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Compound Detail

CHEMBL77913

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COc1ccc(Nc2ncc[nH]2)c(C)c1

Basic Information

ChEMBL ID CHEMBL77913
Phase Preclinical
Structure Type MOL
InChI Key BEAKKNUWBXQLLR-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

203.2
MW (Da)
2.47
ALogP
3
HBA
2
HBD
49.9
PSA (Ų)
0.81
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C11H13N3O
MW 203.25
Aromatic Rings 2
Heavy Atoms 15
NP-Likeness -1.36

Activity Summary

Ki 4 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 8.0 8.0 10.0 1
Alpha-2B adrenergic receptor
CHEMBL266
Ki 6.36 6.36 434.0 1
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 6.29 6.29 512.0 1
Adrenergic receptor alpha-1
CHEMBL2094251
Ki 5.08 5.08 8400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9016324 10.1021/jm9605142 Adrenergic receptor alpha-1 1
9016324 10.1021/jm9605142 Alpha-2A adrenergic receptor 1
9016324 10.1021/jm9605142 Alpha-2B adrenergic receptor 1
9016324 10.1021/jm9605142 Alpha-2C adrenergic receptor 1

Data from ChEMBL 36 via Core Engine