A histamine antagonist that selectively binds to but does not activate histamine H3 receptors, thereby blocking the actions of endogenous histamine.
ChEBI ID: 64176
| 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 |
| conessine | A steroid alkaloid that is con-5-enine substituted by a N,N-dimethylamino group at position 3. It has been isolated from the plant species of the family Apocynaceae. | conessine |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 34 (15.60) | 18.7374 |
| 1990's | 29 (13.30) | 18.2507 |
| 2000's | 89 (40.83) | 29.6817 |
| 2010's | 49 (22.48) | 24.3611 |
| 2020's | 17 (7.80) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 7 (3.08%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 220 (96.92%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 20.5424 | 3 | 3 |
| cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 19.9526 | 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 | 12.5893 | 1 | 1 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 1.5849 | 2 | 2 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 29.8493 | 1 | 1 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 29.8493 | 2 | 2 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 1.5849 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 1.5849 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 1.5849 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 1.5849 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 1.5849 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 1.5849 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 1.5849 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 1.5849 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 1.5849 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 1.5849 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 1.5849 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 1.5849 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 1.5849 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 1.5849 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 1.5849 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 1.5849 | 1 | 1 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 39.8107 | 1 | 2 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 9.1460 | 2 | 5 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 11.0792 | 1 | 2 |
| nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 0.0952 | 1 | 1 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 3.9811 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 22.4505 | 2 | 3 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 2.5119 | 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 |
|---|---|---|---|---|---|
| Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 0.6607 | 1 | 1 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | Ki | 0.0105 | 1 | 2 |
| Histamine H1 receptor | Homo sapiens (human) | Ki | 6.6716 | 2 | 6 |
| Histamine H2 receptor | Homo sapiens (human) | Ki | 6.6716 | 2 | 6 |
| 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 | 1.1568 | 22 | 26 |
| Histamine H3 receptor | Mus musculus (house mouse) | Ki | 0.0006 | 1 | 1 |
| Histamine H3 receptor | Rattus norvegicus (Norway rat) | Ki | 2.3237 | 7 | 13 |
| Histamine H4 receptor | Homo sapiens (human) | Ki | 1.6208 | 21 | 25 |
| Histamine H4 receptor | Mus musculus (house mouse) | Ki | 0.1408 | 2 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 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 | 0.0224 | 1 | 1 |
| Histamine H4 receptor | Mus musculus (house mouse) | EC50 | 0.8511 | 1 | 1 |
| Histamine H4 receptor | Homo sapiens (human) | Kd | 0.0310 | 1 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Histamine H3 receptor | Homo sapiens (human) | Kb | 0.0002 | 1 | 1 |