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Compound Detail

CHEMBL244563

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O=C(O)COc1c(C(=O)O)sc(-c2cccc(NC3CCN(S(=O)(=O)Cc4ccccc4)CC3)c2)c1Cl

Basic Information

ChEMBL ID CHEMBL244563
Phase Preclinical
Structure Type MOL
InChI Key DWEJNLIPYPXTQR-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

565.1
MW (Da)
4.64
ALogP
7
HBA
3
HBD
133.2
PSA (Ų)
0.32
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H25ClN2O7S2
MW 565.07
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.35

Activity Summary

Ki 1 meas. best 9.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein phosphatase non-receptor type 1
CHEMBL335
Ki 9.17 9.17 0.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein phosphatase non-receptor type 1 Ki = 0.68 nM 9.17 Inhibition of human recombinant PTP1B 17705360

Literature References

PubMed DOI Target Context # Activities
17705360 10.1021/jm0702478 Tyrosine-protein phosphatase non-receptor type 1 1

Data from ChEMBL 36 via Core Engine