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Compound Detail

CHEMBL4208981

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CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2COC)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O

Basic Information

ChEMBL ID CHEMBL4208981
Phase Preclinical
Structure Type MOL
InChI Key MIDCBJMXHQZYDG-BDVREWPYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

823.0
MW (Da)
-1.03
ALogP
12
HBA
8
HBD
281.4
PSA (Ų)
0.12
QED
3
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H54N8O10S2
MW 823.01
Aromatic Rings 1
Heavy Atoms 56
NP-Likeness 0.84

Activity Summary

EC50 1 meas. best 9.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxytocin receptor
CHEMBL2049
EC50 9.36 9.36 0.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Oxytocin receptor EC50 = 0.44 nM 9.36 Agonist activity at human OTR expressed in CHO cells assessed as increase in cal... 29273395

Literature References

PubMed DOI Target Context # Activities
29273395 10.1016/j.bmcl.2017.12.027 Oxytocin receptor 2
29273395 10.1016/j.bmcl.2017.12.027 ADMET 1
29273395 10.1016/j.bmcl.2017.12.027 Vasopressin V1a receptor 1

Data from ChEMBL 36 via Core Engine