A 228839: an immunosuppressive agent; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 447312 |
| CHEMBL ID | 29982 |
| SCHEMBL ID | 629301 |
| MeSH ID | M0461010 |
| Synonym |
|---|
| 2-{(5-{[butyl-(2-cyclohexyl-ethyl)-amino]-methyl}-2'-methyl-biphenyl-2-carbonyl)-amino]-4-methylsulfanyl-butyric acid |
| 1N94 |
| (2s)-2-[(4-{[butyl(2-cyclohexylethyl)amino]methyl}-2-(2-methylphenyl)phenyl)formamido]-4-(methylsulfanyl)butanoic acid |
| chembl29982 , |
| bdbm17325 |
| abt-839 |
| (2s)-2-[[4-[[butyl(2-cyclohexylethyl)amino]methyl]-2-(2-methylphenyl)benzoyl]amino]-4-methylsulfanylbutanoic acid |
| SCHEMBL629301 |
| n-[(5-{[butyl(2-cyclohexylethyl)amino]methyl}-2'-methylbiphenyl-2-yl)carbonyl]-l-methionine |
| Q27466421 |
| a 228839 |
| 216234-25-2 |
| a-228839 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, Protein farnesyltransferase alpha subunit | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0011 | 0.0011 | 0.0011 | 0.0011 | AID977608 |
| Chain B, Protein farnesyltransferase beta subunit | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0011 | 0.0011 | 0.0011 | 0.0011 | AID977608 |
| Chain A, Protein farnesyltransferase alpha subunit | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0011 | 0.0011 | 0.0011 | 0.0011 | AID977608 |
| Chain B, Protein farnesyltransferase beta subunit | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0011 | 0.0011 | 0.0011 | 0.0011 | AID977608 |
| Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Bos taurus (cattle) | IC50 (µMol) | 0.0011 | 0.0005 | 0.2819 | 1.1000 | AID1797620; AID241504; AID72677 |
| Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 0.0011 | 0.0005 | 0.4716 | 10.0000 | AID71312; AID72816 |
| Protein farnesyltransferase subunit beta | Bos taurus (cattle) | IC50 (µMol) | 0.0011 | 0.0005 | 0.1183 | 1.1000 | AID1797620; AID241504; AID72677 |
| Protein farnesyltransferase subunit beta | Homo sapiens (human) | IC50 (µMol) | 0.0011 | 0.0005 | 0.2177 | 2.5000 | AID71312; AID72816 |
| [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 | Homo sapiens (human) | EC50 (µMol) | 0.0160 | 0.0160 | 2.3027 | 6.8000 | AID71302 |
| Protein farnesyltransferase subunit beta | Homo sapiens (human) | EC50 (µMol) | 0.0160 | 0.0160 | 0.0540 | 0.0920 | AID71302 |
| Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Mus musculus (house mouse) | EC50 (µMol) | 0.0160 | 0.0016 | 0.0338 | 0.1000 | AID240087; AID41569 |
| Protein farnesyltransferase subunit beta | Mus musculus (house mouse) | EC50 (µMol) | 0.0160 | 0.0016 | 0.0338 | 0.1000 | AID240087; AID41569 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID226605 | Selectivity ratio for farnesyltransferase compared to geranylgeranyltransferase type I(GGT-I) | 2003 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22 | Pyridone-containing farnesyltransferase inhibitors: synthesis and biological evaluation. |
| AID226831 | Selectivity for farnesyl over geranylgeranyl transferase | 2003 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7 | Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives. |
| AID71302 | In vitro effective concentration against farnesyltransferase (FT) | 2003 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22 | Pyridone-containing farnesyltransferase inhibitors: synthesis and biological evaluation. |
| AID244256 | Selectivity for Bovine farnesyl transferase over geranylgeranyl transferase | 2005 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1 | Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase. |
| AID241504 | Inhibition of Bovine farnesyl transferase | 2005 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1 | Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase. |
| AID240087 | Effective concentration against H-ras processing in NIH 3T3 cells | 2005 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1 | Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase. |
| AID72677 | In vitro inhibitory activity against farnesyltransferase (FTase) | 2003 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7 | Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase. |
| AID72816 | In vitro inhibitory activity against farnesyl transferase | 2003 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7 | Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives. |
| AID71312 | In vitro inhibitory activity against farnesyltransferase (FT) | 2003 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22 | Pyridone-containing farnesyltransferase inhibitors: synthesis and biological evaluation. |
| AID41569 | Inhibition of Ras farnesylation in Human Ha-Ras-transformed BALB/c 3T3 cells | 2003 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7 | Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives. |
| AID1797620 | FTase Activity Assay from Article 10.1016/S0960-894X(03)00095-7: \\Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.\\ | 2003 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7 | Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2003 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7 | Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives. |
| [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 | 5 (100.00) | 29.6817 |
| 2010's | 0 (0.00) | 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] | ||
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 (12.56) 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 | 5 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||