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Compound Detail

CHEMBL4083038

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Cn1c(C(=O)Nc2cccc(COc3ccc(OC4CCNCC4)cc3)c2)cc2sccc21

Basic Information

ChEMBL ID CHEMBL4083038
Phase Preclinical
Structure Type MOL
InChI Key NCKQOQVVTYHFPU-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

461.6
MW (Da)
5.20
ALogP
6
HBA
2
HBD
64.5
PSA (Ų)
0.40
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H27N3O3S
MW 461.59
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.23

Activity Summary

IC50 3 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
LSD1/CoREST complex
CHEMBL3137262
IC50 6.8 6.8 160.0 2
Amine oxidase [flavin-containing] B
CHEMBL2039
IC50 5.14 5.14 7160.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28186755 10.1021/acs.jmedchem.6b01018 Lysine-specific histone demethylase 1A 3
28186755 10.1021/acs.jmedchem.6b01018 THP-1 3
28186755 10.1021/acs.jmedchem.6b01018 Lysine-specific histone demethylase 2 1
28186755 10.1021/acs.jmedchem.6b01018 LSD1/CoREST complex 1
28186755 10.1021/acs.jmedchem.6b01018 Amine oxidase [flavin-containing] A 1
28186755 10.1021/acs.jmedchem.6b01018 Amine oxidase [flavin-containing] B 1
28186757 10.1021/acs.jmedchem.6b01019 LSD1/CoREST complex 1

Data from ChEMBL 36 via Core Engine