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Compound Detail

CHEMBL1807818

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O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCOCCc3ccccc3)c2s1

Basic Information

ChEMBL ID CHEMBL1807818
Phase Preclinical
Structure Type MOL
InChI Key GIBUZEJUJJDWTJ-IBGZPJMESA-N
2
Targets
2
Activities
2
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

448.6
MW (Da)
3.30
ALogP
7
HBA
4
HBD
94.6
PSA (Ų)
0.30
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 C22H28N2O4S2
MW 448.61
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.46

Activity Summary

EC50 1 meas. best 10.1
IC50 1 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-2 adrenergic receptor
CHEMBL210
EC50 10.1 10.1 0.1 1
Beta-1 adrenergic receptor
CHEMBL213
IC50 8.1 8.1 7.9 1

Pharmacokinetic Data

Parameter Value Units Species
CL 33.0 mL.min-1.g-1 Homo sapiens
CL 113.0 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