A drug that acts as an antagonist, agonist, reverse agonist, or in some other fashion when interacting with cellular receptors.
ChEBI ID: 90710
| Member | Definition | Class |
|---|---|---|
| 1-(2-(4-(4-fluoro-benzoyl)-piperidin-1-yl)-ethyl)-3,3-dimethyl-1,2-dihydro-indol-2-one | A hydrochloride resulting from the formal reation of equimolar amount of LY-310762 with hydrogen chloride. A potent and selective antagonist for the 5-hydroxytryptamine 1D (5-HT1D) receptor. | LY-310762 hydrochloride |
| LY-310762 | A member of the class of oxindoles that is 1-ethyl-3,3-dimethyl-1,3-dihydro-2H-indol-2-one in which the ethyl group has been substituted at position 2 by a 4-(p-fluorobenzoyl)piperidin-1-yl group. It is a potent and selective antagonist for the 5-hydroxytryptamine 1D (5-HT1D) receptor. | LY-310762 |
| n-(1-methyl-5-indolyl)-n'-(3-methyl-5-isothiazolyl)urea | A member of ther class of ureas that is urea in which a hydrogen attached to one of the nitrogens has been replaced by an N-methylindol-5-yl group, while a hydrogen attached to the other nitrogen has been replaced by a 3-methyl-1,2-thiazol-5-yl group. It is a potent and selective antagonist for the 5-hydroxytryptamine 2B (5-HT2B) receptor. | 1-(1-methylindol-5-yl)-3-(3-methyl-1,2-thiazol-5-yl)urea |
| n,n-dipropyl-2-(4-methoxy-3-(2-phenylethoxy)phenyl)ethylamine monohydrochloride | An aromatic ether that is (2-phenoxyethyl)benzene which carries a 2-(dipropylamino)ethyl group at position 3 and a methoxy group at position 6. It is a potent and selective sigma1 receptor antagonist. | N-{2-[4-methoxy-3-(2-phenylethoxy)phenyl]ethyl}-N-propylpropan-1-amine hydrochloride |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 4 (8.89) | 18.2507 |
| 2000's | 11 (24.44) | 29.6817 |
| 2010's | 22 (48.89) | 24.3611 |
| 2020's | 8 (17.78) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | 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 | 67 (100.00%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 16.2149 | 4 | 6 |
| Ataxin-2 | Homo sapiens (human) | Potency | 19.0919 | 1 | 2 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 35.8704 | 1 | 2 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 16.0537 | 2 | 5 |
| BRCA1 | Homo sapiens (human) | Potency | 10.0000 | 1 | 1 |
| cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 15.8489 | 2 | 2 |
| Chain A, ATP-DEPENDENT DNA HELICASE Q1 | Homo sapiens (human) | Potency | 0.2818 | 1 | 1 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 2.8184 | 1 | 1 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 35.4813 | 1 | 1 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 70.7946 | 1 | 1 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 64.9290 | 2 | 3 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 3.1623 | 1 | 1 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 2.0484 | 1 | 2 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 20.5348 | 1 | 2 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 14.2191 | 2 | 4 |
| D(1A) dopamine receptor | Homo sapiens (human) | Potency | 5.4256 | 2 | 4 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 37.6858 | 1 | 1 |
| endonuclease IV | Escherichia coli | Potency | 13.6996 | 1 | 2 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 13.9761 | 4 | 7 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 18.5187 | 1 | 4 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 20.9310 | 1 | 1 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 63.4054 | 1 | 2 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1 | 2 |
| geminin | Homo sapiens (human) | Potency | 5.2651 | 3 | 3 |
| GLS protein | Homo sapiens (human) | Potency | 0.3162 | 1 | 1 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa) | Homo sapiens (human) | Potency | 5.8479 | 2 | 2 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 6.5244 | 2 | 8 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 14.2191 | 2 | 4 |
| Integrin alpha-IIb | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| Integrin beta-3 | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 10.2175 | 1 | 2 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 25.1189 | 1 | 1 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 31.6228 | 1 | 1 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 56.2341 | 1 | 1 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 10.4111 | 2 | 3 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 35.7168 | 2 | 2 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 17.0374 | 2 | 3 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 1.0000 | 1 | 1 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 0.0316 | 2 | 2 |
| nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 7.9433 | 1 | 1 |
| NPC intracellular cholesterol transporter 1 precursor | Homo sapiens (human) | Potency | 7.3078 | 1 | 1 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 19.9526 | 1 | 1 |
| Ornithine decarboxylase | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 1 |
| parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 27.3342 | 1 | 2 |
| Parkin | Homo sapiens (human) | Potency | 5.8048 | 1 | 1 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 67.4555 | 1 | 1 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 79.4328 | 1 | 1 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 0.8913 | 1 | 1 |
| pyruvate kinase | Leishmania mexicana mexicana | Potency | 15.8489 | 2 | 2 |
| pyruvate kinase PKM isoform b | Homo sapiens (human) | Potency | 15.8489 | 2 | 2 |
| ras-related protein Rab-9A | Homo sapiens (human) | Potency | 6.5131 | 1 | 1 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 10.0000 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 23.0632 | 2 | 6 |
| Thrombopoietin | Homo sapiens (human) | Potency | 5.7924 | 2 | 4 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 39.8107 | 2 | 2 |
| transcriptional regulator ERG isoform 3 | Homo sapiens (human) | Potency | 11.2202 | 1 | 1 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 2.5119 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | IC50 | 6.4600 | 1 | 1 |
| 5-hydroxytryptamine receptor 1D | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 5-hydroxytryptamine receptor 1E | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| 5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 1 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Ki | 6.3096 | 2 | 2 |
| 5-hydroxytryptamine receptor 2B | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 1 |
| 5-hydroxytryptamine receptor 2C | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 1 |
| 5-hydroxytryptamine receptor 2C | Mus musculus (house mouse) | Ki | 1.5136 | 1 | 1 |
| 5-hydroxytryptamine receptor 3A | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| 5-hydroxytryptamine receptor 3B | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 10.8000 | 1 | 1 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 3.1623 | 1 | 1 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 10.8000 | 1 | 1 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 3.1623 | 1 | 1 |
| Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 10.8000 | 1 | 1 |
| Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 3.1623 | 1 | 1 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| D | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 1 |
| D | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 2 |
| D(1A) dopamine receptor | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| D(1A) dopamine receptor | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| D(2) dopamine receptor | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 2 | 2 |
| D(2) dopamine receptor | Homo sapiens (human) | Ki | 31.6228 | 1 | 1 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 31.6228 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 1 | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| fibroblast growth factor 22 isoform 1 precursor | Homo sapiens (human) | AbsAC0.47_uM | 24.7200 | 1 | 1 |
| fibroblast growth factor 22 isoform 1 precursor | Homo sapiens (human) | AbsAC1_uM | 3.4200 | 1 | 1 |