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Compound Detail

CHEMBL427284

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COc1ccc(CN2C(=O)C(=C(C#N)C#N)c3cc(S(=O)(=O)N4CCC[C@H]4COc4cccnc4)ccc32)cc1

Basic Information

ChEMBL ID CHEMBL427284
Phase Preclinical
Structure Type MOL
InChI Key GCMPIGBMARKLRF-QFIPXVFZSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

555.6
MW (Da)
3.67
ALogP
8
HBA
0
HBD
136.6
PSA (Ų)
0.30
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H25N5O5S
MW 555.62
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -1.32

Activity Summary

IC50 4 meas. best 8.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Caspase-3
CHEMBL2334
IC50 8.11 8.11 7.8 1
Caspase-7
CHEMBL3468
IC50 7.53 7.53 29.6 1
Caspase-6
CHEMBL3308
IC50 6.21 6.21 610.0 1
Caspase-1
CHEMBL4801
IC50 5.41 5.41 3900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17585855 10.1021/jm070506t Caspase-1 1
17585855 10.1021/jm070506t Caspase-3 1
17585855 10.1021/jm070506t Caspase-6 1
17585855 10.1021/jm070506t Caspase-7 1
17585855 10.1021/jm070506t Caspase-8 1
17585855 10.1021/jm070506t No relevant target 1

Data from ChEMBL 36 via Core Engine