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Compound Detail

CHEMBL125377

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CC(=O)O[C@@]12CO[C@@H]1C[C@H](O)[C@@]1(C)C(=O)[C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)Nc4ccccc4)C(C)(C)C)C[C@@](O)([C@@H](OC(=O)c4ccccc4)[C@H]21)C3(C)C

Basic Information

ChEMBL ID CHEMBL125377
Phase Preclinical
Structure Type MOL
InChI Key MPEFNICYZITKCK-DGZIGSSISA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

806.9
MW (Da)
3.23
ALogP
13
HBA
6
HBD
227.2
PSA (Ų)
0.13
QED
3
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C43H54N2O13
MW 806.91
Aromatic Rings 2
Heavy Atoms 58
NP-Likeness 1.76

Activity Summary

Kd 1 meas. best 5.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL4566
Kd 5.41 5.41 3920.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor Kd = 3920.0 nM 5.41 Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth ... -

Literature References

PubMed DOI Target Context # Activities
7562913 10.1021/jm00019a012 Tubulin 2
7562913 10.1021/jm00019a012 B16 2
7562913 10.1021/jm00019a012 ADMET 2
7562913 10.1021/jm00019a012 Unchecked 2
- 10.1016/S0960-894X(01)81085-4 Oryctolagus cuniculus 1
- 10.1016/S0960-894X(01)81085-4 Endothelin-1 receptor 1

Data from ChEMBL 36 via Core Engine