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Compound Detail

CHEMBL322862

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CS(=O)(=O)Nc1cc([C@@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)cc2)ccc1O

Basic Information

ChEMBL ID CHEMBL322862
Phase Preclinical
Structure Type MOL
InChI Key XWLVOJZVWRCRMD-OFNKIYASSA-N
2
Targets
3
Activities
1
Assay Types
4
PK Parameters
12
Publications
0
Known Names

Molecular Properties

492.5
MW (Da)
3.97
ALogP
6
HBA
4
HBD
107.9
PSA (Ų)
0.30
QED
0
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H26F2N2O5S
MW 492.54
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.90

Activity Summary

Ki 3 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-3 adrenergic receptor
CHEMBL246
Ki 7.68 7.68 21.0 2
Beta-3 adrenergic receptor
CHEMBL4030
Ki 5.4 5.4 4000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 36.0 mL.min-1.kg-1 Cercopithecidae
F 5.0 % Cercopithecidae
T1/2 7.3 hr Cercopithecidae
Vd 10.0 L.kg-1 Cercopithecidae

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17533126 10.1016/j.bmcl.2007.05.030 African green monkey 6
11714606 10.1016/s0960-894x(01)00629-1 ADMET 4
11714606 10.1016/s0960-894x(01)00629-1 Beta-3 adrenergic receptor 3
11714606 10.1016/s0960-894x(01)00629-1 Unchecked 3
11714606 10.1016/s0960-894x(01)00629-1 Beta-1 adrenergic receptor 2
17533126 10.1016/j.bmcl.2007.05.030 Beta-3 adrenergic receptor 2
11714606 10.1016/s0960-894x(01)00629-1 Beta-2 adrenergic receptor and beta-3 adrenergic receptor 1
11714606 10.1016/s0960-894x(01)00629-1 Adrenergic receptor beta; ADRB1 & ADRB3 1
11714606 10.1016/s0960-894x(01)00629-1 NON-PROTEIN TARGET 1
11714606 10.1016/s0960-894x(01)00629-1 Beta-2 adrenergic receptor 1
11714606 10.1016/s0960-894x(01)00629-1 Homo sapiens 1
17533126 10.1016/j.bmcl.2007.05.030 ADMET 1

Data from ChEMBL 36 via Core Engine