Assay ID | Title | Year | Journal | Article |
AID457030 | Inhibition of EGFR autophosphorylation in human A431 cells at 1 uM after 1 hr by Western blot | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
| Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion. |
AID502962 | Inhibition of Fyn T342G mutant expressed in Escherichia coli C43 by radioactive phosphotransfer assay | 2007 | Nature chemical biology, Apr, Volume: 3, Issue:4
| Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. |
AID124668 | In vivo activity against A431 xenograft in nude mice, weight change at 1150 mg/kg peroral dose | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. |
AID661578 | Drug degradation of the compound assessed as thiol-conjugate formation at 1 uM up to 24 hrs at pH 7.4 in the presence of NAC | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides. |
AID502966 | Inhibition of EFG-stimulated EGFR phosphorylation transfected in mouse NIH/3T3 cells at 0.1 to 2 uM by radioactive phosphotransfer assay | 2007 | Nature chemical biology, Apr, Volume: 3, Issue:4
| Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. |
AID719907 | Inhibition of chicken c-Src T338G mutant | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| Irreversible protein kinase inhibitors: balancing the benefits and risks. |
AID392131 | Inhibition of HER4 | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. |
AID457032 | Inhibition of EGFR autophosphorylation in human A431 cells after 1 hr by Western blot | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
| Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion. |
AID502959 | Inhibition of c-src S345C mutant by radioactive phosphotransfer assay | 2007 | Nature chemical biology, Apr, Volume: 3, Issue:4
| Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. |
AID381970 | Inhibition of drug-resistant EGFR-T790 mutant | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR. |
AID661580 | Drug uptake in human A549 cells at 1 uM after 1 hr by LC-MS analysis | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides. |
AID661581 | Drug uptake in human A549 cells at 1 uM incubated for 1 hr measured 8 hrs post-wash out by LC-MS analysis | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides. |
AID1303337 | Irreversible inhibition of EGFR-TK in human A431 cells assessed as reduction in cell proliferation at 0.3 to 30 uM incubated for 4 hrs followed by 68 hrs of recovery in compound free medium by MTT assay | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Combined inhibition of the EGFR/AKT pathways by a novel conjugate of quinazoline with isothiocyanate. |
AID8077 | Irreversible inhibition of formation of phosphorylated EGFR in A431 cells 8 hr after washing cells free of compound | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| Tyrosine kinase inhibitors. 18. 6-Substituted 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as soluble, irreversible inhibitors of the epidermal growth factor receptor. |
AID67282 | Inhibition of phosphorylation of glutamic acid/tyrosine random copolymer by isolated epidermal growth factor receptor (EGFR) | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. |
AID502960 | Inhibition of c-src T338G/S345C double mutant by radioactive phosphotransfer assay | 2007 | Nature chemical biology, Apr, Volume: 3, Issue:4
| Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. |
AID473326 | Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 mutant after 96 hrs by cell titer-glo assay | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
| Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor. |
AID661579 | Drug degradation of the compound assessed as thiol-conjugate formation at 1 uM up to 24 hrs at pH 7.4 in the presence of cysteamine | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides. |
AID661568 | Chemical stability of the compound assessed as compound remaining at 1 uM after 1 hr at pH 7.4 in the presence of DTT | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides. |
AID69714 | Inhibition of human epidermal growth factor receptor (HER-2) using enzyme assay | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
| 6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity. |
AID502965 | Inhibition of human recombinant EGFR expressed in baculovirus-infected Sf9 cells by radioactive phosphotransfer assay | 2007 | Nature chemical biology, Apr, Volume: 3, Issue:4
| Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. |
AID120557 | In vivo activity against A431 xenograft in nude mice, ratio of treated/control median tumor mass at 47 mg/kg ip dose | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. |
AID1303332 | Inhibition of EGFR-TK in human A431 cell lysate assessed as reduction in EGF stimulated kinase activity after 60 mins using biotinylated peptide substrate by ELISA | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Combined inhibition of the EGFR/AKT pathways by a novel conjugate of quinazoline with isothiocyanate. |
AID395851 | Inhibition of autophosphorylation of immunoprecipitated flag-tagged Bmx expressed in human LNCaP cells assessed as incorporation of [32P]ATP at 10 uM pretreated for 2 hrs before transfection by immunoblot analysis | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. |
AID502957 | Inhibition of c-src in by radioactive phosphotransfer assay | 2007 | Nature chemical biology, Apr, Volume: 3, Issue:4
| Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. |
AID719906 | Inhibition of chicken c-Src | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| Irreversible protein kinase inhibitors: balancing the benefits and risks. |
AID121287 | Difference in days for treated (T) and control (C) A431 cell tumors to reach 750 mg at 47 mg/kg ip dose | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. |
AID66614 | Inhibition of autophosphorylation of EGFR in A431 cells | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| Tyrosine kinase inhibitors. 18. 6-Substituted 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as soluble, irreversible inhibitors of the epidermal growth factor receptor. |
AID473324 | Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 mutant after 96 hrs by cell titer-glo assay | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
| Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor. |
AID118101 | In vivo activity against A431 xenograft in nude mice, net reduction in tumor burden at 47 mg/kg ip dose | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. |
AID381969 | Inhibition of EGFR | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR. |
AID392133 | Inhibition of Blk | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. |
AID661567 | Metabolic stability in rat plasma assessed as compound remaining at 1 uM after 24 hrs | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides. |
AID118109 | In vivo activity against H125 xenograft in nude mice, net reduction in tumor burden at 50 mg/kg ip dose | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. |
AID661586 | Drug metabolism in human A549 cell lysate assessed as cysteine adduct level at 10 uM after 1 hr by HPLC-HRMS analysis | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides. |
AID661571 | Chemical stability of the compound assessed as compound remaining at 1 uM after 1 hr at pH 7.4 in the presence of cysteamine | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides. |
AID392132 | Inhibition of JAK3 | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. |
AID69432 | Inhibition of autophosphorylation of cytoplasmic domain of epidermal growth factor receptor | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epi |
AID661565 | Chemical stability of the compound in 0.01 M PBS buffer assessed as compound remaining at 1 uM after 24 hrs at pH 7.4 | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides. |
AID473325 | Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 mutant after 96 hrs by cell titer-glo assay | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
| Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor. |
AID473329 | Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 and Thr790Met mutant after 96 hrs by cell titer-glo assay | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
| Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor. |
AID69422 | Inhibition of epidermal growth factor receptor using enzyme assay | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
| 6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity. |
AID202224 | Inhibition of cell growth of SW620 cell lines using cell-based assay | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
| 6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity. |
AID392135 | Inhibition of Bmx | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. |
AID771339 | Cellular uptake in human A549 cells incubated for 1 hr followed by compound washout measured after 8 hrs by HPLC-MS/MS analysis | 2013 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 23, Issue:19
| Long-lasting inhibition of EGFR autophosphorylation in A549 tumor cells by intracellular accumulation of non-covalent inhibitors. |
AID457029 | Inhibition of human recombinant EGFR expressed in insect cells by time-resolved fluorimetry | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
| Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion. |
AID1469828 | Ratio of Kinact to Ki for chicken c-Src S345C mutant (251 to 533 residues) expressed in Escherichia coli | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
| Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions. |
AID68096 | Inhibition of heregulin-stimulated autophosphorylation of ERBB2 receptor kinase in MDA-MB-453 cells. | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. |
AID381972 | Inhibition of drug-resistant chicken cSrc double mutant expressed in Escherichia coli | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR. |
AID661577 | Drug degradation of the compound assessed as thiol-conjugate formation at 1 uM up to 24 hrs at pH 7.4 in the presence of GSH | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides. |
AID502961 | Inhibition of Fyn expressed in Escherichia coli C43 by radioactive phosphotransfer assay | 2007 | Nature chemical biology, Apr, Volume: 3, Issue:4
| Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. |
AID1303342 | Inhibition of EGFR-TK in human A431 cell lysate assessed as reduction in EGF stimulated kinase activity at highest concentration after 60 mins using biotinylated peptide substrate by ELISA analysis | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Combined inhibition of the EGFR/AKT pathways by a novel conjugate of quinazoline with isothiocyanate. |
AID7911 | Irreversible inhibition of ATP binding site of EGFR (lack of phosphorylated EGFR) in A431 cells 8 hour after washing cells free of the inhibitor) | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. |
AID771340 | Cellular uptake in human A549 cells incubated for 1 hr followed by compound washout measured at 1 hr by HPLC-MS/MS analysis | 2013 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 23, Issue:19
| Long-lasting inhibition of EGFR autophosphorylation in A549 tumor cells by intracellular accumulation of non-covalent inhibitors. |
AID124672 | In vivo activity against A431 xenograft in nude mice, weight change at 47 mg/kg ip dose | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. |
AID271844 | Induction of necrosis in human A431 cells measured as increase of LDH release | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Multitarget-directed drug design strategy: a novel molecule designed to block epidermal growth factor receptor (EGFR) and to exert proapoptotic effects. |
AID67281 | Inhibition of EGF-stimulated autophosphorylation of epidermal growth factor receptor (EGFR) in A431 cells | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. |
AID473523 | Growth inhibition of mouse BA/F3 cells expressing EGFR L858R and Thr790Met mutant after 96 hrs by cell titer-glo assay | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
| Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor. |
AID271838 | Inhibition of EGFR tyrosine kinase activity | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Multitarget-directed drug design strategy: a novel molecule designed to block epidermal growth factor receptor (EGFR) and to exert proapoptotic effects. |
AID392140 | Inhibition of Bmx expressed in mouse BAF3 cells assessed as cytotoxicity | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. |
AID392136 | Inhibition of Btk | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. |
AID473322 | Inhibition of EGFR Leu858Arg mutant by HTRF assay | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
| Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor. |
AID124786 | In vivo activity against H125 xenograft in nude mice, weight change at 50 mg/kg peroral dose | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. |
AID118108 | In vivo activity against H125 xenograft in nude mice, net reduction in tumor burden at 50 mg/kg ip dose | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. |
AID473330 | Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 and Thr790Met mutant after 96 hrs by cell titer-glo assay | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
| Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor. |
AID121288 | Difference in days for treated (T) and control (C) H125 cell tumors to reach 750 mg at 50 mg/kg ip dose | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. |
AID392129 | Inhibition of EGFR | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. |
AID457031 | Inhibition of EGFR autophosphorylation in human A431 cells at 1 uM after 8 hrs by Western blot | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
| Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion. |
AID120554 | In vivo activity against A431 xenograft in nude mice, ratio of treated/control median tumor mass at 150 mg/kg peroral dose | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. |
AID345876 | Inhibition of human recombinant EGFR | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Computational studies of epidermal growth factor receptor: docking reliability, three-dimensional quantitative structure-activity relationship analysis, and virtual screening studies. |
AID502963 | Inhibition of Fyn S349C mutant in expressed in Escherichia coli C43 by radioactive phosphotransfer assay | 2007 | Nature chemical biology, Apr, Volume: 3, Issue:4
| Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. |
AID661569 | Chemical stability of the compound assessed as compound remaining at 1 uM after 1 hr at pH 7.4 in the presence of GSH | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides. |
AID1303341 | Induction of apoptosis in human A431 cells assessed as DNA fragmentation at 2 uM after 24 hrs by ELISA analysis | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Combined inhibition of the EGFR/AKT pathways by a novel conjugate of quinazoline with isothiocyanate. |
AID661566 | Chemical stability of the compound in 0.01 M borate buffer assessed as compound remaining at 1 uM after 24 hrs at pH 9 | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides. |
AID771346 | Ratio of IC50 for wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured after 8 hrs to IC50 for wild type EGFR autophosphorylation in human A549 cells at 1 uM incubated for 1 hr followed by compoun | 2013 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 23, Issue:19
| Long-lasting inhibition of EGFR autophosphorylation in A549 tumor cells by intracellular accumulation of non-covalent inhibitors. |
AID392139 | Inhibition of Blk expressed in mouse BAF3 cells assessed as cytotoxicity | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. |
AID771341 | Inhibition of wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured after 8 hrs by Western blot analysis | 2013 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 23, Issue:19
| Long-lasting inhibition of EGFR autophosphorylation in A549 tumor cells by intracellular accumulation of non-covalent inhibitors. |
AID120560 | In vivo activity against H125 xenograft in nude mice, ratio of treated/control median tumor mass at 50 mg/kg ip dose | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. |
AID395850 | Inhibition of Bmx C496S mutant expressed in mouse BAF3 cells | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. |
AID120561 | In vivo activity against H125 xenograft in nude mice, ratio of treated/control median tumor mass at 50 mg/kg peroral dose | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. |
AID719884 | Irreversible inhibition of EGFR | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| Irreversible protein kinase inhibitors: balancing the benefits and risks. |
AID473321 | Inhibition of wild type EGFR by HTRF assay | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
| Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor. |
AID661562 | Irreversible inhibition of EGFR autophosphorylation in human A549 cells at 1 uM for 1 hr by Western blot analysis | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides. |
AID124785 | In vivo activity against H125 xenograft in nude mice, weight change at 50 mg/kg ip dose | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. |
AID392138 | Inhibition of JAK3 expressed in mouse BAF3 cells assessed as cytotoxicity | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. |
AID771342 | 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 analysis | 2013 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 23, Issue:19
| Long-lasting inhibition of EGFR autophosphorylation in A549 tumor cells by intracellular accumulation of non-covalent inhibitors. |
AID457044 | Cytotoxicity against human SW620 cells after 72 hrs by MTT assay | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
| Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion. |
AID661587 | Drug metabolism in human A549 cell lysate assessed as cysteine adduct level at 10 uM at 4 hrs by HPLC-HRMS analysis | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides. |
AID392405 | Inhibition of wild type Bmx expressed in mouse BAF3 cells assessed as cytotoxicity | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. |
AID1469826 | Inhibition of chicken c-Src S345C mutant (251 to 533 residues) expressed in Escherichia coli by fluorescence assay | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
| Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions. |
AID1303328 | Antiproliferative activity against human A431 cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Combined inhibition of the EGFR/AKT pathways by a novel conjugate of quinazoline with isothiocyanate. |
AID457033 | Inhibition of EGFR autophosphorylation in human A431 cells after 8 hrs by Western blot | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
| Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion. |
AID69562 | Inhibition of phosphorylation of a polyglutamic acid/tyrosine random copolymer by EGFR enzyme (from human A431 carcinoma cell vesicles) | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| Tyrosine kinase inhibitors. 18. 6-Substituted 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as soluble, irreversible inhibitors of the epidermal growth factor receptor. |
AID202681 | Inhibition of cell growth of SKBr3 cell lines using cell-based assay | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
| 6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity. |
AID271840 | Reversibility of antiproliferative activity against human A431 cells after recovery for 68 hrs by MTT assay | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Multitarget-directed drug design strategy: a novel molecule designed to block epidermal growth factor receptor (EGFR) and to exert proapoptotic effects. |
AID67285 | Irreversible inhibition of formation of phosphorylated EGFR enzyme in A431 cells 8 hr after washing cells free of the inhibitor | 2000 | Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
| Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions. |
AID67284 | Inhibition of phosphorylation of a polyglutamic acid/tyrosine random copolymer by EGFR enzyme prepared from human A431 carcinoma cell vesicles by immunoaffinity chromatography | 2000 | Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
| Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions. |
AID392130 | Inhibition of HER2 | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. |
AID118099 | In vivo activity against A431 xenograft in nude mice, net reduction in tumor burden at 150 mg/kg peroral dose | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
| Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. |
AID67283 | Inhibition of EGF-stimulated autophosphorylation of EGFR enzyme in A431 cells detected by immunoblotting | 2000 | Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
| Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions. |
AID473323 | Inhibition of EGFR Leu858Arg and Thr790Met mutant by HTRF assay | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
| Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor. |
AID68098 | Inhibition of autophosphorylation of ERBB2 receptor kinase in MDA-MB 453 cells | 2000 | Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
| Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions. |
AID661561 | Irreversible inhibition of EGFR autophosphorylation in human A549 cells at 1 uM for 1 hr measured 8 hrs post-washout by Western blot analysis | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides. |
AID502964 | Inhibition of Fyn T342G/S349C double mutant expressed in Escherichia coli C43 by radioactive phosphotransfer assay | 2007 | Nature chemical biology, Apr, Volume: 3, Issue:4
| Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. |
AID473328 | Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 and Thr790Met mutant after 96 hrs by cell titer-glo assay | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
| Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor. |
AID473327 | Growth inhibition of mouse BA/F3 cells expressing EGFR L858R mutant after 96 hrs by cell titer-glo assay | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
| Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor. |
AID392137 | Inhibition of Itk | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. |
AID392134 | Inhibition of Lkb1 | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. |
AID771338 | Irreversible inhibition of recombinant EGFR tyrosine kinase (unknown origin) at 1 uM after 60 mins by real-time fluorescence assay | 2013 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 23, Issue:19
| Long-lasting inhibition of EGFR autophosphorylation in A549 tumor cells by intracellular accumulation of non-covalent inhibitors. |
AID7878 | Inhibition of human epidermoid carcinoma xenograft (A431) tumor growth | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
| 6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity. |
AID271839 | Antiproliferative activity against human A431 cells after 72 hrs by MTT assay | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Multitarget-directed drug design strategy: a novel molecule designed to block epidermal growth factor receptor (EGFR) and to exert proapoptotic effects. |
AID395852 | Inhibition of autophosphorylation of immunopurified flag-tagged Bmx in human LNCaP cells assessed as incorporation of [32P]ATP at 10 uM pretreated for 4 hrs before immunopurification by immunoblot analysis | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. |
AID661570 | Chemical stability of the compound assessed as compound remaining at 1 uM after 1 hr at pH 7.4 in the presence of NAC | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides. |
AID381971 | Inhibition of chicken cSrc single mutant expressed in Escherichia coli | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR. |
AID661582 | Irreversible inhibition of EGFR assessed as increase in fluorescence at 1 uM by fluorometry | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides. |
AID457035 | Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
| Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion. |
AID502958 | Inhibition of c-src T338G mutant by radioactive phosphotransfer assay | 2007 | Nature chemical biology, Apr, Volume: 3, Issue:4
| Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1799179 | Src IC50 Determination from Article 10.1016/j.bmc.2008.02.053: \\Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR.\\ | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR. |
AID1795681 | Kinase Inhibition Assay from Article 10.1021/jm000372i: \\Tyrosine kinase inhibitors. 18. 6-Substituted 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as soluble, irreversible inhibitors of the epidermal growth factor receptor.\\ | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| Tyrosine kinase inhibitors. 18. 6-Substituted 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as soluble, irreversible inhibitors of the epidermal growth factor receptor. |
AID1799178 | EGFR IC50 Determination from Article 10.1016/j.bmc.2008.02.053: \\Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR.\\ | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR. |
AID1795646 | Kinase Inhibition Assay from Article 10.1021/jm0005555: \\6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinase | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
| 6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity. |
AID493017 | Wombat Data for BeliefDocking | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
| 6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |