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Compound Detail

CHEMBL2178256

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Nc1ccn2ncc(C(=O)Nc3cnoc3-c3cccc(Cl)c3)c2n1

Basic Information

ChEMBL ID CHEMBL2178256
Phase Preclinical
Structure Type MOL
InChI Key AAENIXAZGRAAII-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

354.8
MW (Da)
2.87
ALogP
7
HBA
2
HBD
111.3
PSA (Ų)
0.58
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 C16H11ClN6O2
MW 354.76
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -1.84

Activity Summary

IC50 1 meas. best 6.3
Ki 1 meas. best 7.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK2
CHEMBL2971
Ki 7.5 7.5 31.9 1
Cytochrome P450 1A2
CHEMBL3356
IC50 6.3 6.3 500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase JAK2 Ki = 31.9 nM 7.5 Inhibition of purified JAK2 incubated for 30 mins 23061660
Cytochrome P450 1A2 IC50 = 500.0 nM 6.3 Inhibition of CYP1A2 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 1A2 1

Data from ChEMBL 36 via Core Engine