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(6R,7R,8S,3'R) -8alpha-(3,4-dihydroxy-2-methylenebutanoyloxy)-15-acetoxyhelianga-1(10),4(5),11(13)-trien-6-olide
- Family: Plantae - Asteraceae
- Kingdom: Plantae
-
Class: Terpenoid
- Subclass: Sesquiterpene Lactone
Canonical Smiles | OC[C@H](C(=C)C(=O)O[C@H]1C/C(=C/CC/C(=C\[C@@H]2[C@@H]1C(=C)C(=O)O2)/COC(=O)C)/C)O |
---|---|
InChI | InChI=1S/C22H28O8/c1-12-6-5-7-16(11-28-15(4)24)9-19-20(14(3)22(27)30-19)18(8-12)29-21(26)13(2)17(25)10-23/h6,9,17-20,23,25H,2-3,5,7-8,10-11H2,1,4H3/b12-6+,16-9+/t17-,18+,19-,20-/m1/s1 |
InChIKey | WRINAAVIHYRMOF-DLWFREQBSA-N |
Formula | C22H28O8 |
HBA | 8 |
HBD | 2 |
MW | 420.46 |
Rotatable Bonds | 6 |
TPSA | 119.36 |
LogP | 1.53 |
Number Rings | 2 |
Number Aromatic Rings | 0 |
Heavy Atom Count | 30 |
Formal Charge | 0 |
Fraction CSP3 | 0.5 |
Exact Mass | 420.18 |
Number of Lipinski Rule Violations | 0 |
# | Species | Family | Kingdom | NCBI Taxonomy ID |
---|---|---|---|---|
1 | Centaurea tougourensis | Asteraceae | Plantae | 1486586 |
Showing of synonyms
(6R,7R,8S,3'R) -8alpha-(3,4-dihydroxy-2-methylenebutanoyloxy)-15-acetoxyhelianga-1(10),4(5),11(13)-trien-6-olide
- Nacer A, Merza J, et al. (2012). Sesquiterpene lactones from Centaurea tougourensis. Biochemical Systematics and Ecology,2012,43,163-165. [View]
No compound-protein relationship available.
SMILES: C=C1C(=O)OC(C12)C=CCCC=CCC2
Level: 0
Mol. Weight: 420.46 g/mol
No bioactivities available.
Absorption
- Caco-2 (logPapp)
- -4.74
- Human Oral Bioavailability 20%
- Non-Bioavailable
- Human Intestinal Absorption
- Absorbed
- Madin-Darby Canine Kidney
- -4.73
- Human Oral Bioavailability 50%
- Non-Bioavailable
- P-Glycoprotein Inhibitor
- Inhibitor
- P-Glycoprotein Substrate
- Non-Substrate
- Skin Permeability
- -2.85
Distribution
- Blood-Brain Barrier (CNS)
- -
- Blood-Brain Barrier
- Penetrable
- Fraction Unbound (Human)
- 0.54
- Plasma Protein Binding
- 54.88
- Steady State Volume of Distribution
- -
Metabolism
- Breast Cancer Resistance Protein
- Non-Inhibitor
- CYP 1A2 Inhibitor
- Non-Inhibitor
- CYP 1A2 Substrate
- Non-Substrate
- CYP 2C19 Inhibitor
- Non-Inhibitor
- CYP 2C19 Substrate
- Non-Substrate
- CYP 2C9 Inhibitor
- Non-Inhibitor
- CYP 2C9 Substrate
- Non-Substrate
- CYP 2D6 Inhibitor
- Non-Inhibitor
- CYP 2D6 Substrate
- Non-Substrate
- CYP 3A4 Inhibitor
- Inhibitor
- CYP 3A4 Substrate
- Non-Substrate
- OATP1B1
- Non-Inhibitor
- OATP1B3
- Non-Inhibitor
Excretion
- Clearance
- 8.96
- Organic Cation Transporter 2
- Non-Inhibitor
- Half-Life of Drug
- -
Toxicity
- AMES Mutagenesis
- Toxic
- Avian
- Safe
- Bee
- Toxic
- Bioconcentration Factor
- -1.26
- Biodegradation
- Toxic
- Carcinogenesis
- Toxic
- Crustacean
- Safe
- Liver Injury I (DILI)
- Safe
- Eye Corrosion
- Safe
- Eye Irritation
- Safe
- Maximum Tolerated Dose
- 0.73
- Liver Injury II
- Toxic
- hERG Blockers
- Safe
- Daphnia Maga
- 6.12
- Micronucleos
- Toxic
- NR-AhR
- Safe
- NR-AR
- Safe
- NR-AR-LBD
- Toxic
- NR-Aromatase
- Safe
- NR-ER
- Safe
- NR-ER-LBD
- Safe
- NR-GR
- Toxic
- NR-PPAR-gamma
- Safe
- NR-TR
- Safe
- T. Pyriformis
- -16.33
- Rat (Acute)
- 3.27
- Rat (Chronic Oral)
- 2.57
- Fathead Minnow
- 4.48
- Respiratory Disease
- Safe
- Skin Sensitisation
- Safe
- SR-ARE
- Toxic
- SR-ATAD5
- Safe
- SR-HSE
- Safe
- SR-MMP
- Safe
- SR-p53
- Toxic
General Properties
- Boiling Point
- 423.07
- Hydration Free Energy
- -6.12
- Log(D) at pH=7.4
- 1.73
- Log(P)
- 1.48
- Log S
- -2.9
- Log(Vapor Pressure)
- -8.9
- Melting Point
- 133.47
- pKa Acid
- 7.54
- pKa Basic
- 4.18
Protein Name | UniProt ID | Entry Name | Species | #Pharmacophore Points | Probability (0.7 ≤ Tversky Score ≤ 1.0) |
---|---|---|---|---|---|
Serpin domain-containing protein | H0ZQY2 | H0ZQY2_TAEGU | Taeniopygia guttata | 3 | 0.8744 |
Serpin domain-containing protein | H0ZQY2 | H0ZQY2_TAEGU | Taeniopygia guttata | 3 | 0.8744 |
Xylose isomerase | P24300 | XYLA_STRRU | Streptomyces rubiginosus | 3 | 0.7904 |
Xylose isomerase | P24300 | XYLA_STRRU | Streptomyces rubiginosus | 3 | 0.7904 |
Lysozyme C II | P11941 | LYSC2_ONCMY | Oncorhynchus mykiss | 3 | 0.7812 |
Lysozyme C II | P11941 | LYSC2_ONCMY | Oncorhynchus mykiss | 3 | 0.7812 |
Succinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrial | Q0QF01 | SDHA_PIG | Sus scrofa | 3 | 0.7763 |
Succinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrial | Q0QF01 | SDHA_PIG | Sus scrofa | 3 | 0.7763 |
Macrophage metalloelastase | P39900 | MMP12_HUMAN | Homo sapiens | 3 | 0.7589 |
Macrophage metalloelastase | P39900 | MMP12_HUMAN | Homo sapiens | 3 | 0.7589 |
14-3-3 protein gamma | P61981 | 1433G_HUMAN | Homo sapiens | 3 | 0.7587 |
14-3-3 protein gamma | P61981 | 1433G_HUMAN | Homo sapiens | 3 | 0.7587 |
Methionine aminopeptidase 2 | P9WK19 | MAP12_MYCTU | Mycobacterium tuberculosis | 3 | 0.7293 |
Methionine aminopeptidase 2 | P9WK19 | MAP12_MYCTU | Mycobacterium tuberculosis | 3 | 0.7293 |
Sex hormone-binding globulin | P04278 | SHBG_HUMAN | Homo sapiens | 3 | 0.7042 |
Sex hormone-binding globulin | P04278 | SHBG_HUMAN | Homo sapiens | 3 | 0.7042 |