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Compound Detail

CHEMBL578159

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N#Cc1nc(Nc2cc(F)cc(F)c2)c2ncn(CC(F)F)c2n1

Basic Information

ChEMBL ID CHEMBL578159
Phase Preclinical
Structure Type MOL
InChI Key VMJFQUMKCMNFSX-UHFFFAOYSA-N
10
Targets
12
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

336.2
MW (Da)
2.98
ALogP
6
HBA
1
HBD
79.4
PSA (Ų)
0.74
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H8F4N6
MW 336.25
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.64

Activity Summary

IC50 12 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cruzipain
CHEMBL3563
IC50 7.89 7.89 13.0 1
Dipeptidyl peptidase 1
CHEMBL2252
IC50 5.16 5.16 6918.3 1
Procathepsin L
CHEMBL3837
IC50 5.1 5.1 7943.3 1
Kallikrein-4
CHEMBL4446
IC50 5.01 5.01 9772.4 1
Cathepsin Z
CHEMBL4160
IC50 4.83 4.83 14791.1 1
Caspase-1
CHEMBL4801
IC50 4.79 4.79 16218.1 1
Cathepsin S
CHEMBL2954
IC50 4.57 4.57 26915.3 1
Unchecked
CHEMBL612545
IC50 4.19 4.19 64565.4 1
Neutrophil elastase
CHEMBL248
IC50 4.07 4.07 85113.8 1
Chymase
CHEMBL4068
IC50 4.05 4.05 89125.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19908842 10.1021/jm901069a Cruzipain 1
19908842 10.1021/jm901069a Caspase-1 1
19908842 10.1021/jm901069a Dipeptidyl peptidase 1 1
19908842 10.1021/jm901069a Procathepsin L 1
19908842 10.1021/jm901069a Cathepsin S 1
19908842 10.1021/jm901069a Cathepsin Z 1
19908842 10.1021/jm901069a Matrix metalloproteinase-14 1
19908842 10.1021/jm901069a Cathepsin G 1
19908842 10.1021/jm901069a Chymase 1
19908842 10.1021/jm901069a Unchecked 1
19908842 10.1021/jm901069a Neutrophil elastase 1
19908842 10.1021/jm901069a Kallikrein-4 1

Data from ChEMBL 36 via Core Engine