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Compound Detail

CHEMBL246740

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CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cc[n+]([O-])cc1)C(=O)N[C@H](C(=O)O)[C@@H](C)O

Basic Information

ChEMBL ID CHEMBL246740
Phase Preclinical
Structure Type MOL
InChI Key PDLKKPWJIQINFZ-GQHROEFJSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

687.8
MW (Da)
-3.01
ALogP
10
HBA
9
HBD
276.2
PSA (Ų)
0.05
QED
2
Ro5 Violations
19
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H45N7O10
MW 687.75
Aromatic Rings 2
Heavy Atoms 49

Activity Summary

Ki 1 meas. best 6.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL236
Ki 6.44 6.44 360.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Delta-type opioid receptor Ki = 360.0 nM 6.44 Displacement of [3H]diprenorphine from human cloned delta opioid receptor 17350835

Literature References

PubMed DOI Target Context # Activities
17350835 10.1016/j.bmcl.2007.01.092 Mu-type opioid receptor 2
17350835 10.1016/j.bmcl.2007.01.092 Delta-type opioid receptor 2
17350835 10.1016/j.bmcl.2007.01.092 Kappa-type opioid receptor 1

Data from ChEMBL 36 via Core Engine