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Compound Detail

CHEMBL3898452

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COc1cc(-c2ncn(/C=C\C(=O)OC(C)C)n2)cc(C(F)(F)F)c1

Basic Information

ChEMBL ID CHEMBL3898452
Phase Preclinical
Structure Type MOL
InChI Key NLNGWFLRRRYNIL-PLNGDYQASA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

355.3
MW (Da)
3.39
ALogP
6
HBA
0
HBD
66.2
PSA (Ų)
0.61
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H16F3N3O3
MW 355.32
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -0.82

Activity Summary

EC50 2 meas. best 8.3
IC50 2 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Jurkat
CHEMBL397
EC50 8.3 8.3 5.0 1
Exportin-1
CHEMBL5661
EC50 8.3 8.3 5.0 1
Exportin-1
CHEMBL5661
IC50 7.8 7.375 16.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
36155354 10.1016/j.ejmech.2022.114742 Exportin-1 2
39005064 10.1021/acs.jmedchem.4c00754 Exportin-1 2
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1
39005064 10.1021/acs.jmedchem.4c00754 Jurkat 1
39005064 10.1021/acs.jmedchem.4c00754 ADMET 1

Data from ChEMBL 36 via Core Engine