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Compound Detail

CHEMBL5565713

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

Basic Information

ChEMBL ID CHEMBL5565713
Phase Preclinical
Structure Type MOL
InChI Key ZJTHRAYTYMYRHI-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

510.4
MW (Da)
2.84
ALogP
9
HBA
3
HBD
145.2
PSA (Ų)
0.44
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H19F5N8O2
MW 510.43
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.89

Activity Summary

EC50 2 meas. best 5.76
IC50 2 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein kinase C theta type
CHEMBL3920
IC50 8.0 8.0 10.0 1
Protein kinase C alpha type
CHEMBL299
IC50 7.96 7.96 11.0 1
Unchecked
CHEMBL612545
EC50 5.76 5.76 1740.0 1
5-hydroxytryptamine receptor 2B
CHEMBL1833
EC50 5.7 5.7 2000.0 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