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Compound Detail

CHEMBL4781688

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C#CCNC(=O)/C=C/c1c[nH]c2ccc(OC)cc12

Basic Information

ChEMBL ID CHEMBL4781688
Phase Preclinical
Structure Type MOL
InChI Key XQWAYIDPXUATOJ-QPJJXVBHSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

254.3
MW (Da)
1.94
ALogP
2
HBA
2
HBD
54.1
PSA (Ų)
0.65
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H14N2O2
MW 254.29
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness -0.62

Activity Summary

Ki 1 meas. best 8.03

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 8.03 8.03 9.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Ki = 9.3 nM 8.03 Displacement of [125l]-lodomelatonin from hamster brain cell QR2 incubated for 6... 32018096

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 ADMET 1

Data from ChEMBL 36 via Core Engine