Page last updated: 2024-11-12
wk-x-34
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
WK-X-34: inhibitor of P-glycoprotein and BCRP (breast cancer resistance protein); structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 11957988 |
| CHEMBL ID | 247473 |
| MeSH ID | M0499805 |
Synonyms (8)
| Synonym |
|---|
| CHEMBL247473 , |
| n-(2-{4-[2-(6,7-dimethoxy-3,4-dihydro-1h-isoquinolin-2-yl)-ethyl]-phenylcarbamoyl}-phenyl)-3,4-dimethoxy-benzamide |
| n-(2-(4-(2-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1h)-yl)ethyl)phenylcarbamoyl)phenyl)-3,4-dimethoxybenzamide |
| bdbm50305080 |
| 908859-10-9 |
| wk-x-34 |
| n-(2-((4-(2-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1h)-yl)ethyl)phenyl)carbamoyl)phenyl)-3,4-dimethoxybenzamide |
| n-[2-[[4-[2-(6,7-dimethoxy-3,4-dihydro-1h-isoquinolin-2-yl)ethyl]phenyl]carbamoyl]phenyl]-3,4-dimethoxybenzamide |
Research Excerpts
Dosage Studied
A2780/Adr xenograft mice were dosed with mdr1 antisense oligodeoxynucleotides intratumorally for three days. Next, mice were treated with WK-X-34, followed by (99m)Tc-sestamibi injection.
| Excerpt | Relevance | Reference |
|---|---|---|
| " A2780/Adr xenograft mice were dosed with mdr1 antisense oligodeoxynucleotides intratumorally for three days; next, mice were treated with WK-X-34, followed by (99m)Tc-sestamibi injection." | ( 99mTc-Sestamibi, a sensitive probe for in vivo imaging of P-glycoprotein inhibition by modulators and mdr1 antisense oligodeoxynucleotides. Jekerle, V; Piquette-Miller, M; Reilly, RM; Scollard, DA; Wang, JH; Wiese, M, ) | 0.33 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (3)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | IC50 (µMol) | 0.3342 | 0.0002 | 2.3185 | 10.0000 | AID310120; AID310122; AID326367; AID326368; AID364884 |
| Multidrug resistance-associated protein 1 | Homo sapiens (human) | IC50 (µMol) | 20.0000 | 0.0015 | 3.7110 | 9.6600 | AID451989 |
| Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | IC50 (µMol) | 1.2931 | 0.0040 | 1.9666 | 10.0000 | AID364887; AID451987; AID451988 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (39)
Molecular Functions (27)
Ceullar Components (14)
Bioassays (21)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1288622 | Reversal of P-gp-mediated resistance to adriamycin in human K562/A02 cells assessed as adriamycin IC50 at 5 uM after 48 hrs by MTT assay (Rvb = 38.02 +/- 1.65 uM) | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10 | Design, synthesis and biological evaluation of LBM-A5 derivatives as potent P-glycoprotein-mediated multidrug resistance inhibitors. |
| AID326367 | Inhibition of human Pgp in A2780 cells after 30 mins by Hoechst 33342 assay | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5 | Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors. |
| AID451987 | Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1 | Novel lead for potent inhibitors of breast cancer resistance protein (BCRP). |
| AID1481909 | Effect on plasma concentration of doxorubicin in Sprague-Dawley rat at 5 mg/kg, iv co-administered with doxorubicin measured after 8 hrs by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8 | Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance. |
| AID1481890 | Inhibition of P-gp in human K562/A02 cells assessed as accumulation of doxorubicin at 0.1 uM to 5.0 uM after 150 mins by fluorescence spectrophotometric analysis | 2017 | Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8 | Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance. |
| AID1481868 | Cytotoxicity against human K562 cells assessed as cell viability at 1.0 uM after 48 hrs by MTT assay (Rvb = >99%) | 2017 | Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8 | Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance. |
| AID364884 | Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2). |
| AID1481872 | Inhibition of P-gp in human K562/A02 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring fold reduction in doxorubicin IC50 at 1.0 uM after 48 hrs by MTT assay relative to doxorubicin alone | 2017 | Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8 | Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance. |
| AID310122 | Inhibition of P-glycoprotein by Hoechst assay | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | New functional assay of P-glycoprotein activity using Hoechst 33342. |
| AID1288623 | Reversal of P-gp-mediated resistance to adriamycin in human K562/A02 cells assessed as reduction in adriamycin IC50 at 5 uM after 48 hrs by MTT assay relative to control | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10 | Design, synthesis and biological evaluation of LBM-A5 derivatives as potent P-glycoprotein-mediated multidrug resistance inhibitors. |
| AID310121 | Inhibition of P-glycoprotein expressed in MDCK-MDR1 cells by calcein AM assay | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | New functional assay of P-glycoprotein activity using Hoechst 33342. |
| AID1481869 | Cytotoxicity against human K562/A02 cells assessed as cell viability at 1.0 uM after 48 hrs by MTT assay (Rvb = >99%) | 2017 | Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8 | Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance. |
| AID451989 | Inhibition of MRP1 assessed as calcein AM accumulation by fluorescence assay | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1 | Novel lead for potent inhibitors of breast cancer resistance protein (BCRP). |
| AID1288621 | Cytotoxicity against human K562/A02 cells assessed as cell viability after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10 | Design, synthesis and biological evaluation of LBM-A5 derivatives as potent P-glycoprotein-mediated multidrug resistance inhibitors. |
| AID451988 | Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1 | Novel lead for potent inhibitors of breast cancer resistance protein (BCRP). |
| AID1288620 | Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10 | Design, synthesis and biological evaluation of LBM-A5 derivatives as potent P-glycoprotein-mediated multidrug resistance inhibitors. |
| AID326368 | Inhibition of human Pgp in A2780 cells after 30 mins by calcein AM assay | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5 | Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors. |
| AID1481893 | Inhibition of ATPase activity in human P-gp membrane fraction at 0.5 uM in presence of ATP after 1 hr by luciferase reporter gene assay | 2017 | Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8 | Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance. |
| AID1481891 | Inhibition of P-gp mediated efflux in human K562/A02 cells assessed as intracellular Rh123 accumulation at 1.0 uM measure up to 90 mins by flow cytometric analysis | 2017 | Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8 | Design, Synthesis, and Pharmacological Characterization of N-(4-(2 (6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amine Derivatives: Novel Inhibitors Reversing P-Glycoprotein-Mediated Multidrug Resistance. |
| AID310120 | Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | New functional assay of P-glycoprotein activity using Hoechst 33342. |
| AID364887 | Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2). |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (9)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 5 (55.56) | 29.6817 |
| 2010's | 4 (44.44) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 11.97
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 (11.97) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 10 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||