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Compound Detail

CHEMBL4783536

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COc1ccc2[nH]cc(/C=C/c3n[nH]c(=O)o3)c2c1

Basic Information

ChEMBL ID CHEMBL4783536
Phase Preclinical
Structure Type MOL
InChI Key MBWWTUVCPDXVML-GORDUTHDSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

257.2
MW (Da)
2.02
ALogP
4
HBA
2
HBD
83.9
PSA (Ų)
0.75
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H11N3O3
MW 257.25
Aromatic Rings 3
Heavy Atoms 19
NP-Likeness -0.26

Activity Summary

IC50 2 meas. best 4.28
Ki 1 meas. best 8.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 8.18 8.18 6.6 1
Amine oxidase [flavin-containing] A
CHEMBL1951
IC50 4.28 4.28 53000.0 1
Amine oxidase [flavin-containing] B
CHEMBL2039
IC50 4.17 4.17 68300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32018096 10.1016/j.ejmech.2020.112090 Melatonin receptor type 1A 2
32018096 10.1016/j.ejmech.2020.112090 Melatonin receptor type 1B 2
32018096 10.1016/j.ejmech.2020.112090 Unchecked 1
32018096 10.1016/j.ejmech.2020.112090 No relevant target 1
32018096 10.1016/j.ejmech.2020.112090 Nuclear factor erythroid 2-related factor 2 1
32018096 10.1016/j.ejmech.2020.112090 Kelch-like ECH-associated protein 1 1
32018096 10.1016/j.ejmech.2020.112090 Amine oxidase [flavin-containing] A 1
32018096 10.1016/j.ejmech.2020.112090 Amine oxidase [flavin-containing] B 1
32018096 10.1016/j.ejmech.2020.112090 Polyunsaturated fatty acid 5-lipoxygenase 1
32018096 10.1016/j.ejmech.2020.112090 ADMET 1

Data from ChEMBL 36 via Core Engine