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Compound Detail

CHEMBL186527

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Cc1[nH]c([C@@H]2CCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)nc1-c1ccccc1

Basic Information

ChEMBL ID CHEMBL186527
Phase Preclinical
Structure Type MOL
InChI Key WTLPGZMNWBXIHT-PMACEKPBSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

390.5
MW (Da)
3.32
ALogP
4
HBA
3
HBD
95.2
PSA (Ų)
0.62
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H26N4O2
MW 390.49
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.36

Activity Summary

EC50 1 meas. best 5.89
Ki 1 meas. best 7.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL270
Ki 7.64 7.64 23.1 1
Mu-type opioid receptor
CHEMBL4354
EC50 5.89 5.89 1300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15456245 10.1021/jm030548r Delta-type opioid receptor 2
15456245 10.1021/jm030548r Mu-type opioid receptor 2
15456245 10.1021/jm030548r Opioid receptors; mu & delta 1

Data from ChEMBL 36 via Core Engine