Page last updated: 2024-12-08
l 734005
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
5-chloro-3-phenylthioindole-2-carboxamide: structure given in first source; an inhibitor of HIV-1 reverse transcriptase [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 189896 |
| CHEMBL ID | 286759 |
| SCHEMBL ID | 2343449 |
| MeSH ID | M0221415 |
Synonyms (19)
| Synonym |
|---|
| 148473-16-9 |
| 5-chloro-3-(phenylsulfanyl)-1h-indole-2-carboxamide |
| bdbm2284 |
| 5cl3phs-2indolconh2 inhibitor 10 |
| 5cl3phs-2indolconh2 |
| 5-chloro-3-(phenylthio)-2-indolecarboxamide |
| 5-chloro-3-phenylsulfanyl-1h-indole-2-carboxamide |
| CHEMBL286759 |
| 1h-indole-2-carboxamide, 5-chloro-3-(phenylthio)- |
| 5-chloro-3-phenylthioindole-2-carboxamide |
| l 734005 |
| l-734,005 |
| l 734,005 |
| l-734005 |
| SCHEMBL2343449 |
| DTXSID10163993 |
| FT-0758550 |
| 5-chloro-3-(phenylthio)-1h-indole-2-carboxamide; 1h-indole-2-carboxamide, 5-chloro-3-(phenylthio)-; 5-chloro-3-phenylthioindole-2-carboxamide |
| BCP29746 |
Research Excerpts
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| " Good oral bioavailability was observed in rhesus monkeys upon oral dosing of 1 as a suspension in methocel." | ( 5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase. Balani, SK; Ciccarone, TM; Condra, JH; Emini, EA; Goldman, ME; Greenlee, WJ; Kauffman, LR; MacTough, SC; Rooney, CS; Williams, TM, 1993) | 0.29 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " Good oral bioavailability was observed in rhesus monkeys upon oral dosing of 1 as a suspension in methocel." | ( 5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase. Balani, SK; Ciccarone, TM; Condra, JH; Emini, EA; Goldman, ME; Greenlee, WJ; Kauffman, LR; MacTough, SC; Rooney, CS; Williams, TM, 1993) | 0.29 |
| "Rhesus monkeys were dosed orally with 10 mg/kg 5-chloro-3-phenylthioindole-2-carboxamide (L-734,005), a nonnucleoside human immunodeficiency virus type 1 (HIV-1) reverse transcriptase inhibitor, in polyethylene glycol 300." | ( Biotransformation of 5-chloro-3-phenylthioindole-2-carboxamide (L-734,005) in rhesus monkeys and rat liver microsomes to a potent HIV-1 reverse transcriptase inhibitor. Balani, SK; Goldman, ME; Kauffman, LR; O'Brien, JA; Olah, TV; Pitzenberger, SM; Ramjit, HG; Schorn, TW; Smith, SJ; Varga, SL, ) | 0.13 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (4)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Gag-Pol polyprotein | HIV-1 M:B_HXB2R | IC50 (µMol) | 0.8380 | 0.0006 | 0.9141 | 8.3200 | AID1795381 |
| Adenosine receptor A2a | Homo sapiens (human) | IC50 (µMol) | 1.0400 | 0.0007 | 1.5594 | 10.0000 | AID3047 |
| Adenosine receptor A2b | Homo sapiens (human) | IC50 (µMol) | 1.0400 | 0.0005 | 0.3023 | 1.5000 | AID3047 |
| Protease | Human immunodeficiency virus 1 | IC50 (µMol) | 0.8380 | 0.0001 | 0.2248 | 7.3200 | AID200169; AID3047; AID94311 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (63)
Molecular Functions (12)
Ceullar Components (13)
Bioassays (10)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID106775 | Inhibition of cell culture in MT-4 cells | 1993 | Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9 | 5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase. |
| AID94311 | Compound is evaluated in vitro for the inhibition single mutant of HIV-1 RT (K103 N) | 1993 | Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9 | 5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase. |
| AID3047 | Compound is evaluated in vitro for the inhibition single mutant of HIV-1 RT (Y181C) | 1993 | Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9 | 5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase. |
| AID106942 | Anti-HIV activity protecting MT-4 cells from HIV-1 induced cytopathogenicity | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies. |
| AID246359 | Protection of infected MT-4 cells from wtIIIB-HIV-1-induced cytopathogenicity | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1 | Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives. |
| AID232923 | Selectivity ratio of CC50/EC50 | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies. |
| AID265460 | Antiviral activity against HIV1 | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11 | Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide. |
| AID106747 | Cytotoxicity, reducing the vaiability of mock-infected cells | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies. |
| AID200169 | Inhibition of HIV-1 RT using rC-dG as template | 1993 | Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9 | 5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase. |
| AID1795381 | HIV-1 RT Assay from Article 10.1021/jm00061a022: \\5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.\\ | 1993 | Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9 | 5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (6)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (16.67) | 18.2507 |
| 2000's | 3 (50.00) | 29.6817 |
| 2010's | 2 (33.33) | 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: 12.66
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 (12.66) 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 | 7 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||