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Compound Detail

CHEMBL274896

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CCOc1ccc2c(c1)c(CCNC(C)=O)c1n2Cc2ccccc2-1

Basic Information

ChEMBL ID CHEMBL274896
Phase Preclinical
Structure Type MOL
InChI Key LSWRLJBFCSSIGO-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

334.4
MW (Da)
3.75
ALogP
3
HBA
1
HBD
43.3
PSA (Ų)
0.60
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H22N2O2
MW 334.42
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -0.65

Activity Summary

Ki 2 meas. best 9.68
EC50 1 meas. best 6.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melatonin receptor type 1B
CHEMBL1946
Ki 9.68 9.68 0.2 1
Melatonin receptor type 1A
CHEMBL1945
Ki 7.74 7.74 18.2 1
Unchecked
CHEMBL612545
EC50 6.5 6.5 316.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10737738 10.1021/jm980684+ Unchecked 2
12672242 10.1021/jm020982d Melatonin receptor type 1A 1
12672242 10.1021/jm020982d Melatonin receptor type 1B 1
10737738 10.1021/jm980684+ Melatonin receptor type 1A 1
10737738 10.1021/jm980684+ Melatonin receptor type 1B 1
10737738 10.1021/jm980684+ Melatonin receptor 1

Data from ChEMBL 36 via Core Engine