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Compound Detail

CHEMBL2407759

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CC(=O)N1CCC(n2cc(-c3cnc(N)c4oc(-c5cccc6nnsc56)cc34)cn2)CC1

Basic Information

ChEMBL ID CHEMBL2407759
Phase Preclinical
Structure Type MOL
InChI Key XDCWLOMVUOZXFY-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

459.5
MW (Da)
4.13
ALogP
9
HBA
1
HBD
116.0
PSA (Ų)
0.43
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 C23H21N7O2S
MW 459.54
Aromatic Rings 5
Heavy Atoms 33
NP-Likeness -0.95

Activity Summary

IC50 2 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
TAK1/TAB1
CHEMBL3038499
IC50 8.4 8.4 4.0 1
Mitogen-activated protein kinase kinase kinase 7
CHEMBL5776
IC50 7.92 7.92 12.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23850198 10.1016/j.bmcl.2013.06.053 Liver 1
23850198 10.1016/j.bmcl.2013.06.053 Liver microsomes 1
23850198 10.1016/j.bmcl.2013.06.053 Mitogen-activated protein kinase kinase kinase 7 1
23850198 10.1016/j.bmcl.2013.06.053 TAK1/TAB1 1

Data from ChEMBL 36 via Core Engine