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Compound Detail

CHEMBL4228272

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CC1=C(C(=O)Nc2ccc3[nH]ncc3c2)C(c2ccc(F)c(CCC(=O)N(CC(C)C)C(C)C)c2)NC(=O)N1

Basic Information

ChEMBL ID CHEMBL4228272
Phase Preclinical
Structure Type MOL
InChI Key OBNJNGUUJLDGGC-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

534.6
MW (Da)
4.79
ALogP
4
HBA
4
HBD
119.2
PSA (Ų)
0.32
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H35FN6O3
MW 534.64
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -1.87

Activity Summary

IC50 1 meas. best 4.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-adrenergic receptor kinase 1
CHEMBL4079
IC50 4.92 4.92 12000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29627263 10.1016/j.bmcl.2018.03.082 Beta-adrenergic receptor kinase 1 1
29627263 10.1016/j.bmcl.2018.03.082 Rhodopsin kinase GRK1 1
29627263 10.1016/j.bmcl.2018.03.082 G protein-coupled receptor kinase 5 1

Data from ChEMBL 36 via Core Engine