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Compound Detail

CHEMBL2111686

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COc1cccc([C@]23CCN(C)[C@H](CC(=O)C2)C3)c1

Basic Information

ChEMBL ID CHEMBL2111686
Phase Preclinical
Structure Type MOL
InChI Key RMXPANLFBPCCIX-CJNGLKHVSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

259.4
MW (Da)
2.39
ALogP
3
HBA
0
HBD
29.5
PSA (Ų)
0.82
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 C16H21NO2
MW 259.35
Aromatic Rings 1
Heavy Atoms 19
NP-Likeness 0.40

Activity Summary

Ki 5 meas. best 7.45

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL270
Ki 7.45 7.45 35.5 1
Muscarinic acetylcholine receptor
CHEMBL1907609
Ki 7.41 7.41 39.1 1
Delta-type opioid receptor
CHEMBL269
Ki 6.3 6.3 504.9 1
Sigma non-opioid intracellular receptor 1
CHEMBL287
Ki 6.12 6.12 762.3 1
Kappa-type opioid receptor
CHEMBL3952
Ki 5.6 5.6 2536.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7932540 10.1021/jm00045a022 Sigma non-opioid intracellular receptor 1 1
7932540 10.1021/jm00045a022 Glutamate NMDA receptor 1
7932540 10.1021/jm00045a022 Muscarinic acetylcholine receptor 1
7932540 10.1021/jm00045a022 Mu-type opioid receptor 1
7932540 10.1021/jm00045a022 Delta-type opioid receptor 1
7932540 10.1021/jm00045a022 Kappa-type opioid receptor 1
7932540 10.1021/jm00045a022 Unchecked 1

Data from ChEMBL 36 via Core Engine