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Compound Detail

CHEMBL5195322

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N#CCNC(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCC(n5cncn5)CC4)cc3)n2)cc1

Basic Information

ChEMBL ID CHEMBL5195322
Phase Preclinical
Structure Type MOL
InChI Key CHYGCIUZUYLHGP-UHFFFAOYSA-N
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

479.6
MW (Da)
3.57
ALogP
9
HBA
2
HBD
124.7
PSA (Ų)
0.39
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H25N9O
MW 479.55
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.88

Activity Summary

IC50 6 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 7.77 7.77 17.0 2
Tyrosine-protein kinase JAK1
CHEMBL2835
IC50 7.68 7.68 21.0 2
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 7.18 7.18 66.0 2

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 JAK3 2
35413417 10.1016/j.bmcl.2022.128728 Tyrosine-protein kinase JAK1 1
35413417 10.1016/j.bmcl.2022.128728 Tyrosine-protein kinase JAK2 1

Data from ChEMBL 36 via Core Engine