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Compound Detail

CHEMBL1669170

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O=C(CN1CCOCC1)Nc1ccc(-c2cccc3c(=O)cc(N4CCOCC4)oc23)cc1-c1ccccc1

Basic Information

ChEMBL ID CHEMBL1669170
Phase Preclinical
Structure Type MOL
InChI Key KJQZPWWZMYOHNZ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

525.6
MW (Da)
4.23
ALogP
7
HBA
1
HBD
84.2
PSA (Ų)
0.40
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H31N3O5
MW 525.61
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -0.84

Activity Summary

IC50 1 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA-dependent protein kinase catalytic subunit
CHEMBL3142
IC50 7.85 7.85 14.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 123.03 uL.min-1.(10^6cells)-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA-dependent protein kinase catalytic subunit IC50 = 14.0 nM 7.85 Inhibition of DNA-PK 21216595

Literature References

PubMed DOI Target Context # Activities
21216595 10.1016/j.bmcl.2010.12.047 HeLa 2
- 10.6019/CHEMBL3301361 ADMET 2
- 10.6019/CHEMBL3301361 No relevant target 2
21216595 10.1016/j.bmcl.2010.12.047 DNA-dependent protein kinase catalytic subunit 1

Data from ChEMBL 36 via Core Engine