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Compound Detail

CHEMBL300042

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CCOC(=O)c1cn(CCOCC2=NC(C)=C(C(=O)OC)C(c3ccccc3Cl)/C2=C(\O)OCC)nn1

Basic Information

ChEMBL ID CHEMBL300042
Phase Preclinical
Structure Type MOL
InChI Key HOAHEVZYQDBJKP-YYDJUVGSSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

533.0
MW (Da)
3.62
ALogP
11
HBA
1
HBD
134.4
PSA (Ų)
0.26
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H29ClN4O7
MW 532.98
Aromatic Rings 2
Heavy Atoms 37
NP-Likeness -1.47

Activity Summary

IC50 1 meas. best 7.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rattus norvegicus
CHEMBL376
IC50 7.3 7.3 50.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Rattus norvegicus IC50 = 50.12 nM 7.3 Concentration required to block Ca+2-induced contraction of K+ depolarized rat a... 2342074

Literature References

PubMed DOI Target Context # Activities
2342074 10.1021/jm00168a041 Rattus norvegicus 1
2342074 10.1021/jm00168a041 Cavia porcellus 1
2342074 10.1021/jm00168a041 Unchecked 1

Data from ChEMBL 36 via Core Engine