5-methyl-N-(4-methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine: an mGlu4 positive modulator; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 46836872 |
| CHEMBL ID | 3609729 |
| SCHEMBL ID | 369060 |
| MeSH ID | M000598434 |
| Synonym |
|---|
| 1235318-89-4 |
| adx 88178 |
| gtpl6238 |
| 4-methyl-n-[5-methyl-4-(1h-pyrazol-4-yl)-1,3-thiazol-2-yl]pyrimidin-2-amine |
| adx88178 |
| adx-88178 |
| SCHEMBL369060 |
| CHEMBL3609729 , |
| AKOS030228680 |
| AS-72883 |
| 5-methyl-n-(4-methylpyrimidin-2-yl)-4-(1h-pyrazol-4-yl)thiazol-2-amine |
| bdbm50116515 |
| HY-18654 |
| CS-6961 |
| FT-0756913 |
| 2-pyrimidinamine, 4-methyl-n-[5-methyl-4-(1h-pyrazol-4-yl)-2-thiazolyl]- |
| mfcd21340285 |
| 2-pyrimidinamine,4-methyl-n-[5-methyl-4-(1h-pyrazol-4-yl)-2-thiazolyl]- |
| Q27074322 |
| SB16992 |
| BCP32622 |
| adx 88178; adx88178 |
| 5-methyl-n-(4-methylpyrimidin-2-yl)-4-(1h-pyrazol-4-yl)-1,3-thiazol-2-amine |
| adx88178? |
| A857273 |
| bqi , |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Oral administration of ADX88178 in rats is associated with high bioavailability and results in cerebrospinal fluid exposure of >50-fold the in vitro EC(50) value." | ( A potent and selective metabotropic glutamate receptor 4 positive allosteric modulator improves movement in rodent models of Parkinson's disease. Bessif, A; Boléa, C; Bortoli, J; Browne, SE; Campo, B; Charvin, D; DiLella, AG; Girard, F; Hess, F; Hodge, LM; Koser, AJ; Le Poul, E; Liverton, N; Luo, B; Poli, S; Reynolds, IJ; Smith, KM, 2012) | 0.38 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cytochrome P450 3A4 | Homo sapiens (human) | EC50 (µMol) | 0.0520 | 0.0001 | 0.2328 | 3.2000 | AID1492909 |
| Cytochrome P450 2C9 | Homo sapiens (human) | EC50 (µMol) | 0.0090 | 0.0008 | 0.4170 | 2.3000 | AID1242926 |
| Metabotropic glutamate receptor 4 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.0090 | 0.0090 | 2.5440 | 9.4900 | AID1242926 |
| Metabotropic glutamate receptor 7 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 10.0000 | 0.1460 | 0.8230 | 1.5000 | AID1492913 |
| Metabotropic glutamate receptor 8 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 1.2000 | 0.0310 | 1.1813 | 8.0000 | AID1492915 |
| Metabotropic glutamate receptor 4 | Homo sapiens (human) | EC50 (µMol) | 0.0280 | 0.0040 | 1.7193 | 9.8000 | AID1242925; AID1492909 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1346283 | Rat mGlu4 receptor (Metabotropic glutamate receptors) | 2012 | The Journal of pharmacology and experimental therapeutics, Oct, Volume: 343, Issue:1 | A potent and selective metabotropic glutamate receptor 4 positive allosteric modulator improves movement in rodent models of Parkinson's disease. |
| AID1346285 | Human mGlu4 receptor (Metabotropic glutamate receptors) | 2012 | The Journal of pharmacology and experimental therapeutics, Oct, Volume: 343, Issue:1 | A potent and selective metabotropic glutamate receptor 4 positive allosteric modulator improves movement in rodent models of Parkinson's disease. |
| AID1242928 | Half life in Wistar rat liver microsomes in presence of NADPH generation system by HPLC method | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability. |
| AID1242925 | Positive allosteric modulator activity at human mGlu4 receptor | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability. |
| AID1242929 | Effective permeability by PAMPA method | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability. |
| AID1492915 | Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based f | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10 | Discovery of VU6005649, a CNS Penetrant mGlu |
| AID1492913 | Positive allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based f | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10 | Discovery of VU6005649, a CNS Penetrant mGlu |
| AID1242926 | Positive allosteric modulator activity at rat mGlu4 receptor | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability. |
| AID1492909 | Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye b | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10 | Discovery of VU6005649, a CNS Penetrant mGlu |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 7 (100.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (12.43) All Compounds (24.57) |
| Publication Type | This drug (%) | 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 | 7 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||