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Compound Detail

CHEMBL329960

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COc1ccc2oc(Cc3ccccc3OC)c(CCNC(C)=O)c2c1

Basic Information

ChEMBL ID CHEMBL329960
Phase Preclinical
Structure Type MOL
InChI Key UUCZUAXLGXFIDX-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

353.4
MW (Da)
3.72
ALogP
4
HBA
1
HBD
60.7
PSA (Ų)
0.70
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23NO4
MW 353.42
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -0.25

Activity Summary

Ki 2 meas. best 9.47
EC50 1 meas. best 9.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melatonin receptor type 1B
CHEMBL1946
Ki 9.47 9.47 0.3 1
Melatonin receptor type 1B
CHEMBL1946
EC50 9.39 9.39 0.4 1
Melatonin receptor type 1A
CHEMBL1945
Ki 7.84 7.84 14.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12061881 10.1021/jm0005252 Melatonin receptor type 1A 4
12061881 10.1021/jm0005252 Melatonin receptor type 1B 4
15177448 10.1016/j.bmcl.2004.04.073 Melatonin receptor type 1A 1
15177448 10.1016/j.bmcl.2004.04.073 Melatonin receptor type 1B 1
15177448 10.1016/j.bmcl.2004.04.073 Melatonin receptor 1
12061881 10.1021/jm0005252 Melatonin receptor 1

Data from ChEMBL 36 via Core Engine