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Compound Detail

CHEMBL5080554

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COc1ccsc1CNCC[C@@]1(c2ccccn2)CCO[C@]2(CCOC2)C1

Basic Information

ChEMBL ID CHEMBL5080554
Phase Preclinical
Structure Type MOL
InChI Key ILILGGPBJCSIFA-NHCUHLMSSA-N
2
Targets
3
Activities
2
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

388.5
MW (Da)
3.54
ALogP
6
HBA
1
HBD
52.6
PSA (Ų)
0.74
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H28N2O3S
MW 388.53
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.51

Activity Summary

EC50 2 meas. best 8.0
IC50 1 meas. best 4.45

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL233
EC50 8.0 7.85 10.0 2
Cytochrome P450 2D6
CHEMBL289
IC50 4.45 4.45 35500.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 9.3 mL.min-1.kg-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34802839 10.1016/j.ejmech.2021.113986 Mu-type opioid receptor 4
34802839 10.1016/j.ejmech.2021.113986 ADMET 1

Data from ChEMBL 36 via Core Engine