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Compound Detail

CHEMBL5088930

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Brc1cnc(Nc2cccc(CN3CCOCC3)c2)nc1NCCc1c[nH]cn1

Basic Information

ChEMBL ID CHEMBL5088930
Phase Preclinical
Structure Type MOL
InChI Key IOYFYUOBKSQTFF-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

458.4
MW (Da)
3.19
ALogP
7
HBA
3
HBD
91.0
PSA (Ų)
0.48
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H24BrN7O
MW 458.36
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.62

Activity Summary

IC50 3 meas. best 6.67

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MAP/microtubule affinity-regulating kinase 4
CHEMBL5754
IC50 6.67 6.67 214.0 1
Serine/threonine-protein kinase 17A
CHEMBL4525
IC50 6.2 6.2 638.0 1
MAP/microtubule affinity-regulating kinase 3
CHEMBL5600
IC50 6.06 6.06 872.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34333981 10.1021/acs.jmedchem.1c00440 Serine/threonine-protein kinase 17A 2
34333981 10.1021/acs.jmedchem.1c00440 MAP/microtubule affinity-regulating kinase 4 2
34333981 10.1021/acs.jmedchem.1c00440 MAP/microtubule affinity-regulating kinase 3 1
34333981 10.1021/acs.jmedchem.1c00440 Serine/threonine-protein kinase TBK1 1
34333981 10.1021/acs.jmedchem.1c00440 No relevant target 1
34333981 10.1021/acs.jmedchem.1c00440 ADMET 1

Data from ChEMBL 36 via Core Engine