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Compound Detail

CHEMBL4597193

VALEMETOSTAT
🧪 Phase II
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🧪 Phase II
Cc1cc(C)c(CNC(=O)c2cc(Cl)c3c(c2C)O[C@@](C)([C@H]2CC[C@H](N(C)C)CC2)O3)c(=O)[nH]1

Basic Information

ChEMBL ID CHEMBL4597193
Name VALEMETOSTAT
Phase Phase II
Structure Type MOL
InChI Key SSDRNUPMYCFXGM-UYPAYLBCSA-N

Known Names

Valemetostat
4
Targets
15
Activities
1
Assay Types
0
PK Parameters
20
Publications
1
Known Names
4
Indications

Molecular Properties

488.0
MW (Da)
4.49
ALogP
5
HBA
2
HBD
83.7
PSA (Ų)
0.65
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer
USAN Stem -stat

Extended Properties

Molecular Formula C26H34ClN3O4
MW 488.03
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.67

Indications

Breast Neoplasms Carcinoma, Hepatocellular Lymphoma Lymphoma, Non-Hodgkin

Activity Summary

IC50 15 meas. best 9.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone-lysine N-methyltransferase EZH1
CHEMBL2189116
IC50 9.36 8.145 0.4 4
Unchecked
CHEMBL612545
IC50 9.36 8.68 0.4 3
Histone-lysine N-methyltransferase EZH2
CHEMBL2189110
IC50 8.87 8.3614 1.4 7
HCT-116
CHEMBL394
IC50 7.62 7.62 24.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone-lysine N-methyltransferase EZH1 IC50 = 0.44 nM 9.36 Inhibition of EZH1 (unknown origin) 35531606
Unchecked IC50 = 0.44 nM 9.36 Inhibition of EZH1/2 in human HCT-116 cells assessed as reduction in H3K27me3 le... 28741798
Histone-lysine N-methyltransferase EZH2 IC50 = 1.36 nM 8.87 Inhibitory Activity Assay: The inhibitory activity of the synthesized compounds ... -
Histone-lysine N-methyltransferase EZH2 IC50 = 2.5 nM 8.6 Inhibition of EZH2 (unknown origin) 35531606
Histone-lysine N-methyltransferase EZH2 IC50 = 2.5 nM 8.6 Inhibition of wild type EZH2 (unknown origin) by AlphaLISA assay 37156182
Unchecked IC50 = 2.5 nM 8.6 Inhibition of N-terminal GST/His tagged human recombinant PRC2-EZH2 complex (2 t... 28741798
Histone-lysine N-methyltransferase EZH2 IC50 = 5.08 nM 8.29 Inhibition of human EZH2 using Core Histone and [3H]SAM as substrate incubated f... 28741798
Histone-lysine N-methyltransferase EZH2 IC50 = 5.08 nM 8.29 Inhibition of human EZH2 Y641F mutant using Core Histone and [3H]SAM as substrat... 28741798
Histone-lysine N-methyltransferase EZH2 IC50 = 8.4 nM 8.08 Inhibition of EZH2 (unknown origin) assessed as reduction in H3K27me3 level 35531606
Histone-lysine N-methyltransferase EZH1 IC50 = 8.4 nM 8.08 Inhibition of human EZH1 by radiometric analysis 37156182
Unchecked IC50 = 8.4 nM 8.08 Inhibition of PRC2-EZH1 (unknown origin) using biotinylated histone H3 peptide a... 28741798
Histone-lysine N-methyltransferase EZH2 IC50 = 16.0 nM 7.8 Inhibition of EZH2 (unknown origin) 37156182
Histone-lysine N-methyltransferase EZH1 IC50 = 23.0 nM 7.64 Inhibition of wildtype EZH1 (unknown origin) 37156182
HCT-116 IC50 = 24.0 nM 7.62 Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability... 37156182
Histone-lysine N-methyltransferase EZH1 IC50 = 31.5 nM 7.5 Inhibitory Activity Assay: The inhibitory activity of the synthesized compounds ... -

Literature References

PubMed DOI Target Context # Activities
28741798 10.1111/cas.13326 Unchecked 31
28741798 10.1111/cas.13326 Histone-lysine N-methyltransferase NSD2 3
28741798 10.1111/cas.13326 Histone-lysine N-methyltransferase EZH2 2
37156182 10.1016/j.ejmech.2023.115461 Histone-lysine N-methyltransferase EZH1 2
37156182 10.1016/j.ejmech.2023.115461 Histone-lysine N-methyltransferase EZH2 2
- 10.6019/CHEMBL5724709 U2OS 2
28741798 10.1111/cas.13326 Protein kinase C beta type 2
- 10.6019/CHEMBL5724709 Fibroblast 2
28741798 10.1111/cas.13326 Tyrosine-protein kinase Lyn 2
35531606 10.1021/acs.jmedchem.2c00047 Histone-lysine N-methyltransferase EZH2 2
28741798 10.1111/cas.13326 KARPAS-422 2
- 10.6019/CHEMBL5724709 HEK-293T 2
28741798 10.1111/cas.13326 CCRF-CEM 1
28741798 10.1111/cas.13326 SUP-B15 1
28741798 10.1111/cas.13326 RS4-11 1
28741798 10.1111/cas.13326 MOLT-4 1
- 10.6019/CHEMBL5724796 Bromodomain-containing protein 4 1
37156182 10.1016/j.ejmech.2023.115461 MV4-11 1
37156182 10.1016/j.ejmech.2023.115461 HCT-116 1
35531606 10.1021/acs.jmedchem.2c00047 KARPAS-422 1

Data from ChEMBL 36 via Core Engine