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Compound Detail

CHEMBL1085387

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Cc1cc(CN2CCN(c3c(Cl)cnc4[nH]c(-c5ccc(OCCO)cc5)nc34)CC2)no1

Basic Information

ChEMBL ID CHEMBL1085387
Phase Preclinical
Structure Type MOL
InChI Key JRZOYDCGHBZCQE-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

468.9
MW (Da)
3.27
ALogP
8
HBA
2
HBD
103.5
PSA (Ų)
0.43
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25ClN6O3
MW 468.95
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.61

Activity Summary

IC50 2 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aurora kinase A
CHEMBL4722
IC50 7.7 7.62 20.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aurora kinase A IC50 = 20.0 nM 7.7 Inhibition of human recombinant Aurora A expressed in baculovirus system 20565112
Aurora kinase A IC50 = 29.0 nM 7.54 Inhibition of Aurora A 21093113

Literature References

PubMed DOI Target Context # Activities
20565112 10.1021/jm100262j Aurora kinase A 1
20565112 10.1021/jm100262j HCT-116 1
20565112 10.1021/jm100262j ADMET 1
21093113 10.1016/j.ejmech.2010.10.017 Aurora kinase A 1

Data from ChEMBL 36 via Core Engine