| Assay ID | Title | Year | Journal | Article |
|---|
| AID580194 | Lipophilicity log P of the compound | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
| Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors. |
| AID776745 | Inhibition of HER-2 (unknown origin) using poly-(Glu4-Tyr) as substrate after 1 hr by ELISA-based spectrophotometry | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer. |
| AID776743 | Cytotoxicity against human BT474 cells after 72 hrs by SRB assay | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer. |
| AID580193 | Ratio of IC50 for human BT474 cells to IC50 for Her2 | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
| Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors. |
| AID638084 | Inhibition of EGFR phosphorylation in EGF-stimulated human A431 after 2 hrs by Western blot analysis | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases. |
| AID776728 | Tmax in Wistar rat at 100 mg/kg, po | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer. |
| AID776716 | Relative bioavailability based on AUC (0 to t) in Wistar rat at 100 mg/kg, po | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer. |
| AID776744 | Cytotoxicity against human NCI-N87 cells after 72 hrs by SRB assay | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer. |
| AID776747 | Aqueous solubility of the compound at 25 degC by shake-flask method | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer. |
| AID1219760 | Cmax in healthy human at 250 mg, po administered as single dose | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
| Human metabolism of lapatinib, a dual kinase inhibitor: implications for hepatotoxicity. |
| AID776724 | AUC (0 to t) in Wistar rat at 100 mg/kg, po | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer. |
| AID472051 | Inhibition of EGFR by HTRF assay | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
| Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors. |
| AID776746 | Inhibition of EGFR (unknown origin) using poly-(Glu4-Tyr) as substrate after 1 hr by ELISA-based spectrophotometry | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer. |
| AID1219761 | Tmax in healthy human at 250 mg, po administered as single dose | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
| Human metabolism of lapatinib, a dual kinase inhibitor: implications for hepatotoxicity. |
| AID410943 | Inhibition of EGFR by HTRF assay | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1
| Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors. |
| AID776718 | Elimination half life in Wistar rat at 100 mg/kg, po | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer. |
| AID367179 | Antiproliferative activity against human BT474 cells expressing ErbB2 by MEB assay | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
| Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors. |
| AID1219763 | Half life in healthy human at 250 mg, po administered as single dose | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
| Human metabolism of lapatinib, a dual kinase inhibitor: implications for hepatotoxicity. |
| AID472048 | Inhibition of HER2 in human SKBR3 cells by HTRF assay | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
| Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors. |
| AID638085 | Antitumor activity against human NCI-N87 cells xenografted in athymic mouse assessed as tumor volume at 20 mg/kg, po QD for 14 days measured after 19 days relative to control | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases. |
| AID410945 | Antiproliferative activity against human HN5 cells overexpressing EGFR after 3 days by methylene blue staining | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1
| Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors. |
| AID776730 | Antitumor activity against human NCI-N87 cells xenografted in BALB/c athymic mouse assessed as tumor regression at 200 mg/kg, po qd after 28 days relative to vehicle-treated control | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer. |
| AID776726 | Cmax in Wistar rat at 100 mg/kg, po | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer. |
| AID1219762 | AUC (infinity) in healthy human at 250 mg, po administered as single dose | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
| Human metabolism of lapatinib, a dual kinase inhibitor: implications for hepatotoxicity. |
| AID472050 | Inhibition of EGFR in human A431 cells by HTRF assay | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
| Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors. |
| AID367173 | Inhibition of EGFR | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
| Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors. |
| AID580190 | Inhibition of EGFR by homogeneous time-resolved fluorescence assay | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
| Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors. |
| AID638086 | Antitumor activity against human NCI-N87 cells xenografted in athymic mouse assessed as tumor volume at 80 mg/kg, po QD for 14 days measured after 19 days relative to control | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases. |
| AID367174 | Inhibition of ErbB2 | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
| Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors. |
| AID580191 | Antiproliferative activity against human BT474 cells by methylene blue staining method | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
| Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors. |
| AID580189 | Inhibition of HER2 by homogeneous time-resolved fluorescence assay | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
| Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors. |
| AID410946 | Antiproliferative activity against human BT474 cells overexpressing ERBb2 after 3 days by methylene blue staining | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1
| Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors. |
| AID776720 | Mean residence time in Wistar rat at 100 mg/kg, po | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer. |
| AID776729 | Antitumor activity against human SKOV3 cells xenografted in BALB/c athymic mouse assessed as tumor regression at 200 mg/kg, po qd after 28 days relative to vehicle-treated control | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer. |
| AID638068 | Inhibition of Her-2 by time-resolved fluorescence assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases. |
| AID776722 | AUC (0 to infinity) in Wistar rat at 100 mg/kg, po | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer. |
| AID1219765 | Drug recovery in healthy human feces at 250 mg, po administered as single dose | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
| Human metabolism of lapatinib, a dual kinase inhibitor: implications for hepatotoxicity. |
| AID472049 | Inhibition of HER2 by HTRF assay | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
| Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors. |
| AID367178 | Antiproliferative activity against human HN5 cells expressing EGFR by MEB assay | 2009 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
| Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors. |
| AID410944 | Inhibition of ERBb2 by HTRF assay | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1
| Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors. |
| AID580192 | Aqueous solubility of the compound at pH 6.8 | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
| Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |