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Compound Detail

CHEMBL2178251

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Cn1cc(-c2cccc(Cl)c2)c(NC(=O)c2cnn3cccnc23)n1

Basic Information

ChEMBL ID CHEMBL2178251
Phase Preclinical
Structure Type MOL
InChI Key OSUIVZWZMLHYTB-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

352.8
MW (Da)
3.04
ALogP
6
HBA
1
HBD
77.1
PSA (Ų)
0.61
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 C17H13ClN6O
MW 352.79
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -2.37

Activity Summary

Ki 1 meas. best 6.99

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK2
CHEMBL2971
Ki 6.99 6.99 103.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase JAK2 Ki = 103.0 nM 6.99 Inhibition of purified JAK2 incubated for 30 mins 23061660

Literature References

PubMed DOI Target Context # Activities
23061660 10.1021/jm3012239 Unchecked 3
23061660 10.1021/jm3012239 Tyrosine-protein kinase JAK2 2
23061660 10.1021/jm3012239 Cytochrome P450 2D6 1
23061660 10.1021/jm3012239 Cytochrome P450 2C19 1
23061660 10.1021/jm3012239 Cytochrome P450 1A2 1
23061660 10.1021/jm3012239 Cytochrome P450 3A4 1
23061660 10.1021/jm3012239 Cytochrome P450 2C9 1

Data from ChEMBL 36 via Core Engine