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Compound Detail

CHEMBL5410109

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COc1cc(-c2cnc3cc(N4CC(N(C)C)C4)ccn23)cc(OC(F)F)c1C(=O)NC1CC1

Basic Information

ChEMBL ID CHEMBL5410109
Phase Preclinical
Structure Type MOL
InChI Key JDNFAAUUFUBZKC-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

471.5
MW (Da)
3.25
ALogP
7
HBA
1
HBD
71.3
PSA (Ų)
0.54
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H27F2N5O3
MW 471.51
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.27

Activity Summary

IC50 3 meas. best 8.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase SIK3
CHEMBL6149
IC50 8.36 8.36 4.4 1
Serine/threonine-protein kinase SIK2
CHEMBL5699
IC50 8.0 8.0 10.1 1
Serine/threonine-protein kinase SIK1
CHEMBL6082
IC50 6.95 6.95 112.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38552030 10.1021/acs.jmedchem.3c02246 Cytochrome P450 2
38552030 10.1021/acs.jmedchem.3c02246 Serine/threonine-protein kinase SIK1 1
38552030 10.1021/acs.jmedchem.3c02246 Serine/threonine-protein kinase SIK2 1
38552030 10.1021/acs.jmedchem.3c02246 Serine/threonine-protein kinase SIK3 1

Data from ChEMBL 36 via Core Engine