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Compound Detail

CHEMBL3218778

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Cc1cc(NC(=O)Cn2nnc(-c3ccc(NC(=O)c4ccc(F)cc4)cc3)n2)no1

Basic Information

ChEMBL ID CHEMBL3218778
Phase Preclinical
Structure Type MOL
InChI Key MFILMPVTFCSPMR-UHFFFAOYSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

421.4
MW (Da)
2.67
ALogP
8
HBA
2
HBD
127.8
PSA (Ų)
0.49
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H16FN7O3
MW 421.39
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -2.83

Activity Summary

IC50 5 meas. best 5.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 5.66 5.48 2200.0 2
Cathepsin K
CHEMBL268
IC50 5.42 5.42 3830.0 1
Procathepsin L
CHEMBL3837
IC50 4.61 4.61 24390.0 1
Cathepsin B
CHEMBL4072
IC50 4.43 4.43 37140.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 2200.0 nM 5.66 Inhibition of Plasmodium falciparum recombinant falcipain 2 -
Cathepsin K IC50 = 3830.0 nM 5.42 Inhibition of human cathepsin K -
Unchecked IC50 = 4950.0 nM 5.3 Inhibition of Plasmodium falciparum recombinant falcipain 3 -
Procathepsin L IC50 = 24390.0 nM 4.61 Inhibition of human cathepsin L1 -
Cathepsin B IC50 = 37140.0 nM 4.43 Inhibition of human cathepsin B -

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C1MD00129A Unchecked 2
- 10.1039/C1MD00129A Plasmodium falciparum 1
- 10.1039/C1MD00129A Cathepsin K 1
- 10.1039/C1MD00129A Procathepsin L 1
- 10.1039/C1MD00129A Cathepsin B 1

Data from ChEMBL 36 via Core Engine