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Compound Detail

CHEMBL511968

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CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1C1CCCC1.Cl

Basic Information

ChEMBL ID CHEMBL511968
Phase Preclinical
Structure Type MOL
InChI Key CXEJQKAZNHTVAJ-JCOPYZAKSA-N
Parent Compound CHEMBL1187617
Active Moiety CHEMBL1187617
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
4
Publications
0
Known Names

Molecular Properties

506.7
MW (Da)
4.57
ALogP
5
HBA
3
HBD
95.5
PSA (Ų)
0.35
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H35ClN2O4S
MW 543.13
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.30

Activity Summary

EC50 1 meas. best 9.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-3 adrenergic receptor
CHEMBL246
EC50 9.39 9.39 0.4 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 211.1 ng.hr.mL-1 Canis lupus familiaris
CL 4.0 mL.min-1.kg-1 Canis lupus familiaris
Cmax 33.75 nM Canis lupus familiaris
F 50.0 % Canis lupus familiaris
T1/2 4.7 hr 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