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Compound Detail

CHEMBL248648

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O=c1[nH]c(C2=C[C@@H](N3CCC(c4ccccc4)CC3)CC2)nc2c(Cl)cccc12

Basic Information

ChEMBL ID CHEMBL248648
Phase Preclinical
Structure Type MOL
InChI Key WGBZFQJXRNSUNB-IBGZPJMESA-N
1
Targets
2
Activities
1
Assay Types
2
PK Parameters
6
Publications
0
Known Names

Molecular Properties

405.9
MW (Da)
5.00
ALogP
3
HBA
1
HBD
49.0
PSA (Ų)
0.67
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H24ClN3O
MW 405.93
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.43

Activity Summary

IC50 2 meas. best 8.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Poly [ADP-ribose] polymerase 1
CHEMBL3105
IC50 8.06 8.06 8.7 2

Pharmacokinetic Data

Parameter Value Units Species
CL 1164.0 mL.min-1.kg-1 Mus musculus
CL 22.0 mL.min-1.kg-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Poly [ADP-ribose] polymerase 1 IC50 = 8.7 nM 8.06 Inhibition of human PARP1 17804225
Poly [ADP-ribose] polymerase 1 IC50 = 8.7 nM 8.06 Inhibition of PARP1 20364863

Literature References

PubMed DOI Target Context # Activities
17804225 10.1016/j.bmcl.2007.07.091 Brain 2
17804225 10.1016/j.bmcl.2007.07.091 Plasma 2
17804225 10.1016/j.bmcl.2007.07.091 Poly [ADP-ribose] polymerase 1 1
17804225 10.1016/j.bmcl.2007.07.091 Liver 1
17804225 10.1016/j.bmcl.2007.07.091 Liver microsomes 1
20364863 10.1021/jm100012m Poly [ADP-ribose] polymerase 1 1

Data from ChEMBL 36 via Core Engine