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Compound Detail

CHEMBL1257798

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O=C(O)c1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O

Basic Information

ChEMBL ID CHEMBL1257798
Phase Preclinical
Structure Type MOL
InChI Key NPOJTLRAMYFXPE-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

520.6
MW (Da)
3.76
ALogP
9
HBA
4
HBD
128.0
PSA (Ų)
0.26
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H28N4O5S
MW 520.61
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.13

Activity Summary

Ki 2 meas. best 5.46
EC50 1 meas. best 6.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-3 adrenergic receptor
CHEMBL246
EC50 6.51 6.51 310.0 1
Beta-3 adrenergic receptor
CHEMBL246
Ki 5.46 5.46 3500.0 1
Beta-1 adrenergic receptor
CHEMBL213
Ki 5.17 5.17 6710.0 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-1 adrenergic receptor 1

Data from ChEMBL 36 via Core Engine