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Compound Detail

CHEMBL4865307

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COc1cc(CCC(C)NCc2ccc(C(F)(F)F)cc2)ccc1O

Basic Information

ChEMBL ID CHEMBL4865307
Phase Preclinical
Structure Type MOL
InChI Key JWMMMNZRBWMHKZ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

353.4
MW (Da)
4.53
ALogP
3
HBA
2
HBD
41.5
PSA (Ų)
0.77
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H22F3NO2
MW 353.38
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -0.40

Activity Summary

Ki 1 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sigma intracellular receptor 2
CHEMBL4105907
Ki 8.05 8.05 9.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.2667 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sigma intracellular receptor 2 Ki = 9.0 nM 8.05 Binding affinity to Sigma 2-receptor (unknown origin) 34531947

Literature References

PubMed DOI Target Context # Activities
34531947 10.1021/acsmedchemlett.1c00048 N2a 1
34531947 10.1021/acsmedchemlett.1c00048 Sigma intracellular receptor 2 1
34531947 10.1021/acsmedchemlett.1c00048 ADMET 1

Data from ChEMBL 36 via Core Engine