Rel-Pentazocine

Details

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Internal ID 17758b8f-cfb6-44b8-a023-7698fb9c258c
Taxonomy Alkaloids and derivatives > 6,7-benzomorphans > 2,6-dimethyl-3-benzazocines
IUPAC Name (1R,9R,13S)-1,13-dimethyl-10-(3-methylbut-2-enyl)-10-azatricyclo[7.3.1.02,7]trideca-2(7),3,5-trien-4-ol
SMILES (Canonical)
SMILES (Isomeric)
InChI InChI=1S/C19H27NO/c1-13(2)7-9-20-10-8-19(4)14(3)18(20)11-15-5-6-16(21)12-17(15)19/h5-7,12,14,18,21H,8-11H2,1-4H3/t14-,18-,19-/m1/s1
InChI Key VOKSWYLNZZRQPF-NIKGAXFTSA-N
Popularity 19 references in papers

Physical and Chemical Properties

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Molecular Formula C19H27NO
Molecular Weight 285.40 g/mol
Exact Mass 285.209264485 g/mol
Topological Polar Surface Area (TPSA) 23.50 Ų
XlogP 3.30
Atomic LogP (AlogP) 3.88
H-Bond Acceptor 2
H-Bond Donor 1
Rotatable Bonds 2

Synonyms

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(1R,9R,13S)-1,13-dimethyl-10-(3-methylbut-2-enyl)-10-azatricyclo(7.3.1.02,7)trideca-2(7),3,5-trien-4-ol
(1R,9R,13S)-1,13-dimethyl-10-(3-methylbut-2-enyl)-10-azatricyclo[7.3.1.02,7]trideca-2(7),3,5-trien-4-ol
RefChem:178808
CHEMBL397705
SCHEMBL135685
39188-58-4
BDBM50001033
BDBM50407300
PDSP2_001111
Pentazocine, Pentazocin, Sosegon, WIN 20228

2D Structure

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2D Structure of Rel-Pentazocine

3D Structure

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ADMET Properties (via admetSAR 2)

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Target Value Probability (raw) Probability (%)
Human Intestinal Absorption + 0.9761 97.61%
Caco-2 + 0.9546 95.46%
Blood Brain Barrier + 0.9750 97.50%
Human oral bioavailability - 0.9000 90.00%
Subcellular localzation Mitochondria 0.5665 56.65%
OATP2B1 inhibitior - 0.8624 86.24%
OATP1B1 inhibitior + 0.8283 82.83%
OATP1B3 inhibitior + 0.9387 93.87%
MATE1 inhibitior - 0.8400 84.00%
OCT2 inhibitior + 0.6000 60.00%
BSEP inhibitior - 0.5951 59.51%
P-glycoprotein inhibitior - 0.6050 60.50%
P-glycoprotein substrate + 0.9343 93.43%
CYP3A4 substrate - 0.5408 54.08%
CYP2C9 substrate - 1.0000 100.00%
CYP2D6 substrate + 0.6379 63.79%
CYP3A4 inhibition - 0.8155 81.55%
CYP2C9 inhibition - 0.8321 83.21%
CYP2C19 inhibition - 0.8585 85.85%
CYP2D6 inhibition + 0.8147 81.47%
CYP1A2 inhibition + 0.5886 58.86%
CYP2C8 inhibition - 0.7536 75.36%
CYP inhibitory promiscuity - 0.7780 77.80%
UGT catelyzed + 1.0000 100.00%
Carcinogenicity (binary) - 0.9600 96.00%
Carcinogenicity (trinary) Non-required 0.6851 68.51%
Eye corrosion - 0.9891 98.91%
Eye irritation - 0.9832 98.32%
Skin irritation - 0.7351 73.51%
Skin corrosion - 0.8220 82.20%
Ames mutagenesis - 0.7300 73.00%
Human Ether-a-go-go-Related Gene inhibition + 0.9005 90.05%
Micronuclear - 0.7100 71.00%
Hepatotoxicity - 0.9875 98.75%
skin sensitisation - 0.7681 76.81%
Respiratory toxicity + 0.9333 93.33%
Reproductive toxicity + 0.8000 80.00%
Mitochondrial toxicity + 0.9250 92.50%
Nephrotoxicity - 0.8449 84.49%
Acute Oral Toxicity (c) III 0.8066 80.66%
Estrogen receptor binding - 0.8682 86.82%
Androgen receptor binding - 0.8512 85.12%
Thyroid receptor binding + 0.8461 84.61%
Glucocorticoid receptor binding - 0.7385 73.85%
Aromatase binding - 0.5071 50.71%
PPAR gamma - 0.5752 57.52%
Honey bee toxicity - 0.8757 87.57%
Biodegradation - 0.8250 82.50%
Crustacea aquatic toxicity + 0.5300 53.00%
Fish aquatic toxicity + 0.9617 96.17%

Targets

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Proven Targets:

CHEMBL ID UniProt ID Name Min activity Assay type Source
CHEMBL4931 Q15125 3-beta-hydroxysteroid-delta(8),delta(7)-isomerase 500 nM
Ki
via Super-PRED
CHEMBL236 P41143 Delta opioid receptor 180 nM
49 nM
49 nM
Ki
Ki
Ki
PMID: 19027293
PMID: 20055417
via Super-PRED
CHEMBL237 P41145 Kappa opioid receptor 2.2 nM
2.2 nM
3 nM
Ki
Ki
Ki
via Super-PRED
PMID: 20055417
PMID: 19027293
CHEMBL233 P35372 Mu opioid receptor 3.9 nM
3.9 nM
6.9 nM
Ki
Ki
Ki
via Super-PRED
PMID: 20055417
PMID: 19027293
CHEMBL287 Q99720 Sigma opioid receptor 3.1 nM
83.1 nM
83.1 nM
83.1 nM
Ki
Ki
Ki
Ki
via Super-PRED
PMID: 10579824
PMID: 7636861
PMID: 7636860

Predicted Targets (via Super-PRED):

CHEMBL ID UniProt ID Name Probability Model accuracy
CHEMBL5619 P27695 DNA-(apurinic or apyrimidinic site) lyase 97.68% 91.11%
CHEMBL3251 P19838 Nuclear factor NF-kappa-B p105 subunit 97.57% 96.09%
CHEMBL5697 Q9GZT9 Egl nine homolog 1 95.95% 93.40%
CHEMBL2581 P07339 Cathepsin D 94.56% 98.95%
CHEMBL1293249 Q13887 Kruppel-like factor 5 94.25% 86.33%
CHEMBL4203 Q9HAZ1 Dual specificity protein kinase CLK4 92.91% 94.45%
CHEMBL5608 Q16288 NT-3 growth factor receptor 89.05% 95.89%
CHEMBL4208 P20618 Proteasome component C5 87.41% 90.00%
CHEMBL1994 P08235 Mineralocorticoid receptor 85.32% 100.00%
CHEMBL225 P28335 Serotonin 2c (5-HT2c) receptor 84.14% 89.62%
CHEMBL1907603 Q05586 Glutamate NMDA receptor; GRIN1/GRIN2B 83.84% 95.89%
CHEMBL4681 P42330 Aldo-keto-reductase family 1 member C3 83.70% 89.05%
CHEMBL5469 Q14289 Protein tyrosine kinase 2 beta 81.69% 91.03%

Plants that contains it

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Below are displayed all the plants proven (via scientific papers) to contain this compound!
To see more specific details click the taxa you are interested in.
Papaver somniferum

Cross-Links

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PubChem 9669
NPASS NPC8305
ChEMBL CHEMBL397705