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Compound Detail

CHEMBL5414047

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O=C(NCc1[nH]nc2ccccc12)c1cc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)ccc1F

Basic Information

ChEMBL ID CHEMBL5414047
Phase Preclinical
Structure Type MOL
InChI Key KGSBEYKVWODBRD-ICSRJNTNSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

502.6
MW (Da)
4.13
ALogP
6
HBA
3
HBD
97.5
PSA (Ų)
0.35
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H27FN4O4
MW 502.55
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -0.75

Activity Summary

IC50 1 meas. best 7.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-adrenergic receptor kinase 1
CHEMBL4079
IC50 7.75 7.75 18.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Beta-adrenergic receptor kinase 1 IC50 = 18.0 nM 7.75 Inhibition of human GRK2 36055000

Literature References

PubMed DOI Target Context # Activities
36055000 10.1016/j.ejmech.2022.114668 Beta-adrenergic receptor kinase 1 1

Data from ChEMBL 36 via Core Engine