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Compound Detail

CHEMBL476131

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COc1ccc2cc(-c3cccc(CO)c3)cc(CCNC(C)=O)c2c1

Basic Information

ChEMBL ID CHEMBL476131
Phase Preclinical
Structure Type MOL
InChI Key BHDVJMSEODZSTD-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

349.4
MW (Da)
3.69
ALogP
3
HBA
2
HBD
58.6
PSA (Ų)
0.71
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23NO3
MW 349.43
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -0.02

Activity Summary

Ki 2 meas. best 9.44
EC50 1 meas. best 9.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melatonin receptor type 1B
CHEMBL1946
Ki 9.44 9.44 0.4 1
Melatonin receptor type 1B
CHEMBL1946
EC50 9.12 9.12 0.8 1
Melatonin receptor type 1A
CHEMBL1945
Ki 6.56 6.56 275.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18778943 10.1016/j.bmc.2008.08.052 Melatonin receptor type 1B 5
18778943 10.1016/j.bmc.2008.08.052 Melatonin receptor type 1A 1
18778943 10.1016/j.bmc.2008.08.052 Unchecked 1

Data from ChEMBL 36 via Core Engine