ogerin: a GPR68 modulator; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 56707820 |
| CHEMBL ID | 4548689 |
| MeSH ID | M000612457 |
| Synonym |
|---|
| ZINC67740571 , |
| AKOS027322977 |
| 1309198-71-7 |
| ogerin |
| 2-[4-amino-6-[(phenylmethyl)amino]-1,3,5-triazin-2-yl]benzenemethanol |
| ogerin, >=98% (hplc) |
| Z2289799517 |
| {2-[4-amino-6-(benzylamino)-1,3,5-triazin-2-yl]phenyl}methanol |
| [2-[4-amino-6-(benzylamino)-1,3,5-triazin-2-yl]phenyl]methanol |
| gtpl9155 |
| BCP30307 |
| zinc67740571; zinc-67740571; zinc 67740571 |
| (2-(4-amino-6-(benzylamino)-1,3,5-triazin-2-yl)phenyl)methanol |
| CS-0033147 |
| HY-110279 |
| SB73726 |
| MS-24454 |
| CHEMBL4548689 |
| EN300-254871 |
| 2-[4-amino-6-[(phenylmethyl)amino]-1,3,5-triazin-2-yl]-benzenemethanol |
Ogerin is a positive allosteric modulator of human and mouse ovarian cancer G protein-coupled receptors (OGR1s) It induces a leftward shift of the dose response curve to proton induced signaling.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Ogerin is a positive allosteric modulator (PAM) of GPR68, inducing a leftward shift of the dose response curve to proton induced signaling." | ( Ogerin mediated inhibition of TGF-β(1) induced myofibroblast differentiation is potentiated by acidic pH. Bell, TJ; Kottmann, RM; Nagel, DJ; Woeller, CF, 2022) | 2.89 |
| "Ogerin is a positive allosteric modulator of human and mouse ovarian cancer G protein-coupled receptors (OGR1s). " | ( Species-Dependent Enhancement of Ovarian Cancer G Protein-Coupled Receptor 1 Activation by Ogerin. Deai, M; Kojima, R; Mochimaru, Y; Mogi, C; Murakami, S; Musha, S; Okajima, F; Sato, K; Tomura, H, 2020) | 2.22 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2B | Homo sapiens (human) | Ki | 0.4964 | 0.0003 | 0.7693 | 10.0000 | AID1915068 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Ovarian cancer G-protein coupled receptor 1 | Homo sapiens (human) | EC50 (µMol) | 0.1480 | 0.1479 | 0.1480 | 0.1480 | AID1792973; AID1912832 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| Gq/11-coupled serotonin receptor activity | 5-hydroxytryptamine receptor 2B | Homo sapiens (human) |
| G-protein alpha-subunit binding | 5-hydroxytryptamine receptor 2B | Homo sapiens (human) |
| G protein-coupled serotonin receptor activity | 5-hydroxytryptamine receptor 2B | Homo sapiens (human) |
| GTPase activator activity | 5-hydroxytryptamine receptor 2B | Homo sapiens (human) |
| protein binding | 5-hydroxytryptamine receptor 2B | Homo sapiens (human) |
| serotonin binding | 5-hydroxytryptamine receptor 2B | Homo sapiens (human) |
| neurotransmitter receptor activity | 5-hydroxytryptamine receptor 2B | Homo sapiens (human) |
| G protein-coupled receptor activity | Ovarian cancer G-protein coupled receptor 1 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| nucleoplasm | 5-hydroxytryptamine receptor 2B | Homo sapiens (human) |
| cytoplasm | 5-hydroxytryptamine receptor 2B | Homo sapiens (human) |
| plasma membrane | 5-hydroxytryptamine receptor 2B | Homo sapiens (human) |
| synapse | 5-hydroxytryptamine receptor 2B | Homo sapiens (human) |
| G protein-coupled serotonin receptor complex | 5-hydroxytryptamine receptor 2B | Homo sapiens (human) |
| dendrite | 5-hydroxytryptamine receptor 2B | Homo sapiens (human) |
| plasma membrane | 5-hydroxytryptamine receptor 2B | Homo sapiens (human) |
| plasma membrane | Ovarian cancer G-protein coupled receptor 1 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1608006 | Positive allosteric modulation of mouse GPR68 expressed in HEK293T cells co-expressing Gs assessed as stimulation of proton-mediated cAMP production by measuring allosteric binding affinity in HBSS buffer containing pH 6.8 to 8.2 HEPES/pH 8.3 to 8.6 TAPS | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68). |
| AID1607983 | Positive allosteric modulation of human GPR68 expressed in HEK293T cells co-expressing Gs assessed as stimulation of proton-mediated cAMP production by measuring allosteric affinity cooperativity in HBSS buffer containing pH 6.8 to 8.2 HEPES/pH 8.3 to 8.6 | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68). |
| AID1608007 | Positive allosteric modulation of mouse GPR68 expressed in HEK293T cells co-expressing Gs assessed as stimulation of proton-mediated cAMP production by measuring allosteric index in HBSS buffer containing pH 6.8 to 8.2 HEPES/pH 8.3 to 8.6 TAPS measured af | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68). |
| AID1608004 | Positive allosteric modulation of mouse GPR68 expressed in HEK293T cells co-expressing Gs assessed as stimulation of proton-mediated cAMP production by measuring allosteric affinity cooperativity in HBSS buffer containing pH 6.8 to 8.2 HEPES/pH 8.3 to 8.6 | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68). |
| AID1608005 | Positive allosteric modulation of mouse GPR68 expressed in HEK293T cells co-expressing Gs assessed as stimulation of proton-mediated cAMP production by measuring efficacy cooperativity in HBSS buffer containing pH 6.8 to 8.2 HEPES/pH 8.3 to 8.6 TAPS measu | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68). |
| AID1607984 | Positive allosteric modulation of human GPR68 expressed in HEK293T cells co-expressing Gs assessed as stimulation of proton-mediated cAMP production by measuring efficacy cooperativity in HBSS buffer containing pH 6.8 to 8.2 HEPES/pH 8.3 to 8.6 TAPS measu | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68). |
| AID1607986 | Positive allosteric modulation of human GPR68 expressed in HEK293T cells co-expressing Gs assessed as stimulation of proton-mediated cAMP production by measuring allosteric index in HBSS buffer containing pH 6.8 to 8.2 HEPES/pH 8.3 to 8.6 TAPS measured af | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68). |
| AID1607987 | Positive allosteric modulation of human GPR68 expressed in HEK293T cells co-expressing Gs assessed as stimulation of proton-mediated cAMP production in HBSS buffer containing pH 6.8 to 8.2 HEPES/pH 8.3 to 8.6 TAPS measured after 20 to 30 mins in presence | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68). |
| AID1607985 | Positive allosteric modulation of human GPR68 expressed in HEK293T cells co-expressing Gs assessed as stimulation of proton-mediated cAMP production by measuring allosteric binding affinity in HBSS buffer containing pH 6.8 to 8.2 HEPES/pH 8.3 to 8.6 TAPS | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68). |
| [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 | 2 (40.00) | 24.3611 |
| 2020's | 3 (60.00) | 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 moderate demand-to-supply ratio for research on this compound.
| This Compound (27.59) 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 | 5 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||