.16,)| Show InChI InChI=1S/C25H28Cl2N6O4/c1-6-19(34)32-12-15(13-32)31(3)7-8-33-23-14(11-29-25(28-2)30-23)9-16(24(33)35)20-21(26)17(36-4)10-18(37-5)22(20)27/h6,9-11,15H,1,7-8,12-13H2,2-5H3,(H,28,29,30) | 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 | 1.30 | 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)) | BDBM287067
(8-(2-((1-acryloylazetidin-3-yl)(methyl)amino)ethyl...)Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCN(C)C3CN(C3)C(=O)C=C)c2n1 |(-6.94,-1.38,;-6.94,.16,;-5.61,.93,;-5.61,2.47,;-4.28,3.24,;-2.94,2.47,;-1.61,3.24,;-.28,2.47,;1.06,3.24,;1.06,4.78,;-.28,5.55,;2.39,5.55,;2.39,7.09,;1.06,7.86,;3.72,4.78,;3.72,3.24,;5.06,2.47,;6.39,3.24,;2.39,2.47,;2.39,.93,;-.28,.93,;1.06,.16,;-1.61,.16,;-1.61,-1.38,;-.28,-2.15,;-.28,-3.69,;-1.61,-4.46,;1.06,-4.46,;1.46,-5.95,;2.94,-5.55,;2.55,-4.06,;4.28,-6.32,;4.28,-7.86,;5.61,-5.55,;6.94,-6.32,;-2.94,.93,;-4.28,.16,)| Show InChI InChI=1S/C25H28Cl2N6O4/c1-6-19(34)32-12-15(13-32)31(3)7-8-33-23-14(11-29-25(28-2)30-23)9-16(24(33)35)20-21(26)17(36-4)10-18(37-5)22(20)27/h6,9-11,15H,1,7-8,12-13H2,2-5H3,(H,28,29,30) | 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 | 3.40 | 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 | |