Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL3759008

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
Cc1cc(-c2ccc(CC(=O)Nc3ccc4c(c3)[nH]c3ccccc34)cc2)ccn1

Basic Information

ChEMBL ID CHEMBL3759008
Phase Preclinical
Structure Type MOL
InChI Key LESYZLGMOGDETQ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
13
PK Parameters
8
Publications
0
Known Names

Molecular Properties

391.5
MW (Da)
5.87
ALogP
2
HBA
2
HBD
57.8
PSA (Ų)
0.40
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H21N3O
MW 391.47
Aromatic Rings 5
Heavy Atoms 30
NP-Likeness -0.93

Activity Summary

IC50 2 meas. best 8.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 8.64 8.64 2.3 1
Molecular identity unknown
CHEMBL612546
IC50 8.64 8.64 2.3 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 7442.0 ng.hr.mL-1 Rattus norvegicus
AUC 11293.0 ng.hr.mL-1 Rattus norvegicus
CL 41.0 mL.min-1.kg-1 Homo sapiens
CL 67.0 mL.min-1.kg-1 Mus musculus
CL 22.4 mL.min-1.kg-1 Rattus norvegicus
Cmax 4981.22 nM Rattus norvegicus
Cmax 7356.89 nM Rattus norvegicus
F 30.0 % Rattus norvegicus
T1/2 0.7167 hr Homo sapiens
T1/2 1.517 hr Mus musculus
T1/2 2.5 hr Rattus norvegicus
T1/2 3.1 hr Rattus norvegicus
Tmax 1.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26647303 10.1016/j.ejmech.2015.11.026 Rattus norvegicus 10
26647303 10.1016/j.ejmech.2015.11.026 ADMET 4
26647303 10.1016/j.ejmech.2015.11.026 No relevant target 2
26647303 10.1016/j.ejmech.2015.11.026 Liver microsome 2
26647303 10.1016/j.ejmech.2015.11.026 Protein-serine O-palmitoleoyltransferase porcupine 1
26647303 10.1016/j.ejmech.2015.11.026 Molecular identity unknown 1
26647303 10.1016/j.ejmech.2015.11.026 Plasma 1
33822624 10.1021/acs.jmedchem.0c01799 Unchecked 1

Data from ChEMBL 36 via Core Engine