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Compound Detail

CHEMBL2112716

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COC(OC)[C@]1(C)Oc2ccc([N+](=O)[O-])cc2[C@@H](/N=C(\NC#N)Nc2ccc(Cl)cc2)[C@@H]1O

Basic Information

ChEMBL ID CHEMBL2112716
Phase Preclinical
Structure Type MOL
InChI Key MQYJKKAHTAOTTM-LVCYWYKZSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

475.9
MW (Da)
2.96
ALogP
8
HBA
3
HBD
151.3
PSA (Ų)
0.11
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H22ClN5O6
MW 475.89
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.46

Activity Summary

IC50 1 meas. best 4.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rattus norvegicus
CHEMBL376
IC50 4.76 4.76 17500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Rattus norvegicus IC50 = 17500.0 nM 4.76 Inhibition of methoxamine-contracted rat aorta (Vasorelaxant potency) 11708922

Literature References

PubMed DOI Target Context # Activities
11708922 10.1021/jm010183f Rattus norvegicus 4

Data from ChEMBL 36 via Core Engine