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Compound Detail

CHEMBL3601307

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CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C4CCC4)n[nH]c3c2)c1

Basic Information

ChEMBL ID CHEMBL3601307
Phase Preclinical
Structure Type MOL
InChI Key VTBFNPMSMPHALX-NRFANRHFSA-N
1
Targets
2
Activities
1
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

444.6
MW (Da)
2.90
ALogP
6
HBA
4
HBD
116.3
PSA (Ų)
0.36
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H28N4O4S
MW 444.56
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.05

Activity Summary

EC50 2 meas. best 7.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-3 adrenergic receptor
CHEMBL246
EC50 7.18 7.18 66.0 2

Pharmacokinetic Data

Parameter Value Units Species
CL 641.0 mL.min-1.kg-1 Rattus norvegicus
CL 463.0 mL.min-1.kg-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26125514 10.1021/acs.jmedchem.5b00638 Beta-3 adrenergic receptor 2
26125514 10.1021/acs.jmedchem.5b00638 Alpha-1A adrenergic receptor 2
28355078 10.1021/acs.jmedchem.6b01197 Liver 2
28355078 10.1021/acs.jmedchem.6b01197 Alpha-1A adrenergic receptor 2
28355078 10.1021/acs.jmedchem.6b01197 Beta-3 adrenergic receptor 2
26125514 10.1021/acs.jmedchem.5b00638 Unchecked 1
28355078 10.1021/acs.jmedchem.6b01197 Unchecked 1

Data from ChEMBL 36 via Core Engine