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Compound Detail

CHEMBL1907786

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CCN(CC)CC.CN(C(=O)Cc1ccc(Cl)c(Cl)c1)[C@H](CN1CCCC1)c1cccc(N/C(S)=N/c2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)c1

Basic Information

ChEMBL ID CHEMBL1907786
Phase Preclinical
Structure Type MOL
InChI Key NZWHASPXKHIDIB-SKRAEFHRSA-N
Parent Compound CHEMBL308813
Active Moiety CHEMBL308813
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

795.8
MW (Da)
9.14
ALogP
7
HBA
4
HBD
135.7
PSA (Ų)
0.05
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C48H51Cl2N5O6S
MW 896.94
Aromatic Rings 4
Heavy Atoms 55
NP-Likeness -0.58

Activity Summary

IC50 2 meas. best 9.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kappa-type opioid receptor
CHEMBL3952
IC50 9.43 9.43 0.4 1
Kappa-type opioid receptor
CHEMBL4329
IC50 8.92 8.92 1.2 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
8648612 10.1021/jm950813b Cavia porcellus 2
8648612 10.1021/jm950813b Mus musculus 1

Data from ChEMBL 36 via Core Engine