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Compound Detail

CHEMBL3718710

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N#Cc1ccccc1-c1ccc2c(c1)CCn1c-2cc(OCC2COCCO2)nc1=O

Basic Information

ChEMBL ID CHEMBL3718710
Phase Preclinical
Structure Type MOL
InChI Key YYMRQEAZLNSZOV-UHFFFAOYSA-N
1
Targets
3
Activities
1
Assay Types
6
PK Parameters
3
Publications
0
Known Names

Molecular Properties

415.4
MW (Da)
2.80
ALogP
7
HBA
0
HBD
86.4
PSA (Ų)
0.65
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H21N3O4
MW 415.45
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.79

Activity Summary

IC50 3 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
G-protein coupled receptor 84
CHEMBL3714079
IC50 7.0 6.89 100.0 3

Pharmacokinetic Data

Parameter Value Units Species
AUC 2645.0 ng.hr.mL-1 Rattus norvegicus
CL 193.33 mL.min-1.kg-1 Macaca mulatta
CL 150.83 mL.min-1.kg-1 Mus musculus
CL 86.67 mL.min-1.kg-1 Homo sapiens
CL 105.0 mL.min-1.kg-1 Rattus norvegicus
CL 166.67 mL.min-1.kg-1 Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32902984 10.1021/acs.jmedchem.0c00272 ADMET 7
32902984 10.1021/acs.jmedchem.0c00272 G-protein coupled receptor 84 1
32902984 10.1021/acs.jmedchem.0c00272 Mus musculus 1

Data from ChEMBL 36 via Core Engine