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Compound Detail

CHEMBL4762354

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Cn1cc(Nc2cc(-c3cccc(NC(=O)CNC(=O)CC#N)c3)ncn2)cn1

Basic Information

ChEMBL ID CHEMBL4762354
Phase Preclinical
Structure Type MOL
InChI Key TZWDIXOVJWDFDR-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

390.4
MW (Da)
1.59
ALogP
8
HBA
3
HBD
137.6
PSA (Ų)
0.56
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H18N8O2
MW 390.41
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -2.32

Activity Summary

IC50 3 meas. best 7.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 7.16 7.16 69.0 1
Tyrosine-protein kinase JAK1
CHEMBL2835
IC50 7.05 7.05 89.0 1
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 7.02 7.02 95.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32097841 10.1016/j.ejmech.2020.112148 Unchecked 2
32097841 10.1016/j.ejmech.2020.112148 Tyrosine-protein kinase JAK3 1
32097841 10.1016/j.ejmech.2020.112148 Tyrosine-protein kinase JAK2 1
32097841 10.1016/j.ejmech.2020.112148 Tyrosine-protein kinase JAK1 1
32097841 10.1016/j.ejmech.2020.112148 Non-receptor tyrosine-protein kinase TYK2 1

Data from ChEMBL 36 via Core Engine