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Compound Detail

CHEMBL5418169

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C[C@@](O)(C(=O)N1CCC(O)(CCNC2=C(Cl)C(=O)c3cccnc3C2=O)CC1)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL5418169
Phase Preclinical
Structure Type MOL
InChI Key WEFIEAQCGYECIG-GOSISDBHSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

475.9
MW (Da)
1.56
ALogP
7
HBA
3
HBD
119.8
PSA (Ų)
0.59
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H21ClF3N3O5
MW 475.85
Aromatic Rings 1
Heavy Atoms 32
NP-Likeness -0.17

Activity Summary

IC50 2 meas. best 6.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone-lysine N-methyltransferase NSD2
CHEMBL3108645
IC50 6.62 6.62 240.0 1
KMS-11
CHEMBL4296454
IC50 5.09 5.09 8100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
36642961 10.1021/acs.jmedchem.2c01920 Histone-lysine N-methyltransferase NSD2 1
36642961 10.1021/acs.jmedchem.2c01920 KMS-11 1
36642961 10.1021/acs.jmedchem.2c01920 ADMET 1

Data from ChEMBL 36 via Core Engine