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Compound Detail

CHEMBL52739

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COc1ccccc1CNCCCCCCCCCCCCN(C)CCSSCCN(C)CCCCCCCCCCCCNCc1ccccc1OC

Basic Information

ChEMBL ID CHEMBL52739
Phase Preclinical
Structure Type MOL
InChI Key RJLLHLQUTSFJHZ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

787.3
MW (Da)
11.63
ALogP
8
HBA
2
HBD
49.0
PSA (Ų)
0.05
QED
2
Ro5 Violations
39
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C46H82N4O2S2
MW 787.32
Aromatic Rings 2
Heavy Atoms 54
NP-Likeness -0.28

Activity Summary

IC50 1 meas. best 4.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rattus norvegicus
CHEMBL376
IC50 4.33 4.33 46900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Rattus norvegicus IC50 = 46900.0 nM 4.33 Alpha-1-adrenoceptor blocking activity by antagonism of (-)-norepinephrine induc... 2900899

Literature References

PubMed DOI Target Context # Activities
2900899 10.1021/jm00117a030 Rattus norvegicus 1
2900899 10.1021/jm00117a030 Adrenergic receptor alpha-2 1
2900899 10.1021/jm00117a030 Adrenergic receptor alpha 1

Data from ChEMBL 36 via Core Engine