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Compound Detail

CHEMBL208307

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COc1ccc2c(c1)c(C(C)(C)CNC(C)=O)cn2C

Basic Information

ChEMBL ID CHEMBL208307
Phase Preclinical
Structure Type MOL
InChI Key ZSIPGILAUKWEQQ-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

274.4
MW (Da)
2.60
ALogP
3
HBA
1
HBD
43.3
PSA (Ų)
0.93
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H22N2O2
MW 274.36
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness -0.64

Activity Summary

Ki 2 meas. best 8.89
EC50 1 meas. best 8.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melatonin receptor type 1B
CHEMBL1946
Ki 8.89 8.89 1.3 1
Melanophore
CHEMBL614313
EC50 8.2 8.2 6.3 1
Melatonin receptor type 1A
CHEMBL1945
Ki 7.94 7.94 11.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16759094 10.1021/jm0512544 Melanophore 2
16759094 10.1021/jm0512544 Melatonin receptor type 1A 1
16759094 10.1021/jm0512544 Melatonin receptor type 1B 1
16759094 10.1021/jm0512544 Melatonin receptor 1

Data from ChEMBL 36 via Core Engine