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Compound Detail

CHEMBL5085430

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O=C(NCCCNc1nc(Nc2cccc(NC(=O)N3CCCC3)c2)ncc1Br)C1CCC1

Basic Information

ChEMBL ID CHEMBL5085430
Phase Preclinical
Structure Type MOL
InChI Key ZSZOBRBJIJWWHH-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

516.4
MW (Da)
4.33
ALogP
6
HBA
4
HBD
111.3
PSA (Ų)
0.37
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H30BrN7O2
MW 516.44
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.79

Activity Summary

IC50 4 meas. best 8.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase 17A
CHEMBL4525
IC50 8.35 8.35 4.5 1
MAP/microtubule affinity-regulating kinase 4
CHEMBL5754
IC50 7.14 7.14 72.0 1
MAP/microtubule affinity-regulating kinase 3
CHEMBL5600
IC50 6.86 6.86 137.0 1
Serine/threonine-protein kinase TBK1
CHEMBL5408
IC50 6.47 6.47 338.0 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