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Compound Detail

CHEMBL553665

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CN(C(=O)Cc1cccc2occc12)[C@@H]1CCCC[C@H]1N1CCC(COC(=O)CCCC(=O)OCC2CCN([C@H]3CCCC[C@@H]3N(C)C(=O)Cc3cccc4occc34)C2)C1.Cl.Cl

Basic Information

ChEMBL ID CHEMBL553665
Phase Preclinical
Structure Type MOL
InChI Key DKVDIKPWFXJOOZ-BLCHAVQKSA-N
Parent Compound CHEMBL1194991
Active Moiety CHEMBL1194991
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

837.1
MW (Da)
7.40
ALogP
10
HBA
0
HBD
126.0
PSA (Ų)
0.11
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 C49H66Cl2N4O8
MW 909.99
Aromatic Rings 4
Heavy Atoms 61
NP-Likeness -0.06

Activity Summary

Ki 2 meas. best 6.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kappa-type opioid receptor
CHEMBL237
Ki 6.75 6.75 180.0 1
Mu-type opioid receptor
CHEMBL233
Ki 6.12 6.12 760.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2567782 10.1021/jm00127a036 Mu-type opioid receptor 2
2567782 10.1021/jm00127a036 Kappa-type opioid receptor 1
2567782 10.1021/jm00127a036 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine