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Compound Detail

CHEMBL339929

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Cn1cncc1CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C

Basic Information

ChEMBL ID CHEMBL339929
Phase Preclinical
Structure Type MOL
InChI Key RPBDHIOXHLKZGJ-HYBHZXASSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

652.9
MW (Da)
2.33
ALogP
7
HBA
3
HBD
156.5
PSA (Ų)
0.34
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H48N6O5S
MW 652.86
Aromatic Rings 2
Heavy Atoms 46
NP-Likeness -0.27

Activity Summary

IC50 1 meas. best 8.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxytocin receptor
CHEMBL3996
IC50 8.64 8.64 2.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Oxytocin receptor IC50 = 2.3 nM 8.64 Inhibition of radioligand [3H]oxytocin binding at the oxytocin (OT) receptor in ... 8258821

Literature References

PubMed DOI Target Context # Activities
8258821 10.1021/jm00077a002 Oxytocin receptor 1
8258821 10.1021/jm00077a002 Vasopressin V1 receptor 1
8258821 10.1021/jm00077a002 Vasopressin V2 receptor 1

Data from ChEMBL 36 via Core Engine