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Compound Detail

CHEMBL3946659

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Nc1ncc(-c2ncccc2OC(F)(F)F)nc1C(=O)Nc1ncccc1N1CCC(N)C(F)C1

Basic Information

ChEMBL ID CHEMBL3946659
Phase Preclinical
Structure Type MOL
InChI Key SUKUYCBPKLCSMU-UHFFFAOYSA-N
4
Targets
6
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

492.4
MW (Da)
2.54
ALogP
9
HBA
3
HBD
145.2
PSA (Ų)
0.46
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H20F4N8O2
MW 492.44
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.97

Activity Summary

IC50 4 meas. best 9.7
EC50 2 meas. best 7.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein kinase C alpha type
CHEMBL299
IC50 9.7 9.61 0.2 2
Protein kinase C theta type
CHEMBL3920
IC50 8.7 8.68 2.0 2
5-hydroxytryptamine receptor 2B
CHEMBL1833
EC50 7.37 7.37 43.0 1
Unchecked
CHEMBL612545
EC50 6.82 6.82 153.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38198520 10.1021/acs.jmedchem.3c02002 Protein kinase C alpha type 1
38198520 10.1021/acs.jmedchem.3c02002 Protein kinase C theta type 1
38198520 10.1021/acs.jmedchem.3c02002 Unchecked 1
38198520 10.1021/acs.jmedchem.3c02002 5-hydroxytryptamine receptor 2B 1
38198520 10.1021/acs.jmedchem.3c02002 No relevant target 1

Data from ChEMBL 36 via Core Engine