| ID Source | ID |
|---|---|
| PubMed CID | 78357766 |
| CHEMBL ID | 4303250 |
| SCHEMBL ID | 16065674 |
| MeSH ID | M0592039 |
| Synonym |
|---|
| S7318 |
| hth-01-015 , |
| CS-3344 |
| HY-12334 |
| SCHEMBL16065674 |
| AC-32959 |
| 1613724-42-7 |
| gtpl8977 |
| hth01-015 |
| AKOS026750455 |
| hth 01 015 |
| EX-A1038 |
| 4,5,13-trimethyl-2-((1-(piperidin-4-yl)-1h-pyrazol-4-yl)amino)-5h-naphtho[2,3-e]pyrimido[5,4-b][1,4]diazepin-6(13h)-one |
| hth 01-015 |
| 5,13-dihydro-4,5,13-trimethyl-2-[[1-(4-piperidinyl)-1h-pyrazol-4-yl]amino]-6h-naphtho[2,3-e]pyrimido[5,4-b][1,4]diazepin-6-one |
| 2,7,9-trimethyl-5-{[1-(piperidin-4-yl)-1h-pyrazol-4-yl]amino}-2,4,6,9-tetraazatetracyclo[9.8.0.0(3),?.0(1)(3),(1)?]nonadeca-1(19),3,5,7,11,13,15,17-octaen-10-one |
| AS-75146 |
| hth-01-015, >=98% (hplc) |
| NCGC00389591-02 |
| FT-0700228 |
| 4,5,13-trimethyl-2-((1-(piperidin-4-yl)-1h-pyrazol-4-yl)amino)-5,13-dihydro-6h-naphtho[2,3-e]pyrimido[5,4-b][1,4]diazepin-6-one |
| Q27077996 |
| BCP14400 |
| 2,7,9-trimethyl-5-[(1-piperidin-4-ylpyrazol-4-yl)amino]-2,4,6,9-tetrazatetracyclo[9.8.0.03,8.013,18]nonadeca-1(19),3,5,7,11,13,15,17-octaen-10-one |
| NCGC00389591-08 |
| CCG-269434 |
| CHEMBL4303250 , |
| 2,7,9-trimethyl-5-[(1-piperidin-4-ylpyrazol-4-yl)amino]-2,4,6,9-tetrazatetracyclo[9.8.0.0^{3,8.0^{13,18]nonadeca-1(19),3,5,7,11,13,15,17-octaen-10-one |
| A858199 |
| bdbm50587671 |
| 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 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 11.9877 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 1.0684 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 15.0916 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 1.0684 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 1.0684 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 1.0684 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 1.0684 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [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) |
|---|---|---|---|---|---|---|---|
| NUAK family SNF1-like kinase 1 | Homo sapiens (human) | IC50 (µMol) | 0.1000 | 0.0013 | 0.2918 | 5.0900 | AID1845553 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1755885 | Inhibition of NUAK2 (unknown origin) at 10 uM using CHKtide as substrate in presence of ATP measured after 60 mins by ADP-Glo assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer. |
| AID1755884 | Inhibition of NUAK1 (unknown origin) at 10 uM using CHKtide as substrate in presence of ATP measured after 60 mins by ADP-Glo assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer. |
| AID1845553 | Inhibition of N-terminal GST-tagged wild type human NUAK1 expressed in Escherichia coli DH5alpha incubated for 30 mins in presence of gamma-[32P]ATP by cerenkov counting analysis | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1 | Development and Therapeutic Potential of NUAKs Inhibitors. |
| AID1755886 | Antiproliferative activity against human U2OS cells assessed as reduction in cell viability at 10 uM measured after 1 to 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer. |
| 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. |
| 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. |
| 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. |
| AID1345741 | Human NUAK family kinase 1 (NuaK subfamily) | 2014 | The Biochemical journal, Jan-01, Volume: 457, Issue:1 | Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. |
| [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 | 0 (0.00) | 29.6817 |
| 2010's | 2 (33.33) | 24.3611 |
| 2020's | 4 (66.67) | 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 moderate demand-to-supply ratio for research on this compound.
| This Compound (20.35) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (16.67%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (83.33%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||