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Compound Detail

CHEMBL5549773

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COC1=CC(c2ccc(Cc3ccc(OC)cc3)[nH]2)=N/C1=C\NC12CC3CC(CC(C3)C1)C2.Cl

Basic Information

ChEMBL ID CHEMBL5549773
Phase Preclinical
Structure Type MOL
InChI Key ZIDBJYNZXSKSEF-SJBLSZAKSA-N
Parent Compound CHEMBL6069257
Active Moiety CHEMBL6069257
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

443.6
MW (Da)
5.35
ALogP
4
HBA
2
HBD
58.6
PSA (Ų)
0.61
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H34ClN3O2
MW 480.05
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.02

Activity Summary

EC50 1 meas. best 7.95

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Leishmania mexicana
CHEMBL612880
EC50 7.95 7.95 11.3 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 1.0 hr Homo sapiens
T1/2 1.0 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Leishmania mexicana EC50 = 11.3 nM 7.95 Antileishmanial activity against Leishmania mexicana MNYC/BZ/62/M379 amastigotes... 38722757

Literature References

PubMed DOI Target Context # Activities
38722757 10.1021/acs.jmedchem.4c00517 ADMET 3
38722757 10.1021/acs.jmedchem.4c00517 Leishmania mexicana 2
38722757 10.1021/acs.jmedchem.4c00517 J774.A1 2

Data from ChEMBL 36 via Core Engine