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Compound Detail

CHEMBL4078052

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COc1ccc([C@H]2CN(Cc3c(C)cccc3F)C[C@@H]2N(C)C)cc1OC

Basic Information

ChEMBL ID CHEMBL4078052
Phase Preclinical
Structure Type MOL
InChI Key NHZYKXLISRSSLC-QUCCMNQESA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

372.5
MW (Da)
3.68
ALogP
4
HBA
0
HBD
24.9
PSA (Ų)
0.77
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H29FN2O2
MW 372.48
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.66

Activity Summary

Kd 1 meas. best 6.68
Ki 1 meas. best 7.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Polycomb protein EED
CHEMBL2189117
Ki 7.92 7.92 12.0 1
Polycomb protein EED
CHEMBL2189117
Kd 6.68 6.68 210.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28926243 10.1021/acs.jmedchem.7b00576 Polycomb protein EED 4

Data from ChEMBL 36 via Core Engine