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Compound Detail

CHEMBL5185244

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N#CCNC(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCC(n5cccn5)CC4)cc3)n2)cc1

Basic Information

ChEMBL ID CHEMBL5185244
Phase Preclinical
Structure Type MOL
InChI Key JFSZGTXFEWOOQY-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

478.6
MW (Da)
4.18
ALogP
8
HBA
2
HBD
111.8
PSA (Ų)
0.38
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H26N8O
MW 478.56
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.93

Activity Summary

IC50 3 meas. best 7.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 7.28 7.28 52.0 1
Tyrosine-protein kinase JAK1
CHEMBL2835
IC50 7.24 7.24 57.0 1
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 7.01 7.01 97.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35413417 10.1016/j.bmcl.2022.128728 Tyrosine-protein kinase JAK1 2
35413417 10.1016/j.bmcl.2022.128728 Tyrosine-protein kinase JAK2 2
35413417 10.1016/j.bmcl.2022.128728 Tyrosine-protein kinase JAK3 1

Data from ChEMBL 36 via Core Engine