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Compound Detail

CHEMBL414836

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CCCCc1nc2c(C)cc(C)nc2n1C1CCc2cc(-c3ccccc3-c3nn[nH]n3)ccc21

Basic Information

ChEMBL ID CHEMBL414836
Phase Preclinical
Structure Type MOL
InChI Key HBYVOFWUGXPDMO-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

463.6
MW (Da)
5.77
ALogP
6
HBA
1
HBD
85.2
PSA (Ų)
0.35
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H29N7
MW 463.59
Aromatic Rings 5
Heavy Atoms 35
NP-Likeness -0.86

Activity Summary

IC50 2 meas. best 7.52
EC50 1 meas. best 5.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Angiotensin II receptor (AT-1) type-1
CHEMBL2094250
IC50 7.52 7.52 30.0 1
Type-1 angiotensin II receptor
CHEMBL227
IC50 6.62 6.62 238.0 1
Peroxisome proliferator-activated receptor gamma
CHEMBL235
EC50 5.66 5.66 2200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21557540 10.1021/jm200409s Peroxisome proliferator-activated receptor gamma 2
- 10.1016/S0960-894X(01)81128-8 Angiotensin II receptor (AT-1) type-1 1
21557540 10.1021/jm200409s Type-1 angiotensin II receptor 1

Data from ChEMBL 36 via Core Engine