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Compound Detail

CHEMBL2178265

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O=C(Nc1cn(CCN2CCOCC2)nc1-c1cccc(Cl)c1)c1cnn2cccnc12

Basic Information

ChEMBL ID CHEMBL2178265
Phase Preclinical
Structure Type MOL
InChI Key QCQOXIPCXCSSLX-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

451.9
MW (Da)
2.83
ALogP
8
HBA
1
HBD
89.6
PSA (Ų)
0.48
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22ClN7O2
MW 451.92
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -2.49

Activity Summary

Ki 1 meas. best 7.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK2
CHEMBL2971
Ki 7.2 7.2 63.3 1

Pharmacokinetic Data

Parameter Value Units Species
CL 47.0 mL.min-1.kg-1 Rattus norvegicus
CL 20.0 mL.min-1.kg-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase JAK2 Ki = 63.3 nM 7.2 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 Liver microsomes 2
23061660 10.1021/jm3012239 No relevant target 1
23061660 10.1021/jm3012239 Tyrosine-protein kinase JAK2 1

Data from ChEMBL 36 via Core Engine