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Compound Detail

CHEMBL473493

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CCCSc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O.Cl

Basic Information

ChEMBL ID CHEMBL473493
Phase Preclinical
Structure Type MOL
InChI Key YTFUWGQHTMHDEV-UQIIZPHYSA-N
Parent Compound CHEMBL1186640
Active Moiety CHEMBL1186640
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
4
Publications
0
Known Names

Molecular Properties

512.7
MW (Da)
4.41
ALogP
6
HBA
3
HBD
95.5
PSA (Ų)
0.25
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H33ClN2O4S2
MW 549.16
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.70

Activity Summary

EC50 1 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-3 adrenergic receptor
CHEMBL246
EC50 8.85 8.85 1.4 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 91.9 ng.hr.mL-1 Canis lupus familiaris
CL - - Canis lupus familiaris
Cmax 15.8 nM Canis lupus familiaris
F - % Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19366244 10.1021/jm9000709 Canis familiaris 5
19366244 10.1021/jm9000709 Beta-3 adrenergic receptor 1
19366244 10.1021/jm9000709 Beta-2 adrenergic receptor 1
19366244 10.1021/jm9000709 Beta-1 adrenergic receptor 1

Data from ChEMBL 36 via Core Engine