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Compound Detail

CHEMBL4637596

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Cc1[nH]nc2[nH]c(=O)cc([C@H]3CC[C@H](C#N)CC3)c12

Basic Information

ChEMBL ID CHEMBL4637596
Phase Preclinical
Structure Type MOL
InChI Key ZKANCMWBNLSWJW-MGCOHNPYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

256.3
MW (Da)
2.36
ALogP
3
HBA
2
HBD
85.3
PSA (Ų)
0.82
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H16N4O
MW 256.31
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness -0.75

Activity Summary

IC50 3 meas. best 6.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK1
CHEMBL2835
IC50 6.14 6.14 730.0 1
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 5.29 5.29 5100.0 1
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 4.96 4.96 11000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32462873 10.1021/acs.jmedchem.0c00359 Tyrosine-protein kinase JAK1 2
32462873 10.1021/acs.jmedchem.0c00359 Tyrosine-protein kinase JAK2 2
32462873 10.1021/acs.jmedchem.0c00359 No relevant target 2
32462873 10.1021/acs.jmedchem.0c00359 Tyrosine-protein kinase JAK3 1
32462873 10.1021/acs.jmedchem.0c00359 Non-receptor tyrosine-protein kinase TYK2 1

Data from ChEMBL 36 via Core Engine