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Compound Detail

CHEMBL12127

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CC(C)Oc1ccccc1N1CCN(C/C=C/C(=O)CN2CCCCC2=O)CC1

Basic Information

ChEMBL ID CHEMBL12127
Phase Preclinical
Structure Type MOL
InChI Key KSRMLSMXMVIXSF-BQYQJAHWSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

399.5
MW (Da)
2.73
ALogP
5
HBA
0
HBD
53.1
PSA (Ų)
0.63
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H33N3O3
MW 399.54
Aromatic Rings 1
Heavy Atoms 29
NP-Likeness -0.92

Activity Summary

Ki 3 meas. best 7.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
Ki 7.75 7.75 18.0 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 6.22 6.22 602.0 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 5.27 5.27 5316.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10843225 10.1016/s0960-894x(00)00169-4 Alpha-1A adrenergic receptor 1
10843225 10.1016/s0960-894x(00)00169-4 Alpha-1B adrenergic receptor 1
10843225 10.1016/s0960-894x(00)00169-4 Alpha-1D adrenergic receptor 1
10843225 10.1016/s0960-894x(00)00169-4 Adrenergic receptors; alpha-1 A & B 1
10843225 10.1016/s0960-894x(00)00169-4 Alpha adrenergic receptor (1a and 1d) 1

Data from ChEMBL 36 via Core Engine