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Compound Detail

CHEMBL2024110

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COc1ccc([C@@H]2c3[nH]c4ccccc4c3C[C@@H]3C(=O)N([C@@H]4CCN(CCNC(=O)OC(C)(C)C)C4)CC(=O)N23)cc1OC

Basic Information

ChEMBL ID CHEMBL2024110
Phase Preclinical
Structure Type MOL
InChI Key PJDAELFJPWFTQG-WIISGGPLSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

603.7
MW (Da)
3.47
ALogP
7
HBA
2
HBD
116.4
PSA (Ų)
0.42
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 C33H41N5O6
MW 603.72
Aromatic Rings 3
Heavy Atoms 44
NP-Likeness -0.68

Activity Summary

IC50 1 meas. best 6.13

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 6.13 6.13 740.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasmodium falciparum IC50 = 740.0 nM 6.13 Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum K1 i... 22204607

Literature References

PubMed DOI Target Context # Activities
22204607 10.1021/jm201422e Unchecked 1
22204607 10.1021/jm201422e Plasmodium falciparum 1
22204607 10.1021/jm201422e cGMP-specific 3',5'-cyclic phosphodiesterase 1
22204607 10.1021/jm201422e ADMET 1
22204607 10.1021/jm201422e MRC5 1

Data from ChEMBL 36 via Core Engine