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Compound Detail

CHEMBL3736173

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COC(=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(C)[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O

Basic Information

ChEMBL ID CHEMBL3736173
Phase Preclinical
Structure Type MOL
InChI Key MRYARPAVKVJRIQ-IIZANFQQSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

828.0
MW (Da)
-0.71
ALogP
11
HBA
7
HBD
272.5
PSA (Ų)
0.05
QED
3
Ro5 Violations
23
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C39H53N7O11S
MW 827.96
Aromatic Rings 2
Heavy Atoms 58
NP-Likeness -0.09

Activity Summary

EC50 1 meas.
IC50 1 meas. best 8.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuromedin-K receptor
CHEMBL4429
IC50 8.39 8.39 4.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neuromedin-K receptor IC50 = 4.1 nM 8.39 Displacement of ([125I]His3-MePhe7)-NKB from NK3 receptor (unknown origin) expre... -

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C4MD00514G Neuromedin-K receptor 2
- 10.1039/C4MD00514G Substance-P receptor 1
- 10.1039/C4MD00514G Substance-K receptor 1

Data from ChEMBL 36 via Core Engine