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Compound Detail

CHEMBL2380836

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O=C(Nc1ccc(Nc2ccnc3[nH]c(=O)c4ccccc4c23)cc1)c1ccc(C(F)(F)F)cc1F

Basic Information

ChEMBL ID CHEMBL2380836
Phase Preclinical
Structure Type MOL
InChI Key ATLTVHRPWMFWKI-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

492.4
MW (Da)
6.23
ALogP
4
HBA
3
HBD
86.9
PSA (Ų)
0.21
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H16F4N4O2
MW 492.43
Aromatic Rings 5
Heavy Atoms 36
NP-Likeness -1.31

Activity Summary

IC50 2 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aurora kinase A
CHEMBL4722
IC50 8.05 8.05 9.0 1
MIA PaCa-2
CHEMBL614725
IC50 5.3 5.3 4990.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aurora kinase A IC50 = 9.0 nM 8.05 Inhibition of aurora-A (unknown origin) 23570792
MIA PaCa-2 IC50 = 4990.0 nM 5.3 Antiproliferative activity against human MIAPaCa2 cells 23570792

Literature References

PubMed DOI Target Context # Activities
23570792 10.1016/j.bmcl.2013.03.008 MIA PaCa-2 1
23570792 10.1016/j.bmcl.2013.03.008 Aurora kinase B 1
23570792 10.1016/j.bmcl.2013.03.008 Aurora kinase A 1

Data from ChEMBL 36 via Core Engine