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Compound Detail

CHEMBL209147

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Cc1cc(Cl)ccc1NC(=O)OC[C@H]1N=C(c2ccccc2)c2ccccc2N(CC(=O)N[C@H]2CC(=O)OC2O)C1=O

Basic Information

ChEMBL ID CHEMBL209147
Phase Preclinical
Structure Type MOL
InChI Key PBQHVEWSGIMXQE-ODCDIBDESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

591.0
MW (Da)
3.20
ALogP
8
HBA
3
HBD
146.6
PSA (Ų)
0.36
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H27ClN4O7
MW 591.02
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness -0.79

Activity Summary

IC50 2 meas. best 5.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Falcipain 2
CHEMBL5800
IC50 5.08 5.08 8250.0 1
Falcipain 2B
CHEMBL3488
IC50 4.95 4.95 11190.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16722625 10.1021/jm060405f Falcipain 2 1
16722625 10.1021/jm060405f Falcipain 2B 1
16722625 10.1021/jm060405f Caspase-1 1
16722625 10.1021/jm060405f Caspase-2 1
16722625 10.1021/jm060405f Caspase-3 1
16722625 10.1021/jm060405f Caspase-4 1
16722625 10.1021/jm060405f Caspase-5 1
16722625 10.1021/jm060405f Caspase-6 1
16722625 10.1021/jm060405f Caspase-7 1
16722625 10.1021/jm060405f Caspase-8 1
16722625 10.1021/jm060405f Caspase-9 1

Data from ChEMBL 36 via Core Engine