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Compound Detail

CHEMBL61425

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CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)[O-])NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)[O-])NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O.[Na+].[Na+]

Basic Information

ChEMBL ID CHEMBL61425
Phase Preclinical
Structure Type MOL
InChI Key UWHBIISPHYTOGL-PFSAEEMXSA-L
Parent Compound CHEMBL1205177
Active Moiety CHEMBL1205177
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

928.0
MW (Da)
0.80
ALogP
11
HBA
9
HBD
288.5
PSA (Ų)
0.10
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 C45H51N9Na2O11S
MW 972.00
Aromatic Rings 4
Heavy Atoms 66
NP-Likeness -0.21

Activity Summary

IC50 1 meas. best 9.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL252
IC50 9.62 9.62 0.2 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 1.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor IC50 = 0.24 nM 9.62 Displacement of [125I]ET-1 from Endothelin A receptor 15055997

Literature References

PubMed DOI Target Context # Activities
15055997 10.1021/jm030528p Rattus norvegicus 2
15055997 10.1021/jm030528p Endothelin-1 receptor 1
15055997 10.1021/jm030528p Endothelin receptor 1

Data from ChEMBL 36 via Core Engine