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Compound Detail

CHEMBL247758

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Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)O

Basic Information

ChEMBL ID CHEMBL247758
Phase Preclinical
Structure Type MOL
InChI Key MNNRFUWQCDJULI-CGIBELHQSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

624.7
MW (Da)
0.24
ALogP
7
HBA
7
HBD
222.8
PSA (Ų)
0.14
QED
2
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H44N6O7
MW 624.74
Aromatic Rings 2
Heavy Atoms 45
NP-Likeness -0.23

Activity Summary

Ki 3 meas. best 9.11
EC50 2 meas. best 8.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL236
Ki 9.11 9.11 0.8 1
Delta-type opioid receptor
CHEMBL236
EC50 8.6 8.6 2.5 1
Mu-type opioid receptor
CHEMBL233
Ki 8.01 8.01 9.8 1
Mu-type opioid receptor
CHEMBL233
EC50 7.31 7.31 49.0 1
Kappa-type opioid receptor
CHEMBL237
Ki 5.62 5.62 2400.0 1

Activity Data Samples

Top measurements by pChEMBL value

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
17350835 10.1016/j.bmcl.2007.01.092 Unchecked 1

Data from ChEMBL 36 via Core Engine