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Compound Detail

CHEMBL424494

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COC(=O)C1=C(C)NC(=O)N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)C1c1ccc(F)c(F)c1

Basic Information

ChEMBL ID CHEMBL424494
Phase Preclinical
Structure Type MOL
InChI Key VOWPOPUYBMDWNA-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

552.6
MW (Da)
4.56
ALogP
5
HBA
2
HBD
91.0
PSA (Ų)
0.41
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H34F2N4O4
MW 552.62
Aromatic Rings 2
Heavy Atoms 40
NP-Likeness -1.08

Activity Summary

Ki 3 meas. best 8.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
Ki 8.96 8.96 1.1 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 6.64 6.64 230.0 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 6.39 6.39 410.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10579841 10.1021/jm990201h Alpha-1A adrenergic receptor 1
10579841 10.1021/jm990201h Alpha-1B adrenergic receptor 1
10579841 10.1021/jm990201h Alpha-1D adrenergic receptor 1

Data from ChEMBL 36 via Core Engine