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Compound Detail

CHEMBL4635876

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OCCn1cc(Nc2ncc(Cl)c(NCc3cc(F)ccc3F)n2)cn1

Basic Information

ChEMBL ID CHEMBL4635876
Phase Preclinical
Structure Type MOL
InChI Key NROLQUCDBSGNQD-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

380.8
MW (Da)
2.95
ALogP
7
HBA
3
HBD
87.9
PSA (Ų)
0.58
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H15ClF2N6O
MW 380.79
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -2.39

Activity Summary

IC50 3 meas. best 9.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 9.5 9.5 0.3 1
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 9.0 9.0 1.0 1
JAK3/JAK1
CHEMBL3038491
IC50 8.1 8.1 7.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32001089 10.1016/j.bmc.2020.115326 Unchecked 2
32001089 10.1016/j.bmc.2020.115326 Tyrosine-protein kinase JAK1 1
32001089 10.1016/j.bmc.2020.115326 Tyrosine-protein kinase JAK2 1
32001089 10.1016/j.bmc.2020.115326 Tyrosine-protein kinase JAK3 1
32001089 10.1016/j.bmc.2020.115326 JAK3/JAK1 1
32001089 10.1016/j.bmc.2020.115326 No relevant target 1

Data from ChEMBL 36 via Core Engine