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Compound Detail

CHEMBL5082031

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CCC(=O)N(CC1(N2CCNCC2)CCOCC1)c1cccc(C(F)(F)F)n1

Basic Information

ChEMBL ID CHEMBL5082031
Phase Preclinical
Structure Type MOL
InChI Key RQLWHDZQVHWZQP-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

400.4
MW (Da)
2.30
ALogP
5
HBA
1
HBD
57.7
PSA (Ų)
0.82
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H27F3N4O2
MW 400.44
Aromatic Rings 1
Heavy Atoms 28
NP-Likeness -1.10

Activity Summary

EC50 1 meas. best 5.91
Ki 1 meas. best 6.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mu-type opioid receptor
CHEMBL233
Ki 6.68 6.68 209.0 1
Mu-type opioid receptor
CHEMBL233
EC50 5.91 5.91 1237.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34236190 10.1021/acs.jmedchem.1c00417 Mu-type opioid receptor 2
34236190 10.1021/acs.jmedchem.1c00417 Sigma non-opioid intracellular receptor 1 1
34236190 10.1021/acs.jmedchem.1c00417 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine