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Compound Detail

CHEMBL158083

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COS(=O)(=O)[O-].Cc1cc2c3c([n+](C)c4ccc(F)cc4c3c1)-c1cc(F)ccc1N2C

Basic Information

ChEMBL ID CHEMBL158083
Phase Preclinical
Structure Type MOL
InChI Key VRWGYMXWYZBBGF-UHFFFAOYSA-M
Parent Compound CHEMBL1181174
Active Moiety CHEMBL1181174
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

347.4
MW (Da)
5.15
ALogP
1
HBA
0
HBD
7.1
PSA (Ų)
0.32
QED
1
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H20F2N2O4S
MW 458.49
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -0.35

Activity Summary

IC50 4 meas. best 6.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Telomerase reverse transcriptase
CHEMBL2916
IC50 6.48 6.48 330.0 2
Unchecked
CHEMBL612545
IC50 6.48 6.48 330.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18247546 10.1021/jm070587t Unchecked 16
16279778 10.1021/jm058031y Unchecked 2
11806711 10.1021/jm011015q Telomerase reverse transcriptase 1
11806711 10.1021/jm011015q NON-PROTEIN TARGET 1
11806711 10.1021/jm011015q Unchecked 1
16279778 10.1021/jm058031y NON-PROTEIN TARGET 1
16279778 10.1021/jm058031y Liver microsomes 1
16279778 10.1021/jm058031y No relevant target 1
16279778 10.1021/jm058031y ADMET 1
18247546 10.1021/jm070587t NON-PROTEIN TARGET 1
27624081 10.1016/j.bmcl.2016.09.016 Unchecked 1
36669398 10.1016/j.ejmech.2023.115121 Telomerase reverse transcriptase 1

Data from ChEMBL 36 via Core Engine