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Compound Detail

CHEMBL22062

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CC(=O)Nc1ccc(Nc2c3ccccc3nc3ccccc23)cc1

Basic Information

ChEMBL ID CHEMBL22062
Phase Preclinical
Structure Type MOL
InChI Key OSHKKYSYOUUOFF-UHFFFAOYSA-N
4
Targets
7
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

327.4
MW (Da)
5.09
ALogP
3
HBA
2
HBD
54.0
PSA (Ų)
0.52
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H17N3O
MW 327.39
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -0.84

Activity Summary

EC50 5 meas. best 6.27
IC50 2 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
L1210
CHEMBL386
IC50 7.0 7.0 100.0 1
Unchecked
CHEMBL612545
EC50 6.27 5.845 536.0 4
Lysine-specific histone demethylase 1A
CHEMBL6136
IC50 5.45 5.45 3540.0 1
ATP-dependent molecular chaperone HSP82
CHEMBL1293251
EC50 5.22 5.22 5981.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20485427 10.1038/nature09107 Plasmodium falciparum 4
7205885 10.1021/jm00134a009 Nucleic Acid 2
36913900 10.1016/j.ejmech.2023.115255 Lysine-specific histone demethylase 1A 2
20485428 10.1038/nature09099 Plasmodium falciparum 2
3820217 10.1021/jm00386a006 L1210 2
7143362 10.1021/jm00352a027 P388 2
7205885 10.1021/jm00134a009 Mus musculus 2
7143362 10.1021/jm00352a027 L1210 1
7143362 10.1021/jm00352a027 Nucleic Acid 1
7069706 10.1021/jm00345a015 L1210 1
7069706 10.1021/jm00345a015 Mus sp. 1
7069706 10.1021/jm00345a015 No relevant target 1
7120279 10.1021/jm00350a004 L1210 1
20485427 10.1038/nature09107 Unchecked 1
20485427 10.1038/nature09107 HepG2 1
7205885 10.1021/jm00134a009 Calf thymus DNA 1
- 10.6019/CHEMBL3433997 Solute carrier family 2, facilitated glucose transporter member 1 1
- 10.6019/CHEMBL3433997 Hexose transporter 1 1
- 10.6019/CHEMBL3433997 Glucose transporter 1
7205885 10.1021/jm00134a009 No relevant target 1

Data from ChEMBL 36 via Core Engine