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Compound Detail

CHEMBL272211

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COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1c(-c2cccc(OC(F)(F)F)c2)nc2sccn12

Basic Information

ChEMBL ID CHEMBL272211
Phase Preclinical
Structure Type MOL
InChI Key CNRYCFMEVIGJCK-UHFFFAOYSA-N
2
Targets
4
Activities
3
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

507.5
MW (Da)
4.54
ALogP
9
HBA
1
HBD
91.2
PSA (Ų)
0.51
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H20F3N3O5S
MW 507.49
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.27

Activity Summary

IC50 2 meas. best 7.75
EC50 1 meas. best 6.08
Kd 1 meas. best 5.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.75 7.75 18.0 1
NON-PROTEIN TARGET
CHEMBL3879801
IC50 7.24 7.24 58.0 1
Unchecked
CHEMBL612545
EC50 6.08 6.08 830.0 1
Unchecked
CHEMBL612545
Kd 5.85 5.85 1400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18303827 10.1021/jm070681+ Unchecked 5
21568323 10.1021/jm200199r Unchecked 3
21568323 10.1021/jm200199r Cystic fibrosis transmembrane conductance regulator 2
21568323 10.1021/jm200199r NON-PROTEIN TARGET 2

Data from ChEMBL 36 via Core Engine