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Compound Detail

CHEMBL3798679

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CC1(C)NC(=O)c2ccc(-n3c(=O)[nH]c4ncccc43)cc2N1Cc1ccccc1

Basic Information

ChEMBL ID CHEMBL3798679
Phase Preclinical
Structure Type MOL
InChI Key LOPPJVYTMBRTCK-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
4
PK Parameters
3
Publications
0
Known Names

Molecular Properties

399.4
MW (Da)
3.20
ALogP
5
HBA
2
HBD
83.0
PSA (Ų)
0.55
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 C23H21N5O2
MW 399.45
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -0.73

Activity Summary

IC50 2 meas. best 9.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein kinase C theta type
CHEMBL3920
IC50 9.34 8.57 0.5 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 16.0 ng.hr.mL-1 Mus musculus
CL 142.84 mL.min-1.kg-1 Mus musculus
CL 0.16 mL.min-1.kg-1 Mus musculus
F 12.0 % Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27117263 10.1016/j.bmc.2016.04.008 Mus musculus 3
27117263 10.1016/j.bmc.2016.04.008 Protein kinase C theta type 2
27117263 10.1016/j.bmc.2016.04.008 ADMET 1

Data from ChEMBL 36 via Core Engine