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Compound Detail

CHEMBL4759590

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CN(C)CCN1CCN(Cc2cc(Nc3c4ccc(Cl)cc4nc4ccc(O)cc34)ccc2O)CC1

Basic Information

ChEMBL ID CHEMBL4759590
Phase Preclinical
Structure Type MOL
InChI Key BQWNIOWWZCEWFX-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

506.1
MW (Da)
4.88
ALogP
7
HBA
3
HBD
75.1
PSA (Ų)
0.24
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H32ClN5O2
MW 506.05
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -0.98

Activity Summary

Kd 2 meas. best 7.07
IC50 1 meas. best 6.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA excision repair protein ERCC-1/DNA repair endonuclease XPF
CHEMBL3883316
Kd 7.07 7.07 85.0 1
DNA excision repair protein ERCC-1/DNA repair endonuclease XPF
CHEMBL3883316
IC50 6.31 6.31 490.0 1
Unchecked
CHEMBL612545
Kd 5.98 5.98 1050.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32738410 10.1016/j.ejmech.2020.112658 DNA excision repair protein ERCC-1/DNA repair endonuclease XPF 5
32738410 10.1016/j.ejmech.2020.112658 HCT-116 3
32738410 10.1016/j.ejmech.2020.112658 Unchecked 1

Data from ChEMBL 36 via Core Engine