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Compound Detail

CHEMBL381724

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COc1cc2c(Nc3cnc(NC(=O)c4ccccc4)nc3)ncnc2cc1OCCCN1CCOCC1

Basic Information

ChEMBL ID CHEMBL381724
Phase Preclinical
Structure Type MOL
InChI Key LYDTZBUSUCDSRL-UHFFFAOYSA-N
3
Targets
5
Activities
1
Assay Types
1
PK Parameters
8
Publications
0
Known Names

Molecular Properties

515.6
MW (Da)
3.53
ALogP
10
HBA
2
HBD
123.6
PSA (Ų)
0.30
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H29N7O4
MW 515.57
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.37

Activity Summary

IC50 5 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aurora kinase B
CHEMBL2185
IC50 9.0 9.0 1.0 1
Aurora kinase A
CHEMBL4722
IC50 8.52 8.52 3.0 3
MCF7
CHEMBL387
IC50 6.68 6.68 210.0 1

Pharmacokinetic Data

Parameter Value Units Species
Fu 0.045 - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3301361 No relevant target 2
16337122 10.1016/j.bmcl.2005.11.053 Aurora kinase A 1
16337122 10.1016/j.bmcl.2005.11.053 MCF7 1
16337122 10.1016/j.bmcl.2005.11.053 No relevant target 1
16337122 10.1016/j.bmcl.2005.11.053 Rattus norvegicus 1
16884290 10.1021/jm060522a Aurora kinase A 1
19320489 10.1021/jm8012129 Aurora kinase A 1
19320489 10.1021/jm8012129 Aurora kinase B 1

Data from ChEMBL 36 via Core Engine