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Compound Detail

CHEMBL5438800

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CNc1ncc2cc(-c3cc(Br)ccc3Cl)c(=O)n(C[C@H]3OC[C@H](N)CO3)c2n1

Basic Information

ChEMBL ID CHEMBL5438800
Phase Preclinical
Structure Type MOL
InChI Key QHGBYRNKDSLEHW-YGUOUDRMSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

480.8
MW (Da)
2.62
ALogP
8
HBA
2
HBD
104.3
PSA (Ų)
0.59
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H19BrClN5O3
MW 480.75
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.75

Activity Summary

IC50 3 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase SIK3
CHEMBL6149
IC50 6.0 6.0 1000.0 1
Serine/threonine-protein kinase SIK1
CHEMBL6082
IC50 5.62 5.62 2400.0 1
Serine/threonine-protein kinase SIK2
CHEMBL5699
IC50 5.36 5.36 4400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
37094449 10.1016/j.ejmech.2023.115347 Serine/threonine-protein kinase 4 1
37094449 10.1016/j.ejmech.2023.115347 Serine/threonine-protein kinase 3 1
37094449 10.1016/j.ejmech.2023.115347 Serine/threonine-protein kinase 24 1
37094449 10.1016/j.ejmech.2023.115347 Serine/threonine-protein kinase 26 1
37094449 10.1016/j.ejmech.2023.115347 Serine/threonine-protein kinase PAK 1 1
37094449 10.1016/j.ejmech.2023.115347 Serine/threonine-protein kinase SIK1 1
37094449 10.1016/j.ejmech.2023.115347 Serine/threonine-protein kinase SIK2 1
37094449 10.1016/j.ejmech.2023.115347 Serine/threonine-protein kinase SIK3 1

Data from ChEMBL 36 via Core Engine