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Compound Detail

CHEMBL1684573

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COc1cccc(-c2nc3ccc(OCCCN4CCCCC4)cc3c(=O)n2CC(=O)NC(C)C)c1

Basic Information

ChEMBL ID CHEMBL1684573
Phase Preclinical
Structure Type MOL
InChI Key NQOZPTYIJQUKTJ-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
5
PK Parameters
6
Publications
0
Known Names

Molecular Properties

492.6
MW (Da)
3.85
ALogP
7
HBA
1
HBD
85.7
PSA (Ų)
0.43
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H36N4O4
MW 492.62
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -1.52

Activity Summary

IC50 3 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vasopressin V1b receptor
CHEMBL2659
IC50 8.7 8.7 2.0 1
Vasopressin V1b receptor
CHEMBL1921
IC50 8.52 8.52 3.0 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 759.0 ng.hr.mL-1 Rattus norvegicus
AUC 515.0 ng.hr.mL-1 Rattus norvegicus
CL 43.0 mL.min-1.kg-1 Rattus norvegicus
F 55.0 % Rattus norvegicus
T1/2 1.2 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21353540 10.1016/j.bmcl.2010.12.081 Rattus norvegicus 6
21353540 10.1016/j.bmcl.2010.12.081 Vasopressin V1b receptor 3
21353540 10.1016/j.bmcl.2010.12.081 Liver microsomes 2
21353540 10.1016/j.bmcl.2010.12.081 Vasopressin V1a receptor 1
21353540 10.1016/j.bmcl.2010.12.081 Vasopressin V2 receptor 1
21353540 10.1016/j.bmcl.2010.12.081 Oxytocin receptor 1

Data from ChEMBL 36 via Core Engine