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Compound Detail

CHEMBL2159213

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Cc1nc2cnc3[nH]ccc3c2n1[C@@H]1CCCC[C@H]1O

Basic Information

ChEMBL ID CHEMBL2159213
Phase Preclinical
Structure Type MOL
InChI Key HZGWWIQIWYFBPE-CHWSQXEVSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

270.3
MW (Da)
2.70
ALogP
4
HBA
2
HBD
66.7
PSA (Ų)
0.71
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H18N4O
MW 270.34
Aromatic Rings 3
Heavy Atoms 20
NP-Likeness -0.24

Activity Summary

Ki 2 meas. best 7.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK1
CHEMBL2835
Ki 7.05 7.05 90.0 1
Tyrosine-protein kinase JAK2
CHEMBL2971
Ki 6.28 6.28 520.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 8.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22698084 10.1021/jm300628c Unchecked 2
22698084 10.1021/jm300628c Tyrosine-protein kinase JAK2 2
22698084 10.1021/jm300628c Tyrosine-protein kinase JAK1 2
22698084 10.1021/jm300628c Hepatocyte 1
22698084 10.1021/jm300628c MDCK 1
22698084 10.1021/jm300628c No relevant target 1

Data from ChEMBL 36 via Core Engine