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Compound Detail

CHEMBL509156

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C[C@H](Cc1ccc(-c2ccc(C(=O)O)c(OC3CCCCC3)c2)cc1)NC[C@H](O)c1ccccc1

Basic Information

ChEMBL ID CHEMBL509156
Phase Preclinical
Structure Type MOL
InChI Key BTGYMCRAGAZJTI-PIKZIKFNSA-N
2
Targets
2
Activities
1
Assay Types
9
PK Parameters
7
Publications
0
Known Names

Molecular Properties

473.6
MW (Da)
6.02
ALogP
4
HBA
3
HBD
78.8
PSA (Ų)
0.34
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 C30H35NO4
MW 473.61
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.04

Activity Summary

EC50 2 meas. best 10.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-3 adrenergic receptor
CHEMBL246
EC50 10.38 10.38 0.0 1
Beta-1 adrenergic receptor
CHEMBL213
EC50 7.55 7.55 28.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC - ng.hr.mL-1 Canis lupus familiaris
AUC 24.3 ng.hr.mL-1 Canis lupus familiaris
CL 68.9 mL.min-1.kg-1 Canis lupus familiaris
CL - - Rattus norvegicus
CL - - Macaca mulatta
CL - - Homo sapiens
CL 0.1 mL.min-1.kg-1 Canis lupus familiaris
F - % Canis lupus familiaris
T1/2 0.35 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18553954 10.1021/jm8000345 Canis familiaris 8
18553954 10.1021/jm8000345 Beta-3 adrenergic receptor 2
18553954 10.1021/jm8000345 Liver microsomes 2
18553954 10.1021/jm8000345 Beta-1 adrenergic receptor 1
18553954 10.1021/jm8000345 Unchecked 1
18553954 10.1021/jm8000345 Beta-2 adrenergic receptor 1
18553954 10.1021/jm8000345 ADMET 1

Data from ChEMBL 36 via Core Engine