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Compound Detail

CHEMBL209082

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CCOc1nc(NC(=O)C(C)C)cc(N)c1C#N

Basic Information

ChEMBL ID CHEMBL209082
Phase Preclinical
Structure Type MOL
InChI Key ZVTJLFMPNKAXHW-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

248.3
MW (Da)
1.53
ALogP
5
HBA
2
HBD
101.0
PSA (Ų)
0.84
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H16N4O2
MW 248.29
Aromatic Rings 1
Heavy Atoms 18
NP-Likeness -1.53

Activity Summary

IC50 2 meas. best 5.4
Ki 2 meas. best 5.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 8
CHEMBL2276
Ki 5.9 5.9 1258.9 1
Mitogen-activated protein kinase 8
CHEMBL2276
IC50 5.4 5.4 4000.0 1
Serine/threonine-protein kinase D3
CHEMBL2595
Ki 5.1 5.1 7943.3 1
Mitogen-activated protein kinase 9
CHEMBL4179
IC50 5.08 5.08 8400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16759099 10.1021/jm060199b Mitogen-activated protein kinase 8 1
16759099 10.1021/jm060199b Mitogen-activated protein kinase 9 1

Data from ChEMBL 36 via Core Engine