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Compound Detail

CHEMBL3582268

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COc1cc2nc(N3CCN(C(=O)c4cc5ccc(O)cc5oc4=O)CC3)nc(N)c2cc1OC

Basic Information

ChEMBL ID CHEMBL3582268
Phase Preclinical
Structure Type MOL
InChI Key CNMNBFPDHZVEGX-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

477.5
MW (Da)
2.00
ALogP
10
HBA
2
HBD
144.2
PSA (Ų)
0.42
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H23N5O6
MW 477.48
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.63

Activity Summary

IC50 1 meas. best 8.41
Ki 1 meas. best 8.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
Ki 8.68 8.68 2.1 1
Alpha-1A adrenergic receptor
CHEMBL229
IC50 8.41 8.41 3.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26005522 10.1021/ml5004298 ADMET 6
26005522 10.1021/ml5004298 Alpha-1A adrenergic receptor 4
26005522 10.1021/ml5004298 Alpha-1D adrenergic receptor 3
26005522 10.1021/ml5004298 Alpha-1B adrenergic receptor 1

Data from ChEMBL 36 via Core Engine