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Compound Detail

CHEMBL81465

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CCOc1ccc(Cc2nc3cc([N+]#N)ccc3n2CCN(CC)CC)cc1

Basic Information

ChEMBL ID CHEMBL81465
Phase Preclinical
Structure Type MOL
InChI Key MSXQHUDFYMEGJM-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

378.5
MW (Da)
4.85
ALogP
5
HBA
0
HBD
58.4
PSA (Ų)
0.50
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H28N5O+
MW 378.50
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.48

Activity Summary

Ki 2 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL270
Ki 7.96 7.96 11.0 1
Opioid receptor
CHEMBL2094129
Ki 7.75 7.75 18.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.8 hr -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2167979 10.1021/jm00171a020 Mu-type opioid receptor 4
2167979 10.1021/jm00171a020 Delta-type opioid receptor 1
2167979 10.1021/jm00171a020 Opioid receptor 1
2167979 10.1021/jm00171a020 ADMET 1

Data from ChEMBL 36 via Core Engine