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Compound Detail

CHEMBL2029589

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CC[C@H]1OC(=O)[C@H](C)[C@@H](O[C@H]2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)C)[C@H]2O)[C@](C)(O)C[C@@H](C)CN(CCCNc2ccnc3cc(Cl)ccc23)[C@H](C)[C@@H](O)[C@]1(C)O

Basic Information

ChEMBL ID CHEMBL2029589
Phase Preclinical
Structure Type MOL
InChI Key CCWRKUNMUSQVNW-AWGVHYQESA-N
2
Targets
3
Activities
1
Assay Types
5
PK Parameters
8
Publications
0
Known Names

Molecular Properties

953.7
MW (Da)
4.97
ALogP
16
HBA
6
HBD
205.0
PSA (Ų)
0.12
QED
3
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C49H81ClN4O12
MW 953.66
Aromatic Rings 2
Heavy Atoms 66
NP-Likeness 0.97

Activity Summary

IC50 3 meas. best 7.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 7.66 7.66 22.0 2
HepG2
CHEMBL395
IC50 4.52 4.52 30000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 4.0 mL.min-1.kg-1 Mus musculus
CL 9.5 mL.min-1.kg-1 Mus musculus
F 20.4 % Mus musculus
Fu 0.0042 - Mus musculus
T1/2 17.8 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22148880 10.1021/jm201615t Plasmodium berghei 6
22148880 10.1021/jm201615t Mus musculus 5
22148880 10.1021/jm201615t Liver microsomes 2
22148880 10.1021/jm201615t Plasma 2
22148880 10.1021/jm201615t Plasmodium falciparum 1
22148880 10.1021/jm201615t HepG2 1
22148880 10.1021/jm201615t Liver 1
37357390 10.1021/acs.jmedchem.3c00206 Plasmodium falciparum 1

Data from ChEMBL 36 via Core Engine