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Compound Detail

CHEMBL518323

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Nc1ncc(-c2cnn(C3CCNCC3)c2)cc1OCc1c(Cl)ccc(F)c1Cl

Basic Information

ChEMBL ID CHEMBL518323
Phase Preclinical
Structure Type MOL
InChI Key SZSQAKDNRSCZOY-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

436.3
MW (Da)
4.48
ALogP
6
HBA
2
HBD
78.0
PSA (Ų)
0.58
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H20Cl2FN5O
MW 436.32
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.13

Activity Summary

IC50 3 meas. best 7.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase kinase kinase kinase 3
CHEMBL5432
IC50 7.41 7.41 39.0 1
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 6.24 6.24 572.0 1
HEL
CHEMBL613888
IC50 4.83 4.83 14857.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29636220 10.1016/j.bmcl.2018.03.032 Mitogen-activated protein kinase kinase kinase kinase 3 2
30981578 10.1016/j.bmcl.2019.04.011 Tyrosine-protein kinase JAK2 1
30981578 10.1016/j.bmcl.2019.04.011 HEL 1

Data from ChEMBL 36 via Core Engine