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Compound Detail

CHEMBL1947152

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O=c1[nH]c2c(O)ccc(CCNCCc3cccc(-c4cccc(CNCc5ccccc5)c4)c3)c2s1

Basic Information

ChEMBL ID CHEMBL1947152
Phase Preclinical
Structure Type MOL
InChI Key UGGHXKYYWLVRAE-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

509.7
MW (Da)
5.63
ALogP
5
HBA
4
HBD
77.2
PSA (Ų)
0.17
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H31N3O2S
MW 509.68
Aromatic Rings 5
Heavy Atoms 37
NP-Likeness -0.32

Activity Summary

EC50 1 meas. best 9.3
IC50 1 meas. best 7.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-2 adrenergic receptor
CHEMBL5414
EC50 9.3 9.3 0.5 1
Beta-2 adrenergic receptor
CHEMBL210
IC50 7.5 7.5 31.6 1

Pharmacokinetic Data

Parameter Value Units Species
CL 23.0 mL.min-1.kg-1 Rattus norvegicus
T1/2 14.0 hr Rattus norvegicus
Vd 29.0 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22079756 10.1016/j.bmcl.2011.10.049 Beta-2 adrenergic receptor 3
22079756 10.1016/j.bmcl.2011.10.049 Rattus norvegicus 3
22079756 10.1016/j.bmcl.2011.10.049 No relevant target 1

Data from ChEMBL 36 via Core Engine