Page last updated: 2024-11-13
tak-063
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
1-(2-fluoro-4-(1H-pyrazol-1-yl)phenyl)-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one: an inhibitor of phosphodiesterase 10A; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
ID Source | ID |
---|---|
PubMed CID | 46848915 |
CHEMBL ID | 3989972 |
SCHEMBL ID | 518714 |
MeSH ID | M000601779 |
Synonyms (43)
Synonym |
---|
KVHRYLNQDWXAGI-UHFFFAOYSA-N |
S8459 |
3k9 , |
1-[2-fluoro-4-(1h-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1h-pyrazol-5-yl)pyridazin-4(1h)-one |
SCHEMBL518714 |
CS-3551 |
balipodect |
HY-12472 |
AC-32915 |
tak 063 |
1-(2-fluoro-4-(1h-pyrazol-1-yl)phenyl)-5-methoxy-3-(1-phenyl-1h-pyrazol-5-yl)pyridazin-4(1h)-one |
1238697-26-1 |
tak063 |
TAK-063 , |
3WYM |
J-690093 |
AKOS026750192 |
EX-A568 |
balipodect [usan:inn:who-dd] |
unii-6650w303h0 |
balipodect [inn] |
1-[2-fluoro-4-(1h-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1h-pyrazol-5-yl)-1,4-dihydropyridazin-4-one |
balipodect [who-dd] |
6650W303H0 , |
4(1h)-pyridazinone, 1-(2-fluoro-4-(1h-pyrazol-1-yl)phenyl)-5-methoxy-3-(1-phenyl-1h-pyrazol-5-yl)- |
balipodect [usan] |
1-(2-fluoro-4-(1h-pyrazol-1-yl)phenyl)-5-methoxy- 3-(1-phenyl-1h-pyrazol-5-yl)pyridazin-4(1h)-one |
mfcd28385852 |
NCGC00390654-01 |
1-(2-fluoro-4-pyrazol-1-ylphenyl)-5-methoxy-3-(2-phenylpyrazol-3-yl)pyridazin-4-one |
FT-0700141 |
DB14774 |
BS-15045 |
c23h17fn6o2 |
CHEMBL3989972 |
BCP14040 |
balipodect (usan/inn) |
D11245 |
SB17000 |
HMS3886P10 |
CCG-268978 |
Q27453873 |
A857435 |
Research Excerpts
Toxicity
TAK-063 was safe and well tolerated at doses up to 1000 mg. Most adverse events were mild or moderate in severity and did not result in discontinuation.
Pharmacokinetics
Excerpt | Reference | Relevance |
---|---|---|
"TAK-063 was safe and well tolerated at doses up to 1000 mg and demonstrated a pharmacokinetic profile supporting once-daily dosing." | ( A phase 1 study of the safety, tolerability, pharmacokinetics, and pharmacodynamics of TAK-063, a selective PDE10A inhibitor. Chrones, L; Gevorkyan, H; Macek, TA; Tsai, M; Xie, J, 2016) | 2.1 |
Bioavailability
Excerpt | Reference | Relevance |
---|---|---|
"3 mg/kg, bioavailability of TAK-063 was 27." | ( Pre-clinical Characterization of Absorption, Distribution, Metabolism and Excretion Properties of TAK-063. Kato, S; Morohashi, A; Sudo, M; Tagawa, Y; Takahashi, J; Tohyama, K, 2018) | 0.99 |
"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 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (7)
Potency Measurements
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 | 26.8370 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
G | Vesicular stomatitis virus | Potency | 15.0916 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 26.8370 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
Interferon beta | Homo sapiens (human) | Potency | 15.0916 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 15.0916 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 15.0916 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 15.0916 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Biological Processes (45)
Molecular Functions (18)
Ceullar Components (22)
Bioassays (5)
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
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. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Research
Studies (24)
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 | 18 (75.00) | 24.3611 |
2020's | 6 (25.00) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Market Indicators
Research Demand Index: 21.72
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 (21.72) All Compounds (24.57) |
Study Types
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 5 (20.83%) | 5.53% |
Reviews | 1 (4.17%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 18 (75.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |