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Compound Detail

CHEMBL2092927

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COc1ccccc1N1CCN(C[C@@H]2CN=C3c4ccccc4N=C(SC)N32)CC1

Basic Information

ChEMBL ID CHEMBL2092927
Phase Preclinical
Structure Type MOL
InChI Key DVYBIZHLZSDANU-KRWDZBQOSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

421.6
MW (Da)
3.31
ALogP
7
HBA
0
HBD
43.7
PSA (Ų)
0.76
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 C23H27N5OS
MW 421.57
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -1.07

Activity Summary

Ki 5 meas. best 6.91

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL319
Ki 6.91 6.91 122.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 6.84 6.84 144.0 1
Alpha-1B adrenergic receptor
CHEMBL315
Ki 6.18 6.18 667.0 1
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 5.52 5.52 3000.0 1
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 5.05 5.05 9000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9703460 10.1021/jm970159v Adrenergic receptor alpha-1 1
9703460 10.1021/jm970159v Alpha-1A adrenergic receptor 1
9703460 10.1021/jm970159v Alpha-1B adrenergic receptor 1
9703460 10.1021/jm970159v Adrenergic receptor alpha-2 1
9703460 10.1021/jm970159v Alpha-2A adrenergic receptor 1
9703460 10.1021/jm970159v Alpha-2B adrenergic receptor 1
9703460 10.1021/jm970159v Unchecked 1

Data from ChEMBL 36 via Core Engine