A retinoic acid receptor antagonist that antagonises retinoic acid receptor alpha.
ChEBI ID: 90713
| Member | Definition | Class |
|---|---|---|
| bms 195614 | A carboxamide resulting from the formal condensation of the carboxy group of 5,5-dimethyl-8-(quinolin-3-yl)-5,6-dihydronaphthalene-2-carboxylic acid with the amino group of p-aminobenzoic acid. It is a neutral retinoic acid receptor (RAR) alpha-selective antagonist (Ki = 2.5 nM). It displays no significant effect on nuclear receptor corepressor (NCoR) binding; moderately decreases SMRT binding to RAR. It antagonizes agonist-induced coactivator (CoA) recruitment. | BMS 195614 |
| bms453 | A member of the class of dihydronaphthalenes that is 1,2-dihydronaphthalene which is substituted at positions 1, 1, 4, and 6 by methyl, methyl, phenyl, and 2-(p-carboxyphenyl)vinyl groups, respectively (the E isomer). It is a potent retinoic acid receptor gamma (RARbeta) agonist that acts as an antagonist against RARalpha and RARgamma. | BMS-453 |
| o-(chloroacetylcarbamoyl)fumagillol | A carbamate ester that is fumagillol in which the hydroxy group has been converted to the corresponding N-(chloroacetyl)carbamate derivative. | O-(chloroacetylcarbamoyl)fumagillol |
| ro 41-5253 | A thiochromane that is 3,4-dihydro-2H-1-benzothiopyran S,S-dioxide in which the hydrogens at position 4 are both replaced by methyl groups, the hydrogens at position 7 is replaced by a heptyloxy group, while the hydrogen at position 6 is replaced by a 1-phenylprop-1-en-2-yl group, the phenyl group of which is substituted at the para position by a carboxy group. It is a selective antagonist for retinoic acid receptor alpha. | Ro 41-5253 |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 225 (43.10) | 18.2507 |
| 2000's | 228 (43.68) | 29.6817 |
| 2010's | 60 (11.49) | 24.3611 |
| 2020's | 9 (1.72) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 10 (1.75%) | 5.53% |
| Reviews | 47 (8.20%) | 6.00% |
| Case Studies | 2 (0.35%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 514 (89.70%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| AR protein | Homo sapiens (human) | Potency | 17.6216 | 3 | 3 |
| Ataxin-2 | Homo sapiens (human) | Potency | 18.7824 | 1 | 1 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 18.7824 | 1 | 1 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 18.7824 | 2 | 2 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 21.3174 | 1 | 1 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 37.9083 | 1 | 1 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 30.1116 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 1.6866 | 2 | 2 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 21.5325 | 2 | 2 |
| G | Vesicular stomatitis virus | Potency | 21.3174 | 1 | 1 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 13.7369 | 2 | 2 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 21.3174 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 21.3174 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 21.3174 | 1 | 1 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 2.4346 | 2 | 2 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 0.1056 | 1 | 1 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 11.4396 | 2 | 2 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 10.5621 | 1 | 1 |
| progesterone receptor | Homo sapiens (human) | Potency | 0.1492 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 18.7824 | 2 | 2 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 10.0591 | 1 | 1 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 6.6633 | 2 | 2 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 10.0758 | 2 | 2 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 1.2314 | 2 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Methionine aminopeptidase 2 | Homo sapiens (human) | IC50 | 0.5930 | 4 | 4 |
| Methionine aminopeptidase 2 | Homo sapiens (human) | Ki | 0.0010 | 2 | 2 |
| Retinoic acid receptor alpha | Homo sapiens (human) | Ki | 0.0037 | 2 | 3 |
| Retinoic acid receptor beta | Homo sapiens (human) | Ki | 0.0167 | 1 | 1 |
| Retinoic acid receptor gamma | Homo sapiens (human) | Ki | 0.0069 | 2 | 3 |
| Retinoic acid receptor RXR-alpha | Homo sapiens (human) | Ki | 0.0139 | 3 | 3 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Retinoic acid receptor gamma | Homo sapiens (human) | Kb | 0.0185 | 1 | 1 |