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Compound Detail

CHEMBL215322

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CCN(CCO)CCCOc1ccc2c(Nc3cc(CC(=O)Nc4cccc(F)c4F)[nH]n3)ncnc2c1

Basic Information

ChEMBL ID CHEMBL215322
Phase Preclinical
Structure Type MOL
InChI Key CNWZWPQCJCOBHA-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

525.6
MW (Da)
3.64
ALogP
8
HBA
4
HBD
128.3
PSA (Ų)
0.19
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H29F2N7O3
MW 525.56
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.79

Activity Summary

IC50 2 meas. best 8.12
Ki 2 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
SW-620
CHEMBL612262
Ki 8.15 8.15 7.0 1
Aurora kinase B
CHEMBL2185
IC50 8.12 8.12 7.5 1
Aurora kinase A
CHEMBL4722
Ki 6.8 6.8 160.0 1
Aurora kinase A
CHEMBL4722
IC50 6.1 6.1 800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17373783 10.1021/jm061335f Aurora kinase B 1
17373783 10.1021/jm061335f Aurora kinase A 1
17373783 10.1021/jm061335f SW-620 1
19320489 10.1021/jm8012129 Aurora kinase A 1
19320489 10.1021/jm8012129 Aurora kinase B 1
- 10.6019/CHEMBL3301361 No relevant target 1

Data from ChEMBL 36 via Core Engine