Target Validation Information
TTD ID T59328
Target Name Epidermal growth factor receptor (EGFR)
Type of Target
Successful
Drug Potency against Target Drug Info Ki = 10.8 nM [35]
Cetuximab Drug Info IC50 = 150 nM [27]
Erlotinib Drug Info IC50 = 2.7 nM [28]
Gefitinib Drug Info IC50 = 2.1 nM [28]
Lapatinib Drug Info IC50 = 3 nM [33]
Drug Info Ki = 22 nM [30]
Drug Info IC50 = 0.8 nM [33]
AEE-788 Drug Info IC50 = 6 nM [32]
BIBW 2992 Drug Info Ki = 0.5 nM [31]
HKI-272 Drug Info IC50 = 59 nM [34]
Lapatinib Drug Info Ki = 10.8 nM [26]
TAK165 Drug Info IC50 = 25000 nM [29]
Vandetanib Drug Info IC50 = 500 nM [33]
Drug Info IC50 = 355 nM [19]
Drug Info IC50 = 1000 nM [7]
Drug Info IC50 = 10000 nM
Drug Info IC50 < 100 nM [1]
Drug Info IC50 = 10500 nM [3]
Drug Info IC50 = 1600 nM [25]
(3-Bromo-phenyl)-quinazolin-4-yl-amine Drug Info IC50 = 27 nM [24]
(E)-5-(4-Hydroxybenzylidene)-1-phenethylhydantoin Drug Info IC50 = 19000 nM [16]
2-(4,5-Dihydroxy-indan-1-ylidene)-malononitrile Drug Info IC50 = 7000 nM [8]
2-(5,6-Dihydroxy-indan-1-ylidene)-malononitrile Drug Info IC50 = 500 nM [8]
2-benzoyl-3-(3,4-dihydroxyphenyl)acrylonitrile Drug Info IC50 = 1000 nM
2-cyano-3-(3,4-dihydroxyphenyl)acrylamide Drug Info IC50 = 10000 nM
2-methoxy-4-(2-nitrovinyl)phenol Drug Info IC50 = 8000 nM
3-(3-Chloro-phenyl)-5,7-dihydroxy-chromen-4-one Drug Info IC50 = 16000 nM [1]
3-Pyridin-4-yl-quinoline-6,7-diol Drug Info IC50 = 5000 nM [21]
4-(2-nitroprop-1-enyl)benzene-1,2-diol Drug Info IC50 = 9000 nM
4-(2-nitrovinyl)benzene-1,2-diol Drug Info IC50 = 9000 nM
4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinazoline Drug Info IC50 = 70 nM
4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinoline Drug Info IC50 = 2500 nM
4-(3-Bromo-phenylamino)-quinazoline-6,7-diol Drug Info IC50 = 0.17 nM [24]
4-(4-(2-nitrovinyl)phenoxysulfonyl)benzoic acid Drug Info IC50 = 1000 nM
4-(5-Bromoindole-3-yl)-6,7-dimethoxyquinazoline Drug Info IC50 = 131 nM [14]
4-biphenyl-2-ylethynyl-6,7-dimethoxy-quinazoline Drug Info IC50 = 26 nM [13]
5,6-Bis-p-tolylamino-isoindole-1,3-dione Drug Info IC50 = 4500 nM [22]
6,7-diethoxy-4-(4-phenylbut-1-enyl)quinazoline Drug Info IC50 = 5 nM [13]
6,7-diethoxy-4-(5-phenylpent-1-enyl)quinazoline Drug Info IC50 = 140 nM [13]
6,7-diethoxy-4-styrylquinazoline Drug Info IC50 = 15 nM [13]
6,7-dimethoxy-4-(2-phenylethynyl)quinazoline Drug Info IC50 = 5600 nM [13]
6,7-dimethoxy-4-(3-phenoxyprop-1-ynyl)quinazoline Drug Info IC50 = 15 nM [13]
6,7-dimethoxy-4-(4-phenylbut-1-ynyl)quinazoline Drug Info IC50 = 14 nM [13]
6,7-dimethoxy-N-m-tolylquinazolin-4-amine Drug Info IC50 = 4.6 nM [15]
6-chloro-N-(3-chlorophenyl)quinazolin-4-amine Drug Info IC50 = 2700 nM [17]
AG-213 Drug Info IC50 = 1310 nM [14]
AG-538 Drug Info IC50 = 400 nM
Benzyl-quinazolin-4-yl-amine Drug Info IC50 = 320 nM [19]
CGP-53353 Drug Info IC50 = 2200 nM [22]
CL-387785 Drug Info IC50 = 8 nM [15]
HKI-272 Drug Info IC50 = 0.18 nM [11]
HKI-9924129 Drug Info IC50 = 390 nM [4]
HTS-00213 Drug Info IC50 = 6300 nM [15]
LAVENDUSTIN A Drug Info IC50 = 4100 nM [20]
N*4*-(3-Bromo-phenyl)-quinazoline-4,6,7-triamine Drug Info IC50 = 0.12 nM [24]
N*4*-(3-Bromo-phenyl)-quinazoline-4,6-diamine Drug Info IC50 = 40 nM [5]
N*4*-(3-Bromo-phenyl)-quinazoline-4,7-diamine Drug Info IC50 = 0.1 nM [19]
N*4*-Benzyl-pyrido[4,3-d]pyrimidine-4,7-diamine Drug Info IC50 = 2085 nM [23]
N-(4-(phenylamino)quinazolin-6-yl)acrylamide Drug Info IC50 < 1 nM [10]
N-(4-m-Tolylamino-quinazolin-6-yl)-acrylamide Drug Info IC50 = 4.7 nM [2]
N-(4-m-Tolylamino-quinazolin-7-yl)-acrylamide Drug Info IC50 = 90 nM [2]
N4-(3-chlorophenyl)quinazoline-4,6-diamine Drug Info IC50 = 200 nM [12]
PD-0166326 Drug Info IC50 = 82 nM [4]
PD-0173956 Drug Info IC50 = 380 nM [4]
PD-153035 Drug Info IC50 = 200 nM [18]
PD-158780 Drug Info IC50 = 15 nM [23]
PD-168393 Drug Info IC50 < 1 nM [10]
RG-50810 Drug Info IC50 = 10000 nM
Ro-4396686 Drug Info IC50 = 545 nM [6]
SKI-758 Drug Info IC50 = 230 nM [9]
VATALANIB Drug Info IC50 = 457.7 nM [11]
References
REF 1 Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones. J Med Chem. 1999 Mar 25;42(6):1018-26.
REF 2 Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP... J Med Chem. 1999 May 20;42(10):1803-15.
REF 3 Anthraquinones and betaenone derivatives from the sponge-associated fungus Microsphaeropsis species: novel inhibitors of protein kinases. J Nat Prod. 2000 Jun;63(6):739-45.
REF 4 Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors. Biochem Pharmacol. 2000 Oct 1;60(7):885-98.
REF 5 Synthesis of a prodrug designed to release multiple inhibitors of the epidermal growth factor receptor tyrosine kinase and an alkylating agent: a n... J Med Chem. 2003 Dec 4;46(25):5546-51.
REF 6 Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3.
REF 7 The combi-targeting concept: synthesis of stable nitrosoureas designed to inhibit the epidermal growth factor receptor (EGFR). J Med Chem. 2006 Jun 15;49(12):3544-52.
REF 8 Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine... J Med Chem. 1991 Jun;34(6):1896-907.
REF 9 Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76.
REF 10 Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. Nat Chem Biol. 2007 Apr;3(4):229-38.
REF 11 Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cyst... Bioorg Med Chem. 2007 Jun 1;15(11):3635-48.
REF 12 Novel nitrogen mustard-armed combi-molecules for the selective targeting of epidermal growth factor receptor overexperessing solid tumors: discover... J Med Chem. 2007 May 31;50(11):2605-8.
REF 13 Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: identification of new scaffolds for potent EGFR tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5863-7.
REF 14 Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors. Eur J Med Chem. 2008 Jul;43(7):1478-88.
REF 15 Computational studies of epidermal growth factor receptor: docking reliability, three-dimensional quantitative structure-activity relationship anal... J Med Chem. 2009 Feb 26;52(4):964-75.
REF 16 5-Benzylidene-hydantoins: synthesis and antiproliferative activity on A549 lung cancer cell line. Eur J Med Chem. 2009 Sep;44(9):3471-9.
REF 17 Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6.
REF 18 Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endo... Bioorg Med Chem. 2010 May 15;18(10):3575-87.
REF 19 Tyrosine kinase inhibitors. 5. Synthesis and structure-activity relationships for 4-[(phenylmethyl)amino]- and 4-(phenylamino)quinazolines as poten... J Med Chem. 1995 Sep 1;38(18):3482-7.
REF 20 Novel antiproliferative agents derived from lavendustin A. J Med Chem. 1994 Nov 25;37(24):4079-84.
REF 21 5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyro... J Med Chem. 1994 Aug 19;37(17):2627-9.
REF 22 Dianilinophthalimides: potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase. J Med Chem. 1994 Apr 1;37(7):1015-27.
REF 23 Tyrosine kinase inhibitors. 10. Isomeric 4-[(3-bromophenyl)amino]pyrido[d]-pyrimidines are potent ATP binding site inhibitors of the tyrosine kinas... J Med Chem. 1996 Apr 26;39(9):1823-35.
REF 24 Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase acti... J Med Chem. 1996 Feb 16;39(4):918-28.
REF 25 Cochliobolic acid, a novel metabolite produced by Cochliobolus lunatus, inhibits binding of TGF-alpha to the EGF receptor in a SPA assay. J Nat Prod. 1997 Jan;60(1):6-8.
REF 26 The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94.
REF 27 AMPA receptor antagonists as potential anticonvulsant drugs. Curr Top Med Chem. 2005;5(1):31-42.
REF 28 A small molecule-kinase interaction map for clinical kinase inhibitors. Nat Biotechnol. 2005 Mar;23(3):329-36.
REF 29 Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo. Int J Urol. 2006 May;13(5):587-92.
REF 30 Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling. Clin Cancer Res. 2006 Oct 15;12(20 Pt 1):6186-93.
REF 31 Dual inhibition of ErbB1 (EGFR/HER1) and ErbB2 (HER2/neu). Eur J Cancer. 2007 Feb;43(3):481-9.
REF 32 Molecular design and clinical development of VEGFR kinase inhibitors. Curr Top Med Chem. 2007;7(14):1379-93.
REF 33 A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32.
REF 34 Therapeutic potential of novel selective-spectrum kinase inhibitors in oncology. Expert Opin Investig Drugs. 2008 Jul;17(7):1013-28.
REF 35 Tofizopam affects binding of [3H]muscimol to gamma-amino-butyric acid receptors in rat and mouse brains. Pharmacol Res Commun. 1982 Sep;14(8):745-57.

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