| Assay ID | Title | Year | Journal | Article |
|---|
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1250397 | Elimination half life in Han Wistar rat at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250399 | Volume of distribution at steady state in Han Wistar rat at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250374 | Elimination half life in Han Wistar rat at 2 mg/kg, po | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250431 | Inhibition of CYP2C9 (unknown origin) | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250408 | Inhibition of EGFR L858R mutant (unknown origin) by HTRF assay in presence of Km of ATP | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1821425 | Unbound brain-to-plasma concentration ratio in rat at 2.5 uM incubated for 4 hrs by equilibrium dialysis method | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
| Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors. |
| AID1420693 | Induction of apoptosis in human H3255 cells assessed as late apoptotic cells at 1000 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 1.77%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1420706 | Induction of apoptosis in human A431 cells assessed as necrotic cells at 1000 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 4.16%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1420729 | Induction of apoptosis in human NCI-H1975 cells assessed as late apoptotic cells at 1000 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 1.91%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1420727 | Induction of apoptosis in human NCI-H1975 cells assessed as viable cells at 1000 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 93.7%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1250410 | Inhibition of EGFR (unknown origin) by HTRF assay in presence of Km of ATP | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1420666 | Antiproliferative activity against human A431 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1420718 | Induction of apoptosis in human HCC827 cells assessed as necrotic cells at 1000 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 1.41%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1420716 | Induction of apoptosis in human HCC827 cells assessed as early apoptotic cells at 1000 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 2.83%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1250426 | Inhibition of recombinant Src (unknown origin) after 40 mins by scintillation counting analysis in presence of [gamma33P]-ATP | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250375 | Oral bioavailability in Han Wistar rat at 2 mg/kg | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250387 | Ratio of unbound AUC (0 to 7 hrs) in brain to blood of Han Wistar rat at 2 mg/kg, po by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250415 | Ratio IC50 for EGFR in human H838 cells to IC50 for EGFR exon19 deletion mutant in human PC9 cells | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250446 | Fraction unbound in cynomolgus monkey plasma at 150 MBq, iv by positron emission tomography | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250418 | Inhibition of recombinant Flt (unknown origin) at 1 uM after 40 mins by scintillation counting analysis in presence of [gamma33P]-ATP | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250412 | Antiproliferative against human PC9 cells expressing EGFR exon19 deletion mutant after 72 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1586911 | Inhibition of human EGFR using poly[Glu:Tyr] (4:1) as substrate measured after 20 mins in presence of [gamma33P]ATP by filter-binding assay | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
| Acrylamide Functional Group Incorporation Improves Drug-like Properties: An Example with EGFR Inhibitors. |
| AID1250435 | Inhibition of CYP3A5 (unknown origin) | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1420704 | Induction of apoptosis in human A431 cells assessed as early apoptotic cells at 1000 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 3.40%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1250444 | Cmax in beagle dog at 2 mg/kg, po | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250407 | Inhibition of EGFR exon19 deletion mutant (unknown origin) by HTRF assay in presence of 2mM of ATP | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250365 | Inhibition of EGFR exon19 deletion mutant phosphorylation in human PC9 cells | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250437 | Elimination half life in beagle dog at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1586915 | 1-Octanol-buffer partition coefficient, log D of compound at pH 7.4 after 24 hrs by shake-flask method | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
| Acrylamide Functional Group Incorporation Improves Drug-like Properties: An Example with EGFR Inhibitors. |
| AID1250448 | Fraction unbound in cynomolgus monkey brain at 155 MBq, iv by positron emission tomography | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250427 | Inhibition of recombinant D2 receptor (unknown origin) | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1420665 | Antiproliferative activity against human H3255 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1250405 | Inhibition of EGFR exon19 deletion mutant (unknown origin) by HTRF assay in presence of Km of ATP | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1586913 | Thermodynamic solubility of the compound in pH 7.4 phosphate buffered saline measured after 24 hrs by UV-HPLC analysis | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
| Acrylamide Functional Group Incorporation Improves Drug-like Properties: An Example with EGFR Inhibitors. |
| AID1250386 | AUC (0 to 7 hrs) in Han Wistar rat blood at 2 mg/kg, po by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1420705 | Induction of apoptosis in human A431 cells assessed as late apoptotic cells at 1000 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 2.11%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1250398 | Clearance in Han Wistar rat at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250419 | Inhibition of recombinant Fyn (unknown origin) at 1 uM after 40 mins by scintillation counting analysis in presence of [gamma33P]-ATP | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250445 | Fraction unbound in cynomolgus monkey brain at 150 MBq, iv by positron emission tomography | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250436 | AUC(0 to 24 hrs) in beagle dog at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250401 | AUC(0 to 24 hrs) in Han Wistar rat at 2 mg/kg, po | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250440 | AUC(0 to 24 hrs) in beagle dog at 2 mg/kg, po | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250406 | Inhibition of EGFR (unknown origin) by HTRF assay in presence of 2 mM of ATP | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250451 | Antitumor activity against human PC9 cells expressing EGFR exon19 deletion mutant xenografted in mouse measured after 4 weeks | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250433 | Inhibition of CYP2D6 (unknown origin) | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250411 | Inhibition of EGFR phosphorylation in human H838 cells | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250416 | Ratio IC50 for EGFR in human H838 cells to IC50 for EGFR L858R mutant in human PC9 cells | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250370 | Fraction unbound in Han Wistar rat blood at 5 uM by equilibrium dialysis method | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250453 | Antitumor activity against human PC9 cells expressing EGFR exon19 deletion mutant xenografted in mouse assessed as tumor regression at 15 mg/kg, qd measured after 4 weeks | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250439 | Volume of distribution at steady state in beagle dog at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250438 | Clearance in beagle dog at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250423 | Inhibition of recombinant Src (unknown origin) at 1 uM after 40 mins by scintillation counting analysis in presence of [gamma33P]-ATP | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250443 | Tmax in beagle dog at 2 mg/kg, po | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250380 | Inhibition of EGFR L858R mutant phosphorylation in human H3255 cells | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1420694 | Induction of apoptosis in human H3255 cells assessed as necrotic cells at 1000 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 7.06%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1420669 | Antiproliferative activity against human PC9 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1250371 | Fraction unbound in Han Wistar rat brain at 5 uM by equilibrium dialysis method | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250447 | Ratio of fraction unbound in brain to plasma of cynomolgus monkey at 150 MBq, iv by positron emission tomography | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250409 | Inhibition of EGFR L858R mutant (unknown origin) by HTRF assay in presence of 2 mM of ATP | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250366 | Permeability from apical to basolateral side in MDCK2-MDR1 cells | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250442 | Oral bioavailability in beagle dog at 2 mg/kg | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1420717 | Induction of apoptosis in human HCC827 cells assessed as late apoptotic cells at 1000 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 1.15%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1250428 | Inhibition of CYP1A2 (unknown origin) | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1420728 | Induction of apoptosis in human NCI-H1975 cells assessed as early apoptotic cells at 1000 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 2.07%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1420692 | Induction of apoptosis in human H3255 cells assessed as early apoptotic cells at 1000 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 3.22%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1250388 | Ratio of unbound AUC (0 to 7 hrs) in CSF to blood of Han Wistar rat at 2 mg/kg, po by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250421 | Inhibition of recombinant Lck (unknown origin) at 1 uM after 40 mins by scintillation counting analysis in presence of [gamma33P]-ATP | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250456 | Antitumor activity against human PC9 cells expressing EGFR exon19 deletion mutant xenografted in mouse assessed as decrease in tumor area in brain at 7.5 mg/kg, qd | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250457 | Antitumor activity against human PC9 cells expressing EGFR exon19 deletion mutant xenografted in mouse assessed as decrease in tumor area in brain at 15 mg/kg, qd | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1586914 | Thermodynamic solubility of the compound in 1-octanol solution measured after 24 hrs by UV-HPLC analysis | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
| Acrylamide Functional Group Incorporation Improves Drug-like Properties: An Example with EGFR Inhibitors. |
| AID1250434 | Inhibition of CYP3A4 (unknown origin) | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1420737 | Cell cycle arrest in human NCI-H1975 cells assessed as accumulation at G2/M phase at 500 nM after 24 hrs by propidium iodide staining based flow cytometry | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1250420 | Inhibition of recombinant KDR (unknown origin) at 1 uM after 40 mins by scintillation counting analysis in presence of [gamma33P]-ATP | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250384 | AUC (0 to 7 hrs) in Han Wistar rat CSF at 2 mg/kg, po by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1821424 | Efflux ratio of apparent permeability across basolateral to apical side over apical to basolateral side in human MDR1-transfected dog MDCKII-MDR1 cells at 0.1 to 1 uM measured after 3 hrs by LC/MS/MS analysis | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
| Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors. |
| AID1250430 | Inhibition of CYP2C8 (unknown origin) | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250425 | Inhibition of recombinant KDR (unknown origin) after 40 mins by scintillation counting analysis in presence of [gamma33P]-ATP | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250422 | Inhibition of recombinant Lyn (unknown origin) at 1 uM after 40 mins by scintillation counting analysis in presence of [gamma33P]-ATP | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1420703 | Induction of apoptosis in human A431 cells assessed as viable cells at 1000 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 90.3%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1420730 | Induction of apoptosis in human NCI-H1975 cells assessed as necrotic cells at 1000 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 2.31%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1250458 | Antitumor activity against human PC9 cells expressing EGFR exon19 deletion mutant xenografted in mouse assessed as modulation of pEGFR expression in brain at 15 mg/kg administered as single dose measured after 1 hr by immunohistochemical analysis | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250403 | Intrinsic clearance in human hepatocytes | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1420667 | Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1420668 | Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1250424 | Inhibition of recombinant Yes (unknown origin) at 1 uM after 40 mins by scintillation counting analysis in presence of [gamma33P]-ATP | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250449 | Fraction unbound in cynomolgus monkey plasma at 155 MBq, iv by positron emission tomography | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1420715 | Induction of apoptosis in human HCC827 cells assessed as viable cells at 1000 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 94.6%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1586912 | Cytotoxicity against human A549 cells after 72 hrs by MTT assay | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
| Acrylamide Functional Group Incorporation Improves Drug-like Properties: An Example with EGFR Inhibitors. |
| AID1821518 | Unbound brain-to-plasma concentration ratio in non-human primates by positron emission tomography | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
| Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors. |
| AID1250450 | Ratio of fraction unbound in brain to plasma of cynomolgus monkey at 155 MBq, iv by positron emission tomography | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250432 | Inhibition of CYP2C19 (unknown origin) | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250417 | Inhibition of recombinant EpHB4 (unknown origin) at 1 uM after 40 mins by scintillation counting analysis in presence of [gamma33P]-ATP | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250413 | Antiproliferative against human H3255 cells expressing EGFR L858R mutant after 72 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250452 | Antitumor activity against human PC9 cells expressing EGFR exon19 deletion mutant xenografted in mouse assessed as tumor growth inhibition at 7.5 mg/kg, qd measured after 4 weeks | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1420691 | Induction of apoptosis in human H3255 cells assessed as viable cells at 1000 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 87.9%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1250414 | Antiproliferative against human NCI-H838 cells expressing EGFR wild-type after 72 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250455 | Toxicity in PC9 cells expressing EGFR exon19 deletion mutant xenografted mouse assessed as loss of body weight at 15 mg/kg, qd | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250429 | Inhibition of CYP2B6 (unknown origin) | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250454 | Toxicity in PC9 cells expressing EGFR exon19 deletion mutant xenografted mouse assessed as loss of body weight at 7.5 mg/kg, qd | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250404 | Cmax in Han Wistar rat at 2 mg/kg, po at 1 hr | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1420670 | Cytotoxicity against human BEAS2B cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer. |
| AID1250367 | Efflux ratio of permeability from basolateral to apical side over apical to basolateral side in MDCK2-MDR1 cells | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250382 | AUC (0 to 7 hrs) in Han Wistar rat brain at 2 mg/kg, po by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1250441 | Elimination half life in beagle dog at 2 mg/kg, po | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |