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Compound Detail

CHEMBL516242

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COCCN(CC1CC1)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12

Basic Information

ChEMBL ID CHEMBL516242
Phase Preclinical
Structure Type MOL
InChI Key VXLDEDKRJNGWMF-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
2
Publications
0
Known Names

Molecular Properties

396.5
MW (Da)
2.98
ALogP
8
HBA
0
HBD
77.7
PSA (Ų)
0.58
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H28N6O2
MW 396.50
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.41

Activity Summary

IC50 1 meas. best 8.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Corticotropin-releasing factor receptor 1
CHEMBL4649
IC50 8.51 8.51 3.1 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 684.76 ng.hr.mL-1 Canis lupus familiaris
Cmax 313.7 nM Canis lupus familiaris
T1/2 11.4 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19361209 10.1021/jm900025h Canis familiaris 3
19361209 10.1021/jm900025h Corticotropin-releasing factor receptor 1 1

Data from ChEMBL 36 via Core Engine