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Compound Detail

CHEMBL314315

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CCCc1nc2c(C)cc(C)nc2n1Cc1ccc(-c2c(C(=O)O)c(Cl)nc3ccccc23)cc1

Basic Information

ChEMBL ID CHEMBL314315
Phase Preclinical
Structure Type MOL
InChI Key CPPCOUAVKSXREI-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

485.0
MW (Da)
6.62
ALogP
5
HBA
1
HBD
80.9
PSA (Ų)
0.27
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 C28H25ClN4O2
MW 484.99
Aromatic Rings 5
Heavy Atoms 35
NP-Likeness -1.09

Activity Summary

IC50 2 meas. best 8.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Angiotensin II receptor (AT-1) type-1
CHEMBL2094250
IC50 8.11 8.11 7.7 1
Type-1 angiotensin II receptor B
CHEMBL263
IC50 8.11 8.11 7.7 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 340.0 ng.hr.mL-1 Rattus norvegicus
T1/2 0.3 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17064065 10.1021/jm0603163 Rattus norvegicus 2
15115399 10.1021/jm031100t Type-1 angiotensin II receptor B 1
17064065 10.1021/jm0603163 Angiotensin II receptor (AT-1) type-1 1

Data from ChEMBL 36 via Core Engine