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Compound Detail

CHEMBL4060962

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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 CHEMBL4060962
Phase Preclinical
Structure Type MOL
InChI Key NRGHCWQGTHPFTE-FVWCLLPLSA-N
3
Targets
7
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

349.4
MW (Da)
1.67
ALogP
4
HBA
1
HBD
58.8
PSA (Ų)
0.57
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C21H23N3O2
MW 349.43
Aromatic Rings 1
Heavy Atoms 26
NP-Likeness 2.90

Activity Summary

IC50 6 meas. best 7.12
Ki 1 meas. best 7.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycine receptor subunit alpha-1
CHEMBL3246
Ki 7.75 7.75 18.0 1
Glycine receptor subunit alpha-1
CHEMBL5845
IC50 7.12 7.1133 76.0 3
Glycine receptor (alpha-1/beta)
CHEMBL2363052
IC50 7.01 6.7133 97.0 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
27966945 10.1021/acs.jnatprod.6b00479 Unchecked 1

Data from ChEMBL 36 via Core Engine