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Compound Detail

CHEMBL142995

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O=C1CSc2c(cccc2OCC(O)CN2CCN(c3ccc(F)cc3)CC2)N1

Basic Information

ChEMBL ID CHEMBL142995
Phase Preclinical
Structure Type MOL
InChI Key PGAIECSQNAEQMI-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

417.5
MW (Da)
2.43
ALogP
6
HBA
2
HBD
65.0
PSA (Ų)
0.75
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 C21H24FN3O3S
MW 417.51
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -1.29

Activity Summary

Ki 3 meas. best 7.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 7.22 7.22 60.0 1
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 5.82 5.82 1500.0 1
Beta-1 adrenergic receptor
CHEMBL3252
Ki 5.17 5.17 6700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10743949 10.1016/s0960-894x(00)00016-0 Adrenergic receptor alpha-1 1
10743949 10.1016/s0960-894x(00)00016-0 Adrenergic receptor alpha-2 1
10743949 10.1016/s0960-894x(00)00016-0 Beta-1 adrenergic receptor 1
10743949 10.1016/s0960-894x(00)00016-0 Beta-2 adrenergic receptor 1

Data from ChEMBL 36 via Core Engine