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Compound Detail

CHEMBL80036

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CC(C)Oc1ccccc1N1CCN(Cc2nc(CN3C(=O)CC4(CCCC4)CC3=O)co2)CC1

Basic Information

ChEMBL ID CHEMBL80036
Phase Preclinical
Structure Type MOL
InChI Key TXCOHHYQPMKABG-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

480.6
MW (Da)
3.99
ALogP
7
HBA
0
HBD
79.1
PSA (Ų)
0.55
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H36N4O4
MW 480.61
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -1.02

Activity Summary

Ki 2 meas. best 7.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
Ki 7.09 7.09 82.0 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 5.38 5.38 4142.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12161153 10.1016/s0960-894x(02)00436-5 Alpha-1A adrenergic receptor 1
12161153 10.1016/s0960-894x(02)00436-5 Alpha-1B adrenergic receptor 1
12161153 10.1016/s0960-894x(02)00436-5 Alpha-1D adrenergic receptor 1
12161153 10.1016/s0960-894x(02)00436-5 Adrenergic receptors; alpha-1 A & B 1
12161153 10.1016/s0960-894x(02)00436-5 Alpha adrenergic receptor (1a and 1d) 1

Data from ChEMBL 36 via Core Engine