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Compound Detail

CHEMBL2369711

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CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O

Basic Information

ChEMBL ID CHEMBL2369711
Phase Preclinical
Structure Type BOTH
InChI Key MKZHMDBHWUGCGW-WSLLFAHXSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

821.9
MW (Da)
0.76
ALogP
9
HBA
9
HBD
284.9
PSA (Ų)
0.07
QED
2
Ro5 Violations
21
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C40H55N9O10
MW 821.93
Aromatic Rings 3
Heavy Atoms 59
NP-Likeness -0.08

Activity Summary

IC50 1 meas. best 4.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin receptor type B
CHEMBL4631
IC50 4.47 4.47 34000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin receptor type B IC50 = 34000.0 nM 4.47 Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) ... -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(95)00152-J Endothelin-1 receptor 1
- 10.1016/0960-894X(95)00152-J Endothelin receptor type B 1

Data from ChEMBL 36 via Core Engine