Page last updated: 2024-12-11
bvt2733
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 6918651 |
| CHEMBL ID | 553071 |
| CHEMBL ID | 463978 |
| SCHEMBL ID | 368251 |
| MeSH ID | M0450206 |
Synonyms (36)
| Synonym |
|---|
| bvt-2733 |
| 3-chloro-2-methyl-n-{4-[2-(4-methyl-piperazin-1-yl)-2-oxo-ethyl]-thiazol-2-yl}-benzenesulfonamide; hydrochloride (bvt.2733) |
| bdbm50117900 |
| CHEMBL553071 , |
| CHEMBL463978 , |
| 3-chloro-2-methyl-n-[4-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1,3-thiazol-2-yl]benzenesulfonamide |
| 376640-41-4 |
| unii-2egd70329u |
| piperazine, 1-((2-(((3-chloro-2-methylphenyl)sulfonyl)amino)-4-thiazolyl)acetyl)-4-methyl- |
| benzenesulfonamide, 3-chloro-2-methyl-n-(4-(2-(4-methyl-1-piperazinyl)-2-oxoethyl)-2-thiazolyl)- |
| 2egd70329u , |
| SCHEMBL368251 |
| 3-chloro-2-methyl-n-(4-(2-(4-methylpiperazin-1-yl)-2-oxoethyl)thiazol-2-yl)benzenesulfonamide |
| c17h21cln4o3s2 |
| AC-35247 |
| HY-18054 |
| bvt 2733 |
| bvt.2733 |
| AKOS026750331 |
| DTXSID00191083 |
| 3-chloro-2-methyl-n-{4-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1,3-thiazol-2-yl}benzene-1-sulfonamide |
| 3-chloro-2-methyl-n-[4-[2-(4-methyl-1-piperazinyl)-2-oxoethyl]-1,3-thiazol-2-yl]benzenesulfonamide |
| mfcd13152134 |
| bvt.2733, >=98% (hplc) |
| NCGC00386635-01 |
| bvt2733 |
| bvt 2733(bvt.2733) |
| BCP15782 |
| F11468 |
| EX-A2997 |
| Q27254628 |
| AS-56001 |
| S0209 |
| A903160 |
| BB179811 |
| BQA64041 |
Research Excerpts
Bioavailability
| 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 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (11)
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 | 15.0916 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 21.3174 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Interferon beta | Homo sapiens (human) | Potency | 21.3174 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 21.3174 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 21.3174 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 21.3174 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| 17-beta-hydroxysteroid dehydrogenase type 1 | Homo sapiens (human) | IC50 (µMol) | 6.6705 | 0.0075 | 1.3612 | 5.5000 | AID366733; AID366734 |
| Corticosteroid 11-beta-dehydrogenase isozyme 1 | Homo sapiens (human) | IC50 (µMol) | 3.3410 | 0.0041 | 1.0667 | 10.0000 | AID1151397 |
| 17-beta-hydroxysteroid dehydrogenase type 2 | Homo sapiens (human) | IC50 (µMol) | 0.0960 | 0.0960 | 3.9400 | 9.9000 | AID366735 |
| Corticosteroid 11-beta-dehydrogenase isozyme 1 | Mus musculus (house mouse) | IC50 (µMol) | 0.0960 | 0.0020 | 0.2410 | 3.7600 | AID1151396 |
| Corticosteroid 11-beta-dehydrogenase isozyme 2 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0004 | 0.6367 | 6.4300 | AID1151395 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (71)
Molecular Functions (37)
Ceullar Components (24)
Bioassays (12)
| 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. |
| 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. |
| AID1151395 | Inhibition of human 11beta-HSD2 | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
| AID366734 | Inhibition of human 11beta-HSD2 | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Blockade of glucocorticoid excess at the tissue level: inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes. |
| AID1151398 | Oral bioavailability in mouse | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
| AID1151396 | Inhibition of mouse 11beta-HSD1 | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
| AID366733 | Inhibition of human 11beta-HSD1 | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Blockade of glucocorticoid excess at the tissue level: inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes. |
| AID1151397 | Inhibition of human 11beta-HSD1 | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
| AID366735 | Inhibition of mouse 11beta-HSD1 | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Blockade of glucocorticoid excess at the tissue level: inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (5)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (20.00) | 29.6817 |
| 2010's | 2 (40.00) | 24.3611 |
| 2020's | 2 (40.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 13.28
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 (13.28) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (20.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 4 (80.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||