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Compound Detail

CHEMBL242330

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NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1

Basic Information

ChEMBL ID CHEMBL242330
Phase Preclinical
Structure Type BOTH
InChI Key MDRZLPSBYOQZRA-QORCZRPOSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

561.6
MW (Da)
-0.08
ALogP
7
HBA
6
HBD
196.5
PSA (Ų)
0.18
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H35N7O5
MW 561.64
Aromatic Rings 3
Heavy Atoms 41
NP-Likeness -0.17

Activity Summary

IC50 1 meas. best 5.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL270
IC50 5.35 5.35 4490.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mu-type opioid receptor IC50 = 4490.0 nM 5.35 Displacement of [3H]DAGO from mu opioid receptor in rat brain membrane 17395470

Literature References

PubMed DOI Target Context # Activities
17395470 10.1016/j.bmc.2007.03.009 Mu-type opioid receptor 1
17395470 10.1016/j.bmc.2007.03.009 Delta-type opioid receptor 1

Data from ChEMBL 36 via Core Engine