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Compound Detail

CHEMBL76089

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Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1COCc1ccccc1

Basic Information

ChEMBL ID CHEMBL76089
Phase Preclinical
Structure Type MOL
InChI Key ZTQQXSLWESVZAR-IGKIAQTJSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

444.6
MW (Da)
4.05
ALogP
4
HBA
2
HBD
75.8
PSA (Ų)
0.58
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H32N2O3
MW 444.58
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.02

Activity Summary

IC50 3 meas. best 9.48
EC50 1 meas. best 9.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL236
IC50 9.48 9.48 0.3 1
Delta-type opioid receptor
CHEMBL236
EC50 9.01 9.01 1.0 1
Mu-type opioid receptor
CHEMBL233
IC50 7.9 7.9 12.5 1
Kappa-type opioid receptor
CHEMBL237
IC50 7.19 7.19 64.6 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11448220 10.1021/jm015532k Delta-type opioid receptor 3
11448220 10.1021/jm015532k Mu-type opioid receptor 2
11448220 10.1021/jm015532k Kappa-type opioid receptor 1
11448220 10.1021/jm015532k Opioid receptors; mu & delta 1
11448220 10.1021/jm015532k Opioid receptors; delta & kappa 1

Data from ChEMBL 36 via Core Engine