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Compound Detail

CHEMBL378717

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O=C1NCc2c(-c3ccccc3Cl)nc(N3CCOCC3)nc2N1c1c(Cl)cccc1Cl

Basic Information

ChEMBL ID CHEMBL378717
Phase Preclinical
Structure Type MOL
InChI Key ANNQXHXXKQEKSO-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

490.8
MW (Da)
5.30
ALogP
5
HBA
1
HBD
70.6
PSA (Ų)
0.54
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H18Cl3N5O2
MW 490.78
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.13

Activity Summary

IC50 2 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 14
CHEMBL260
IC50 8.7 8.7 2.0 1
THP-1
CHEMBL614245
IC50 6.3 6.3 500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16750629 10.1016/j.bmcl.2006.05.045 Homo sapiens 1
16750629 10.1016/j.bmcl.2006.05.045 Voltage-gated inwardly rectifying potassium channel KCNH2 1
16750629 10.1016/j.bmcl.2006.05.045 THP-1 1
16750629 10.1016/j.bmcl.2006.05.045 Mitogen-activated protein kinase 14 1
16750629 10.1016/j.bmcl.2006.05.045 Voltage-gated L-type calcium channel 1

Data from ChEMBL 36 via Core Engine