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Compound Detail

CHEMBL4536380

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CC(C)(O)Cn1c(=O)n(C2CCOCC2)c2nc(-c3cnc4ccc(C#N)cn34)ncc21

Basic Information

ChEMBL ID CHEMBL4536380
Phase Preclinical
Structure Type MOL
InChI Key GVFYFXFHOOSHAM-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

433.5
MW (Da)
1.90
ALogP
10
HBA
1
HBD
123.3
PSA (Ų)
0.52
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23N7O3
MW 433.47
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.24

Activity Summary

IC50 3 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 7.1 7.1 80.0 1
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 6.42 6.42 380.0 1
Tyrosine-protein kinase JAK1
CHEMBL2835
IC50 5.27 5.27 5400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31609613 10.1021/acs.jmedchem.9b00533 Tyrosine-protein kinase JAK3 1
31609613 10.1021/acs.jmedchem.9b00533 Tyrosine-protein kinase JAK2 1
31609613 10.1021/acs.jmedchem.9b00533 Tyrosine-protein kinase JAK1 1

Data from ChEMBL 36 via Core Engine