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Compound Detail

CHEMBL135817

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COc1ccc(CN/C(=N/c2c([N+](=O)[O-])ccc3c2CC(O)C(C)(C(OC)OC)O3)NC#N)cc1

Basic Information

ChEMBL ID CHEMBL135817
Phase Preclinical
Structure Type MOL
InChI Key YXLSYODZSMWKLF-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

485.5
MW (Da)
2.12
ALogP
9
HBA
3
HBD
160.5
PSA (Ų)
0.10
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H27N5O7
MW 485.50
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.06

Activity Summary

IC50 1 meas. best 4.79

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rattus norvegicus
CHEMBL376
IC50 4.79 4.79 16100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Rattus norvegicus IC50 = 16100.0 nM 4.79 Inhibition of methoxamine-contracted rat aorta (Vasorelaxant potency) 11708922

Literature References

PubMed DOI Target Context # Activities
11708922 10.1021/jm010183f Rattus norvegicus 3

Data from ChEMBL 36 via Core Engine