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Compound Detail

CHEMBL206002

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C[C@H](CNc1cccc(-c2ccc(C(=O)O)cc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1

Basic Information

ChEMBL ID CHEMBL206002
Phase Preclinical
Structure Type MOL
InChI Key DNYHEVPHQAGYME-CMJOXMDJSA-N
2
Targets
2
Activities
1
Assay Types
4
PK Parameters
6
Publications
0
Known Names

Molecular Properties

468.9
MW (Da)
4.53
ALogP
5
HBA
5
HBD
118.9
PSA (Ų)
0.30
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 C25H25ClN2O5
MW 468.94
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.56

Activity Summary

EC50 2 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-3 adrenergic receptor
CHEMBL246
EC50 9.7 9.7 0.2 1
Beta-1 adrenergic receptor
CHEMBL213
EC50 5.6 5.6 2511.9 1

Pharmacokinetic Data

Parameter Value Units Species
AUC - - Canis lupus familiaris
CL 9.3 mL.min-1.kg-1 Canis lupus familiaris
F - % Canis lupus familiaris
T1/2 - - Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16640337 10.1021/jm0509445 Canis familiaris 5
16640337 10.1021/jm0509445 Beta-3 adrenergic receptor 2
16640337 10.1021/jm0509445 Beta-2 adrenergic receptor 2
16640337 10.1021/jm0509445 Beta-1 adrenergic receptor 2
16640337 10.1021/jm0509445 Beta-2 adrenergic receptor and beta-3 adrenergic receptor 1
16640337 10.1021/jm0509445 Adrenergic receptor beta; ADRB1 & ADRB3 1

Data from ChEMBL 36 via Core Engine