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Compound Detail

CHEMBL2114249

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C[C@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1

Basic Information

ChEMBL ID CHEMBL2114249
Phase Preclinical
Structure Type MOL
InChI Key DTYAFBJXWWLRMA-WAIKUNEKSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

475.5
MW (Da)
4.97
ALogP
4
HBA
1
HBD
61.9
PSA (Ų)
0.60
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 C25H28F3N3O3
MW 475.51
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -1.22

Activity Summary

Ki 3 meas. best 9.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
Ki 9.05 9.05 0.9 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 7.32 7.32 48.0 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 7.04 7.04 92.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11133073 10.1016/s0960-894x(00)00524-2 Alpha-1A adrenergic receptor 1
11133073 10.1016/s0960-894x(00)00524-2 Alpha-1B adrenergic receptor 1
11133073 10.1016/s0960-894x(00)00524-2 Alpha-1D adrenergic receptor 1
11133073 10.1016/s0960-894x(00)00524-2 Adrenergic receptor alpha-1 1

Data from ChEMBL 36 via Core Engine