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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
|---|
Moligand™, 10mM in DMSO Moligand™ ベースライン干渉を最小限に抑える必要がある、感度の高いクロマトグラフィーおよび分析ワークフロー向け。
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クロマトグラフィー、有機合成、クロスカップリング反応に関する 0 件の査読済み論文で引用されています。
Information
EBI-2511 EBI-2511 is a highly potent and orally active EZH2 inhibitor with an IC50 of 4 nM for EZH2(A667G).
Targets
EZH2(A667G) (Cell-free assay) 4 nM
In vivo
In in vivo experiments, rats are administrated with dosages of 5 mg/kg EBI-2511 (p.o.) and 0.5 mg/kg EBI-2511 (i.v.). Mice are administrated with dosages of 10 mg/kg p.o. and 1.0 mg/kg i.v. For i.v. administration, the clearance of EBI-2511 is modest with CLz/F of 26 and 32 mL/min/kg in rats and mice, respectively. After a single 5 and 10 mg/kg oral dose of a CMC-Na suspension of EBI-2511 to rats and mice, its AUC0‑t reaches 239 and 774 ng/mL·h with oral bioavailability of 9% and 16%, respectively. plasma protein binding of EBI-2511 in human, rat, and mouse are 93.9%, 94.0%, and 92.7%, respectively.
Cell Research(from reference)
Cell lines:Pfeiffer cells
Incubation Time:5 days
危険性、取扱い、保管、および規制遵守を網羅した包括的な文書。
<<<<<<< HEAD SDS をダウンロード → ======= SDS をダウンロード → >>>>>>> release248-p3Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Benzenoids |
| 分類 | Benzene and substituted derivatives |
| Subclass | Benzoic acids and derivatives |
| Intermediate Tree Nodes | Aminobenzoic acids and derivatives |
| Direct Parent | Aminobenzamides |
| Alternative Parents | Benzofurans Dialkylarylamines Pyridinones Methylpyridines Dihydropyridines Aralkylamines Piperidines Oxanes Heteroaromatic compounds Furans Trialkylamines Secondary carboxylic acid amides Lactams Amino acids and derivatives Oxacyclic compounds Dialkyl ethers Azacyclic compounds Organopnictogen compounds Organic oxides Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Aminobenzamide - Benzofuran - Dialkylarylamine - Tertiary aliphatic/aromatic amine - Methylpyridine - Aralkylamine - Pyridinone - Dihydropyridine - Pyridine - Piperidine - Oxane - Hydropyridine - Heteroaromatic compound - Furan - Tertiary aliphatic amine - Tertiary amine - Secondary carboxylic acid amide - Lactam - Carboxamide group - Amino acid or derivatives - Oxacycle - Azacycle - Organoheterocyclic compound - Ether - Dialkyl ether - Carboxylic acid derivative - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Organooxygen compound - Organonitrogen compound - Amine - Aromatic heteropolycyclic compound |
| 説明 | This compound belongs to the class of organic compounds known as aminobenzamides. These are organic compounds containing a benzamide moiety with an amine group attached to the benzene ring. |
| External Descriptors | Not available |
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| DMSO(mg / mL) 最大溶解度 | 30 |
|---|---|
| DMSO(mM) 最大溶解度 | 52.0138009951974 |
| 水(mg / mL) 最大溶解度 | <1 |
| 分子量 | 576.800 g/mol |
| XLogP3 | 5.300 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 9 |
| Exact Mass | 576.368 Da |
| Monoisotopic Mass | 576.368 Da |
| Topological Polar Surface Area | 87.100 Ų |
| Heavy Atom Count | 42 |
| Formal Charge | 0 |
| Complexity | 1030.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
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