An antogonist that blocks chemokine receptor 5 (CCR5).
ChEBI ID: 63673
| Member | Definition | Class |
|---|---|---|
| cenicriviroc | A member of the class of benzazocines that is (5Z)-1,2,3,4-tetrahydro-1-benzazocine which is substituted by a 2-methylpropyl, N-{4-[(S)-(1-propyl-1H-imidazol-5-yl)methanesulfinyl]phenyl}carboxamide and 4-(2-butoxyethoxy)phenyl groups at positions 1, 5 and 8, respectively. It is a potent chemokine 2 and 5 receptor antagonist currently in development for the treatment of liver fibrosis in adults with nonalcoholic steatohepatitis (NASH). | cenicriviroc |
| pentamidine | A diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease. | pentamidine |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 526 (22.78) | 18.7374 |
| 1990's | 827 (35.82) | 18.2507 |
| 2000's | 375 (16.24) | 29.6817 |
| 2010's | 456 (19.75) | 24.3611 |
| 2020's | 125 (5.41) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 148 (6.01%) | 5.53% |
| Reviews | 225 (9.14%) | 6.00% |
| Case Studies | 353 (14.33%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 1,737 (70.52%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 11.1906 | 4 | 4 |
| Interferon beta | Homo sapiens (human) | Potency | 20.8212 | 1 | 3 |
| PPM1D protein | Homo sapiens (human) | Potency | 20.8212 | 1 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 10 kDa chaperonin | Escherichia coli | IC50 | 175.0000 | 2 | 2 |
| 10 kDa heat shock protein, mitochondrial | Homo sapiens (human) | IC50 | 175.0000 | 2 | 2 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | IC50 | 1.6390 | 1 | 1 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Ki | 0.4680 | 1 | 1 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | IC50 | 3.2780 | 1 | 1 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | Ki | 1.7170 | 1 | 1 |
| 5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | IC50 | 3.2780 | 1 | 1 |
| 5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | Ki | 1.7170 | 1 | 1 |
| 60 kDa chaperonin | Escherichia coli | IC50 | 175.0000 | 2 | 2 |
| 60 kDa heat shock protein, mitochondrial | Homo sapiens (human) | IC50 | 175.0000 | 2 | 2 |
| Acrosin | Sus scrofa (pig) | Ki | 2.3000 | 1 | 1 |
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | IC50 | 2.2140 | 1 | 1 |
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | Ki | 2.1960 | 1 | 1 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | IC50 | 1.3750 | 1 | 1 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 0.5160 | 1 | 1 |
| Amiloride-sensitive amine oxidase [copper-containing] | Homo sapiens (human) | Ki | 0.2900 | 1 | 1 |
| Amine oxidase [flavin-containing] A | Homo sapiens (human) | IC50 | 0.7930 | 1 | 1 |
| Angiotensin-converting enzyme | Oryctolagus cuniculus (rabbit) | IC50 | 15.7215 | 1 | 1 |
| Angiotensin-converting enzyme | Oryctolagus cuniculus (rabbit) | Ki | 12.8802 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Aurora kinase B | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 422.6667 | 3 | 3 |
| C-C chemokine receptor type 2 | Homo sapiens (human) | IC50 | 0.0059 | 2 | 2 |
| C-C chemokine receptor type 5 | Homo sapiens (human) | IC50 | 0.0030 | 1 | 1 |
| C-C chemokine receptor type 5 | Mus musculus (house mouse) | IC50 | 0.0002 | 1 | 1 |
| C-C chemokine receptor type 7 | Homo sapiens (human) | IC50 | 0.0031 | 1 | 1 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Coagulation factor X | Homo sapiens (human) | IC50 | 10.4000 | 1 | 1 |
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 | 75.0000 | 3 | 3 |
| Cytochrome P450 2C19 | Homo sapiens (human) | IC50 | 75.0000 | 3 | 3 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 75.0000 | 3 | 3 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 | 19.8667 | 3 | 3 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 75.0000 | 3 | 3 |
| D(3) dopamine receptor | Homo sapiens (human) | IC50 | 3.9980 | 1 | 1 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 1.3580 | 1 | 1 |
| Diamine acetyltransferase 1 | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 1 | Homo sapiens (human) | IC50 | 0.7200 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2A | Homo sapiens (human) | IC50 | 0.7200 | 1 | 1 |
| Glyceraldehyde-3-phosphate dehydrogenase | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| Multidrug and toxin extrusion protein 1 | Homo sapiens (human) | IC50 | 1.7033 | 3 | 3 |
| Multidrug and toxin extrusion protein 2 | Homo sapiens (human) | IC50 | 6.5500 | 2 | 2 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | IC50 | 1.4250 | 1 | 1 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | Ki | 0.5070 | 1 | 1 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | IC50 | 1.5800 | 1 | 1 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | Ki | 0.2200 | 1 | 1 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | IC50 | 2.8850 | 1 | 1 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | Ki | 2.0730 | 1 | 1 |
| Nuclear receptor subfamily 3 group C member 3 | Bos taurus (cattle) | IC50 | 15.7215 | 1 | 1 |
| Nuclear receptor subfamily 3 group C member 3 | Bos taurus (cattle) | Ki | 12.8802 | 1 | 1 |
| Plasminogen | Homo sapiens (human) | IC50 | 28.4000 | 3 | 5 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 15.8054 | 4 | 4 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | Ki | 12.8802 | 1 | 1 |
| Protein arginine N-methyltransferase 1 | Homo sapiens (human) | IC50 | 81.0000 | 2 | 2 |
| Protein arginine N-methyltransferase 5 | Homo sapiens (human) | IC50 | 582.0000 | 1 | 1 |
| Protein S100-B | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Protein tyrosine phosphatase type IVA 1 | Homo sapiens (human) | IC50 | 0.3000 | 1 | 1 |
| Protein tyrosine phosphatase type IVA 2 | Homo sapiens (human) | IC50 | 0.3000 | 1 | 1 |
| Protein tyrosine phosphatase type IVA 3 | Homo sapiens (human) | IC50 | 35.8333 | 3 | 3 |
| Sodium-dependent dopamine transporter | Homo sapiens (human) | IC50 | 3.1590 | 1 | 1 |
| Sodium-dependent dopamine transporter | Homo sapiens (human) | Ki | 2.5100 | 1 | 1 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | IC50 | 2.2140 | 1 | 1 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | Ki | 2.1960 | 1 | 1 |
| Solute carrier family 22 member 1 | Homo sapiens (human) | IC50 | 22.1000 | 1 | 1 |
| Solute carrier family 22 member 2 | Homo sapiens (human) | IC50 | 1.2000 | 1 | 1 |
| Solute carrier family 22 member 3 | Homo sapiens (human) | IC50 | 9.5000 | 1 | 1 |
| Suppressor of tumorigenicity 14 protein | Homo sapiens (human) | Ki | 1.1600 | 1 | 1 |
| Trypsin-1 | Homo sapiens (human) | IC50 | 43.3333 | 1 | 3 |
| Urokinase-type plasminogen activator | Homo sapiens (human) | IC50 | 43.3333 | 1 | 3 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Protein S100-B | Homo sapiens (human) | Kd | 1.0000 | 1 | 1 |
| Protein S100-B | Rattus norvegicus (Norway rat) | Kd | 47.0000 | 2 | 2 |