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Compound Detail

CHEMBL5561941

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CC(C)C[C@H](N)COc1cncc(-c2ccc3[nH]nc(C#Cc4ccsc4)c3c2)c1

Basic Information

ChEMBL ID CHEMBL5561941
Phase Preclinical
Structure Type MOL
InChI Key VEZMWMSMHXKTFY-FQEVSTJZSA-N
5
Targets
5
Activities
2
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

416.6
MW (Da)
4.84
ALogP
5
HBA
2
HBD
76.8
PSA (Ų)
0.44
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H24N4OS
MW 416.55
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.10

Activity Summary

IC50 4 meas. best 8.85
EC50 1 meas. best 5.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dual specificity protein kinase CLK2
CHEMBL4225
IC50 8.85 8.85 1.4 1
Dual specificity protein kinase CLK4
CHEMBL4203
IC50 8.49 8.49 3.2 1
Dual specificity protein kinase CLK1
CHEMBL4224
IC50 7.68 7.68 21.0 1
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
CHEMBL2292
IC50 7.66 7.66 21.7 1
Unchecked
CHEMBL612545
EC50 5.54 5.54 2900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38500250 10.1021/acs.jmedchem.3c02092 Rattus norvegicus 22
38500250 10.1021/acs.jmedchem.3c02092 Unchecked 17
38500250 10.1021/acs.jmedchem.3c02092 Dual specificity tyrosine-phosphorylation-regulated kinase 1A 3
38500250 10.1021/acs.jmedchem.3c02092 Dual specificity protein kinase CLK2 2
38500250 10.1021/acs.jmedchem.3c02092 Dual specificity protein kinase CLK1 2
38500250 10.1021/acs.jmedchem.3c02092 Dual specificity protein kinase CLK4 2
38500250 10.1021/acs.jmedchem.3c02092 Dual specificity protein kinase CLK3 1
38500250 10.1021/acs.jmedchem.3c02092 Serine/arginine-rich splicing factor 6 1
38500250 10.1021/acs.jmedchem.3c02092 Dual specificity tyrosine-phosphorylation-regulated kinase 1B 1
38500250 10.1021/acs.jmedchem.3c02092 Homeodomain-interacting protein kinase 2 1
38500250 10.1021/acs.jmedchem.3c02092 Serine/threonine-protein kinase pim-3 1
38500250 10.1021/acs.jmedchem.3c02092 TRAF2 and NCK-interacting protein kinase 1
38500250 10.1021/acs.jmedchem.3c02092 Receptor-type tyrosine-protein kinase FLT3 1

Data from ChEMBL 36 via Core Engine