Ingredient Details :Brevelin A


TCMI-ID: TCMI14761


Physicochemical Property
Ingredient Name Brevelin A
Pubchem CID 12302076
Iupac name [(1S,3aR,5R,5aR,8aR,9S,9aR)-1,5,8a-trimethyl-2,8-dioxo-3a,4,5,5a,9,9a-hexahydro-1H-azuleno[6,5-b]furan-9-yl] (Z)-2-methylbut-2-enoate
Molecular Formula C20H26O5
Molecular Weight 346.4
Isomeric smiles C/C=C(/C)\C(=O)O[C@H]1[C@@H]2[C@@H](C(=O)O[C@@H]2C[C@H]([C@H]3[C@]1(C(=O)C=C3)C)C)C
InChI InChI=1S/C20H26O5/c1-6-10(2)18(22)25-17-16-12(4)19(23)24-14(16)9-11(3)13-7-8-15(21)20(13,17)5/h6-8,11-14,16-17H,9H2,1-5H3/b10-6-/t11-,12+,13+,14-,16-,17+,20+/m1/s1
InChIKey KUPPZVXLWANEJJ-UXPPPGSFSA-N
External Database Links HERB2.0: HBIN018833   HIT2: C0535   SymMap: SMIT12589   TCM-ID: TCMC2653   ChEMBL: CHEMBL2262842  
Structural Information
nHA(Number of hydrogen bond acceptors) 5
nHD(Number of hydrogen bond donors) 0
nRot(Number of rotatable bonds) 3
nRing(Number of rings) 3
MaxRing(Number of atoms in the biggest ring) 13
nHet(Number of heteroatoms) 5

Stability
nRig(Number of rigid bonds) 19
Flexibility 0.158
Stereo Centers(Number of stereocenters) 7

Solubility
TPSA(Topological polar surface area) 69.67
logS(The logarithm of aqueous solubility value) -3.448
logP(The logarithm of the n-octanol/water distribution coefficient) 2.76
logD7.4(The logarithm of the n-octanol/water distribution coefficients at pH=7.4) 3.025

Pharmacokinetic Property
Quantitative Estimate of Drug-likeness 0.568
Synthetic accessibility score 4.871
Natural Product-likeness score 3.535
Lipinski Rule Accepted
GSK Rule Accepted
Golden Triangle Accepted

Absorption
Caco-2 Permeability -4.665
MDCK Permeability 4.39E-05
Pgp-substrate 0
HIA(human intestinal absorption) 0.004
F20%(20% Oral Bioavailability) 0.144
F30%(30% Oral Bioavailability) 0.985

Distribution
PPB(Plasma protein binding) 92.81%
VD(Volume Distribution) 0.59
BBB Penetration(Blood brain barrier penetration) 0.241
B3 Penetration(Blood brain barrier penetration) Permeable
Fu(The fraction unbound in plasms) 11.55%

Metabolism
CYP1A2 inhibitor 0.545
CYP1A2 substrate 0.104
CYP2C19 inhibitor 0.099
CYP2C19 substrate 0.812
CYP2C9 inhibitor 0.27
CYP2C9 substrate 0.024
CYP2D6 inhibitor 0.008
CYP2D6 substrate 0.056
CYP3A4 inhibitor 0.67
CYP3A4 substrate 0.433

Excretion
CL(The clearance of a drug) 11.084
T1/2 0.669

Toxicology
NonBiodegradable Rule 1
Pfizer Rule Accepted
SR-MMP 0.355

Toxic Dose
FDAMDD(FDA Maximum (Recommended) Daily Dose) 0.455
IGC50 4.314
LC50FM 5.938
LC50DM 6.562

Reproductive Effects
NR-AR(Androgen receptor) 0.182
NR-AR-LBD(Androgen receptor) 0.555
NR-Aromatase 0.847
NR-ER(Estrogen receptor) 0.114
NR-ER-LBD(Estrogen receptor) 0.031

Allergy
Skin Sensitization Rule 2
Skin Sensitization 0.87

Acute Toxicity
Acute Toxicity Rule 5
Rat Oral Acute Toxicity 0.485

Organ Toxicity
hERG Blockers 0.117
H-HT(The human hepatotoxicity) 0.939
DILI(Drug-induced liver injury) 0.608

Primary Irritation
Eye Corrosion 0.062
Eye Irritation 0.151
Respiratory Toxicity 0.901

Mutagenic Effects
AMES Toxicity 0.064

Tumorigenic Effects
Carcinogencity 0.152
SR-ARE(Antioxidant Response Element) 0.634
SR-ATAD5(ATPase family AAA domain-containing protein 5) 0.088
SR-p53 0.875

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