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Compound Detail

CHEMBL70310

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Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccccn3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1

Basic Information

ChEMBL ID CHEMBL70310
Phase Preclinical
Structure Type MOL
InChI Key CUQQKEAZMNXDAZ-AJQTZOPKSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

574.7
MW (Da)
5.34
ALogP
4
HBA
3
HBD
115.4
PSA (Ų)
0.21
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H34N4O4
MW 574.68
Aromatic Rings 5
Heavy Atoms 43
NP-Likeness -0.49

Activity Summary

Ki 2 meas. best 8.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin receptor type B
CHEMBL1785
Ki 8.36 8.36 4.4 1
Endothelin-1 receptor
CHEMBL252
Ki 5.64 5.64 2300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9873521 10.1016/s0960-894x(98)00387-4 Endothelin-1 receptor 1
9873521 10.1016/s0960-894x(98)00387-4 Endothelin receptor type B 1
9873521 10.1016/s0960-894x(98)00387-4 Unchecked 1

Data from ChEMBL 36 via Core Engine