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Compound Detail

CHEMBL5208105

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O=C(O)CC(O)(CC(=O)N1CCN(S(=O)(=O)c2cc3c(c(O)c2O)C(=O)c2ccccc2C3=O)CC1)C(=O)O

Basic Information

ChEMBL ID CHEMBL5208105
Phase Preclinical
Structure Type MOL
InChI Key PYHLNZSMOIJZLQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

562.5
MW (Da)
-0.61
ALogP
10
HBA
5
HBD
227.1
PSA (Ų)
0.23
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H22N2O12S
MW 562.51
Aromatic Rings 2
Heavy Atoms 39
NP-Likeness 0.01

Activity Summary

IC50 1 meas. best 6.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Pyruvate kinase PKLR
CHEMBL1075126
IC50 6.7 6.7 200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Pyruvate kinase PKLR IC50 = 200.0 nM 6.7 Inhibition of PKL (unknown origin) for 30 mins by Kinase-Glo Max reagent based l... 35290845

Literature References

PubMed DOI Target Context # Activities
35290845 10.1016/j.ejmech.2022.114270 Pyruvate kinase PKLR 3

Data from ChEMBL 36 via Core Engine