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Compound Detail

CHEMBL392207

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CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC1

Basic Information

ChEMBL ID CHEMBL392207
Phase Preclinical
Structure Type MOL
InChI Key SCPWCPHTILIICX-WDBFUDDQSA-N
4
Targets
10
Activities
3
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

818.0
MW (Da)
2.77
ALogP
8
HBA
6
HBD
203.3
PSA (Ų)
0.09
QED
2
Ro5 Violations
18
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C46H55N7O7
MW 817.99
Aromatic Rings 4
Heavy Atoms 60
NP-Likeness -0.52

Activity Summary

EC50 4 meas. best 7.43
IC50 4 meas. best 8.75
Ki 2 meas. best 9.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL236
Ki 9.16 9.16 0.7 1
Delta-type opioid receptor
CHEMBL236
IC50 8.75 8.75 1.8 1
Mu-type opioid receptor
CHEMBL270
Ki 7.64 7.64 23.0 1
Delta-type opioid receptor
CHEMBL3222
IC50 7.62 7.62 24.0 1
Delta-type opioid receptor
CHEMBL236
EC50 7.43 7.43 37.0 2
Mu-type opioid receptor
CHEMBL270
EC50 7.39 7.39 40.7 2
Mu-type opioid receptor
CHEMBL270
IC50 7.24 7.24 57.5 1
Mu-opioid receptor
CHEMBL5430
IC50 6.7 6.7 200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17927164 10.1021/jm061465o Delta-type opioid receptor 6
17927164 10.1021/jm061465o Mu-type opioid receptor 5
17927164 10.1021/jm061465o Unchecked 2
17927164 10.1021/jm061465o Mu-opioid receptor 1

Data from ChEMBL 36 via Core Engine