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Compound Detail

CHEMBL242207

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CS(=O)(=O)c1cc(NCc2c[nH]cn2)cc2c(Nc3ccc(F)c(Cl)c3)c(C#N)cnc12

Basic Information

ChEMBL ID CHEMBL242207
Phase Preclinical
Structure Type MOL
InChI Key LGCSEMGADQRDEW-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

470.9
MW (Da)
4.38
ALogP
7
HBA
3
HBD
123.6
PSA (Ų)
0.38
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H16ClFN6O2S
MW 470.92
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.82

Activity Summary

IC50 1 meas. best 6.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase kinase kinase 8
CHEMBL4899
IC50 6.72 6.72 190.0 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 = 190.0 nM 6.72 Inhibition of Tpl2 by ELISA 17715908

Literature References

PubMed DOI Target Context # Activities
17715908 10.1021/jm070436q Mitogen-activated protein kinase kinase kinase 8 1
17715908 10.1021/jm070436q Epidermal growth factor receptor 1
17715908 10.1021/jm070436q Monocyte 1
17715908 10.1021/jm070436q Blood 1

Data from ChEMBL 36 via Core Engine