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Compound Detail

CHEMBL540972

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Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)c1nc2ccccc2[nH]1

Basic Information

ChEMBL ID CHEMBL540972
Phase Preclinical
Structure Type BOTH
InChI Key WYLIUTMBTUOERM-YGPDHOBYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

583.6
MW (Da)
2.55
ALogP
7
HBA
5
HBD
178.7
PSA (Ų)
0.19
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H33N5O6
MW 583.65
Aromatic Rings 4
Heavy Atoms 43
NP-Likeness -0.26

Activity Summary

IC50 2 meas. best 9.92
Ki 2 meas. best 9.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Delta-type opioid receptor
CHEMBL3222
IC50 9.92 9.92 0.1 1
Delta-type opioid receptor
CHEMBL269
Ki 9.35 9.35 0.4 1
Mu-type opioid receptor
CHEMBL270
Ki 7.27 7.27 53.9 1
Mu-type opioid receptor
CHEMBL4354
IC50 5.76 5.76 1724.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19642675 10.1021/jm900686q Delta-type opioid receptor 2
19642675 10.1021/jm900686q Mu-type opioid receptor 2
19642675 10.1021/jm900686q Unchecked 1

Data from ChEMBL 36 via Core Engine