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Compound Detail

CHEMBL1258705

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N#Cc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1

Basic Information

ChEMBL ID CHEMBL1258705
Phase Preclinical
Structure Type MOL
InChI Key YTDOMMMKOKIYBM-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

485.6
MW (Da)
4.23
ALogP
8
HBA
2
HBD
94.3
PSA (Ų)
0.39
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H27N5O2S
MW 485.61
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.70

Activity Summary

Ki 3 meas. best 7.38
EC50 1 meas. best 7.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-3 adrenergic receptor
CHEMBL246
EC50 7.46 7.46 35.0 1
Beta-2 adrenergic receptor
CHEMBL210
Ki 7.38 7.38 42.0 1
Beta-3 adrenergic receptor
CHEMBL246
Ki 7.33 7.33 47.0 1
Beta-1 adrenergic receptor
CHEMBL213
Ki 6.16 6.16 700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20833036 10.1016/j.bmcl.2010.08.039 Beta-3 adrenergic receptor 4
20833036 10.1016/j.bmcl.2010.08.039 Beta-2 adrenergic receptor 1
20833036 10.1016/j.bmcl.2010.08.039 Beta-1 adrenergic receptor 1

Data from ChEMBL 36 via Core Engine