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Compound Detail

CHEMBL537616

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Br.CN(C(=O)Cc1cccc2occc12)[C@@H]1CCCC[C@H]1N1CCCC1

Basic Information

ChEMBL ID CHEMBL537616
Phase Preclinical
Structure Type MOL
InChI Key WCLURLUVZBQRNH-STYNFMPRSA-N
Parent Compound CHEMBL1188870
Active Moiety CHEMBL1188870
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

340.5
MW (Da)
3.84
ALogP
3
HBA
0
HBD
36.7
PSA (Ų)
0.85
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H29BrN2O2
MW 421.38
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -0.26

Activity Summary

Ki 2 meas. best 8.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kappa-type opioid receptor
CHEMBL3952
Ki 8.38 8.38 4.2 1
Mu-type opioid receptor
CHEMBL4354
Ki 5.48 5.48 3300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2832603 10.1021/jm00399a025 Kappa-type opioid receptor 1
2832603 10.1021/jm00399a025 Mu-type opioid receptor 1
2832603 10.1021/jm00399a025 Rattus norvegicus 1
2832603 10.1021/jm00399a025 Opioid receptors; mu & kappa 1

Data from ChEMBL 36 via Core Engine