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Compound Detail

CHEMBL572880

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CO[C@H]1[C@@H](N(C)C(=O)c2ccc(C(=O)[O-])cc2)C[C@@H]2O[C@@]1(C)n1c3ccccc3c3c4c(c5c6ccccc6n2c5c31)C(=O)NC4.[Na+]

Basic Information

ChEMBL ID CHEMBL572880
Phase Preclinical
Structure Type MOL
InChI Key VMSZRAPGFCMZRK-FTPWAYTLSA-M
Parent Compound CHEMBL435809
Active Moiety CHEMBL435809
1
Targets
3
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

614.7
MW (Da)
5.61
ALogP
7
HBA
2
HBD
115.0
PSA (Ų)
0.27
QED
2
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H29N4NaO6
MW 636.64
Aromatic Rings 6
Heavy Atoms 46
NP-Likeness 0.66

Activity Summary

IC50 3 meas. best 5.83

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 5.83 5.7733 1490.0 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 1490.0 nM 5.83 Inhibition of I174A-mutated CK2 holoenzyme 12816539
Unchecked IC50 = 1620.0 nM 5.79 Inhibition of wild-type CK2 holoenzyme 12816539
Unchecked IC50 = 1980.0 nM 5.7 Inhibition of V66A-mutated CK2 holoenzyme 12816539

Literature References

PubMed DOI Target Context # Activities
12816539 10.1042/bj20030674 Unchecked 5

Data from ChEMBL 36 via Core Engine