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Compound Detail

CHEMBL47177

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CCCCc1nc2ccc([C@]3(C)C[C@H]4CCCN4O3)cc2c(=O)n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1

Basic Information

ChEMBL ID CHEMBL47177
Phase Preclinical
Structure Type MOL
InChI Key AAZOKMBAJGOCHB-HPMVVLTCSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

561.7
MW (Da)
5.65
ALogP
8
HBA
1
HBD
101.8
PSA (Ų)
0.26
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H35N7O2
MW 561.69
Aromatic Rings 5
Heavy Atoms 42
NP-Likeness -0.76

Activity Summary

Kd 2 meas. best 10.9
IC50 1 meas. best 7.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Angiotensin II receptor
CHEMBL2094256
Kd 10.9 10.9 0.0 1
Type-1 angiotensin II receptor
CHEMBL227
Kd 10.9 10.9 0.0 1
Type-1 angiotensin II receptor
CHEMBL3374
IC50 7.57 7.57 27.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(00)80365-0 Rattus norvegicus 10
8576904 10.1021/jm9504722 Angiotensin II receptor 1
- 10.1016/S0960-894X(00)80365-0 Type-1 angiotensin II receptor 1
21071232 10.1016/j.bmc.2010.10.043 Type-1 angiotensin II receptor 1
29656203 10.1016/j.ejmech.2018.03.076 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine