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Compound Detail

CHEMBL4793947

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COc1ccc2[nH]cc(CCc3nn(CC4CCC4)c(=O)o3)c2c1

Basic Information

ChEMBL ID CHEMBL4793947
Phase Preclinical
Structure Type MOL
InChI Key FUMDPKVVUNFCGG-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

327.4
MW (Da)
2.91
ALogP
5
HBA
1
HBD
73.0
PSA (Ų)
0.76
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H21N3O3
MW 327.38
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -0.77

Activity Summary

Ki 2 meas. best 6.64
IC50 1 meas. best 4.13

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melatonin receptor type 1B
CHEMBL1946
Ki 6.64 6.64 230.0 1
Melatonin receptor type 1A
CHEMBL1945
Ki 6.26 6.26 550.0 1
Polyunsaturated fatty acid 5-lipoxygenase
CHEMBL215
IC50 4.13 4.13 74200.0 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 1
32018096 10.1016/j.ejmech.2020.112090 Melatonin receptor type 1B 1
32018096 10.1016/j.ejmech.2020.112090 No relevant target 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