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Compound Detail

CHEMBL4091483

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CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O

Basic Information

ChEMBL ID CHEMBL4091483
Phase Preclinical
Structure Type MOL
InChI Key JVJJADDHVNTRGR-BMGWUDNWSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

966.1
MW (Da)
-4.60
ALogP
15
HBA
12
HBD
393.7
PSA (Ų)
0.07
QED
3
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C40H59N11O13S2
MW 966.11
Aromatic Rings 1
Heavy Atoms 66
NP-Likeness 0.42

Activity Summary

EC50 1 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxytocin receptor
CHEMBL2049
EC50 7.4 7.4 40.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Oxytocin receptor EC50 = 40.0 nM 7.4 Agonist activity at human OTR expressed in CHO cells assessed as calcium mobiliz... 28438540

Literature References

PubMed DOI Target Context # Activities
28438540 10.1016/j.bmcl.2017.04.030 Vasopressin V1a receptor 2
28438540 10.1016/j.bmcl.2017.04.030 Unchecked 2
28438540 10.1016/j.bmcl.2017.04.030 Oxytocin receptor 1

Data from ChEMBL 36 via Core Engine