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Compound Detail

CHEMBL1807873

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O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCNCCc3cccc(Cl)c3Cl)c2s1

Basic Information

ChEMBL ID CHEMBL1807873
Phase Preclinical
Structure Type MOL
InChI Key OOXNTGSMQFBSGF-SFHVURJKSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

500.4
MW (Da)
3.46
ALogP
7
HBA
5
HBD
106.6
PSA (Ų)
0.23
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H27Cl2N3O4S
MW 500.45
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.59

Activity Summary

EC50 2 meas. best 9.1
IC50 2 meas. best 7.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-2 adrenergic receptor
CHEMBL210
EC50 9.1 9.1 0.8 1
Beta-1 adrenergic receptor
CHEMBL213
IC50 7.3 7.3 50.1 1
Beta-1 adrenergic receptor
CHEMBL213
EC50 6.8 6.8 158.5 1
D(2) dopamine receptor
CHEMBL217
IC50 5.7 5.7 1995.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21723724 10.1016/j.bmcl.2011.05.097 Unchecked 3
21723724 10.1016/j.bmcl.2011.05.097 Beta-1 adrenergic receptor 2
21723724 10.1016/j.bmcl.2011.05.097 Beta-2 adrenergic receptor 2
21723724 10.1016/j.bmcl.2011.05.097 No relevant target 1
21723724 10.1016/j.bmcl.2011.05.097 D(2) dopamine receptor 1

Data from ChEMBL 36 via Core Engine