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Compound Detail

CHEMBL4756648

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C=CC(=O)NCC(=O)Nc1cccc(-c2cc(Nc3cnn(CCOC)c3)ncn2)c1

Basic Information

ChEMBL ID CHEMBL4756648
Phase Preclinical
Structure Type MOL
InChI Key BUENNZLMRJPBKP-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

421.5
MW (Da)
1.97
ALogP
8
HBA
3
HBD
123.1
PSA (Ų)
0.43
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23N7O3
MW 421.46
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -2.04

Activity Summary

IC50 3 meas. best 7.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK1
CHEMBL2835
IC50 7.25 7.25 56.0 1
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 7.18 7.18 66.0 1
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 5.81 5.81 1542.0 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