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Compound Detail

CHEMBL422756

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CCCCc1nc2ccc(C)cc2c(=O)n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1

Basic Information

ChEMBL ID CHEMBL422756
Phase Preclinical
Structure Type MOL
InChI Key COMHISAZXMNVHW-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

450.6
MW (Da)
4.94
ALogP
6
HBA
1
HBD
89.3
PSA (Ų)
0.38
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H26N6O
MW 450.55
Aromatic Rings 5
Heavy Atoms 34
NP-Likeness -1.26

Activity Summary

IC50 4 meas. best 8.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Type-1 angiotensin II receptor
CHEMBL3948
IC50 8.96 8.5867 1.1 3
Angiotensin II receptor
CHEMBL2094112
IC50 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(00)80335-2 Rattus norvegicus 6
- 10.1016/S0960-894X(00)80335-2 Type-1 angiotensin II receptor 2
- 10.1016/S0960-894X(00)80335-2 Angiotensin II receptor 2
- 10.1016/S0960-894X(01)80243-2 Angiotensin II receptor 1
- 10.1016/S0960-894X(00)80335-2 Type-2 angiotensin II receptor 1
- 10.1016/S0960-894X(00)80334-0 Type-1 angiotensin II receptor 1
- 10.1016/S0960-894X(00)80334-0 No relevant target 1
29656203 10.1016/j.ejmech.2018.03.076 Unchecked 1

Data from ChEMBL 36 via Core Engine