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Compound Detail

CHEMBL226539

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COc1cc2c(cc1OC)CN(CCCCNC(=O)c1cc(C)ccc1OCCF)CC2

Basic Information

ChEMBL ID CHEMBL226539
Phase Preclinical
Structure Type MOL
InChI Key QVRVXSZKCXFBTE-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

444.6
MW (Da)
3.93
ALogP
5
HBA
1
HBD
60.0
PSA (Ų)
0.53
QED
0
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H33FN2O4
MW 444.55
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.05

Activity Summary

Ki 4 meas. best 8.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 8.18 8.17 6.6 2
Sigma non-opioid intracellular receptor 1
CHEMBL3465
Ki 6.48 6.48 330.0 1
Sigma non-opioid intracellular receptor 1
CHEMBL4153
Ki 6.48 6.48 330.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17579383 10.1021/jm0614883 Unchecked 2
24821398 10.1021/jm5001453 Unchecked 2
17579383 10.1021/jm0614883 Sigma non-opioid intracellular receptor 1 1
24821398 10.1021/jm5001453 No relevant target 1
24821398 10.1021/jm5001453 Sigma non-opioid intracellular receptor 1 1

Data from ChEMBL 36 via Core Engine