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Compound Detail

CHEMBL4857832

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COc1ccc(OC)c(-n2cc(CN[C@@H]3C[C@H]3c3ccc(F)c(F)c3)nn2)c1

Basic Information

ChEMBL ID CHEMBL4857832
Phase Preclinical
Structure Type MOL
InChI Key SIGJOOSRQUTZMP-MAUKXSAKSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

386.4
MW (Da)
3.21
ALogP
6
HBA
1
HBD
61.2
PSA (Ų)
0.68
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H20F2N4O2
MW 386.40
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.65

Activity Summary

IC50 2 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lysine-specific histone demethylase 1A
CHEMBL6136
IC50 7.96 7.96 11.0 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 3
33775841 10.1016/j.bmcl.2021.127993 MGC-803 3
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 SGC-7901 1
34915312 10.1016/j.ejmech.2021.114042 Lysine-specific histone demethylase 1A 1

Data from ChEMBL 36 via Core Engine