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Compound Detail

CHEMBL5397299

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CC(=O)c1ccc2c(c1)c1cc(C(C)=O)ccc1n2CCNCCN(C)C

Basic Information

ChEMBL ID CHEMBL5397299
Phase Preclinical
Structure Type MOL
InChI Key XNAJWGNXYVMGEC-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
4
PK Parameters
4
Publications
0
Known Names

Molecular Properties

365.5
MW (Da)
3.35
ALogP
5
HBA
1
HBD
54.3
PSA (Ų)
0.49
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H27N3O2
MW 365.48
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.84

Activity Summary

EC50 2 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei
CHEMBL612849
EC50 8.1 7.13 8.0 2

Pharmacokinetic Data

Parameter Value Units Species
CL 7.9 mL.min-1.g-1 Homo sapiens
CL 30.0 mL.min-1.kg-1 Mus musculus
Cmax 31848.53 nM Mus musculus
T1/2 9.333 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
36695630 10.1021/acs.jmedchem.2c01767 ADMET 14
36695630 10.1021/acs.jmedchem.2c01767 Trypanosoma brucei 3
36695630 10.1021/acs.jmedchem.2c01767 Cytochrome P450 3A4 2
36695630 10.1021/acs.jmedchem.2c01767 No relevant target 1

Data from ChEMBL 36 via Core Engine