A histamine agonist that binds to and activates H4-receptors.
ChEBI ID: 64155
| Member | Definition | Class |
|---|---|---|
| clobenpropit | An imidothiocarbamic ester that consists of isothiourea bearing S-3-(imidazol-4-yl)propyl and N-4-chlorobenzyl substituents. An extremely potent histamine H3 antagonist/inverse agonist (pA2 = 9.93). Also displays partial agonist activity at H4 receptors; induces eosinophil shape change with an EC50 of 3 nM. | clobenpropit |
| imetit | An imidothiocarbamic ester that consists of isothiourea in which the thiol hydrogen is substituted by a 2-(imidazol-4-yl)ethyl group. An extremely potent, high affinity agonist at H3 and H4 receptors (Ki values are 0.3 and 2.7 nM respectively). Induces shape change in eosinophils with an EC50 of 25 nM. Centrally active following systemic administration. | imetit |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 1 (0.49) | 18.7374 |
| 1990's | 42 (20.59) | 18.2507 |
| 2000's | 100 (49.02) | 29.6817 |
| 2010's | 46 (22.55) | 24.3611 |
| 2020's | 15 (7.35) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 5 (2.14%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 229 (97.86%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 2.9081 | 1 | 1 |
| cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 1.4125 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 14.6726 | 1 | 3 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 19.0815 | 2 | 6 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 7.5193 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 19.0815 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 19.0815 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 19.0815 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 19.0815 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 19.0815 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 19.0815 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 19.0815 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 19.0815 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 19.0815 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 19.0815 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 19.0815 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 19.0815 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 19.0815 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 19.0815 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 19.0815 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 19.0815 | 1 | 3 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 39.8107 | 1 | 2 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 11.0611 | 2 | 7 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 15.8489 | 1 | 1 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 9.9150 | 1 | 2 |
| TDP1 protein | Homo sapiens (human) | Potency | 25.4957 | 2 | 2 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 2.8184 | 1 | 1 |
| Thrombopoietin | Homo sapiens (human) | Potency | 0.7943 | 2 | 2 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 14.1254 | 1 | 1 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Histamine H3 receptor | Homo sapiens (human) | IC50 | 0.0011 | 4 | 4 |
| Histamine H3 receptor | Mus musculus (house mouse) | IC50 | 0.0010 | 1 | 1 |
| Histamine H3 receptor | Homo sapiens (human) | Ki | 0.0020 | 20 | 26 |
| Histamine H3 receptor | Mus musculus (house mouse) | Ki | 0.0013 | 1 | 2 |
| Histamine H3 receptor | Rattus norvegicus (Norway rat) | Ki | 0.0008 | 2 | 2 |
| Histamine H4 receptor | Homo sapiens (human) | Ki | 0.0208 | 20 | 25 |
| Histamine H4 receptor | Mus musculus (house mouse) | Ki | 0.1408 | 2 | 2 |
| Metabotropic glutamate receptor 5 | Rattus norvegicus (Norway rat) | Ki | 0.0006 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Histamine H3 receptor | Homo sapiens (human) | EC50 | 0.0018 | 4 | 4 |
| Histamine H3 receptor | Mus musculus (house mouse) | EC50 | 0.0017 | 1 | 1 |
| Histamine H3 receptor | Homo sapiens (human) | Kd | 0.0292 | 2 | 3 |
| Histamine H4 receptor | Homo sapiens (human) | EC50 | 0.0246 | 4 | 4 |
| Histamine H4 receptor | Mus musculus (house mouse) | EC50 | 0.8511 | 1 | 1 |
| Histamine H4 receptor | Homo sapiens (human) | Kd | 0.0310 | 1 | 2 |
| Metabotropic glutamate receptor 5 | Rattus norvegicus (Norway rat) | EC50 | 0.0024 | 1 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Histamine H3 receptor | Homo sapiens (human) | Kb | 0.0002 | 1 | 1 |