Found 18 hits Enz. Inhib. hit(s) with Target = 'Epidermal growth factor receptor' and Ligand = 'BDBM4567' 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 |
Epidermal growth factor receptor
(Homo sapiens (Human)) | BDBM4567
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) | PDB MMDB
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| n/a | n/a | 0.700 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Auckland
Curated by ChEMBL
| Assay Description Inhibition of phosphorylation of glutamic acid/tyrosine random copolymer by isolated epidermal growth factor receptor (EGFR) |
J Med Chem 42: 1803-15 (1999)
Article DOI: 10.1021/jm9806603 BindingDB Entry DOI: 10.7270/Q2B56HZG |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Epidermal growth factor receptor
(Homo sapiens (Human)) | BDBM4567
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) | PDB MMDB
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| n/a | n/a | 0.700 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Auckland
Curated by ChEMBL
| Assay Description Inhibition of phosphorylation of a polyglutamic acid/tyrosine random copolymer by EGFR enzyme prepared from human A431 carcinoma cell vesicles by imm... |
J Med Chem 43: 1380-97 (2001)
BindingDB Entry DOI: 10.7270/Q2H13179 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Epidermal growth factor receptor
(Homo sapiens (Human)) | BDBM4567
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) | PDB MMDB
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| n/a | n/a | 0.700 | n/a | n/a | n/a | n/a | n/a | n/a |
Covalution Pharma BV
Curated by ChEMBL
| Assay Description Irreversible inhibition of EGFR |
J Med Chem 55: 6243-62 (2012)
Article DOI: 10.1021/jm3003203 BindingDB Entry DOI: 10.7270/Q2X92CGP |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Epidermal growth factor receptor
(Homo sapiens (Human)) | BDBM4567
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) | PDB MMDB
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| n/a | n/a | 0.700 | n/a | n/a | n/a | n/a | 7.4 | 25 |
University of Auckland
| Assay Description Enzyme assays for IC50 determinations were performed in 96-well filter plates. IC50 is the inhibitor concentration which inhibits 50% of kinase activ... |
J Med Chem 44: 429-40 (2001)
Article DOI: 10.1021/jm000372i BindingDB Entry DOI: 10.7270/Q2HX19WB |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Epidermal growth factor receptor
(Homo sapiens (Human)) | BDBM4567
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) | PDB MMDB
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| n/a | n/a | 1.69 | n/a | n/a | n/a | n/a | n/a | n/a |
Universit£ degli Studi di Parma
Curated by ChEMBL
| Assay Description Inhibition of human recombinant EGFR expressed in insect cells by time-resolved fluorometry |
J Med Chem 53: 2038-50 (2010)
Article DOI: 10.1021/jm901558p BindingDB Entry DOI: 10.7270/Q2736R1N |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Epidermal growth factor receptor
(Homo sapiens (Human)) | BDBM4567
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) | PDB MMDB
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| n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/a |
Universit£ di Pisa
Curated by ChEMBL
| Assay Description Inhibition of human recombinant EGFR |
J Med Chem 52: 964-75 (2009)
Article DOI: 10.1021/jm800829v BindingDB Entry DOI: 10.7270/Q27W6C7Q |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Epidermal growth factor receptor
(Homo sapiens (Human)) | BDBM4567
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) | PDB MMDB
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| n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/a |
Wyeth Research
Curated by ChEMBL
| Assay Description Inhibition of autophosphorylation of cytoplasmic domain of epidermal growth factor receptor |
J Med Chem 46: 49-63 (2002)
Article DOI: 10.1021/jm020241c BindingDB Entry DOI: 10.7270/Q2PV6M3H |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Epidermal growth factor receptor
(Homo sapiens (Human)) | BDBM4567
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) | PDB MMDB
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| n/a | n/a | 2 | n/a | n/a | n/a | n/a | 7.4 | 22 |
Wyeth-Ayerst Research
| Assay Description The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po... |
J Med Chem 44: 2719-34 (2001)
Article DOI: 10.1021/jm0005555 BindingDB Entry DOI: 10.7270/Q2PN93TS |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Epidermal growth factor receptor
(Homo sapiens (Human)) | BDBM4567
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) | PDB MMDB
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| n/a | n/a | 2.70 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Auckland
Curated by ChEMBL
| Assay Description Inhibition of EGF-stimulated autophosphorylation of EGFR enzyme in A431 cells detected by immunoblotting |
J Med Chem 43: 1380-97 (2001)
BindingDB Entry DOI: 10.7270/Q2H13179 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Epidermal growth factor receptor
(Homo sapiens (Human)) | BDBM4567
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) | PDB MMDB
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| n/a | n/a | 3.90 | n/a | n/a | n/a | n/a | n/a | n/a |
Universit£ degli Studi di Parma
Curated by ChEMBL
| Assay Description Inhibition of wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured at 1 hr by Western blot... |
Bioorg Med Chem Lett 23: 5290-4 (2013)
Article DOI: 10.1016/j.bmcl.2013.08.008 BindingDB Entry DOI: 10.7270/Q24Q7XX1 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Epidermal growth factor receptor
(Homo sapiens (Human)) | BDBM4567
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) | PDB MMDB
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| n/a | n/a | 4.30 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Auckland
Curated by ChEMBL
| Assay Description Inhibition of EGF-stimulated autophosphorylation of epidermal growth factor receptor (EGFR) in A431 cells |
J Med Chem 42: 1803-15 (1999)
Article DOI: 10.1021/jm9806603 BindingDB Entry DOI: 10.7270/Q2B56HZG |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Epidermal growth factor receptor
(Homo sapiens (Human)) | BDBM4567
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) | PDB MMDB
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| n/a | n/a | 12 | n/a | n/a | n/a | n/a | n/a | n/a |
Universit£ degli Studi di Parma
Curated by ChEMBL
| Assay Description Inhibition of EGFR autophosphorylation in human A431 cells after 1 hr by western blot |
J Med Chem 53: 2038-50 (2010)
Article DOI: 10.1021/jm901558p BindingDB Entry DOI: 10.7270/Q2736R1N |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Epidermal growth factor receptor
(Homo sapiens (Human)) | BDBM4567
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) | PDB MMDB
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| n/a | n/a | 18 | n/a | n/a | n/a | n/a | n/a | n/a |
Universit£ degli Studi di Parma
Curated by ChEMBL
| Assay Description Inhibition of wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured after 8 hrs by Western ... |
Bioorg Med Chem Lett 23: 5290-4 (2013)
Article DOI: 10.1016/j.bmcl.2013.08.008 BindingDB Entry DOI: 10.7270/Q24Q7XX1 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Epidermal growth factor receptor
(Homo sapiens (Human)) | BDBM4567
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) | PDB MMDB
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| n/a | n/a | 36 | n/a | n/a | n/a | n/a | n/a | n/a |
Alma Mater Studiorum-University of Bologna
Curated by ChEMBL
| Assay Description Inhibition of EGFR-TK in human A431 cell lysate assessed as reduction in EGF stimulated kinase activity after 60 mins using biotinylated peptide subs... |
Eur J Med Chem 117: 283-91 (2016)
Article DOI: 10.1016/j.ejmech.2016.04.002 BindingDB Entry DOI: 10.7270/Q2V126QC |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Epidermal growth factor receptor
(Homo sapiens (Human)) | BDBM4567
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) | PDB MMDB
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| n/a | n/a | 36 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Bologna
Curated by ChEMBL
| Assay Description Inhibition of EGFR tyrosine kinase activity |
J Med Chem 49: 6642-5 (2006)
Article DOI: 10.1021/jm0608762 BindingDB Entry DOI: 10.7270/Q28P605H |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Epidermal growth factor receptor
(Homo sapiens (Human)) | BDBM4567
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) | PDB MMDB
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| n/a | n/a | 130 | n/a | n/a | n/a | n/a | n/a | n/a |
Duquesne University of the Holy Ghost
US Patent
| Assay Description Inhibition of various kinase enzyme. |
US Patent US9422297 (2016)
BindingDB Entry DOI: 10.7270/Q2MC8XX9 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Epidermal growth factor receptor
(Homo sapiens (Human)) | BDBM4567
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) | PDB MMDB
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| n/a | n/a | 152 | n/a | n/a | n/a | n/a | n/a | n/a |
Universit£ degli Studi di Parma
Curated by ChEMBL
| Assay Description Inhibition of EGFR autophosphorylation in human A431 cells after 8 hrs by western blot |
J Med Chem 53: 2038-50 (2010)
Article DOI: 10.1021/jm901558p BindingDB Entry DOI: 10.7270/Q2736R1N |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Epidermal growth factor receptor
(Homo sapiens (Human)) | BDBM4567
(4-anilinoquinazoline deriv. 2 | BMC163482 Compound...)Show InChI InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) | PDB MMDB
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| n/a | n/a | 521 | n/a | n/a | n/a | n/a | n/a | n/a |
Duquesne University of the Holy Ghost
US Patent
| Assay Description Inhibition of various kinase enzyme. |
US Patent US9422297 (2016)
BindingDB Entry DOI: 10.7270/Q2MC8XX9 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |