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Compound Detail

CHEMBL4090883

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C=CC(=O)N1CCC[C@@H](N(C)c2ncnc3[nH]ccc23)C1

Basic Information

ChEMBL ID CHEMBL4090883
Phase Preclinical
Structure Type MOL
InChI Key BYVMQYSLOHLBEZ-LLVKDONJSA-N
2
Targets
6
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

285.4
MW (Da)
1.57
ALogP
4
HBA
1
HBD
65.1
PSA (Ų)
0.87
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H19N5O
MW 285.35
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness -0.94

Activity Summary

IC50 6 meas. best 7.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 7.75 7.1675 18.0 4
Tyrosine-protein kinase JAK1
CHEMBL2835
IC50 5.94 5.525 1150.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28139931 10.1021/acs.jmedchem.6b01694 Tyrosine-protein kinase JAK3 4
28139931 10.1021/acs.jmedchem.6b01694 Tyrosine-protein kinase JAK1 2
28139931 10.1021/acs.jmedchem.6b01694 Non-receptor tyrosine-protein kinase TYK2 1
28139931 10.1021/acs.jmedchem.6b01694 Tyrosine-protein kinase JAK2 1

Data from ChEMBL 36 via Core Engine