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Compound Detail

CHEMBL4227166

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N#CC1(NC(=O)[C@H](Cc2cccnc2)NC(=O)c2cccc(-c3ncc[nH]3)c2)CC1

Basic Information

ChEMBL ID CHEMBL4227166
Phase Preclinical
Structure Type MOL
InChI Key QWPJTGULBYJGHB-SFHVURJKSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

400.4
MW (Da)
1.99
ALogP
5
HBA
3
HBD
123.6
PSA (Ų)
0.56
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H20N6O2
MW 400.44
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.21

Activity Summary

EC50 1 meas. best 5.7
IC50 1 meas. best 8.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Falcipain 2
CHEMBL5800
IC50 8.57 8.57 2.7 1
Plasmodium falciparum
CHEMBL364
EC50 5.7 5.7 2000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29615344 10.1016/j.bmcl.2018.03.069 Unchecked 4
29615344 10.1016/j.bmcl.2018.03.069 Falcipain 2 1
29615344 10.1016/j.bmcl.2018.03.069 Plasmodium falciparum 1
29615344 10.1016/j.bmcl.2018.03.069 HeLa 1
29615344 10.1016/j.bmcl.2018.03.069 HUVEC 1

Data from ChEMBL 36 via Core Engine