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Compound Detail

CHEMBL330401

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COc1ccc(C2(c3ccccc3)CCN(CCCNC(=O)C3=C(COCCN)NC(C)=C(C(N)=O)C3c3ccc([N+](=O)[O-])cc3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL330401
Phase Preclinical
Structure Type MOL
InChI Key WDDPQFVKUCBXKP-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

682.8
MW (Da)
3.87
ALogP
9
HBA
4
HBD
175.1
PSA (Ų)
0.11
QED
1
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H46N6O6
MW 682.82
Aromatic Rings 3
Heavy Atoms 50
NP-Likeness -0.76

Activity Summary

Ki 3 meas. best 8.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
Ki 8.2 8.2 6.3 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 6.32 6.32 479.0 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 5.68 5.68 2073.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10522703 10.1016/s0960-894x(99)00484-9 Alpha-1D adrenergic receptor 2
10522703 10.1016/s0960-894x(99)00484-9 Alpha-1A adrenergic receptor 1
10522703 10.1016/s0960-894x(99)00484-9 Alpha-1B adrenergic receptor 1
10522703 10.1016/s0960-894x(99)00484-9 Adrenergic receptors; alpha-1 A & B 1

Data from ChEMBL 36 via Core Engine