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Compound Detail

CHEMBL100940

NALTRIBEN
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Oc1ccc2c3c1O[C@H]1c4oc5ccccc5c4C[C@@]4(O)[C@@H](C2)N(CC2CC2)CC[C@]314

Basic Information

ChEMBL ID CHEMBL100940
Name NALTRIBEN
Phase Preclinical
Structure Type MOL
InChI Key ZHVWWEYETMPAMX-IFKAHUTRSA-N
3
Targets
3
Activities
1
Assay Types
9
PK Parameters
20
Publications
0
Known Names

Molecular Properties

415.5
MW (Da)
3.84
ALogP
5
HBA
2
HBD
66.1
PSA (Ų)
0.67
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H25NO4
MW 415.49
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness 1.26

Activity Summary

Ki 3 meas. best 10.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL236
Ki 10.89 10.89 0.0 1
Mu-type opioid receptor
CHEMBL4354
Ki 7.72 7.72 19.0 1
Kappa-type opioid receptor
CHEMBL3952
Ki 6.82 6.82 152.0 1

Pharmacokinetic Data

Parameter Value Units Species
Ke 0.27 - -
Ke 27.0 - Cavia porcellus
Ke 48.0 - Cavia porcellus
Ke 1.1 nM -
Ke 27.0 nM Cavia porcellus
Ke 48.0 nM Cavia porcellus
Ke 0.27 nM -
Ke 27.0 nM Cavia porcellus
Ke 48.0 nM Cavia porcellus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
1851846 10.1021/jm00109a027 Mu-type opioid receptor 5
1851846 10.1021/jm00109a027 Kappa-type opioid receptor 5
15163177 10.1021/jm0342358 Mus musculus 4
1851846 10.1021/jm00109a027 Delta-type opioid receptor 3
10836148 10.1146/annurev.pharmtox.40.1.581 UDP-glucuronosyltransferase 2B7 3
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
21764311 10.1016/j.bmcl.2011.06.085 Plasmodium chabaudi 2
1648136 10.1021/jm00110a001 Opioid receptors; delta & kappa 2
1648136 10.1021/jm00110a001 Opioid receptors; mu & delta 2
1648136 10.1021/jm00110a001 Kappa-type opioid receptor 2
1648136 10.1021/jm00110a001 Mu-type opioid receptor 2
1648136 10.1021/jm00110a001 Delta-type opioid receptor 2
2828619 10.1021/jm00397a001 Opioid receptors; delta & kappa 1
2828619 10.1021/jm00397a001 Opioid receptors; mu & delta 1
17367120 10.1021/jm0612463 Delta-type opioid receptor 1
2828619 10.1021/jm00397a001 Kappa-type opioid receptor 1
2828619 10.1021/jm00397a001 Mu-type opioid receptor 1
24613457 10.1016/j.bmc.2014.02.015 Delta-type opioid receptor 1
28662966 10.1016/j.bmc.2017.06.026 Trichomonas vaginalis 1
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1

Data from ChEMBL 36 via Core Engine