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Compound Detail

CHEMBL4096857

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CCC(=O)Nc1ccc2c(c1)[C@@]13CCN4CC5=CCO[C@H]6CC(=O)N2[C@H]1[C@H]6[C@H]5C[C@H]43

Basic Information

ChEMBL ID CHEMBL4096857
Phase Preclinical
Structure Type MOL
InChI Key BNLMIPXTXOQLRY-VKEHPUIKSA-N
2
Targets
7
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

405.5
MW (Da)
2.44
ALogP
4
HBA
1
HBD
61.9
PSA (Ų)
0.77
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
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 1.94

Activity Summary

IC50 6 meas. best 6.7
Ki 1 meas. best 7.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycine receptor subunit alpha-1
CHEMBL5845
Ki 7.17 7.17 67.0 1
Glycine receptor subunit alpha-1
CHEMBL5845
IC50 6.7 6.4133 201.0 3
Glycine receptor (alpha-1/beta)
CHEMBL2363052
IC50 6.51 6.19 311.0 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