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Compound Detail

CHEMBL386629

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CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC

Basic Information

ChEMBL ID CHEMBL386629
Phase Preclinical
Structure Type BOTH
InChI Key MPARFXYZMNLXHZ-OABNXZHLSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

2433.9
MW (Da)

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C107H157N25O30S5
MW 2433.91

Activity Summary

Kd 1 meas. best 6.73

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL4566
Kd 6.73 6.73 188.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor Kd = 188.0 nM 6.73 Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth ... -

Literature References

PubMed DOI Target Context # Activities
- 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