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Compound Detail

CHEMBL3753047

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CCCc1nc2c(C)cc(C(=O)NCCc3ccc(F)cc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1

Basic Information

ChEMBL ID CHEMBL3753047
Phase Preclinical
Structure Type MOL
InChI Key LZNURXSBVXEBHU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

616.7
MW (Da)
5.89
ALogP
7
HBA
3
HBD
130.5
PSA (Ų)
0.17
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H33FN8O2
MW 616.70
Aromatic Rings 6
Heavy Atoms 46
NP-Likeness -1.63

Activity Summary

IC50 1 meas. best 6.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Type-1 angiotensin II receptor
CHEMBL227
IC50 6.85 6.85 140.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Type-1 angiotensin II receptor IC50 = 140.0 nM 6.85 Displacement of 125I-labelled Sar1-Ile8-angiotensin-2 from human AT1 receptor -

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C5MD00169B Type-1 angiotensin II receptor 1
- 10.1039/C5MD00169B Endothelin-1 receptor 1

Data from ChEMBL 36 via Core Engine