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Compound Detail

CHEMBL5556040

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COc1ccccc1-c1cnccc1C(=O)Nc1nnc(OC2CC3(CCN(C(=O)c4cc(Cc5n[nH]c(=O)c6ccccc56)ccc4F)CC3)C2)s1

Basic Information

ChEMBL ID CHEMBL5556040
Phase Preclinical
Structure Type MOL
InChI Key HNQJSUVHFKKUGJ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

731.8
MW (Da)
6.29
ALogP
10
HBA
2
HBD
152.3
PSA (Ų)
0.17
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C39H34FN7O5S
MW 731.81
Aromatic Rings 6
Heavy Atoms 53
NP-Likeness -1.21

Activity Summary

IC50 1 meas. best 6.78

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA polymerase theta
CHEMBL6025
IC50 6.78 6.78 166.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA polymerase theta IC50 = 166.2 nM 6.78 Inhibition of DNA polymerase theta (unknown origin) ATPase activity incubated fo... 38375763

Literature References

PubMed DOI Target Context # Activities
38375763 10.1021/acs.jmedchem.3c02096 DNA polymerase theta 1
38375763 10.1021/acs.jmedchem.3c02096 Poly [ADP-ribose] polymerase 1 1

Data from ChEMBL 36 via Core Engine