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Compound Detail

CHEMBL1836637

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O=C(O)COc1ncnc2cc(-c3ccc(Cl)cc3)sc12

Basic Information

ChEMBL ID CHEMBL1836637
Phase Preclinical
Structure Type MOL
InChI Key KGLQMZWSWMDATD-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

320.8
MW (Da)
3.48
ALogP
5
HBA
1
HBD
72.3
PSA (Ų)
0.80
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H9ClN2O3S
MW 320.76
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -1.47

Activity Summary

IC50 1 meas. best 4.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase kinase kinase 8
CHEMBL4899
IC50 4.47 4.47 34000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase kinase kinase 8 IC50 = 34000.0 nM 4.47 Inhibition of TPL2 21862328

Literature References

PubMed DOI Target Context # Activities
33215924 10.1021/acs.jmedchem.0c01174 Serine/threonine-protein kinase 17B 3
21862328 10.1016/j.bmcl.2011.07.069 Mitogen-activated protein kinase kinase kinase 8 1
33215924 10.1021/acs.jmedchem.0c01174 Serine/threonine-protein kinase 17A 1

Data from ChEMBL 36 via Core Engine