AZM475271: a Src family kinase inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 5330175 |
| CHEMBL ID | 426161 |
| SCHEMBL ID | 3195079 |
| MeSH ID | M0493488 |
| Synonym |
|---|
| methoxy aniline 7 |
| m475271 |
| bdbm6198 |
| n-(2-chloro-5-methoxyphenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine |
| CHEMBL426161 |
| n-(2-chloro-5-methoxyphenyl)-6-methoxy-7-((1-methylpiperidin-4-yl)methoxy)quinazolin-4-amine |
| 4-quinazolinamine, n-(2-chloro-5-methoxyphenyl)-6-methoxy-7-((1-methyl-4-piperidinyl)methoxy)- |
| unii-0361z8214o |
| azm-475271 |
| m-475271 |
| 0361z8214o , |
| 476159-98-5 |
| azm 475271 |
| azm 475271 [who-dd] |
| SCHEMBL3195079 |
| c23h27cln4o3 |
| n-(2-chloro-5-methoxyphenyl)-6-methoxy |
| azm475271 |
| HY-13561 |
| AKOS024457900 |
| DTXSID00197222 |
| NCGC00370984-01 |
| Q21547118 |
| A914756 |
| F85123 |
| MS-27972 |
| NCGC00370984-02 |
| BUA15998 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " AZD0530 is a potent inhibitor of tumor growth in a c-Src-transfected 3T3-fibroblast xenograft model in vivo and led to a significant increase in survival in a highly aggressive, orthotopic model of human pancreatic cancer when dosed orally once daily." | ( N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. Allen, J; Breed, J; Costello, G; Curwen, J; Fennell, M; Green, TP; Hennequin, LF; Lambert-van der Brempt, C; Morgentin, R; Norman, RA; Olivier, A; Otterbein, L; Plé, PA; Warin, N, 2006) | 0.33 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| PPM1D protein | Homo sapiens (human) | Potency | 20.8212 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| Interferon beta | Homo sapiens (human) | Potency | 20.8212 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Fibroblast growth factor receptor 1 | Homo sapiens (human) | IC50 (µMol) | 0.0100 | 0.0002 | 0.9420 | 10.0000 | AID1795857 |
| Proto-oncogene tyrosine-protein kinase Src | Homo sapiens (human) | IC50 (µMol) | 0.2721 | 0.0002 | 0.5335 | 10.0000 | AID1545500; AID1795857; AID1795858; AID1796878; AID272211; AID272213 |
| Vascular endothelial growth factor receptor 1 | Homo sapiens (human) | IC50 (µMol) | 0.0100 | 0.0001 | 0.2914 | 7.0000 | AID1795857 |
| Vascular endothelial growth factor receptor 2 | Homo sapiens (human) | IC50 (µMol) | 0.4060 | 0.0000 | 0.4830 | 8.8000 | AID1795857; AID1795858; AID1796878; AID272212 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID272218 | Aqueous solubility at pH 7.4 | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. |
| AID1612813 | Inhibition of CSK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID1612828 | Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID272213 | Antiproliferative activity against mouse NIH3T3 cell line transfected with c-SRC | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. |
| AID272248 | Half life in male dog | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. |
| AID1612814 | Inhibition of Fyn A (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID1612826 | Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID1545500 | Inhibition of human recombinant Src expressed in baculovirus infected Sf9 insect cells assessed as reduction in phosphorylation of polyglutamic acid/tyrosine incubated for 15 mins by ELISA | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry. |
| AID1612810 | Inhibition of ABL1 (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID272211 | Inhibition of human c-Src in NIH3T3 cells | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. |
| AID1612816 | Inhibition of Lyn B (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID272217 | Lipophilicity, log D at pH 7.4 | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. |
| AID272256 | Clearance in male dog | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. |
| AID1612830 | Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID272221 | Percent of unbound ligand in rat plasma | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. |
| AID1612812 | Inhibition of BTK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID1612817 | Inhibition of SRC (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID1612829 | Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID1612827 | Antiproliferative activity against p53-/- human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID272212 | Inhibition of KDR | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. |
| AID272214 | Inhibition of A549 cell migration by microdroplet migration assay | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. |
| AID272216 | Dissociation constant, pKa of the basic side chain of compound | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. |
| AID1612811 | Inhibition of BRK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID272252 | Volume of distribution in male dog | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. |
| AID1612815 | Inhibition of LCK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID272260 | Bioavailability in male dog | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. |
| AID272269 | Inhibition of liver metastasis formation in nude mouse xenografted with L3.6p1 at 25 mg/kg/day, po | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. |
| AID1795857 | In Vitro Src Kinase Inhibition Test from Article 10.1021/jm030317k: \\Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src.\\ | 2004 | Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4 | Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src. |
| AID1796878 | In Vitro Src Kinase Inhibition Test from Article 10.1021/jm060434q: \\N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. |
| AID1795858 | VEGF-R Kinase Inhibition Assay from Article 10.1021/jm030317k: \\Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src.\\ | 2004 | Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4 | Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (22.22) | 29.6817 |
| 2010's | 4 (44.44) | 24.3611 |
| 2020's | 3 (33.33) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (12.70) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (11.11%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 8 (88.89%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||