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Compound Detail

CHEMBL5197173

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O=C(Cc1ncc(C(F)(F)F)cc1C(F)(F)F)N(CC#Cc1cnn(C2CNC2)c1)c1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL5197173
Phase Preclinical
Structure Type MOL
InChI Key GBXMTWFYZDBZJF-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

525.4
MW (Da)
4.23
ALogP
5
HBA
1
HBD
63.0
PSA (Ų)
0.40
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H18F7N5O
MW 525.43
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.42

Activity Summary

IC50 1 meas. best 9.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA polymerase theta
CHEMBL6025
IC50 9.12 9.12 0.8 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 7408.56 ng.hr.mL-1 Mus musculus
Fu 0.051 - Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA polymerase theta IC50 = 0.75 nM 9.12 Inhibition of human DNA polymerase theta pol domain (1819 to 2590 residues) expr... 36126059

Literature References

PubMed DOI Target Context # Activities
36126059 10.1021/acs.jmedchem.2c00998 ADMET 2
36126059 10.1021/acs.jmedchem.2c00998 DNA polymerase theta 1
36126059 10.1021/acs.jmedchem.2c00998 Unchecked 1

Data from ChEMBL 36 via Core Engine