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Compound Detail

CHEMBL1203115

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Cl.NC(=O)c1cc(C(O)CN2CCN(c3cccc(C(F)(F)F)c3)CC2)ccc1O

Basic Information

ChEMBL ID CHEMBL1203115
Phase Preclinical
Structure Type MOL
InChI Key MVKZBZHUHWRRMC-UHFFFAOYSA-N
Parent Compound CHEMBL419945
Active Moiety CHEMBL419945
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

409.4
MW (Da)
2.37
ALogP
5
HBA
3
HBD
90.0
PSA (Ų)
0.71
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H23ClF3N3O3
MW 445.87
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -1.29

Activity Summary

Kd 3 meas. best 6.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor beta
CHEMBL2094118
Kd 6.9 6.9 125.9 1
Adrenergic receptor alpha-1
CHEMBL2094251
Kd 6.33 6.33 467.7 1
Cavia porcellus
CHEMBL369
Kd 5.74 5.74 1819.7 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
6115059 10.1021/jm00135a017 Rattus norvegicus 2
6115059 10.1021/jm00135a017 Adrenergic receptor alpha-1 1
6115059 10.1021/jm00135a017 Adrenergic receptor beta 1
6115059 10.1021/jm00135a017 Unchecked 1
6115059 10.1021/jm00135a017 Cavia porcellus 1

Data from ChEMBL 36 via Core Engine