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Compound Detail

CHEMBL356829

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COC(=O)C1(c2ccccc2)CCN(CCCNC(=O)C2=C(C)NC(C)=C(C(N)=O)C2c2ccc([N+](=O)[O-])cc2)CC1

Basic Information

ChEMBL ID CHEMBL356829
Phase Preclinical
Structure Type MOL
InChI Key PAPWWRYYLPOWNO-UHFFFAOYSA-N
4
Targets
6
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

575.7
MW (Da)
3.03
ALogP
8
HBA
3
HBD
156.9
PSA (Ų)
0.17
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H37N5O6
MW 575.67
Aromatic Rings 2
Heavy Atoms 42
NP-Likeness -0.92

Activity Summary

Ki 6 meas. best 9.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
Ki 9.08 8.85 0.8 2
Alpha-1B adrenergic receptor
CHEMBL232
Ki 5.56 5.495 2740.0 2
5-hydroxytryptamine receptor 1D
CHEMBL1983
Ki 5.34 5.34 4520.0 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 5.06 5.06 8800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10579840 10.1021/jm990200p Alpha-1A adrenergic receptor 1
10579840 10.1021/jm990200p Alpha-1B adrenergic receptor 1
10579840 10.1021/jm990200p Alpha-1D adrenergic receptor 1
9857099 10.1021/jm980506g Alpha-1A adrenergic receptor 1
9857099 10.1021/jm980506g Alpha-1B adrenergic receptor 1
9857099 10.1021/jm980506g 5-hydroxytryptamine receptor 1D 1

Data from ChEMBL 36 via Core Engine