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Compound Detail

CHEMBL4518537

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

Basic Information

ChEMBL ID CHEMBL4518537
Phase Preclinical
Structure Type MOL
InChI Key ZYQOFJMYFTVXSE-ODOYRXLASA-N
2
Targets
7
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

405.5
MW (Da)
1.60
ALogP
4
HBA
1
HBD
61.9
PSA (Ų)
0.76
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H27N3O3
MW 405.50
Aromatic Rings 1
Heavy Atoms 30
NP-Likeness 2.06

Activity Summary

IC50 6 meas. best 6.83
Ki 1 meas. best 7.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycine receptor subunit alpha-1
CHEMBL5845
Ki 7.04 7.04 91.0 1
Glycine receptor (alpha-1/beta)
CHEMBL2363052
IC50 6.83 6.05 147.0 3
Glycine receptor subunit alpha-1
CHEMBL5845
IC50 6.76 6.3533 173.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31385511 10.1021/acs.jnatprod.9b00180 Glycine receptor subunit alpha-1 4
31385511 10.1021/acs.jnatprod.9b00180 Glycine receptor (alpha-1/beta) 3

Data from ChEMBL 36 via Core Engine