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Compound Detail

CHEMBL272810

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COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1c(C(F)(F)F)nc2sc(C)cn12

Basic Information

ChEMBL ID CHEMBL272810
Phase Preclinical
Structure Type MOL
InChI Key XAUDUPYNNKYCBB-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

429.4
MW (Da)
3.30
ALogP
8
HBA
1
HBD
81.9
PSA (Ų)
0.75
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H18F3N3O4S
MW 429.42
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -1.06

Activity Summary

IC50 2 meas. best 7.51
Kd 1 meas. best 4.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NON-PROTEIN TARGET
CHEMBL3879801
IC50 7.51 7.51 31.0 1
Unchecked
CHEMBL612545
IC50 7.02 7.02 95.0 1
Unchecked
CHEMBL612545
Kd 4.92 4.92 12000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30861492 10.1016/j.ejmech.2019.02.075 Voltage-gated L-type calcium channel 6
18303827 10.1021/jm070681+ Unchecked 3
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