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Compound Detail

CHEMBL378939

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CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)NC(C)(C)C)c1ccc2c(c1)CCO2

Basic Information

ChEMBL ID CHEMBL378939
Phase Preclinical
Structure Type MOL
InChI Key IQWQOUYCIZPRTH-ZRJLEYOISA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
4
Publications
0
Known Names

Molecular Properties

517.7
MW (Da)
3.73
ALogP
4
HBA
2
HBD
87.7
PSA (Ų)
0.61
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H39N3O4
MW 517.67
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -0.04

Activity Summary

Ki 1 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxytocin receptor
CHEMBL2049
Ki 8.4 8.4 4.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 39.0 mL.min-1.kg-1 Rattus norvegicus
CL 14.0 mL.min-1.kg-1 Canis lupus familiaris
F 27.0 % Rattus norvegicus
F 9.0 % Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Oxytocin receptor Ki = 3.981 nM 8.4 Displacement of [3H]oxytocin from human OTR 16821776

Literature References

PubMed DOI Target Context # Activities
16821776 10.1021/jm060073e Rattus norvegicus 2
16821776 10.1021/jm060073e Canis familiaris 2
16821776 10.1021/jm060073e No relevant target 1
16821776 10.1021/jm060073e Oxytocin receptor 1

Data from ChEMBL 36 via Core Engine