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Compound Detail

CHEMBL2172218

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CC(=O)Nc1ccc2c3c(n(CCCO)c(=O)c2c1)-c1ccccc1C3=O

Basic Information

ChEMBL ID CHEMBL2172218
Phase Preclinical
Structure Type MOL
InChI Key JBTNBSPQXSODJB-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

362.4
MW (Da)
2.55
ALogP
5
HBA
2
HBD
88.4
PSA (Ų)
0.58
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H18N2O4
MW 362.39
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.27

Activity Summary

IC50 1 meas. best 4.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosyl-DNA phosphodiesterase 1
CHEMBL1075138
IC50 4.75 4.75 18000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosyl-DNA phosphodiesterase 1 IC50 = 18000.0 nM 4.75 Gel-Based Assay: Tdp1 reactions were performed as recently described. Briefly, a... -

Literature References

PubMed DOI Target Context # Activities
23472886 10.1021/jm400026k Retinoic acid receptor RXR-alpha 3
22712432 10.1021/jm3006806 Retinoic acid receptor RXR-alpha 1
22712432 10.1021/jm3006806 HEK293 1
22712432 10.1021/jm3006806 COS-1 1
22712432 10.1021/jm3006806 Unchecked 1
23259865 10.1021/jm3014458 DNA topoisomerase 1 1
23259865 10.1021/jm3014458 Tyrosyl-DNA phosphodiesterase 1 1
23472886 10.1021/jm400026k COS-1 1

Data from ChEMBL 36 via Core Engine