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Compound Detail

CHEMBL4239361

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NC(=O)c1cnc2[nH]ccc2c1NC12CC3CC(CC(C3)C1)C2

Basic Information

ChEMBL ID CHEMBL4239361
Phase Preclinical
Structure Type MOL
InChI Key XUWWTDITFKFAPU-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

310.4
MW (Da)
3.04
ALogP
3
HBA
3
HBD
83.8
PSA (Ų)
0.81
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 C18H22N4O
MW 310.40
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -0.73

Activity Summary

IC50 3 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 8.0 8.0 10.0 1
Tyrosine-protein kinase JAK1
CHEMBL2835
IC50 6.96 6.96 110.0 1
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 6.92 6.92 120.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30145050 10.1016/j.bmc.2018.08.005 Unchecked 1
30145050 10.1016/j.bmc.2018.08.005 ADMET 1
30145050 10.1016/j.bmc.2018.08.005 Tyrosine-protein kinase JAK2 1
30145050 10.1016/j.bmc.2018.08.005 Tyrosine-protein kinase JAK1 1
30145050 10.1016/j.bmc.2018.08.005 Tyrosine-protein kinase JAK3 1

Data from ChEMBL 36 via Core Engine