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Compound Detail

CHEMBL499868

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Cl.Nc1ccc(Oc2ccc3c(c2)[C@@]24CCCC[C@@]2(O)[C@@H](C3)N(CC2CCC2)CC4)cc1

Basic Information

ChEMBL ID CHEMBL499868
Phase Preclinical
Structure Type MOL
InChI Key DCKHDZCNJPNFLI-QGNMAPLWSA-N
Parent Compound CHEMBL1187348
Active Moiety CHEMBL1187348
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

418.6
MW (Da)
5.03
ALogP
4
HBA
2
HBD
58.7
PSA (Ų)
0.68
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H35ClN2O2
MW 455.04
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness 0.77

Activity Summary

Ki 3 meas. best 8.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL233
Ki 8.41 8.41 3.9 1
Kappa-type opioid receptor
CHEMBL237
Ki 8.28 8.28 5.2 1
Delta-type opioid receptor
CHEMBL236
Ki 6.03 6.03 930.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18674902 10.1016/j.bmcl.2008.07.054 Unchecked 3
18674902 10.1016/j.bmcl.2008.07.054 Mu-type opioid receptor 1
18674902 10.1016/j.bmcl.2008.07.054 Delta-type opioid receptor 1
18674902 10.1016/j.bmcl.2008.07.054 Kappa-type opioid receptor 1

Data from ChEMBL 36 via Core Engine