| ID Source | ID |
|---|---|
| PubMed CID | 148193 |
| SCHEMBL ID | 94807 |
| MeSH ID | M0446730 |
| Synonym |
|---|
| nsc702818 |
| r 115777 |
| 192185-68-5 |
| 2(1h)-quinolinone, 6-[amino(4-chlorophenyl)(1-methyl-1h-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methyl- |
| (b)-6-[amino(4-chlorophenyl)-1-methyl-1h-imidazol- 5-yl)methyl]-4-(3-chlorophenyl)-1-methyl-2(1h)-quinolinone |
| r-115777 | zarnestra |
| bdbm14434 |
| 6-[amino(4-chlorophenyl)(1-methyl-1h-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methyl-1,2-dihydroquinolin-2-one |
| 6-[amino(4-chlorophenyl)(1-methyl-1h-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2(1h)-one |
| 6-(amino(4-chlorophenyl)(1-methyl-1h-imidazol-5-yl)methyl)-4-(3-chlorophenyl)-1-methylquinolin-2(1h)-one |
| 6-[amino-(4-chlorophenyl)-(3-methylimidazol-4-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2-one |
| A25612 |
| 6-[(r)-amino(4-chlorophenyl)(1-methyl-1h-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methyl-2(1h)-quinolinone |
| nsc 702818 |
| 2(1h)-quinolinone, 6-(amino(4-chlorophenyl)(1-methyl-1h-imidazol-5-yl)methyl)-4-(3-chlorophenyl)-1-methyl- |
| 6-(amino(4-chlorophenyl)(1-methyl-1h-imidazol-5-yl)methyl)-4-(3-chlorophenyl)-1-methyl-2(1h)-quinolinone |
| FT-0675247 |
| SCHEMBL94807 |
| NCGC00389510-02 |
| Q7808830 |
| tipifarnib,freebase |
| DTXSID50861481 |
| AKOS040747327 |
| 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) |
|---|---|---|---|---|---|---|---|
| PPM1D protein | Homo sapiens (human) | Potency | 16.5388 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| Interferon beta | Homo sapiens (human) | Potency | 16.5388 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
| [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) |
|---|---|---|---|---|---|---|---|
| Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Bos taurus (cattle) | IC50 (µMol) | 0.5503 | 0.0005 | 0.2819 | 1.1000 | AID1797222; AID1797224 |
| Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 0.0044 | 0.0005 | 0.4716 | 10.0000 | AID1797478 |
| Protein farnesyltransferase subunit beta | Bos taurus (cattle) | IC50 (µMol) | 0.5503 | 0.0005 | 0.1183 | 1.1000 | AID1797222; AID1797224 |
| Protein farnesyltransferase subunit beta | Homo sapiens (human) | IC50 (µMol) | 0.0044 | 0.0005 | 0.2177 | 2.5000 | AID1797478 |
| Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0170 | 0.0019 | 0.5451 | 2.9860 | AID1797011 |
| Geranylgeranyl transferase type-1 subunit beta | Bos taurus (cattle) | IC50 (µMol) | 0.5503 | 0.0007 | 0.6618 | 1.1000 | AID1797222; AID1797224 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| 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. |
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| 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. |
| 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. |
| AID1797011 | PfPFT and Rat PFT IC50 Determination from Article 10.1021/jm0491039: \\Protein farnesyltransferase inhibitors exhibit potent antimalarial activity.\\ | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11 | Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. |
| AID1797478 | FTase Scintillation Proximity Assay from Article : \\Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro.\\ | 2001 | Cancer research, Jan-01, Volume: 61, Issue:1 | Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro. |
| AID1797222 | FTase Activity Assay from Article 10.1016/j.bmcl.2005.03.049: \\Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity.\\ | 2005 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11 | Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity. |
| AID1797224 | FTase Activity Assay from Article 10.1016/j.bmcl.2005.02.062: \\Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors.\\ | 2005 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8 | Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors. |
| [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 | 4 (50.00) | 29.6817 |
| 2010's | 1 (12.50) | 24.3611 |
| 2020's | 3 (37.50) | 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 (19.94) All Compounds (24.57) |
| 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 | 8 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||