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Compound Detail

CHEMBL4089150

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O=C1/C(=N/O)[C@@H]2OCC=C3CN4CC[C@]56c7ccccc7N1[C@H]5[C@H]2[C@H]3C[C@H]46

Basic Information

ChEMBL ID CHEMBL4089150
Phase Preclinical
Structure Type MOL
InChI Key CMOAVMXESDVBSR-SJOSXICLSA-N
2
Targets
7
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

363.4
MW (Da)
1.53
ALogP
5
HBA
1
HBD
65.4
PSA (Ų)
0.43
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H21N3O3
MW 363.42
Aromatic Rings 1
Heavy Atoms 27
NP-Likeness 2.48

Activity Summary

IC50 6 meas. best 7.1
Ki 1 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycine receptor subunit alpha-1
CHEMBL5845
Ki 7.4 7.4 40.0 1
Glycine receptor (alpha-1/beta)
CHEMBL2363052
IC50 7.1 6.8167 80.0 3
Glycine receptor subunit alpha-1
CHEMBL5845
IC50 7.09 7.0367 82.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27966945 10.1021/acs.jnatprod.6b00479 Glycine receptor subunit alpha-1 4
27966945 10.1021/acs.jnatprod.6b00479 Glycine receptor (alpha-1/beta) 3

Data from ChEMBL 36 via Core Engine