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Compound Detail

CHEMBL47318

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CCN(CC)CC.CN(C(=O)Cc1ccc(Cl)c(Cl)c1)C(CN1CCCC1)c1ccc(NC(=O)CNC(=O)C/N=C(S)\N=C2/C=CC(=C3c4ccc(O)cc4Oc4cc(O)ccc43)C(C(=O)O)=C2)cc1

Basic Information

ChEMBL ID CHEMBL47318
Phase Preclinical
Structure Type MOL
InChI Key JRZWDZRRTRXBLW-RQQDMRFZSA-N
Parent Compound CHEMBL1178866
Active Moiety CHEMBL1178866
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

909.9
MW (Da)
7.21
ALogP
9
HBA
6
HBD
193.5
PSA (Ų)
0.04
QED
3
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C52H57Cl2N7O8S
MW 1011.04
Aromatic Rings 4
Heavy Atoms 63
NP-Likeness -0.56

Activity Summary

IC50 2 meas. best 7.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kappa-type opioid receptor
CHEMBL3952
IC50 7.32 7.32 48.0 1
Kappa-type opioid receptor
CHEMBL4329
IC50 6.77 6.77 170.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8648612 10.1021/jm950813b Kappa-type opioid receptor 2

Data from ChEMBL 36 via Core Engine