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Compound Detail

CHEMBL2323545

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C[C@H](NC(=O)CN1CCc2cccc3c2C1CNC3=O)C(=O)N1CC=C(c2ccc(F)cc2)CC1

Basic Information

ChEMBL ID CHEMBL2323545
Phase Preclinical
Structure Type MOL
InChI Key GXUDQLGOCXKORM-NVHKAFQKSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

476.6
MW (Da)
2.29
ALogP
4
HBA
2
HBD
81.8
PSA (Ų)
0.69
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H29FN4O3
MW 476.55
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.81

Activity Summary

IC50 1 meas. best 7.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Poly [ADP-ribose] polymerase 1
CHEMBL3105
IC50 7.72 7.72 19.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Poly [ADP-ribose] polymerase 1 IC50 = 19.0 nM 7.72 Inhibition of human recombinant PARP1 after 1 hr by ELISA 23473053

Literature References

PubMed DOI Target Context # Activities
23473053 10.1021/jm301825t Poly [ADP-ribose] polymerase 1 1

Data from ChEMBL 36 via Core Engine