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Compound Detail

CHEMBL240870

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O=C1NCN(c2ccccc2)C12CCN(C1c3ccccc3CCc3ccccc31)CC2

Basic Information

ChEMBL ID CHEMBL240870
Phase Preclinical
Structure Type MOL
InChI Key CYUOYAHXHKYGLA-UHFFFAOYSA-N
5
Targets
5
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

423.6
MW (Da)
4.30
ALogP
3
HBA
1
HBD
35.6
PSA (Ų)
0.67
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 C28H29N3O
MW 423.56
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.15

Activity Summary

Ki 4 meas. best 6.65
EC50 1 meas. best 5.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nociceptin receptor
CHEMBL2014
Ki 6.65 6.65 225.0 1
Kappa-type opioid receptor
CHEMBL237
Ki 5.78 5.78 1672.0 1
Mu-type opioid receptor
CHEMBL233
Ki 5.61 5.61 2454.0 1
H4
CHEMBL1075452
EC50 5.29 5.29 5100.0 1
Delta-type opioid receptor
CHEMBL236
Ki 5.01 5.01 9784.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17289383 10.1016/j.bmcl.2007.01.069 Nociceptin receptor 1
17289383 10.1016/j.bmcl.2007.01.069 Delta-type opioid receptor 1
17289383 10.1016/j.bmcl.2007.01.069 Kappa-type opioid receptor 1
17289383 10.1016/j.bmcl.2007.01.069 Mu-type opioid receptor 1
21126871 10.1016/j.bmcl.2010.11.029 H4 1

Data from ChEMBL 36 via Core Engine