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Compound Detail

CHEMBL187525

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COc1cc2c(cc1OC)C(CC(c1ccccc1)c1ccccc1)N(C(C)=O)CC2

Basic Information

ChEMBL ID CHEMBL187525
Phase Preclinical
Structure Type MOL
InChI Key MYRDIKPCKNULKX-UHFFFAOYSA-N
1
Targets
3
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

415.5
MW (Da)
5.37
ALogP
3
HBA
0
HBD
38.8
PSA (Ų)
0.54
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H29NO3
MW 415.53
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness 0.09

Activity Summary

IC50 2 meas. best 8.01
Ki 1 meas. best 8.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melatonin receptor type 1B
CHEMBL1946
IC50 8.01 8.01 9.7 2
Melatonin receptor type 1B
CHEMBL1946
Ki 8.01 8.01 9.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15501061 10.1016/j.bmcl.2004.09.024 Melatonin receptor type 1B 1
15501061 10.1016/j.bmcl.2004.09.024 Melatonin receptor type 1A 1
15501061 10.1016/j.bmcl.2004.09.024 Melatonin receptor 1
15943478 10.1021/jm048956y Melatonin receptor type 1A 1
15943478 10.1021/jm048956y Melatonin receptor type 1B 1
24228714 10.1021/jm401343c Unchecked 1
24228714 10.1021/jm401343c Melatonin receptor type 1A 1
24228714 10.1021/jm401343c Melatonin receptor type 1B 1

Data from ChEMBL 36 via Core Engine