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Compound Detail

CHEMBL3114769

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O=C1NC(=O)C(c2c[nH]c3ccccc23)=C1Nc1ccc(OCCCn2ccnc2)cc1

Basic Information

ChEMBL ID CHEMBL3114769
Phase Preclinical
Structure Type MOL
InChI Key MHRPDZTYNYCVEB-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

427.5
MW (Da)
3.31
ALogP
6
HBA
3
HBD
101.0
PSA (Ų)
0.30
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H21N5O3
MW 427.46
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -0.71

Activity Summary

IC50 2 meas. best 5.94

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 5.94 5.94 1148.0 1
Tyrosine-protein kinase JAK1
CHEMBL2835
IC50 5.06 5.06 8640.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase JAK3 IC50 = 1148.0 nM 5.94 Inhibition of JAK3 (unknown origin) 24461299
Tyrosine-protein kinase JAK1 IC50 = 8640.0 nM 5.06 Inhibition of JAK1 (unknown origin) 24461299

Literature References

PubMed DOI Target Context # Activities
24461299 10.1016/j.bmcl.2014.01.001 Unchecked 1
24461299 10.1016/j.bmcl.2014.01.001 Non-receptor tyrosine-protein kinase TYK2 1
24461299 10.1016/j.bmcl.2014.01.001 Tyrosine-protein kinase JAK3 1
24461299 10.1016/j.bmcl.2014.01.001 Tyrosine-protein kinase JAK2 1
24461299 10.1016/j.bmcl.2014.01.001 Tyrosine-protein kinase JAK1 1

Data from ChEMBL 36 via Core Engine