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Compound Detail

CHEMBL503454

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Cc1c(Cl)c(C(=O)N(c2ccccc2)c2ccccc2)nn1-c1ccccc1C(=O)N1Cc2ccccc2C[C@H]1CN

Basic Information

ChEMBL ID CHEMBL503454
Phase Preclinical
Structure Type MOL
InChI Key MLZCQGFPFQDFLC-NDEPHWFRSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

576.1
MW (Da)
6.34
ALogP
5
HBA
1
HBD
84.5
PSA (Ų)
0.26
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H30ClN5O2
MW 576.10
Aromatic Rings 5
Heavy Atoms 42
NP-Likeness -1.02

Activity Summary

IC50 4 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Apoptosis regulator Bcl-2
CHEMBL4860
IC50 7.52 7.3467 30.0 3
Bcl2-associated agonist of cell death
CHEMBL3817
IC50 5.79 5.79 1610.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19027294 10.1016/j.bmcl.2008.10.113 Apoptosis regulator Bcl-2 2
19027294 10.1016/j.bmcl.2008.10.113 Bcl2-associated agonist of cell death 2
31188592 10.1021/acs.jmedchem.8b01732 Apoptosis regulator Bcl-2 1

Data from ChEMBL 36 via Core Engine