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Compound Detail

CHEMBL3907289

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COC(=O)c1ccc(N2CCN(C)CC2)c(NC(=O)c2cc(N)c(F)c(C)c2Cl)c1

Basic Information

ChEMBL ID CHEMBL3907289
Phase Preclinical
Structure Type MOL
InChI Key PLRPRYDOPJNKDZ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

434.9
MW (Da)
3.16
ALogP
6
HBA
2
HBD
87.9
PSA (Ų)
0.57
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H24ClFN4O3
MW 434.90
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -1.37

Activity Summary

IC50 2 meas. best 7.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
WD repeat-containing protein 5
CHEMBL1075317
IC50 7.33 7.33 46.5 1
MLL1/ASH2L/RBBP5/WDR5 complex
CHEMBL3137282
IC50 5.34 5.34 4600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27720555 10.1016/j.bmc.2016.09.073 NON-PROTEIN TARGET 2
27720555 10.1016/j.bmc.2016.09.073 WD repeat-containing protein 5 1
27720555 10.1016/j.bmc.2016.09.073 ADMET 1
27720555 10.1016/j.bmc.2016.09.073 MLL1/ASH2L/RBBP5/WDR5 complex 1

Data from ChEMBL 36 via Core Engine