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Compound Detail

CHEMBL4102677

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CO/N=C1/C(=O)N2c3ccccc3[C@@]34CCN5CC6=CCO[C@@H]1[C@@H]([C@H]23)[C@H]6C[C@H]54

Basic Information

ChEMBL ID CHEMBL4102677
Phase Preclinical
Structure Type MOL
InChI Key JIEFHNBYMOMHOJ-IBESPKCESA-N
2
Targets
7
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

377.4
MW (Da)
1.70
ALogP
5
HBA
0
HBD
54.4
PSA (Ų)
0.55
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23N3O3
MW 377.44
Aromatic Rings 1
Heavy Atoms 28
NP-Likeness 2.37

Activity Summary

IC50 6 meas. best 7.25
Ki 1 meas. best 6.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycine receptor (alpha-1/beta)
CHEMBL2363052
IC50 7.25 6.8667 56.0 3
Glycine receptor subunit alpha-1
CHEMBL5845
IC50 7.12 7.0333 75.0 3
Glycine receptor subunit alpha-1
CHEMBL5845
Ki 6.72 6.72 189.0 1

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