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Compound Detail

CHEMBL1807822

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O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCOCCc3cccc4ccccc34)c2s1

Basic Information

ChEMBL ID CHEMBL1807822
Phase Preclinical
Structure Type MOL
InChI Key BYUSHVMTXZIAER-QHCPKHFHSA-N
2
Targets
2
Activities
2
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

482.6
MW (Da)
3.74
ALogP
7
HBA
4
HBD
103.8
PSA (Ų)
0.22
QED
0
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H30N2O5S
MW 482.60
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -0.29

Activity Summary

EC50 1 meas. best 9.9
IC50 1 meas. best 8.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-2 adrenergic receptor
CHEMBL210
EC50 9.9 9.9 0.1 1
Beta-1 adrenergic receptor
CHEMBL213
IC50 8.5 8.5 3.2 1

Pharmacokinetic Data

Parameter Value Units Species
CL 35.0 mL.min-1.g-1 Homo sapiens
CL 118.0 uL.min-1.(10^6cells)-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21723724 10.1016/j.bmcl.2011.05.097 Beta-1 adrenergic receptor 2
21723724 10.1016/j.bmcl.2011.05.097 Unchecked 2
21723724 10.1016/j.bmcl.2011.05.097 Beta-2 adrenergic receptor 2
- 10.6019/CHEMBL3301361 ADMET 2
21723724 10.1016/j.bmcl.2011.05.097 D(2) dopamine receptor 1
21723724 10.1016/j.bmcl.2011.05.097 No relevant target 1
- 10.6019/CHEMBL3301361 No relevant target 1

Data from ChEMBL 36 via Core Engine