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Compound Detail

CHEMBL1923577

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COc1ccccc1-c1ccc2cnc(Nc3cccc(N4CCN(C[C@H](C)O)CC4)c3)nn12

Basic Information

ChEMBL ID CHEMBL1923577
Phase Preclinical
Structure Type MOL
InChI Key LPIVFMVCIWTQEK-IBGZPJMESA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
3
Publications
0
Known Names

Molecular Properties

458.6
MW (Da)
3.65
ALogP
8
HBA
2
HBD
78.2
PSA (Ų)
0.44
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H30N6O2
MW 458.57
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.30

Activity Summary

IC50 1 meas. best 9.27

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 9.27 9.27 0.5 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.08333 hr Mus musculus
T1/2 0.1 hr Rattus norvegicus
T1/2 0.15 hr Canis lupus familiaris
T1/2 0.5333 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22041060 10.1016/j.bmcl.2011.10.032 Liver 2
22041060 10.1016/j.bmcl.2011.10.032 Liver microsomes 2
22041060 10.1016/j.bmcl.2011.10.032 Tyrosine-protein kinase JAK2 1

Data from ChEMBL 36 via Core Engine