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Compound Detail

CHEMBL1939095

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Cc1ccc(NS(=O)(=O)c2cc3c(cc2F)NC(=O)CC3)cc1C

Basic Information

ChEMBL ID CHEMBL1939095
Phase Preclinical
Structure Type MOL
InChI Key MSHCFYZEHSRAPG-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

348.4
MW (Da)
3.13
ALogP
3
HBA
2
HBD
75.3
PSA (Ų)
0.89
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 C17H17FN2O3S
MW 348.40
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -1.82

Activity Summary

EC50 1 meas. best 6.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Pyruvate kinase PKM
CHEMBL1075189
EC50 6.68 6.68 210.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.275 hr Homo sapiens
T1/2 0.5717 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Pyruvate kinase PKM EC50 = 210.0 nM 6.68 Activation of human PKM2 assessed as ATP product formation after 1 hr by lumines... 21958545

Literature References

PubMed DOI Target Context # Activities
21958545 10.1016/j.bmcl.2011.08.114 Pyruvate kinase PKM 2
21958545 10.1016/j.bmcl.2011.08.114 Caco-2 2
21958545 10.1016/j.bmcl.2011.08.114 Liver microsomes 1
21958545 10.1016/j.bmcl.2011.08.114 Liver 1

Data from ChEMBL 36 via Core Engine