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Compound Detail

CHEMBL4860694

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COc1ccc(-n2cc(CN[C@@H]3C[C@H]3c3ccc(F)c(F)c3)nn2)cc1

Basic Information

ChEMBL ID CHEMBL4860694
Phase Preclinical
Structure Type MOL
InChI Key AHZPABLWMIVXCR-QFBILLFUSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

356.4
MW (Da)
3.20
ALogP
5
HBA
1
HBD
52.0
PSA (Ų)
0.74
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H18F2N4O
MW 356.38
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -1.90

Activity Summary

IC50 2 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lysine-specific histone demethylase 1A
CHEMBL6136
IC50 7.77 7.77 17.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33775841 10.1016/j.bmcl.2021.127993 Lysine-specific histone demethylase 1A 1
33775841 10.1016/j.bmcl.2021.127993 Amine oxidase [flavin-containing] A 1
33775841 10.1016/j.bmcl.2021.127993 Amine oxidase [flavin-containing] B 1
33775841 10.1016/j.bmcl.2021.127993 PC-3 1
33775841 10.1016/j.bmcl.2021.127993 MCF7 1
33775841 10.1016/j.bmcl.2021.127993 MGC-803 1
33775841 10.1016/j.bmcl.2021.127993 SGC-7901 1
34915312 10.1016/j.ejmech.2021.114042 Lysine-specific histone demethylase 1A 1

Data from ChEMBL 36 via Core Engine