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Compound Detail

CHEMBL53374

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CCO/C(O)=C1\C(COCCN2CC(=O)NC2=O)=NC(C)=C(C(=O)OC)C1c1cccc(Cl)c1Cl

Basic Information

ChEMBL ID CHEMBL53374
Phase Preclinical
Structure Type MOL
InChI Key AIHFEHWVBFPNGQ-ZBJSNUHESA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

526.4
MW (Da)
3.35
ALogP
8
HBA
2
HBD
126.8
PSA (Ų)
0.22
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25Cl2N3O7
MW 526.37
Aromatic Rings 1
Heavy Atoms 35
NP-Likeness -1.02

Activity Summary

IC50 1 meas. best 8.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rattus norvegicus
CHEMBL376
IC50 8.5 8.5 3.2 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.5 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Rattus norvegicus IC50 = 3.162 nM 8.5 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 Canis familiaris 1
2342074 10.1021/jm00168a041 ADMET 1
2342074 10.1021/jm00168a041 Unchecked 1

Data from ChEMBL 36 via Core Engine