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Compound Detail

CHEMBL611144

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CCCCOc1cccc2c1[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(OC)CCC(=O)C3

Basic Information

ChEMBL ID CHEMBL611144
Phase Preclinical
Structure Type MOL
InChI Key ONTSMVMHZIYPME-QLBJFCOMSA-N
3
Targets
3
Activities
1
Assay Types
3
PK Parameters
9
Publications
0
Known Names

Molecular Properties

397.6
MW (Da)
4.28
ALogP
4
HBA
0
HBD
38.8
PSA (Ų)
0.64
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H35NO3
MW 397.56
Aromatic Rings 1
Heavy Atoms 29
NP-Likeness 0.88

Activity Summary

Ki 3 meas. best 7.86

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL270
Ki 7.86 7.86 13.8 1
Kappa-type opioid receptor
CHEMBL3952
Ki 6.58 6.58 263.0 1
Delta-type opioid receptor
CHEMBL269
Ki 6.12 6.12 758.6 1

Pharmacokinetic Data

Parameter Value Units Species
Ke 21.0 nM Mus musculus
Ke 811.0 nM Mus musculus
Ke 2050.0 nM Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2157011 10.1021/jm00166a018 Mu-type opioid receptor 1
2157011 10.1021/jm00166a018 Kappa-type opioid receptor 1
2157011 10.1021/jm00166a018 Delta-type opioid receptor 1
2157011 10.1021/jm00166a018 Opioid receptors; mu & kappa 1
2157011 10.1021/jm00166a018 Opioid receptors; mu & delta 1
15743203 10.1021/jm049117e Delta-type opioid receptor 1
15743203 10.1021/jm049117e Mu-type opioid receptor 1
15743203 10.1021/jm049117e Kappa-type opioid receptor 1
20580236 10.1016/j.bmc.2010.05.071 Acetylcholinesterase 1

Data from ChEMBL 36 via Core Engine