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Compound Detail

CHEMBL4208685

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COc1cc2c(cc1-c1cnn3ccc(-c4ccnc5[nH]ccc45)cc13)CNC(C)C2

Basic Information

ChEMBL ID CHEMBL4208685
Phase Preclinical
Structure Type MOL
InChI Key XWLIHYAUFDQCQF-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

409.5
MW (Da)
4.59
ALogP
5
HBA
2
HBD
67.2
PSA (Ų)
0.46
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H23N5O
MW 409.49
Aromatic Rings 5
Heavy Atoms 31
NP-Likeness -0.06

Activity Summary

IC50 3 meas. best 8.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein kinase C iota type
CHEMBL2598
IC50 8.42 8.42 3.8 1
Protein kinase C alpha type
CHEMBL299
IC50 7.19 7.19 64.0 1
Protein kinase C epsilon type
CHEMBL3582
IC50 6.77 6.77 170.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29688013 10.1021/acs.jmedchem.8b00060 Protein kinase C iota type 1
29688013 10.1021/acs.jmedchem.8b00060 Protein kinase C alpha type 1
29688013 10.1021/acs.jmedchem.8b00060 Protein kinase C epsilon type 1
29688013 10.1021/acs.jmedchem.8b00060 Huh-7 1
29688013 10.1021/acs.jmedchem.8b00060 HCCLM3 1

Data from ChEMBL 36 via Core Engine