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Compound Detail

CHEMBL211605

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

Basic Information

ChEMBL ID CHEMBL211605
Phase Preclinical
Structure Type MOL
InChI Key ZJEWMDXOXBQHAB-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

220.2
MW (Da)
0.29
ALogP
5
HBA
2
HBD
101.0
PSA (Ų)
0.76
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 C10H12N4O2
MW 220.23
Aromatic Rings 1
Heavy Atoms 16
NP-Likeness -1.43

Activity Summary

IC50 2 meas. best 6.21
Ki 1 meas. best 6.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 8
CHEMBL2276
Ki 6.4 6.4 400.0 1
Mitogen-activated protein kinase 9
CHEMBL4179
IC50 6.21 6.21 610.0 1
Mitogen-activated protein kinase 8
CHEMBL2276
IC50 5.92 5.92 1200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase 8 Ki = 400.0 nM 6.4 Inhibition of JNK1 16854050
Mitogen-activated protein kinase 9 IC50 = 610.0 nM 6.21 Inhibition of JNK2 16854050
Mitogen-activated protein kinase 8 IC50 = 1200.0 nM 5.92 Inhibition of JNK1 16854050

Literature References

PubMed DOI Target Context # Activities
16854050 10.1021/jm060465l Mitogen-activated protein kinase 8 2
16854050 10.1021/jm060465l c-Jun N-terminal kinase, JNK 1
16854050 10.1021/jm060465l Mitogen-activated protein kinase 9 1

Data from ChEMBL 36 via Core Engine