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Compound Detail

CHEMBL127134

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COc1ccc2[nH]c(Br)c(CCNC(C)=O)c2c1Br

Basic Information

ChEMBL ID CHEMBL127134
Phase Preclinical
Structure Type MOL
InChI Key YRGTYQWTBUFELP-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

390.1
MW (Da)
3.38
ALogP
2
HBA
2
HBD
54.1
PSA (Ų)
0.84
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 C13H14Br2N2O2
MW 390.08
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness 0.25

Activity Summary

IC50 1 meas. best 7.63
Ki 1 meas. best 8.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melatonin receptor
CHEMBL2094268
Ki 8.24 8.24 5.8 1
Melatonin receptor
CHEMBL2094268
IC50 7.63 7.63 23.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9748358 10.1021/jm9810093 Melatonin receptor 3
9748358 10.1021/jm9810093 Melatonin receptor type 1C 1

Data from ChEMBL 36 via Core Engine